Cynaropicrin is a bitter sesquiterpene lactone found in artichoke (Cynara scolymus) and other plants of the Asteraceae family. It exhibits a range of biological activities, including anti-inflammatory, anti-proliferative, and antioxidant effects. Its unique structure and biological properties make it a promising target for research in the development of new drugs for the treatment of various diseases. Notably, cynaropicrin has been shown to inhibit the growth of cancer cells and to protect against liver damage. The compound's synthesis is complex and involves several steps, including the formation of a sesquiterpene lactone ring system. Studies on cynaropicrin are ongoing to better understand its mechanisms of action and its potential therapeutic applications.'
cynaropicrin: structure given in first source; RN given for ((3aR-(3aalpha,4alpha,6aalpha,8beta,9aalpha,9bbeta)))-isomer
ID Source | ID |
---|---|
PubMed CID | 119093 |
CHEMBL ID | 374146 |
CHEBI ID | 4038 |
SCHEMBL ID | 1711811 |
MeSH ID | M0203869 |
Synonym |
---|
MEGXP0_001095 |
ACON1_000045 |
C09385 |
35730-78-0 |
cynaropicrin |
NCGC00168845-01 |
bdbm50194430 |
chebi:4038 , |
CHEMBL374146 , |
BRD-K51428447-001-01-5 |
[(3ar,4s,6ar,8s,9ar,9br)-8-hydroxy-3,6,9-trimethylidene-2-oxo-3a,4,5,6a,7,8,9a,9b-octahydroazuleno[4,5-b]furan-4-yl] 2-(hydroxymethyl)prop-2-enoate |
2-propenoic acid, 2-(hydroxymethyl)-, (3ar,4s,6ar,8s,9ar,9br)-dodecahydro-8-hydroxy-3,6,9-tris(methylene)-2-oxoazuleno(4,5-b)furan-4-yl ester |
2-propenoic acid, 2-(hydroxymethyl)-, dodecahydro-8-hydroxy-3,6,9-tris(methylene)-2-oxoazuleno(4,5-b)furan-4-yl ester, (3ar-(3aalpha,4alpha,6aalpha,8beta,9aalpha,9bbeta))- |
m9233789i9 , |
unii-m9233789i9 |
cynaropikrin |
2-propenoic acid, 2-(hydroxymethyl)-, dodecahydro-8-hydroxy-3,6,9-tris(methylene)-2-oxoazuleno(4,5-b)furan-4-yl ester, (3ar-(3a.alpha.,4.alpha.,6a.alpha.,8.beta.,9a.alpha.,9b.beta.))- |
SCHEMBL1711811 |
CS-8041 |
HY-N2350 |
NCGC00168845-02 |
AKOS032971358 |
Q15410905 |
DTXSID20957143 |
8-hydroxy-3,6,9-trimethylidene-2-oxododecahydroazuleno[4,5-b]furan-4-yl 2-(hydroxymethyl)prop-2-enoate |
A901510 |
cynaropicrin - cynara cardunculus (artichoke) |
XC160151 |
FS-8077 |
Cynaropicrin is a guaianolide sesquiterpene lactone. It has potent inhibitory activity against Trypanosoma brucei, the protozoan parasite that causes human African trypanosomiasis (HAT; sleeping sickness)
Excerpt | Reference | Relevance |
---|---|---|
"Cynaropicrin is a guaianolide sesquiterpene lactone with a 5-7-5 tricyclic skeleton, four exo-olefins, and two hydroxyl groups. " | ( Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives. Adams, M; Brun, R; Hamburger, M; Hara, S; Kaiser, M; Kondo, R; Sato, M; Usuki, T; Yoshimoto, Y; Zimmermann, S, 2014) | 2.08 |
"Cynaropicrin is a guaianolide sesquiterpene lactone with a 5-7-5 tricyclic skeleton, four exo-olefins, and two hydroxyl groups. " | ( Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. Kurita, M; Li, J; Usuki, T; Yoshida, Y, 2019) | 3.4 |
"Cynaropicrin is a guaianolide sesquiterpene lactone, which has potent in vitro and in vivo inhibitory activity against Trypanosoma brucei, the protozoan parasite that causes human African trypanosomiasis (HAT; sleeping sickness). " | ( Synthesis of cynaropicrin-d(4). Adams, M; Hara, S; Ogawa, K; Sato, M; Sato, T; Usuki, T, 2015) | 2.23 |
"Cynaropicrin is a sesquiterpene lactone displaying immunomodulatory effects on the production of cytokine and nitric oxide from macrophages/monocytes. " | ( Cynaropicrin, a sesquiterpene lactone, as a new strong regulator of CD29 and CD98 functions. Chain, BM; Cho, JY; Joo, HG; Jung, JH; Katz, DR; Kim, AR; Kim, BH; Rhee, MH; Yoo, ES, 2004) | 3.21 |
Cynaropicrin treatment improved the survival rate of the rats with AKI. Treatment increased the level of antioxidant enzymes, IL-10, Nrf-2, and Bcl-2.
Excerpt | Reference | Relevance |
---|---|---|
"Cynaropicrin treatment improved the survival rate of the rats with AKI." | ( Renal Tissue Damage Induced by Acute Kidney Injury in Sepsis Rat Model Is Inhibited by Cynaropicrin via IL-1β and TNF-α Down-Regulation. Cai, D; Cheng, Z; Duan, H; Fu, Y, 2021) | 1.57 |
"Treatment with cynaropicrin in dosage-based manner increased the level of antioxidant enzymes, IL-10, Nrf-2, and Bcl-2 in the animals which indicates the antioxidative effect of cynaropicrin." | ( Cynaropicrin Averts the Oxidative Stress and Neuroinflammation in Ischemic/Reperfusion Injury Through the Modulation of NF-kB. Jin, T; Leng, B, 2023) | 2.69 |
"Treatment with cynaropicrin suppressed AKI induced urea nitrogen and creatinine in the rat serum in dose-dependent manner." | ( Renal Tissue Damage Induced by Acute Kidney Injury in Sepsis Rat Model Is Inhibited by Cynaropicrin via IL-1β and TNF-α Down-Regulation. Cai, D; Cheng, Z; Duan, H; Fu, Y, 2021) | 1.18 |
Excerpt | Reference | Relevance |
---|---|---|
" Fractions 5, 6, 7 and 8 caused concentration-dependent cell death in the culture of substantia nigra, the other fractions were not toxic at the concentrations used." | ( Toxic effects of solstitialin A 13-acetate and cynaropicrin from Centaurea solstitialis L. (Asteraceae) in cell cultures of foetal rat brain. Cheng, CH; Costall, B; Hamburger, M; Hostettmann, K; Jenner, P; Naylor, RJ; Wang, Y, 1992) | 0.54 |
Excerpt | Reference | Relevance |
---|---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Class | Description |
---|---|
sesquiterpene lactone | Any member of a diverse class of complex, multicyclic phytochemicals showing a variety of skeleton arrangements and bioactivities, and having in common a sesquiterpenoid structure including a lactone ring. |
[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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 | IC50 (µMol) | 19.5000 | 0.1000 | 4.2169 | 8.8000 | AID276339 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
peptidoglycan biosynthetic process | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
regulation of cell shape | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
peptidoglycan biosynthetic process | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
UDP-N-acetylgalactosamine biosynthetic process | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
cell division | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
cell wall organization | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
UDP-N-acetylglucosamine 1-carboxyvinyltransferase activity | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
transferase activity | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
cytoplasm | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
cytosol | UDP-N-acetylglucosamine 1-carboxyvinyltransferase | Escherichia coli K-12 |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
AID725399 | Inhibition of NF-kappaB-65 (unknown origin) expressed in human keratinocytes assessed as inhibition of bFGF production at 4 uM by EIA | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID780229 | Reduction of T(SH)2 level in Trypanosoma brucei rhodesiense at 50 uM after 40 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID276342 | Inhibition of MurA at 5 uM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA. |
AID276340 | Inhibition of Pseudomonas aeruginosa PAO1293 MurA in presence of UNAG | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA. |
AID780214 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as extracellular CYN level at 50 uM after 20 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID1069399 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives. |
AID780212 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as extracellular CYN level at 50 uM after 40 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID1544460 | Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells expressing pGL4.32 [luc2p/NF-kBRE/Hygro] at 2.5 uM to 10 uM incubated for 2 hrs followed by TNFalpha addition and measured after 5 hrs by luciferase reporter gene assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. |
AID385429 | Cytotoxicity against human SKOV3 cells by SRB assay | 2008 | Journal of natural products, Apr, Volume: 71, Issue:4 | Guaiane sesquiterpene lactones and amino acid-sesquiterpene lactone conjugates from the aerial parts of Saussurea pulchella. |
AID385428 | Cytotoxicity against human A549 cells by SRB assay | 2008 | Journal of natural products, Apr, Volume: 71, Issue:4 | Guaiane sesquiterpene lactones and amino acid-sesquiterpene lactone conjugates from the aerial parts of Saussurea pulchella. |
AID725402 | Inhibition of NF-kappaB (unknown origin) expressed in TNFalpha-stimulated HEK293 cells expressing pGL3-Luc assessed inhibition of transactivation activity after 24 hrs by luciferase assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID1069397 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB 900 | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives. |
AID780222 | Inhibition of trypanothione reductase in Trypanosoma cruzi using T(S)2 as substrate at 100 to 200 uM after 240 mins by spectrophotometry in presence of NADPH | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID780217 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as GS-CYN monoadduct level at 50 uM after 5 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID276339 | Inhibition of Escherichia coli K12 Mur A in presence of UNAG | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA. |
AID780216 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as T(S-CYN)2 bisadduct level at 50 uM after 5 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID780220 | Induction of T(SH)2-CYN adduct formation by HPLC-MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID725396 | Antiphotoaging activity in DBA-2 mouse assessed as reduction of UVB-induced epidermal hyperproliferation in ear tissue at 462.2 mg/kg, po as powder qd for 12 days relative to untreated control | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID725395 | Antiphotoaging activity in DBA-2 mouse assessed as reduction of UVB-induced epidermal hyperproliferation in ear tissue administered as po as powder qd for 12 days relative to untreated control | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID780228 | Antitrypanosomal activity against Trypanosoma brucei assessed as intermediate phenotype at 50 uM after 5 to 10 mins by Giemsa staining-based light microscopy | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID1544462 | Cytotoxicity against human HEK293 cells at 3 uM after 7 hrs by WST-8 assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. |
AID780218 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as intracellular CYN level at 50 uM after 5 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID1069398 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives. |
AID780213 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as extracellular CYN level at 50 uM after 30 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID725401 | Inhibition of NF-kappaB-65 (unknown origin)-mediated transactivation in TNFalpha-stimulated HEK293 cells assessed inhibition of I-kappaB phosphorylation and degradation after 24 hrs | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID725400 | Inhibition of NF-kappaB-65 (unknown origin) expressed in TNFalpha-stimulated HEK293 cells assessed inhibition of nuclear translocation at 8 uM after 3 hrs | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID1544457 | Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells expressing pGL4.32 [luc2p/NF-kBRE/Hygro] assessed as NFkappaB activity by measuring relative light units at 1.5 uM incubated for 2 hrs followed by TNFalpha addition and measured afte | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. |
AID725397 | Inhibition of NF-kappaB p65 expressed in human keratinocytes co-cultured with human epidermal melanocytes assessed as inhibition of melanocyte proliferation at 4 uM by WST-1 assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID1544459 | Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells expressing pGL4.32 [luc2p/NF-kBRE/Hygro] assessed as NFkappaB activity by measuring relative light units at 3 uM incubated for 2 hrs followed by TNFalpha addition and measured after | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. |
AID402670 | Cytotoxicity against human A549 cells after 3 days by SRB assay | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Cytotoxic activity of some natural and synthetic guaianolides. |
AID725162 | Antiphotoaging activity in DBA-2 mouse assessed as reduction of UVB-induced melanocyte proliferation in ear tissue at 92.4 to 462.2 mg/kg, po as powder qd for 12 days relative to untreated control | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID725393 | Antiphotoaging activity in DBA-2 mouse assessed as reduction of UVB-induced PCNA-positive cell in ear tissue at 92.4 to 462.2 mg/kg, po as powder qd for 12 days | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID402676 | Cytotoxicity against human SK-MEL-2 cells after 3 days by SRB assay | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Cytotoxic activity of some natural and synthetic guaianolides. |
AID780221 | Induction of GS-CYN monoadduct formation by HPLC-MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID402671 | Cytotoxicity against human MCF7 cells after 3 days by SRB assay | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Cytotoxic activity of some natural and synthetic guaianolides. |
AID385430 | Cytotoxicity against human SK-MEL-2 cells by SRB assay | 2008 | Journal of natural products, Apr, Volume: 71, Issue:4 | Guaiane sesquiterpene lactones and amino acid-sesquiterpene lactone conjugates from the aerial parts of Saussurea pulchella. |
AID402673 | Cytotoxicity against human KB cells after 3 days by SRB assay | 2005 | Journal of natural products, Jul, Volume: 68, Issue:7 | Cytotoxic activity of some natural and synthetic guaianolides. |
AID780225 | Reduction of GSH level in Trypanosoma brucei rhodesiense at 50 uM after 40 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID780224 | Inhibition of trypanothione synthatase in Trypanosoma brucei using GSH as substrate at 200 uM | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID780219 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as extracellular CYN level at 50 uM after 5 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID725398 | Inhibition of NF-kappaB-65 (unknown origin) expressed in human dermal fibroblasts assessed as inhibition of MMP1 production at 4 uM by EIA | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID1544458 | Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells expressing pGL4.32 [luc2p/NF-kBRE/Hygro] assessed as NFkappaB activity by measuring relative light units at 0.75 uM incubated for 2 hrs followed by TNFalpha addition and measured aft | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. |
AID780215 | Induction of CYN-thiol adduct formation in Trypanosoma brucei rhodesiense assessed as extracellular CYN level at 50 uM after 10 mins by UHPLC-MS/MS analysis | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID725394 | Antiphotoaging activity in DBA-2 mouse assessed as reduction of UVB-induced epidermal hyperproliferation in ear tissue at 92.4 mg/kg, po as powder qd for 12 days relative to untreated control | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Cynaropicrin from Cynara scolymus L. suppresses photoaging of skin by inhibiting the transcription activity of nuclear factor-kappa B. |
AID1293873 | Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9 | Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay. |
AID780223 | Irreversible inhibition of trypanothione synthatase in Trypanosoma brucei using GSH as substrate at 200 uM after 240 mins | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID780226 | Inhibition of ornithine decarboxylase in Trypanosoma brucei rhodesiense STIB900 assessed as intracellular ornithine level at 50 uM after 20 mins (Rvb = 4 +/- 1 uM) | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID1544456 | Cytotoxicity against human HEK293 cells at 0.75 uM to 3 uM after 7 hrs by WST-8 assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Cynaropicrin and inhibition of NF-κB activation: A structure activity relationship study. |
AID780227 | Antitrypanosomal activity against Trypanosoma brucei assessed as stumpy phenotype at 50 uM after 40 mins by Giemsa staining-based light microscopy | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | Cynaropicrin targets the trypanothione redox system in Trypanosoma brucei. |
AID382836 | Cytotoxicity against human HCT15 cells by SRB assay | 2008 | Journal of natural products, Apr, Volume: 71, Issue:4 | Guaiane sesquiterpene lactones and amino acid-sesquiterpene lactone conjugates from the aerial parts of Saussurea pulchella. |
AID276341 | Inhibition of Escherichia coli K12 Mur A C115D at 50 uM in presence of UNAG | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 3 (5.66) | 18.2507 |
2000's | 9 (16.98) | 29.6817 |
2010's | 31 (58.49) | 24.3611 |
2020's | 10 (18.87) | 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 (32.29) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 53 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |