withaferin A: an antiestrogen and phytogenic antineoplastic agent isolated from leaves of Withania somnifera Dun.; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
withaferin A : A withanolide that is 5,6:22,26-diepoxyergosta-2,24-diene-1,26-dione substituted by hydroxy groups at positions 4 and 27 (the 4beta,5beta,6beta,22R stereoisomer). Isolated from Physalis longifolia, it exhibits cytotoxic activity. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| Flora | Rank | Flora Definition | Family | Family Definition |
|---|---|---|---|---|
| Physalis | genus | A plant genus of the family SOLANACEAE. Members contain physalin and withangulatin.[MeSH] | Solanaceae | A plant family of the order SOLANALES, class MAGNOLIOPSIDA. Among the most noted are POTATOES; TOMATOES; CAPSICUM (green and red peppers); TOBACCO; and BELLADONNA.[MeSH] |
| Withania | genus | A plant genus of the family SOLANACEAE. Members contain withanolides. Withania somnifera is the source of ashwagandha and aswal.[MeSH] | Solanaceae | A plant family of the order SOLANALES, class MAGNOLIOPSIDA. Among the most noted are POTATOES; TOMATOES; CAPSICUM (green and red peppers); TOBACCO; and BELLADONNA.[MeSH] |
| Physalis longifolia | species | [no description available] | Solanaceae | A plant family of the order SOLANALES, class MAGNOLIOPSIDA. Among the most noted are POTATOES; TOMATOES; CAPSICUM (green and red peppers); TOBACCO; and BELLADONNA.[MeSH] |
| Withania somnifera | species | [no description available] | Solanaceae | A plant family of the order SOLANALES, class MAGNOLIOPSIDA. Among the most noted are POTATOES; TOMATOES; CAPSICUM (green and red peppers); TOBACCO; and BELLADONNA.[MeSH] |
| ID Source | ID |
|---|---|
| PubMed CID | 265237 |
| CHEMBL ID | 517080 |
| CHEBI ID | 69120 |
| SCHEMBL ID | 157208 |
| MeSH ID | M0054582 |
| Synonym |
|---|
| ashwagandha |
| 5beta-ergosta-2,24-dien-26-oic acid, 5,6beta-epoxy-4beta,22,27-trihydroxy-1-oxo-, delta-lactone, (20s,22r)- |
| nsc 273757 |
| ergosta-2,24-dien-26-oic acid, 5,6-epoxy-4,22,27-trihydroxy-1-oxo-, gamma-lactone, (4bta,5beta,6beta,22r)- |
| brn 1335150 |
| withaferine a |
| (4beta,5beta,6beta,22r)-5,6-epoxy-4,22,27-trihydroxy-1-oxoergosta-2,24-dien-26-oic acid, delta-lactone |
| 5-beta-ergosta-2,24-dien-26-oic acid, 5,6-beta-epoxy-4-beta,22,27-trihydroxy-1-oxo-, delta-lactone, (20s,22r)- |
| nsc273757 |
| nsc-273757 |
| withaferin deriv jpr, iowa u. compound |
| nsc101088 , |
| 5.beta.-ergosta-2, 5,6.beta.-epoxy-4.beta.,22,27-trihydroxy-1-oxo-, .delta.-lactone, (20s,22r)- |
| 5119-48-2 |
| withaferin a |
| ergosta-2, 5,6-epoxy-4,22,27-trihydroxy-1-oxo-, .delta.-lactone, (4.beta.,5.beta.,6.beta.,22r)- |
| wln: t3 f5 e666 1a r axo ov pu ch&ttttj j1 n1 rq iy1&- ft6ov cutj c1q d1 |
| C08841 |
| NCI60_000031 |
| CHEMBL517080 , |
| chebi:69120 , |
| 4beta,27-dihydroxy-1-oxo-5beta,6beta-epoxywitha-2,24-dienolide |
| (4beta,5beta,6beta,22r)-4,27-dihydroxy-5,6:22,26-diepoxyergosta-2,24-diene-1,26-dione |
| 5-19-06-00604 (beilstein handbook reference) |
| l6do3qw4k5 , |
| unii-l6do3qw4k5 |
| nsc 101088 |
| S8587 |
| BRD-K88378636-001-01-0 |
| smr004701668 |
| MLS006010687 |
| SCHEMBL157208 |
| A1-06845 |
| withaferin a [mi] |
| (4.beta.,5.beta.,6.beta.,22r)-4,27-dihydroxy-5,6:22,26-diepoxyergosta-2,24-diene-1,26-dione |
| withaferin a, analytical standard |
| mfcd10687098 |
| withaferin a, >=95% (hplc) |
| NCGC00180796-02 |
| ncgc00180796-02_c28h38o6_(4beta,5beta,6beta,22r)-4,27-dihydroxy-5,6:22,26-diepoxyergosta-2,24-diene-1,26-dione |
| CS-0018562 |
| HY-N2065 |
| (6s,7r,9r)-6-hydroxy-15-[(2r,3r)-3-hydroxy-4-(4-methyl-5-oxo-2h-furan-3-yl)butan-2-yl]-2,16-dimethyl-8-oxapentacyclo[9.7.0.02,7.07,9.012,16]octadec-4-en-3-one |
| (1s,2r,6s,7r,9r,11s,12s,15r,16s)-6-hydroxy-15-[(1s)-1-[(2r)-5-(hydroxymethyl)-4-methyl-6-oxo-2,3-dihydropyran-2-yl]ethyl]-2,16-dimethyl-8-oxapentacyclo[9.7.0.02,7.07,9.012,16]octadec-4-en-3-one |
| withaferin a 100 microg/ml in acetonitrile |
| Q6606395 |
| ergosta-2,24-dien-26-oicacid, 5,6-epoxy-4,22,27-trihydroxy-1-oxo-, d-lactone, (4b,5b,6b,22r)- |
| A871350 |
| AS-77575 |
| AKOS040758787 |
| bdbm50599323 |
| (4S,4AR,5AR,6AS,6BS,9R,9AS,11AS,11BR)-4-HYDROXY-9-((S)-1-((R)-5-(HYDROXYMETHYL)-4-METHYL-6-OXO-3,6-DIHYDRO-2H-PYRAN-2-YL)ETHYL)-9A,11B-DIMETHYL-5A,6,6A,6B,7,8,9,9A,10,11,11A,11B-DODECAHYDROCYCLOPENTA[1,2]PHENANTHRO[8A,9-B]OXIREN-1(4H)-ONE |
Withaferin A (WA) is a small molecule derived from a medicinal plant (Withania somnifera) inhibits growth of human breast cancer xenografts and mammary tumor development in rodent models without any toxicity.
Withaferin A (Wit A) has reportedly shown cytotoxicity in a variety of tumor cell lines. It has been shown to inhibit the proliferation, metastasis, invasion and angiogenesis of cancer cells.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Withaferin A has been reported to exert cytotoxic effects against human multiple myeloma cells." | ( Withaferin A inhibits cell proliferation of U266B1 and IM-9 human myeloma cells by inducing intrinsic apoptosis. Hou, L; Li, L; Niu, B; Zhang, W; Zheng, Y, 2022) | 2.89 |
| "Withaferin A has been shown to inhibit the proliferation, metastasis, invasion and angiogenesis of cancer cells." | ( Withaferin A induces apoptosis through the generation of thiol oxidation in human head and neck cancer cells. Kim, DE; Kwon, TK; Min, KJ; Park, JW, 2015) | 2.58 |
| "Withaferin A (Wit A) has reportedly shown cytotoxicity in a variety of tumor cell lines. " | ( Withaferin A sensitizes TRAIL-induced apoptosis through reactive oxygen species-mediated up-regulation of death receptor 5 and down-regulation of c-FLIP. Choi, KS; Kwon, TK; Lee, TJ; Min, do S; Park, JW; Um, HJ, 2009) | 3.24 |
Withaferin A can inhibit the proliferation and apoptosis of A549 cells by suppressing activation of the PI3K/Akt pathways. 10μM producing a 54% increase compared with control, suggesting that withaferin is at least partially responsible for W.
Withaferin A treatment to HD mice considerably increased their lifespan as well as restored progressive motor behavioral deficits and declined body weight. Pre-treatment with withafer in A significantly decreased the levels of liver and kidney functional markers and cytokines.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Withaferin A treatment to HD mice considerably increased their lifespan as well as restored progressive motor behavioral deficits and declined body weight." | ( Withaferin A Induces Heat Shock Response and Ameliorates Disease Progression in a Mouse Model of Huntington's Disease. Jana, NR; Joshi, T; Kaznacheyeva, EV; Kumar, V, 2021) | 2.79 |
| "Withaferin A treatment also induced the phosphorylation of stress signalling proteins, including the p38 mitogen-activated protein kinase, the c-Jun N-terminal kinase, c-Jun, the heat shock protein 27 and protein kinase B within 0 to 16 h." | ( Withaferin A activates stress signalling proteins in high risk acute lymphoblastic leukemia. Gao, YB; Liu, JS; Shi, LH; Wu, XJ, 2015) | 2.58 |
| "Withaferin A treatment was followed by slight but significant increase of hemolysis." | ( Withaferin A-stimulated Ca2+ entry, ceramide formation and suicidal death of erythrocytes. Jilani, K; Lang, F; Lupescu, A; Shaik, N; Zbidah, M, 2013) | 2.55 |
| "Pre-treatment with withaferin A not only significantly decreased the levels of liver and kidney functional markers and cytokines but also reduced oxidative stress, as evidenced by improved anti-oxidant status." | ( Assessment of hepatoprotective and nephroprotective potential of withaferin A on bromobenzene-induced injury in Swiss albino mice: possible involvement of mitochondrial dysfunction and inflammation. Sabina, EP; Vedi, M, 2016) | 0.99 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " However, when ashwagandha was added to β-amyloid treated and HIV-1 infected samples, the toxic effects were neutralized." | ( Ashwagandha (Withania somnifera) reverses β-amyloid1-42 induced toxicity in human neuronal cells: implications in HIV-associated neurocognitive disorders (HAND). Atluri, VS; Kurapati, KR; Nair, MP; Samikkannu, T, 2013) | 0.39 |
| " Ashwagandha also provided a significant protection to lipid peroxidation (LPx) levels, catalase, and superoxide dismutase (SOD) but not reduced glutathione (GSH) contents in brain tissue as well as peripheral organs, liver and kidney, suggesting its ability to act as a free radical scavenger protecting cells against toxic insult." | ( Glioprotective effects of Ashwagandha leaf extract against lead induced toxicity. Kataria, H; Kaur, G; Kumar, P; Lakhanpal, D; Nazmi, A; Singh, R, 2014) | 0.4 |
| " Four subjects (8%) (ashwagandha: 1[4%]; Placebo: 3[12%]) out of 50 reported few mild and temporary adverse effects during this study." | ( Efficacy and Safety of Ashwagandha Root Extract in Subclinical Hypothyroid Patients: A Double-Blind, Randomized Placebo-Controlled Trial. Basu, I; Sharma, AK; Singh, S, 2018) | 0.48 |
| " The secondary outcomes of this study were the clinical adverse events and the vital parameters." | ( Safety of Ashwagandha Root Extract: A Randomized, Placebo-Controlled, study in Healthy Volunteers. Gupta, SK; Mishra, AK; Tiwari, S; Verma, N, 2021) | 0.62 |
| " No adverse events were reported by any of the participants in this study." | ( Safety of Ashwagandha Root Extract: A Randomized, Placebo-Controlled, study in Healthy Volunteers. Gupta, SK; Mishra, AK; Tiwari, S; Verma, N, 2021) | 0.62 |
| " The present study revealed that the consumption of Ashwagandha root extract for 8 weeks was safe in both males and females volunteers." | ( Safety of Ashwagandha Root Extract: A Randomized, Placebo-Controlled, study in Healthy Volunteers. Gupta, SK; Mishra, AK; Tiwari, S; Verma, N, 2021) | 0.62 |
| " In this direction, we have explored the radioprotective potential of Withaferin A, a plant withanolide, which was recently shown to be safe and well tolerated in cancer patients in a clinical trial and is also known to be a radio-sensitizer in cancer cells." | ( Withaferin A, a steroidal lactone, selectively protects normal lymphocytes against ionizing radiation induced apoptosis and genotoxicity via activation of ERK/Nrf-2/HO-1 axis. Bhilwade, HN; Checker, R; Nandha, SR; Patwardhan, RS; Sandur, SK; Sharma, D, 2023) | 2.59 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The effect of withaferin A, a plant withanolide, alone or in combination with acute and fractionated radiotherapy and/or hyperthermia, was tested on two mouse tumors, B16F1 melanoma and fibrosarcoma, grown in C57BL and Swiss albino mice, respectively." | ( Radiosensitizing effect of withaferin A combined with hyperthermia on mouse fibrosarcoma and melanoma. Kamath, R; Uma Devi, P, 2003) | 0.98 |
| "Currently, the treatment for ovarian cancer entails cytoreductive surgery followed by chemotherapy, mainly, carboplatin combined with paclitaxel." | ( Withaferin a alone and in combination with cisplatin suppresses growth and metastasis of ovarian cancer by targeting putative cancer stem cells. Batra, SK; Kakar, SS; Miller, DM; Moghadamfalahi, M; Powell, KS; Ratajczak, MZ; Singh, SK, 2014) | 1.85 |
| " Herbs, however, contain biologically active compounds and can potentially interact with prescription medications, including chemotherapy drugs." | ( Herb-Drug Interactions in Cancer Care. Gubili, J; Mao, JJ; Yeung, KS, 2018) | 0.48 |
| " Colon cancer cells were differentiated from the normal cells via investigating light diffusion combined with the fluorescence effect of the Ashwagandha chitosan nanoparticles (Ash C NPs)." | ( Early cancer detection using the fluorescent Ashwagandha chitosan nanoparticles combined with near-infrared light diffusion characterization: in vitro study. Abuelmakarem, HS; Ahmed, WA; El-Azab, J; Hamdy, O; Sliem, MA, 2023) | 0.91 |
Xenografting of the A2780 cell line resulted in a significant rate of mortality, which was attenuated by a therapeutic dosage of Withaferin A.
| Excerpt | Relevance | Reference |
|---|---|---|
| "A 28-year-old man with decreased libido received ashwagandha in the usual daily dosage of 5 g for 10 days." | ( Fixed-drug eruption caused by ashwagandha (Withania somnifera): a widely used Ayurvedic drug. Bhattacharya, SN; Sehgal, VN; Verma, P, ) | 0.13 |
| " Treatment of various epithelial ovarian cancer cell lines (A2780, A2780/CP70 and CaOV3) with combination of WFA and Dox (WFA/DOX) showed a time- and dose-dependent synergistic effect on inhibition of cell proliferation and induction of cell death, thus reducing the dosage requirement of Dox." | ( Withaferin A synergizes the therapeutic effect of doxorubicin through ROS-mediated autophagy in ovarian cancer. Fong, MY; Gupta, R; Jin, S; Kakar, SS; Rane, M; Singh, RK, 2012) | 1.82 |
| "05), which also increased time-dependently with the same dosage of Withaferin A (P<0." | ( Effect of Withaferin A on A549 cellular proliferation and apoptosis in non-small cell lung cancer. Bai, C; Cai, Y; Chen, Y; Sheng, ZY, 2014) | 1.04 |
| " Intraperitoneal administration of WA at a dosage of 4 mg/kg of body weight was initiated from postnatal day 40 until end stage in SOD1(G93A) mice, and from 9 months until end stage in SOD1(G37R) mice." | ( Early-stage treatment with Withaferin A reduces levels of misfolded superoxide dismutase 1 and extends lifespan in a mouse model of amyotrophic lateral sclerosis. Julien, JP; Kriz, J; Patel, P, 2015) | 0.71 |
| " Three studies compared several dosage levels of WS extract with placebos using versions of the Hamilton Anxiety Scale, with two demonstrating significant benefit of WS versus placebo, and the third demonstrating beneficial effects that approached but did not achieve significance (p=0." | ( An alternative treatment for anxiety: a systematic review of human trial results reported for the Ayurvedic herb ashwagandha (Withania somnifera). Morley, CP; Nanavati, KB; Pratte, MA; Young, V, 2014) | 0.4 |
| " The proposed method was found to be reproducible, specific, precise and accurate for simultaneous estimation of these marker compounds in a combined dosage form." | ( Simultaneous Estimation of Withaferin A and Z-Guggulsterone in Marketed Formulation by RP-HPLC. Agrawal, P; Laddha, K; Vegda, R, 2015) | 0.71 |
| " But, according to some available evidences for spermicidal features, further studies should focus on the extract preparation method and also dosage used in their study protocols." | ( Effects of Ahmadi AsrBadr, Y; Fazljou, SMB; Moini Jazani, A; Nasimi Doost Azgomi, R; Nazemyieh, H; Nejatbakhsh, F; Sadeghi Bazargani, H; Zomorrodi, A, 2018) | 0.48 |
| " Isolated compounds were tested in a dose-response for their in vitro NF-κB inhibition and antiproliferative activity in multiple myeloma cells after 5 and 72 h treatment, respectively." | ( Bioactive metabolites from the leaves of Withania adpressa. Bekkouche, K; Ben Bakrim, W; Christen, P; Cretton, S; Cuendet, M; El Bouzidi, L; Monteillier, A; Nuzillard, JM; Saraux, N, 2018) | 0.48 |
| " However, long term study and varying dosage ranges should be investigated in the future." | ( Safety of Ashwagandha Root Extract: A Randomized, Placebo-Controlled, study in Healthy Volunteers. Gupta, SK; Mishra, AK; Tiwari, S; Verma, N, 2021) | 0.62 |
| " The solid dosage form was most preferred." | ( Analysis of Clinical Trial Registry of India for Evidence of Anti-Arthritic Properties of Withania somnifera (Ashwagandha). Dey, A; Gupta, AK; Kanjilal, S; Patnaik, RS, 2021) | 0.62 |
| " Evidence shows a dosage of 6 gm in powder form or extracts in tablets, or 500 -1000 mg capsule consumed for a duration of 8 - 12 weeks may be useful in managing symptoms of arthritis in patients." | ( Analysis of Clinical Trial Registry of India for Evidence of Anti-Arthritic Properties of Withania somnifera (Ashwagandha). Dey, A; Gupta, AK; Kanjilal, S; Patnaik, RS, 2021) | 0.62 |
| "While benefits were seen in the reviewed studies, significant variability in the WS extracts examined prevents a consensus on the optimum WS preparation or dosage for treating neuropsychiatric conditions." | ( Effects of Cabey, KA; Soumyanath, A; Speers, AB; Wright, KM, 2021) | 0.62 |
| " The effects on sleep were more prominent in the subgroup of adults diagnosed with insomnia, treatment dosage ≥600 mg/day, and treatment duration ≥8 weeks." | ( Effect of Ashwagandha (Withania somnifera) extract on sleep: A systematic review and meta-analysis. Abdul Rahman, R; Cheah, KL; Husniati Yaacob, L; Norhayati, MN, 2021) | 0.62 |
| Product Category | Products |
|---|---|
| Beauty & Personal Care | 5 |
| Professional Supplements | 1 |
| Herbs, Botanicals & Homeopathy | 7 |
| Vitamins & Supplements | 2 |
| Pet Supplies | 2 |
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| apoptosis inducer | Any substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| delta-lactone | A lactone having a six-membered lactone ring. |
| 4-hydroxy steroid | Any steroid bearing a 4-hydroxy substituent. |
| enone | An alpha,beta-unsaturated ketone of general formula R(1)R(2)C=CR(3)-C(=O)R(4) (R(4) =/= H) in which the C=O function is conjugated to a C=C double bond at the alpha,beta position. |
| ergostanoid | |
| secondary alcohol | A secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it. |
| withanolide | Any steroid lactone that is a C28 steroid with a modified side chain forming a lactone ring and its substituted derivatives. |
| 27-hydroxy steroid | |
| primary alcohol | A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it. |
| epoxy steroid | Any steroid whose structure includes an epoxy group. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 0.4661 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 0.4661 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 0.5850 | 0.0002 | 2.4585 | 9.9600 | AID1887323; AID1887326 |
| Nuclear factor NF-kappa-B p105 subunit | Homo sapiens (human) | IC50 (µMol) | 0.0470 | 0.0001 | 1.9731 | 8.0000 | AID1771376 |
| Nuclear factor NF-kappa-B p100 subunit | Homo sapiens (human) | IC50 (µMol) | 0.0470 | 0.0001 | 1.8088 | 8.0000 | AID1771376 |
| Transcription factor p65 | Homo sapiens (human) | IC50 (µMol) | 0.0470 | 0.0001 | 1.8981 | 8.8000 | AID1771376 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1492759 | Cytotoxicity against human WI38 cells assessed as inhibition of colony formation at 0.1 to 0.3 uM by crystal violet staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1442760 | Induction of CHOP expression in human ACHN cells at 2.5 to 5 uM measured after 24 hrs by Western blotting method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1492789 | Cytoprotective activity against UV irradiation-induced stress in human TIG3 cells assessed as decrease in CARF level irradiated with 50 mJ/cm2 of UV radiations followed by compound addition by immuno fluorescence staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506415 | Induction of differentiation of human multiple myeloma cancer stem cells assessed as downregulation of CD151 mRNA expression at 0.31 to 5 uM after 24 hrs by qPCR method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1771373 | Antiproliferative activity against human MM1.R cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Structure-Activity Relationships of Withanolides as Antiproliferative Agents for Multiple Myeloma: Comparison of Activity in 2D Models and a 3D Coculture Model. |
| AID1887317 | Inhibition of SARS-COV2 main protease mediated cytotoxicity against human HepG2 cells transfected with pCMV3-2019-nCoV-3CLpro plasmid assessed as increase in cell number and measured at 48 hrs by calcien AM staining based microscopic analysis | |||
| AID1506376 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at G1 phase at 0.62 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 45.1%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506405 | Cytotoxicity against human CD34-positive hematopoietic stem cells assessed as decrease in cell viability at 10 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506391 | Cytotoxicity against human multiple myeloma cancer stem cells assessed as decrease in cell viability after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506379 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at S phase at 0.62 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 40.9%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506399 | Cytotoxicity against human RPMI18226 cells assessed as dead cells at 10 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 21.4%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1631584 | Cytotoxicity against human NCI-H460 cells after 72 hrs by resazurin-based colorimetric assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells. |
| AID1873259 | Anti-obesity activity in male C57BL/6 mouse model of high-fat diet induced obesity assessed as body weight change at 1.25 mg/kg, ip administered once a day for 21 days relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Recent advances in natural anti-obesity compounds and derivatives based on in vivo evidence: A mini-review. |
| AID1506386 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at S phase at 1.25 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 40.9%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1442761 | Induction of BIP expression in human ACHN cells at 2.5 to 5 uM measured after 24 hrs by Western blotting method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1379664 | Induction of apoptosis in human HeLa cells assessed increase in chromatin condensation at 8 uM incubated for 12 hrs by Hoechst 33342 staining based fluorescence microscopy | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1506402 | Induction of apoptosis in human multiple myeloma cancer stem cells assessed as increase in late apoptotic cells at 5 uM after 24 hrs by annexin V/propidium iodide staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1315170 | Neuroprotective activity in transgenic C57/BL6 mouse amyotrophic lateral sclerosis model harboring SOD1 G93A mutant assessed as decrease in misfolded SOD1 levels in spinal cord at 4 mg/kg, ip administered twice weekly started from postnatal day 40 until d | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Recent progress towards an effective treatment of amyotrophic lateral sclerosis using the SOD1 mouse model in a preclinical setting. |
| AID1492765 | Cytotoxicity against human TIG3 cells assessed as induction of senescence at 64 population doubling at 0.1 uM | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1379685 | Induction of apoptosis in human HeLa cells assessed as increase in caspase-3 activity by measuring pNA release level at 24 uM incubated for 8 hrs using c-DEVD-pNA substrate by colorimetric assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492763 | Cytotoxicity against human TIG3 cells assessed as induction of morphological changes at 0.3 to 1.5 uM after 48 hrs by phase contrast microscopy | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1379650 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1574313 | Inhibition of human N-terminal His6-tagged TCPTP catalytic domain (1 to 336 residues) expressed in Escherichia coli strain Rosetta2 (DE3) at 500 uM using DiFMUP as substrate preincubated for 10 mins followed by substrate addition and measured after 10 min | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Celastrol Promotes Weight Loss in Diet-Induced Obesity by Inhibiting the Protein Tyrosine Phosphatases PTP1B and TCPTP in the Hypothalamus. |
| AID1492771 | Effect on mortalin expression level in human TIG3 cells at 0.3 to 3 uM by immuno fluorescence analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1887326 | Inhibition of recombinant SARS-COV2 main protease expressed in Escherichia coli Rosetta cells using DABCYL-KTSAVLQSGFRKME-EDANS as substrate pre-incubated for 60 mins followed by substarte addition measured at 30 min in presence of GSH by FRET-based assay | |||
| AID1768106 | Elongation of circadian rhythms in dexamethasone-induced mouse Sarcoma-180 cells assessed as increase in Bmal1 period time at 5 uM measured for 1 mins at 10 min interval up to 96 hrs by bioluminescence based Bmal1 promoter-reporter gene assay (Rvb = 25.70 | 2021 | Journal of natural products, 07-23, Volume: 84, Issue:7 | Withanolide Derivative 2,3-Dihydro-3β-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor α (RORa). |
| AID1506390 | Cytotoxicity against human RPMI18226 cells assessed as decrease in cell viability after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1315171 | Neuroprotective activity in transgenic C57/BL6 mouse amyotrophic lateral sclerosis model harboring SOD1 G93A mutant assessed as upregulation of HSP70 levels in spinal cord at 4 mg/kg, ip administered twice weekly started from postnatal day 40 until diseas | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Recent progress towards an effective treatment of amyotrophic lateral sclerosis using the SOD1 mouse model in a preclinical setting. |
| AID1506382 | Cell cycle arrest in human RPMI18226 cells assessed as accumulation at sub-G1 phase at 0.62 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 10.8%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1409633 | Ratio of induction of heat shock response in GFP-tagged human 293T cells to IC50 for cytotoxicity against human 293T cells | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation. |
| AID1631583 | Cytotoxicity against human MCF7 cells after 72 hrs by resazurin-based colorimetric assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells. |
| AID1768105 | Cytotoxicity against mouse Sarcoma-180 cells assessed as reduction in cell proliferation at 1 uM measured up to 5 days by WST-8 assay | 2021 | Journal of natural products, 07-23, Volume: 84, Issue:7 | Withanolide Derivative 2,3-Dihydro-3β-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor α (RORa). |
| AID1887318 | Inhibition of SARS-COV2 main protease mediated cytotoxicity against human A549 cells transfected with pCMV3-2019-nCoV-3CLpro plasmid assessed as increase in cell number and measured at 48 hrs by calcien AM staining based microscopic analysis | |||
| AID1506393 | Cytotoxicity against human multiple myeloma cancer stem cells assessed as cell viability at 10 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 95.7%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1887316 | Inhibition of SARS-COV2 main protease mediated cytotoxicity against human A549 cells transfected with pCMV3-2019-nCoV-3CLpro plasmid assessed as increase in cell number at 5 uM measured at 48 hrs by Nucblue dye based microscopic analysis | |||
| AID1506385 | Cell cycle arrest in human RPMI18226 cells assessed as accumulation at G1 phase at 1.25 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 28.2%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492777 | Induction of apoptosis in human TIG3 cells assessed as decrease in Bcl2 levels at 0.3 to 3 uM by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1492768 | Induction of oxidative stress in human TIG3 cells assessed as increase in GADD45alpha mRNA levels by RT-PCR analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506375 | Antiproliferative activity against human RPMI18226 cells after 72 hrs by XTT assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1576644 | Modulation of GABAA receptor in electrically stimulated Sprague-Dawley rat dentate gyrus hippocampal granule neurons assessed as GABA induced IPSC amplitude at 10 uM at holding potential of -65 mV by whole-cell patch-clamp method | 2019 | Journal of natural products, 05-24, Volume: 82, Issue:5 | Ferulic Acid Esters and Withanolides: In Search of Withania somnifera GABA |
| AID1409630 | Cytotoxicity against human CHP100 cells assessed as reduction in cell viability after 24 hrs by resazurin dye based Alamar blue assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation. |
| AID1442752 | Sensitization of TRAIL-induced apoptosis in human Caki1 cells assessed as reduction in cell viability at 125 to 500 nM preincubated for 2 hrs followed by addition of TRAIL measured after 18 hrs by MTS assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1506410 | Induction of morphological changes in human multiple myeloma cancer stem cells assessed as appearance of epithelial/lymphoblastic-like morphology at 0.62 uM after 24 hrs by phalloidin/DAPI staining-based assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492760 | Cytotoxicity against human TIG3 cells assessed as cell death at 0.6 uM | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1771372 | Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Structure-Activity Relationships of Withanolides as Antiproliferative Agents for Multiple Myeloma: Comparison of Activity in 2D Models and a 3D Coculture Model. |
| AID1492767 | Induction of oxidative stress against human TIG3 cells assessed as increase in CARF mRNA levels by RT-PCR analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1379655 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492779 | Cytoprotective activity against H2O2-induced oxidative stress in human TIG3 cells assessed as increase in cell survival at 3 uM pretreated with H2O2 for 2 hrs followed by compound addition measured after 2 days by crystal violet staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506394 | Cytotoxicity against human multiple myeloma cancer stem cells assessed as dying cells at 10 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 3.6%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492805 | Induction of AKT-mediated beta-catenin expression level in H2O2 treated human TIG3 cells at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1492772 | Decrease in keap1 expression level in human TIG3 cells at 0.3 to 3 uM by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1442758 | Reduction cFLIP level in human ACHN cells at 125 to 1000 nM after 16 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1379658 | Ratio of IC50 for cytotoxicity against human MCF7 cells using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay to IC50 for cytotoxicity against human MCF7 cells using compound addition to cell culture ce | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492808 | Cytoprotective activity against H2O2-induced oxidative stress in human TIG3 cells assessed as increase in Bcl2 level at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1379687 | Induction of apoptosis in human HeLa cells assessed as increase in caspase-3 activity by measuring pNA release level at 8 uM incubated for 4 hrs using c-DEVD-pNA substrate by colorimetric assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492786 | Cytoprotective activity against H2O2-induced oxidative stress in human TIG3 cells assessed as decrease in p53 level pretreated with H2O2 for 2 hrs followed by compound addition by immuno fluorescence staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506414 | Induction of differentiation of human multiple myeloma cancer stem cells assessed as downregulation of CD166 mRNA expression at 0.31 to 5 uM after 24 hrs by qPCR method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506401 | Induction of apoptosis in human RPMI18226 cells assessed as decrease in viable cells at 1.25 uM after 24 hrs by annexin V/propidium iodide staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1379653 | Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1887324 | Inhibition of recombinant SARS-COV2 main protease expressed in Escherichia coli Rosetta cells at 5 uM using DABCYL-KTSAVLQSGFRKME-EDANS as substrate pre-incubated for 60 mins followed by substarte addition measured at 5 min by FRET-based assay relative to | |||
| AID1379688 | Induction of apoptosis in human HeLa cells assessed as increase in caspase-3 activity by measuring pNA release level at 12 uM incubated for 4 hrs using c-DEVD-pNA substrate by colorimetric assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492764 | Cytotoxicity against human TIG3 cells assessed as decrease in ROS generation at 1.5 to 3 uM after 48 hrs | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506404 | Cytotoxicity against human CD34-positive hematopoietic stem cells assessed as decrease in cell viability at <5 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492754 | Cytotoxicity against human TIG3 cells assessed as cell death at 1 uM after 48 hrs relative to control | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1409626 | Induction of heat shock response in GFP-tagged human 293T cells at 1 to 5 uM after overnight incubation by luciferase reporter gene based luminometric method | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation. |
| AID1409631 | Cytotoxicity against human 293T cells assessed as reduction in cell viability after 72 hrs by resazurin dye based Alamar blue assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation. |
| AID1554560 | Antiproliferative activity against cisplatin-resistant human A2780/CP70 cells measured after 96 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells. |
| AID1604465 | Antiproliferative activity against human PANC1 cells after 48 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1887319 | Inhibition of SARS-COV2 main protease mediated cytotoxicity against human A549 cells transfected with pCMV3-2019-nCoV-3CLpro plasmid assessed as increase in cell number measured at 48 hrs in presence of buthionine sulfoximine by Nucblue dye based microsco | |||
| AID1442754 | Sensitization of TRAIL-induced apoptosis in human UO31 cells assessed as reduction in cell viability at 125 to 500 nM preincubated for 2 hrs followed by addition of TRAIL measured after 18 hrs by MTS assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1506409 | Induction of morphological changes in human multiple myeloma cancer stem cells assessed as appearance in circular shape at 0.62 uM after 24 hrs by phalloidin/DAPI staining-based assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506381 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at G2/M phase at 2.5 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 22.9%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492796 | Induction of Akt phosphorylation at Ser473 residues in H2O2 treated human TIG3 cells at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1631586 | Cytotoxicity against human HFF cells after 72 hrs by resazurin-based colorimetric assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells. |
| AID1379651 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1887320 | Inhibition of SARS-COV2 main protease mediated cytotoxicity against human A549 cells transfected with pCMV3-2019-nCoV-3CLpro plasmid assessed as GSH level measured at 48 hrs in presence of buthionine sulfoximine by Nucblue dye based microscopic analysis | |||
| AID1506387 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at S phase at 2.5 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 40.9%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1379690 | Induction of apoptosis in human HeLa cells assessed as increase in caspase-3 activity by measuring pNA release level at 24 uM incubated for 4 hrs using c-DEVD-pNA substrate by colorimetric assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1506407 | Antimigratory activity in human multiple myeloma cancer stem cells at 2.5 uM after 24 hrs by scratch assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1442756 | Sensitization of TRAIL-induced apoptosis in human ACHN cells assessed as increase in caspase8 activation at 125 to 1000 nM preincubated for overnight followed by addition of TRAIL for 90 mins measured after 18 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1492776 | Activation of keap1 in human TIG3 cells assessed as Nrf2 nuclear accumulation at 0.6 uM by immuno staining analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506400 | Induction of apoptosis in human multiple myeloma cancer stem cells assessed as decrease in viable cells at 5 uM after 24 hrs by annexin V/propidium iodide staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506389 | Cell cycle arrest in human RPMI18226 cells assessed as accumulation at sub-G1 phase after 30 mins by FxCycle violet staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1379654 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1768118 | Agonist activity at RORalpha in mouse NIH3T3 cells at 1 to 1000 uM incubated for 24 hrs by luminescence based assay | 2021 | Journal of natural products, 07-23, Volume: 84, Issue:7 | Withanolide Derivative 2,3-Dihydro-3β-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor α (RORa). |
| AID1492755 | Cytotoxicity against human WI38 cells assessed as cell death at 1 uM after 48 hrs relative to control | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1554561 | Cytotoxicity against human ARPE19 cells measured after 96 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells. |
| AID1442759 | Cytotoxicity in human ACHN cells assessed as viable cells at 1250 to 5000 nM after 48 hrs by MTS assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1379669 | Induction of cell cycle arrest in human HeLa cells assessed increase in hypoploid phase accumulation at 24 uM incubated for 12 hrs by 33342 propidium iodide based flow cytometry relative to untreated control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1576643 | Activation of GABAA receptor in Sprague-Dawley rat dentate gyrus hippocampal granule neurons assessed as holding current at 10 uM by whole-cell patch-clamp method | 2019 | Journal of natural products, 05-24, Volume: 82, Issue:5 | Ferulic Acid Esters and Withanolides: In Search of Withania somnifera GABA |
| AID1492788 | Cytoprotective activity against UV irradiation-induced stress in human TIG3 cells assessed as decrease in p53 level irradiated with 50 mJ/cm2 of UV radiations followed by compound addition by immuno fluorescence staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506408 | Induction of morphological changes in human multiple myeloma cancer stem cells assessed as cell enlargement at 0.62 uM after 24 hrs by phalloidin/DAPI staining-based assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1887323 | Inhibition of recombinant SARS-COV2 main protease expressed in Escherichia coli Rosetta cells using DABCYL-KTSAVLQSGFRKME-EDANS as substrate pre-incubated for 60 mins followed by substarte addition by FRET-based assay | |||
| AID1409632 | Induction of heat shock response in GFP-tagged human 293T cells after overnight incubation by luciferase reporter gene based luminometric method relative to control | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation. |
| AID1442765 | Induction of DR5 expression in human ACHN cells by Western blotting method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1506418 | Induction of differentiation of human multiple myeloma cancer stem cells assessed as upregulation of Kit mRNA expression at 0.31 to 5 uM after 24 hrs by qPCR method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1887321 | Binding affinity to recombinant SARS-COV2 main protease expressed in Escherichia coli Rosetta cells at 2 uM measured after 16 hrs by LC-MS analysis based equilibrium dialysis method | |||
| AID1442751 | Sensitization of TRAIL-induced apoptosis in human ACHN cells assessed as reduction in cell viability preincubated for 2 hrs followed by addition of TRAIL measured after 18 hrs by MTS assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1506398 | Cytotoxicity against human RPMI18226 cells assessed as increase in dead cells at 1.25 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 21.4%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492753 | Cytoprotective activity against H2O2-induced oxidative stress in human TIG3 cells assessed as increase in full length PARP level at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1442764 | Glutathione reactivity in DMSO assessed as formation of MIchael adduct with GSH at pH 7.4 after 24 hrs in presence of NAC by HPLC method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1604467 | Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1887315 | Inhibition of SARS-COV2 main protease mediated cytotoxicity against human HepG2 cells transfected with pCMV3-2019-nCoV-3CLpro plasmid assessed as increase in cell number at 5 uM measured at 48 hrs by Nucblue dye based microscopic analysis | |||
| AID1379666 | Induction of cell cycle arrest in human HeLa cells assessed increase in subG1 phase accumulation at 24 uM incubated for 12 hrs by 33342 propidium iodide based flow cytometry relative to untreated control | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1506412 | Induction of morphological changes in human multiple myeloma cancer stem cells assessed as appearance in spherical shape at 1.25 uM after 24 hrs by phalloidin/DAPI staining-based assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1492787 | Cytoprotective activity against H2O2-induced oxidative stress in human TIG3 cells assessed as decrease in CARF level pretreated with H2O2 for 2 hrs followed by compound addition by immuno fluorescence staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1492774 | Induction of oxidative stress in human TIG3 cells assessed as increase in CARF expression level at 0.6 uM by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1315172 | Neuroprotective activity in transgenic C57/BL6 mouse amyotrophic lateral sclerosis model harboring SOD1 G93A mutant assessed as upregulation of HSP25 levels in spinal cord at 4 mg/kg, ip administered twice weekly started from postnatal day 40 until diseas | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Recent progress towards an effective treatment of amyotrophic lateral sclerosis using the SOD1 mouse model in a preclinical setting. |
| AID1506383 | Cell cycle arrest in human RPMI18226 cells assessed as accumulation at sub-G1 phase at 1.25 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 10.8%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1442762 | Induction of HSP70 expression in human ACHN cells at 2.5 to 5 uM measured after 24 hrs by Western blotting method | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1506380 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at G2/M phase at 1.25 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 22.9%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506396 | Cytotoxicity against human RPMI18226 cells assessed as cell viability at 1.25 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 67.7%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1887325 | Inhibition of recombinant SARS-COV2 main protease expressed in Escherichia coli Rosetta cells at 0.5 uM using DABCYL-KTSAVLQSGFRKME-EDANS as substrate pre-incubated for 60 mins followed by substarte addition and measured at 30 min by FRET-based assay rela | |||
| AID1492775 | Induction of oxidative stress in human TIG3 cells assessed as increase in p53 expression level at 0.6 uM by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1492798 | Induction of p38 MAPK phosphorylation at Thr180/Tyr182 residues in H2O2 treated human TIG3 cells at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1442753 | Sensitization of TRAIL-induced apoptosis in human SN12C cells assessed as reduction in cell viability at 125 to 500 nM preincubated for 2 hrs followed by addition of TRAIL measured after 18 hrs by MTS assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | 17β-Hydroxywithanolides as Sensitizers of Renal Carcinoma Cells to Tumor Necrosis Factor-α Related Apoptosis Inducing Ligand (TRAIL) Mediated Apoptosis: Structure-Activity Relationships. |
| AID1379689 | Induction of apoptosis in human HeLa cells assessed as increase in caspase-3 activity by measuring pNA release level at 16 uM incubated for 4 hrs using c-DEVD-pNA substrate by colorimetric assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1506406 | Antimigratory activity in human multiple myeloma cancer stem cells at 0.62 to 1.25 uM after 24 hrs by scratch assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506374 | Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506378 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at G1 phase at 2.5 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 45.1%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1631585 | Cytotoxicity against human SF268 cells after 72 hrs by resazurin-based colorimetric assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells. |
| AID1631582 | Cytotoxicity against human PC3M cells after 72 hrs by resazurin-based colorimetric assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells. |
| AID1492803 | Induction of ERK2 phosphorylation at Tyr204 residues in H2O2 treated human TIG3 cells at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1492800 | Induction of ERK1 phosphorylation at Thr202 residues in H2O2 treated human TIG3 cells at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1554563 | Selectivity index, ratio of IC50 for human ARPE19 cells to IC50 for cisplatin-resistant human A2780/CP70 cells | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells. |
| AID1492778 | Induction of apoptosis in human TIG3 cells assessed as increase in Bax levels at 0.3 to 3 uM by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1379665 | Induction of apoptosis in human HeLa cells assessed increase in apoptotic nuclei formation at 8 uM incubated for 12 hrs by Hoechst 33342 staining based fluorescence microscopy | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1379656 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1379684 | Induction of apoptosis in human HeLa cells assessed increase in phosphatidylserine externalization at 2 uM incubated for 4 hrs by annexin V and propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1411730 | Inhibition of recombinant human CYP1A1 expressed in baker's yeast-derived microsomes (Sacchrosomes) at 10 uM using 7-ethoxyresorufin substrate by EROD assay relative to control | 2018 | MedChemComm, Feb-01, Volume: 9, Issue:2 | Identification of karanjin isolated from the Indian beech tree as a potent CYP1 enzyme inhibitor with cellular efficacy |
| AID1506397 | Cytotoxicity against human RPMI18226 cells assessed as cell viability at 10 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 67.7%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1631581 | Cytotoxicity against human LNCAP cells after 72 hrs by resazurin-based colorimetric assay | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | 17β-Hydroxy-18-acetoxywithanolides from Aeroponically Grown Physalis crassifolia and Their Potent and Selective Cytotoxicity for Prostate Cancer Cells. |
| AID1379657 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492773 | Decrease in Nrf2 expression level in human TIG3 cells at 0.3 to 3 uM by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1574312 | Inhibition of human N-terminal His6-tagged PTP1B catalytic domain (1 to 393 residues) expressed in Escherichia coli strain Rosetta2 (DE3) at 500 uM using DiFMUP as substrate preincubated for 10 mins followed by substrate addition and measured after 10 min | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Celastrol Promotes Weight Loss in Diet-Induced Obesity by Inhibiting the Protein Tyrosine Phosphatases PTP1B and TCPTP in the Hypothalamus. |
| AID1379691 | Induction of apoptosis in human HeLa cells assessed as increase in caspase-3 activity by measuring pNA release level at 32 uM incubated for 4 hrs using c-DEVD-pNA substrate by colorimetric assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1492807 | Induction of AKT/p38/p44 MAPK-mediated survivin expression level in H2O2 treated human TIG3 cells at 0.3 uM pretreated with H2O2 for 2 hrs followed by compound addition by immunoblot analysis | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1554562 | Selectivity index, ratio of IC50 for human ARPE19 cells to IC50 for cisplatin-sensitive human A2780 cells | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells. |
| AID1409629 | Cytotoxicity against human 293T cells assessed as reduction in cell viability at 1 to 5 uM after 72 hrs by resazurin dye based Alamar blue assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation. |
| AID1506411 | Induction of morphological changes in human multiple myeloma cancer stem cells assessed as appearance of larger cytoplasmic area at 1.25 uM after 24 hrs by phalloidin/DAPI staining-based assay | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1768104 | Cytotoxicity against mouse Sarcoma-180 cells assessed as reduction in cell proliferation by measuring growth rate at 1 uM measured after 3 days by WST-8 assay relative to control | 2021 | Journal of natural products, 07-23, Volume: 84, Issue:7 | Withanolide Derivative 2,3-Dihydro-3β-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor α (RORa). |
| AID1771375 | Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Structure-Activity Relationships of Withanolides as Antiproliferative Agents for Multiple Myeloma: Comparison of Activity in 2D Models and a 3D Coculture Model. |
| AID1506388 | Cell cycle arrest in human RPMI18226 cells assessed as accumulation at G2/M phase at 1.25 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 20.2%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506416 | Induction of differentiation of human multiple myeloma cancer stem cells assessed as downregulation of SOX2 mRNA expression at 0.31 to 5 uM after 24 hrs by qPCR method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1771376 | Inhibition of TNF-alpha stimulated NF-KappaB in human HEK293 cells transfected with NF-kappaB-Luc incubated for 5 hrs by luciferase reporter gene assay | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Structure-Activity Relationships of Withanolides as Antiproliferative Agents for Multiple Myeloma: Comparison of Activity in 2D Models and a 3D Coculture Model. |
| AID1506417 | Induction of differentiation of human multiple myeloma cancer stem cells assessed as upregulation of CD44 mRNA expression at 0.31 to 5 uM after 24 hrs by qPCR method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1771374 | Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Structure-Activity Relationships of Withanolides as Antiproliferative Agents for Multiple Myeloma: Comparison of Activity in 2D Models and a 3D Coculture Model. |
| AID1506413 | Induction of differentiation of human multiple myeloma cancer stem cells assessed as downregulation of MSI2 mRNA expression at 0.31 to 5 uM after 24 hrs by qPCR method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1554559 | Antiproliferative activity against cisplatin-sensitive human A2780 cells measured after 96 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells. |
| AID1379652 | Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Structure-based design, synthesis, and biological evaluation of withaferin A-analogues as potent apoptotic inducers. |
| AID1506395 | Cytotoxicity against human multiple myeloma cancer stem cells assessed as dead cells at 10 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 0.7%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1873242 | Anti-obesity activity in male C57BL/6 mouse model of high-fat diet induced obesity assessed as body weight change at 0.002 mg/kg, ip administered once a day for 8 weeks relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Recent advances in natural anti-obesity compounds and derivatives based on in vivo evidence: A mini-review. |
| AID1604466 | Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID1492758 | Cytotoxicity against human TIG3 cells assessed as inhibition of colony formation at 0.1 to 0.3 uM by crystal violet staining based assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | 2,3-Dihydro-3β-methoxy Withaferin-A Protects Normal Cells against Stress: Molecular Evidence of Its Potent Cytoprotective Activity. |
| AID1506377 | Cell cycle arrest in human multiple myeloma cancer stem cells assessed as accumulation at G1 phase at 1.25 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 45.1%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506403 | Induction of apoptosis in human RPMI18226 cells assessed as increase in late apoptotic cells at 1.25 uM after 24 hrs by annexin V/propidium iodide staining-based flow cytometric method | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506392 | Cytotoxicity against human multiple myeloma cancer stem cells assessed as cell viability at 2.5 uM after 24 hrs by calcein AM/ethidium homodimer staining-based flow cytometric method (Rvb = 95.7%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1506384 | Cell cycle arrest in human RPMI18226 cells assessed as accumulation at sub-G1 phase at 2.5 uM after 30 mins by FxCycle violet staining-based flow cytometric method (Rvb = 10.8%) | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Withaferin A induces cell death and differentiation in multiple myeloma cancer stem cells. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347415 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 14 (2.46) | 18.7374 |
| 1990's | 15 (2.64) | 18.2507 |
| 2000's | 65 (11.42) | 29.6817 |
| 2010's | 329 (57.82) | 24.3611 |
| 2020's | 146 (25.66) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (29.84) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 22 (3.73%) | 5.53% |
| Reviews | 59 (10.00%) | 6.00% |
| Case Studies | 6 (1.02%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 503 (85.25%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||