1-1-diphenyl-2-picrylhydrazyl and Neoplasms

Chronic diseases such as cancer, diabetes, neurodegenerative and cardiovascular diseases are characterized by an enhanced state of oxidative stress, which may result from the overproduction of reactive species and/or a decrease in antioxidant defenses. The search for new chemical entities with antioxidant profile is still thus an emerging field on ongoing interest. Due to the lack of reviews concerning the antioxidant activity of lichen-derived natural compounds, we performed a review of the antioxidant potential and mechanisms of action of natural compounds isolated from lichens. The search terms "lichens", "antioxidants" and "antioxidant response elements" were used to retrieve articles in LILACS, PubMed and Web of Science published until February 2014. From a total of 319 articles surveyed, 32 met the established inclusion and exclusion criteria. It was observed that the most common isolated compound studied was usnic acid, cited in 14 out of the 32 articles. The most often described antioxidant assays for the study of in vitro antioxidant activity were mainly DPPH, LPO and SOD. The most suggested mechanisms of action were scavenging of reactive species, enzymatic activation and inhibition of iNOS. Thus, compounds isolated from lichens are possible candidates for the management of oxidative stress, and may be useful in the treatment of chronic diseases.

Topics: Antioxidant Response Elements; Antioxidants; Benzofurans; Biphenyl Compounds; Free Radical Scavengers; Humans; Lichens; Neoplasms; Oxidation-Reduction; Oxidative Stress; Picrates

Topics: A549 Cells; Anti-Bacterial Agents; Antineoplastic Agents; Bacteria; Biphenyl Compounds; Cell Survival; Disk Diffusion Antimicrobial Tests; Drug Compounding; Free Radical Scavengers; Green Chemistry Technology; Hep G2 Cells; Humans; Metal Nanoparticles; Nanotechnology; Neoplasms; Picrates; Polysaccharides; Silver Nitrate

Humans rely on plants as a necessitous source of their food, energy, cosmetics and medicines, as medicinal plants are rich source of new therapeutically active compounds from decades. Current study was designed to separate and identify active constituents of Erythrina suberosa bark extract using phytochemical screening and gas chromatography and mass spectroscopy, respectively and evaluated their therapeutic activities. E. suberosa bark extract contained saponins, glycosides, alkaloids, tannins, terpenoids, phenols and 44 active compounds identified by phytochemical and gas chromatography and mass spectroscopic analysis. Therapeutic potentials of E. suberosa bark extract was evaluated by such as cytotoxicity, anti-inflammatory and antioxidant assay. Surprisingly, bark extract shows the concentration dependent cytotoxicity against human fibroblast malignant melanoma-144 cell lines and remarkably inhibited (15.18(plusmn;1.13%, at 400mg/ml) growth of cancer cells after 24 hours treatment. In addition, the E. suberosa bark extract also exhibited anti-inflammatory effect at higher doses (400mg/kg) and moderate antioxidant activity is also noticed through (2, 2-diphenyl-1-picrylhydrazyl radical) assay. These findings indicate that E. suberosa bark extract exhibited prominent anticancer and anti-inflammatory activities and might be serve as a potent therapeutic agent in future.

Topics: Animals; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Carrageenan; Cell Line, Tumor; Cell Proliferation; Chemical Fractionation; Disease Models, Animal; Erythrina; Gas Chromatography-Mass Spectrometry; Humans; Inflammation; Neoplasms; Phytochemicals; Picrates; Plant Bark; Plant Extracts; Rats

Gallic acid (GA) is a natural phenolic compound with therapeutic effects that are often challenged by its rapid metabolism and clearance. Therefore,  GA was encapsulated using gum arabic into nanoparticles to increase its bioavailability. The formulated nanoparticles (GANPs) were characterized for physicochemical properties and size and were then evaluated for antioxidant and antihypertensive effects using various established in vitro assays, including 1,1-diphenyl-2-picrylhydrazyl (DPPH), nitric oxide scavenging (NO), β-carotene bleaching and angiotensin-converting enzyme (ACE) inhibitory assays. The GANPs were further evaluated for the in vitro cytotoxicity, cell uptake and cell migration in four types of human cancer cell lines including (MCF-7, MDA-MB231) breast adenocarcinoma, HepG2 hepatocellular cancer, HT-29 colorectal adenocarcinoma, and MCF-10A breast epithelial cell lines. The GANPs demonstrated potent antioxidant effects and have shown promising anti-cancer properties in a dose-dependent manner with a predilection toward HepG2 and MCF7 cancer cells. The uptake of GANPs was successful in the majority of cancer cells with a propensity to accumulate in the nuclear region of the cells. The HepG2 and MCF7 cancer cells also had a significantly higher percentage of apoptosis and were more sensitive to gallic acid nanoparticle treatment in the cell migration assay. This study is the first to confirm the synergistic effects of gum arabic in the encapsulation of gallic acid by increasing the selectivity towards cancer cells and enhancing  the antioxidant properties. The formulated nanoparticles also had remarkably low toxicity in normal cells. Based on these findings, GANPs may have promising therapeutic applications towards the development of more effective treatments with a probable targeting precision in cancer cells.

Topics: Angiotensin-Converting Enzyme Inhibitors; Antineoplastic Agents; Antioxidants; Apoptosis; Biphenyl Compounds; Cell Movement; Epithelial Cells; Gallic Acid; Gum Arabic; Hep G2 Cells; HT29 Cells; Humans; Hypertension; MCF-7 Cells; Nanoparticles; Neoplasms; Nitric Oxide; Picrates

Premna resinosa (Hochst.) Schauer (Lamiaceae) is used in many places to treat bronchitis, respiratory illness and convulsions of the rib cage.. This study evaluates the anticancer, antimicrobial and antioxidant activities of P. resinosa, and isolates some responsible constituents.. The methanol extract of P. resinosa aerial parts and its fractions (n-hexane, dichloromethane, ethyl acetate and n-butanol) were tested. Antimicrobial activity was tested using microdilution method against three Gram-positive and four Gram-negative bacteria. The tested concentrations ranged from 4000 to 7.8 μg/mL and MIC values were determined after 24 h incubation. Anticancer activity was evaluated against three human cancer cell lines (Daoy, HepG2 and SK-MEL28) using MTT assay. Antioxidant activity was investigated by DPPH scavenging method and β-carotene-linoleic acid assay.. The greatest antimicrobial activity was exhibited by n-hexane fraction (MIC 10 μg/mL) against Staphylococcus aureus, Enterococcus faecalis, and Shigella flexneri. The n-hexane fraction induced the greatest cytotoxic activity against Daoy, HepG2, and SK-MEL28 cell lines with IC. Our results indicate that P. resinosa is a source for antimicrobial and cytotoxic compounds. However, further work is required to isolate other active principles and to determine the mechanism of action.

Topics: Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; beta Carotene; Biphenyl Compounds; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Gram-Negative Bacteria; Gram-Positive Bacteria; Hep G2 Cells; Humans; Inhibitory Concentration 50; Lamiaceae; Microbial Sensitivity Tests; Neoplasms; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Plants, Medicinal; Saudi Arabia; Solvents

Echinacea (Asteraceae) is used because of its pharmacological properties. However, there are few studies that integrate phytochemical analyses with pharmacological effects.. Evaluate the chemical profile and biological activity of hydroalcoholic Echinacea extracts.. The difference in the chemical and pharmacological properties among extracts highlights the need to consider strategies and policies for standardization of commercial herbal extracts in order to guarantee the safety and identity of this type of products.

Topics: Alloxan; Animals; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Benzothiazoles; Biomarkers; Biphenyl Compounds; Blood Glucose; Carrageenan; Cell Proliferation; Diabetes Mellitus, Experimental; Echinacea; Edema; HeLa Cells; Humans; Hypoglycemic Agents; Male; MCF-7 Cells; Neoplasms; Phytochemicals; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats, Wistar; Sulfonic Acids; Time Factors

The current work reports the synthesis, spectroscopic studies, antiradical and antiproliferative properties of four ruthenium(III) complexes of heterocyclic tridentate Schiff base bearing a simple 2',4'-dihydroxyacetophenone functionality and ethylenediamine as the bridging ligand with RCHO moiety. The reaction of the tridentate ligands with RuCl₃·3H₂O lead to the formation of neutral complexes of the type [Ru(L)Cl₂(H₂O)] (where L = tridentate NNO ligands). The compounds were characterized by elemental analysis, UV-vis, conductivity measurements, FTIR spectroscopy and confirmed the proposed octahedral geometry around the Ru ion. The Ru(III) compounds showed antiradical potentials against 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, with DPPH scavenging capability in the order: [(PAEBOD)RuCl₂] > [(BZEBOD)RuCl₂] > [(MOABOD)RuCl₂] > [Vit. C] > [rutin] > [(METBOD)RuCl₂], and ABTS radical in the order: [(PAEBOD)RuCl₂] < [(MOABOD)RuCl₂] < [(BZEBOD)RuCl₂] < [(METBOD)RuCl₂]. Furthermore, in vitro anti-proliferative activity was investigated against three human cancer cell lines: renal cancer cell (TK-10), melanoma cancer cell (UACC-62) and breast cancer cell (MCF-7) by SRB assay.

Topics: Antineoplastic Agents; Benzothiazoles; Biphenyl Compounds; Cell Line, Tumor; Cell Proliferation; Coordination Complexes; Free Radical Scavengers; Heterocyclic Compounds; Humans; Ligands; Neoplasms; Picrates; Ruthenium; Schiff Bases; Sulfonic Acids

Context Psidium guajava L. (Myrtaceae) leaves are used in traditional medicines for the treatment of cancer, inflammation and other ailments. Objective The current study explores scientific validation for this traditional medication. Materials and methods We used ferric-reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picryl hydrazil (DPPH) assays to estimate antioxidant activity of P. guajava leaf extracts (methanol, hexane and chloroform). Antitumour and in vivo cytotoxic activities were determined using potato disc assay (PDA) and brine shrimp lethality assay, respectively. Three human carcinoma cell lines (KBM5, SCC4 and U266) were incubated with different doses (10-100 μg/mL) of extracts and the anticancer activity was estimated by MTT assay. NF-κB suppressing activity was determined using electrophoretic mobility shift assay (EMSA). Chemical composition of the three extracts was identified by GC-MS. Total phenolic and flavonoid contents were measured by colorimetric assays. Results and discussions The order of antioxidant activity of three extracts was methanol > chloroform > hexane. The IC50 values ranged from 22.73 to 51.65 μg/mL for KBM5; 22.82 to 70.25 μg/mL for SCC4 and 20.97 to 89.55 μg/mL for U266 cells. The hexane extract exhibited potent antitumour (IC50  value = 65.02 μg/mL) and cytotoxic (LC50  value = 32.18 μg/mL) activities. This extract also completely inhibited the TNF-α induced NF-κB activation in KBM5 cells. GC-MS results showed that pyrogallol, palmitic acid and vitamin E were the major components of methanol, chloroform and hexane extracts. We observed significant (p < 0.05) difference in total phenolic and flavonoid contents of different solvent extracts. Conclusion The present study demonstrates that P. guajava leaf extracts play a substantial role against cancer and down-modulate inflammatory nuclear factor kB.

Topics: Animals; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Artemia; Biphenyl Compounds; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Electrophoretic Mobility Shift Assay; Gas Chromatography-Mass Spectrometry; Humans; Inhibitory Concentration 50; Lethal Dose 50; Neoplasms; NF-kappa B; Palmitic Acid; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Psidium; Pyrogallol; Solvents; Vitamin E

Bergenia ciliata (locally known as Zakhm-e-hayat; wound healer) is commonly employed for wound healing, curing diarrhea and vomiting, fever, cough and pulmonary affections. Local community uses this plant as tea decoction with table salt. B. ciliata crude extract and its fractions were subjected to antibacterial, antioxidant effects as well as determination of total flavonoids and phenolics, DNA damage and anticancerous activities following standard protocols. Increased percentage inhibition of free radical in DPPH assay as well as elevated phenolic and flavonoid contents revealed antioxidant potential of this potent herb. Ethyl acetate and aqueous extracts showed IC(50) of 0.7 and 0.3 mg/ml respectively, against H157 cell line. Antibacterial analysis showed MIC 0.4-10mg/ml for crude extract and fractions. The results obtained conclude that extracts of B. ciliata contain remedial latent and can be used as possible source for drug development by pharmaceutical industries.

Topics: Acetates; Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Bacteria; Biphenyl Compounds; Cell Line, Tumor; Cell Survival; Chemical Fractionation; Dose-Response Relationship, Drug; Humans; Inhibitory Concentration 50; Microbial Sensitivity Tests; Neoplasms; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rhizome; Saxifragaceae; Water

The synthesis of derivatives of 4-Methylumbelliferone (4-MUs), which are structurally interesting antioxidants, was performed in this study. The modification of 4-Methylumbelliferone (4-MU) by different reaction steps was performed to yield the target compounds, the 4-MUs. The 4-MUs were characterized by different spectroscopic techniques (Fourier transform infrared; FT-IR and Nuclear magnetic resonance; NMR) and micro-elemental analysis (CHNS). The in vitro antioxidant activity of the 4-MUs was evaluated in terms of their free radical scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH), Nitric oxide radical scavenging activity assay, chelating activity and their (FRAP) ferric-reducing antioxidant power, which were compared with a standard antioxidant. Our results reveal that the 4-MUs exhibit excellent radical scavenging activities. The antioxidant mechanisms of the 4-MUs were also studied. Density Function Theory (DFT)-based quantum chemical studies were performed with the basis set at 3-21G. Molecular models of the synthesized compounds were studied to understand the antioxidant activity. The electron levels, namely HOMO (highest occupied molecular orbital) and LUMO (lowest unoccupied molecular orbital), for these synthesized antioxidants were also studied.

Topics: Biphenyl Compounds; Cell Line, Tumor; Free Radical Scavengers; Humans; Hydrogen Peroxide; Hymecromone; Models, Molecular; Neoplasms; Nitric Oxide; Nuclear Magnetic Resonance, Biomolecular; Oxidation-Reduction; Picrates; Spectroscopy, Fourier Transform Infrared; Triazines

Pyridazinones are widely recognized as versatile scaffolds with a wide spectrum of biological activities. In the present work, a series of new 4-chloro-2-(3-chloro-4-fluorophenyl)-5-(aliphatic/cyclic saturated amino)pyridazin-3(2H)-one derivatives 4a-i were synthesized and characterized by spectral techniques. The inhibitory effects of the synthesized compounds 4a-i on the viability of three human cancer cell lines, HEP3BPN 11 (liver), MDA 453 (breast), and HL 60 (leukemia), were assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay. Among the compounds 4a-i screened, 4g and 4i exhibited inhibitory activity very close to the standard methotrexate; therefore, these lead compounds were further tested for their potential to inhibit the proangiogenic cytokines involved in tumor progression. Compound 4g was found to be a potent antiangiogenic agent against TNFα, VEGF, FGFb, and TGFβ, whereas 4i showed potent antiangiogenic activity against TNFα, VEGF, FGFb, and leptin. All the compounds 4a-i were screened for their antioxidant activities using 2,2-diphenyl-1-picryl hydrazine (DPPH), OH, and superoxide anion radicals. Compound 4f showed better OH radical scavenging activity than the standard ascorbic acid.

Topics: Angiogenesis Inhibitors; Angiogenic Proteins; Antioxidants; Biphenyl Compounds; Cell Survival; Dose-Response Relationship, Drug; Drug Design; Female; HL-60 Cells; Humans; Molecular Structure; Neoplasms; Picrates; Pyridones; Structure-Activity Relationship; Superoxides

Cancer is an unnatural type of tissue growth in which the cells exhibit unrestrained division, leading to a progressive increase in the number of dividing cells. It is now the second largest cause of death in the world. The present study concerned antioxidant, anticancer and anticholinesterase activities and protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in methanol extracts of flowers, fruits and seeds of Hypericum amblysepalum.. Antioxidant properties including free radical scavenging activity and reducing power, and amounts of total phenolic compounds were evaluated using different tests. Protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in extracts were determined by HPLC. Cytotoxic effects were determined using the MTT test with human cervix cancer (HeLa) and rat kidney epithelium cell (NRK-52E) lines. Acetyl and butyrylcholinesterase inhibitory activities were measured by by Ellman method.. Total phenolic content of H. amblysepalum seeds was found to be higher than in fruit and flower extracts. DPPH free radical scavenging activity of the obtained extracts gave satisfactory results versus butylated hydroxyanisole and butylated hydroxytoluene as controls. Reducing power activity was linearly proportional to the studied concentration range: 10-500 μg/ mL LC50 values for H. amblysepalum seeds were 11.7 and 2.86 respectively for HeLa and NRK-52E cell lines. Butyryl-cholinesterase inhibitory activity was 76.9±0.41 for seed extract and higher than with other extracts.. The present results suggested that H. amblysepalum could be a potential candidate anti-cancer drug for the treatment of human cervical cancer, and good source of natural antioxidants.

Topics: Acetylcholinesterase; Animals; Antineoplastic Agents; Antioxidants; Biphenyl Compounds; Butyrylcholinesterase; Cell Proliferation; Cells, Cultured; Cholinesterase Inhibitors; Chromatography, High Pressure Liquid; Flowers; Free Radical Scavengers; Fruit; HeLa Cells; Humans; Hypericum; Neoplasms; Picrates; Plant Extracts; Rats; Seeds

Mangifera pajang Kosterm is a plant species from the mango family (Anacardiaceae). The fruits are edible and have been reported to have high antioxidant content. However, the detailed phytochemical studies of the plant have not been reported previously. This study investigates the phytochemicals and biological activities of different parts of Mangifera pajang.. The plant samples were extracted with solvents of different polarity to obtain the crude extracts. The isolated compounds were characterized using spectroscopic methods. The extracts and isolated compounds were subjected to cytotoxicity tests using human breast cancer (MCF-7), human cervical cancer (HeLa) and human colon cancer (HT-29) cells. The free radical scavenging activity test was conducted using the DPPH assay. Antimicrobial activity tests were carried out by using the disc diffusion method.. Phytochemical investigation on the kernel, stem bark and leaves of Mangifera pajang led to the isolation of methyl gallate (1), mixture of benzaldehyde (2) and benzyl alcohol (3), mangiferonic acid (4), 3β-hydroxy-cycloart-24-ene-26-oic acid (5), 3β,23-dihydroxy-cycloart-24-ene-26-oic acid (6), lupeol(7) lupenone(8), β-sitosterol(9), stigmasterol(10), trans-sobrerol(11) and quercitrin (12). Crude ethyl acetate and methanol extracts from the kernel indicated strong cytotoxic activity towards MCF-7 and HeLa cells with IC50 values of less than 10 μg/mL, while petroleum ether, chloroform and ethyl acetate extracts of the stem bark showed strong to moderate activity against MCF-7, HeLa and HT-29 cancer cell lines with IC50 values ranging from 5 to 30 μg/mL. As for the antimicrobial assays, only the ethyl acetate and methanol extracts from the kernel displayed some inhibition against the microbes in the antibacterial assays. The kernel extracts showed highest free radical scavenging activity with IC50 values of less than 10 μg/mL, while the ethyl acetate and methanol extracts of leaves displayed only weak activity in the DPPH assays.. Phytochemical investigations on various parts of Mangifera pajang have identified terpenoids and a flavonol derivative as major constituents. Bioassay studies have indicated that the crude extracts and isolated compounds have potential as naturally-derived anticancer and antimicrobial agents, besides possess high free radical scavenging activity.

Topics: Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Flavonols; Fruit; HeLa Cells; HT29 Cells; Humans; Mangifera; MCF-7 Cells; Neoplasms; Phytochemicals; Phytotherapy; Picrates; Plant Extracts; Plant Structures; Terpenes

Rosa rugosa petals are used for production of teas, jams, wines and juices. Despite the wide availability of rose cultivars, comprehensive information on petal chemical composition and healthful properties is still lacking. Therefore, the aim of this study was analysis of cytotoxic, antioxidant and antimicrobial activity and chemical composition of rugosa rose petals.. Petals of R. rugosa were evaluated for their cytotoxic effect against cervical (HeLa) and breast cancer (T47D) cell lines and for antiradical activity (with DPPH•). As a result, significant cytotoxic (up to 100% of dead cells) and antiradical properties (IC₅₀ 1.33-0.08 mg mg⁻¹ DPPH•) were demonstrated. Moreover, notable antimicrobial activity against eight bacterial (i.e. Staphylococcus. epidermidis, S. aureus, Bacillus subtilis, Micrococcus luteus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus mirabilis) and two yeast strains (Candida. albicans, C. parapsilosis) was shown. Total phenolic, flavonoid, phenolic acid, tannin, carotenoid and polysaccharide content in petals was determined using spectrophotometric methods. Liquid chromatography-electrospray ionization-tandem mass spectrometry was used to thoroughly analyze phenolic acids and flavonoid glycosides in the methanolic extract and fractions obtained after its separation. Five phenolic acids and six flavonoids previously not reported in the plant material were identified.. This is the first such detailed report on chemical composition and biological activity of R. rugosa petals.

Topics: Anti-Bacterial Agents; Anti-Infective Agents; Antifungal Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Bacteria; Biphenyl Compounds; Breast Neoplasms; Candida; Female; Flavonoids; Flowers; Glycosides; HeLa Cells; Humans; Neoplasms; Phenols; Phytotherapy; Picrates; Plant Extracts; Rosa; Uterine Cervical Neoplasms

The methanolic extract obtained from the root portion of Caltha palustris var. alba was evaluated for its anthelmintic efficacy against gastrointestinal nematodes of sheep under both in vitro and in vivo conditions using worm motility inhibition (WMI) assay and fecal egg count reduction (FECR) assay, respectively. The extract was subjected to antimicrobial activity using agar-well diffusion method against different bacterial strains. In addition the extract was evaluated for cytotoxic and antioxidant activity against cultured THP-1(Leukemia), A-549 (Lung), HCT-15 (Colon), Cervix (HeLa) and PC-3(Prostrate) cell lines by SRB and DPPH radical scavenging assays. The extract used resulted in mean %WMI of 94.44%, as observed when the worms were put in lukewarm buffer for 30 min after exposure to different treatments. The mean mortality index of the sample was 0.95. The lethal concentration (LC50) was 0.11 mg·mL(-1). Cell lines were exposed to concentration of 100 μg·mL(-1) of extract for 48 h, which reduced the viability of these cell lines. The same plant extract also showed 55.58% DPPH radical scavenging activity.

Topics: Animals; Anthelmintics; Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Bacteria; Biphenyl Compounds; Feces; Gastrointestinal Tract; HeLa Cells; Humans; Nematoda; Neoplasms; Phytotherapy; Picrates; Plant Extracts; Ranunculaceae; Sheep

Elaeocarpus floribundus is higher plant that has been used as traditional medicine for treating several diseases. There is no previous report on phytochemicals and bioactivity studies of this species. In this investigation, triterpenoids friedelin, epifriedelanol and β-sitosterol were isolated from its leaves and stem bark. Determination of total phenolic content of methanolic extract of leaves and stem bark was carried out using Folin-Ciocalteu reagent. All extracts and isolated compounds were subjected to screening of antioxidant activity using DPPH free radical scavenging method and cytotoxic activities by MTT assay towards human T4 lymphoblastoid (CEM-SS) and human cervical (HeLa) cancer cells. In the total phenolic content determination, methanolic extract of leaves gave higher value of 503.08±16.71 mg GAE/g DW than stem bark with value of 161.5±24.81 mg GAE/g DW. Polar extracts of leaves and stem bark possessed promising antioxidant activity with methanol extract of stem bark exhibited strongest activity with IC50 value of 7.36±0.01 μg/ml. In the cytotoxic activity assay, only chloroform extract of leaves showed significant activity with IC50 value of 25.6±0.06 μg/ml against CEM-SS cancer cell, while friedelin and epifriedelanol were found to be active against the two cancer cells with IC50 values ranging from 3.54 to 11.45 μg/ml.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Cell Survival; Chloroform; Dose-Response Relationship, Drug; Elaeocarpaceae; HeLa Cells; Humans; Inhibitory Concentration 50; Methanol; Neoplasms; Phenols; Picrates; Plant Bark; Plant Extracts; Plant Leaves; Plants, Medicinal; Solvents; Terpenes

Eight new dihydrobenzofuran neolignans, pinnatifidanin C I-VIII (1-8), together with two known analogs (9-10) were isolated from the seeds of Crataegus pinnatifida. Their structures were elucidated by spectroscopic analyses, especially 1D, 2D NMR and CD spectra. The cytotoxic activities of all isolates against human cancer cell lines were assayed, and most interestingly, compound 10 revealed preferred cytotoxicity on the HT-1080 cell line and displayed much stronger inhibitory activity (IC50=8.86 μM) compared with positive control 5-fluorouracil (IC50=35.62 μM). Meanwhile, antioxidant activities of all the isolates were evaluated using 2,2-diphenyl-1-pikrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays, and the results showed that most of the isolates exhibited potent antioxidant activity.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Benzofurans; Benzothiazoles; Biphenyl Compounds; Cell Line, Tumor; Crataegus; Humans; Inhibitory Concentration 50; Lignans; Molecular Structure; Neoplasms; Phytotherapy; Picrates; Plant Extracts; Seeds; Sulfonic Acids

Alpinia pahangensis, a wild ginger distributed in the lowlands of Pahang, Malaysia, is used by the locals to treat flatulence. In this study, the antioxidant and cytotoxic activities of the crude aqueous methanol and fractionated extracts of Alpinia pahangensis against five different cancer and one normal cell lines were investigated. The total phenolic content of each extract and its fractions were also quantified. This is the first report on the antioxidant and cytotoxic activities of Alpinia pahangensis extract.. In the current study, the crude methanol and fractionated extract of the rhizomes of Alpinia pahangensis were investigated for their antioxidant activity using four different assays namely, the DPPH scavenging activity, superoxide anion scavenging, β-carotene bleaching and reducing power assays whilst their phenolic contents were measured by the Folin-Ciocalteu's method.In vitro neutral red cytotoxicity assay was employed to evaluate the cytotoxic activity against five different cancer cell lines, colon cancer (HCT 116 and HT-29), cervical cancer (Ca Ski), breast cancer (MCF7) and lung cancer (A549) cell lines, and one normal cell line (MRC-5). The extract that showed high cytotoxic activity was further investigated for its chemical constituents by GC-MS (gas chromatography-mass spectrometry) analysis.. The ethyl acetate fraction showed the strongest DPPH radical scavenging (0.35 ± 0.094 mg/ml) and SOD activities (51.77 ± 4.9%) whilst the methanol extract showed the highest reducing power and also the strongest antioxidant activity in the β-carotene bleaching assays in comparison to other fractions. The highest phenolic content was found in the ethyl acetate fraction, followed by the crude methanol extract, hexane and water fractions. The results showed a positive correlation between total phenolic content with DPPH radical scavenging capacities and SOD activities. The hexane fraction showed potent cytotoxic effect against KB, Ca Ski and HCT 116 cell lines with IC₅₀ of 5.8 ± 0.1 and 9.1 ± 2.0 ug/ml, respectively. The major components of hexane fraction analysed by GC-MS analysis were mostly methyl esters.. The current study suggests that the methanol extract and ethyl acetate fraction of A. pahangensis is a potential source of natural antioxidant for protective as well as prevention of life-threatening diseases. The hexane fraction of A. pahangensis may have the potential to be developed into therapeutic option for treating cancer.

Topics: Alpinia; Analysis of Variance; Antioxidants; beta Carotene; Biphenyl Compounds; Cell Line, Tumor; Cell Survival; Gas Chromatography-Mass Spectrometry; HCT116 Cells; HT29 Cells; Humans; MCF-7 Cells; Neoplasms; Neutral Red; Oxidation-Reduction; Phenols; Picrates; Plant Extracts; Rhizome; Superoxides

This study aimed to evaluate the variations of the chemical composition and bioactivity of essential oils of Liquidambar styraciflua L. (Altingiaceae) collected in different seasons.. The oils were analysed by GLC/FID and GLC/MS. The antioxidant activity was investigated by diphenylpicrylhydrazyl (DPPH) and superoxide anion radical scavenging assays and the deoxyribose degradation assay. Inhibition of both 5-lipoxygenase (5-LOX) and prostaglandin E2 (PGE2) production in hepatic cancer (HepG-2) cells were used to assess the anti-inflammatory activity. The cytotoxic activity was investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.. Altogether, 64 volatile secondary metabolites were identified. The major components of the leaf oil were d-limonene, α-pinene and β-pinene, and of the stem oil were germacrine D, α-cadinol, d-limonene, α-pinene, and β-pinene. Leaf and stem oils collected in spring could reduce DPPH● (IC50 = 3.17 and 2.19 mg/ml) and prevent the degradation of the deoxyribose sugar (IC50 = 17.55 and 14.29 μg/ml). The stem oil exhibited a higher inhibition of both 5-LOX and PGE2 than the leaf oil. The cytotoxic activity of leaf and stem oils was low in cancer cell lines (IC50 = 136.27 and 119.78 μg/ml in cervical cancer (HeLa) cells).. Essential oils of L. styraciflua exhibited an interesting anti-inflammatory activity with low cytotoxicity, supporting its traditional use to treat inflammation.

Topics: Anti-Inflammatory Agents; Antioxidants; Arachidonate 5-Lipoxygenase; Bicyclic Monoterpenes; Biphenyl Compounds; Bridged Bicyclo Compounds; Cyclohexenes; Deoxyribose; Dinoprostone; HeLa Cells; Hep G2 Cells; Humans; Limonene; Liquidambar; Monoterpenes; Neoplasms; Oils, Volatile; Picrates; Plant Extracts; Plant Leaves; Plant Stems; Sesquiterpenes, Germacrane; Superoxides; Terpenes

An efficient one-pot syntheses of aryl-3,3'-bis(indolyl)methanes (BIMs) from indole/2-methylindole and formylphenoxyaliphatic acid(s) is described. Esterification of carboxylic acid and aromatic electrophilic substitution reactions are achieved simultaneous in the presence of potash alum as a catalyst. This catalyst could be recovered and reused without substantial loss in its catalytic activity and the methodology could be applied on a range of closely related substrates. The solvation characteristics in ground and excited states of the compounds by monitoring the absorbance and fluorescence band maxima have been studied. The fluorescence studies in protic and aprotic solvents were rationalized on the basis of solute-solvent interaction and substituents effect on these photophysical processes analyzed. The compounds prepared showed efficient antimicrobial effect against human pathogens, cytotoxicity against A431 cell line, and DPPH radical scavenging effect. Single crystal XRD studies have been carried out for a few compounds synthesized in this work.

Topics: Anti-Infective Agents; Antineoplastic Agents; Antitubercular Agents; Bacteria; Bacterial Infections; Biphenyl Compounds; Cell Line, Tumor; Cell Survival; Chemistry Techniques, Synthetic; Crystallography, X-Ray; Free Radical Scavengers; Fungi; Humans; Indoles; Models, Molecular; Mycoses; Neoplasms; Picrates; Spectrometry, Fluorescence

A new linderone A, namely 2-cinnamoyl-3-hydroxy-4, 5-dimethoxycyclopenta-2, 4-dienone (5), together with three known flavonoids (1-3) and one linderone (4), were isolated from the bark of Lindera oxyphylla. Extensive spectroscopic analysis including 1D and 2D-NMR spectra determined their sturctures. In addition, the antioxidant activity of all the compounds has been determined using 2, 2-diphenyl-1-picrylhydrazyl radical scavenging (DPPH), ferric reducing antioxidant power (FRAP) and ferrous ion chelating (FIC) methods. Compound 3 showed excellent DPPH scavenging activity with IC50% value of 8.5 ± 0.004% (μg/mL) which is comparable with vitamin C. This compound, also showed an absorbance value of 1.00 ± 0.06% through FRAP test when compared with Butyl Hydroxy Aniline (BHA). However, FIC showed low activity for all the isolated compounds (chelating activity less than 50%) in comparison with ethylene diamine tetra acetic acid (EDTA). Anticancer activity for all compounds has also been measured on A375 human melanoma, HT-29 colon adenocarcinoma, MCF-7 human breast adenocarcinoma cells, WRL-68 normal hepatic cells, A549 non-small cell lung cancer cells and PC-3 prostate adenocarcinoma cell line. Compound 1 showed A549=65.03%, PC-3=30.12%, MCF-7=47.67, compound 2 showed PC-3=90.13%, compound 3 showed MCF-7=79.57 and for compound 5 MCF-7 is 96.33.

Topics: Antineoplastic Agents; Antioxidants; Biphenyl Compounds; Cell Line; Cell Line, Tumor; Cell Survival; Chelating Agents; Flavonoids; Free Radicals; Humans; Lindera; Neoplasms; Picrates

Annona dioica St. Hill (Annonacaeae) is a Brazilian plant used in folk medicine for the treatment of several types of rheumatisms and diarrhoea. The focus of this work was to evaluate the in vitro antiproliferative and antioxidant activity and the in vivo hypoglycaemic and anti-inflammatory activity of A. dioica and identify the principal constituents of this plant.. The crude methanol extract (EAD) and hexane (HF), chloroform (CF), ethyl acetate (EAF) and hydromethanol fractions (HMF) were evaluated for free radical scavenging activity using the DPPH assay. The EAD and EAF were assayed for hypoglycaemic activity in rats. The EAD was tested in an antiproliferation assay and for anti-inflammatory effects in paw oedema, in addition to myeloperoxidase activity induced by carrageenan (Cg) in mice. The EAF was assayed using chromatographic methods.. The fractionation of the EAF through chromatographic methods identified derivatives of the flavonoids quercetin and kaempferol. Among all the tested fractions, the ethyl acetate and hydromethanol fractions were the most potent, exhibiting an IC50 of 8.53 and 10.57 μg/mL, respectively, which is comparable to that of the commercial antioxidant butylated hydroxytoluene (BHT). The oral administration of the EAD (100 mg/kg) and EAF (15 mg/kg) inhibited the increase of glucose levels, resulting in a hypoglycaemic effect. The EAD (30 to 300 mg/kg) exhibited an anti-oedematogenic effect in Cg-induced paw oedema in a time- and dose-dependent manner. The results showed a reduction of MPO activity by A. dioica 6 h after the induction of paw oedema at all doses tested with maximal inhibition at 300 mg/kg.. Our results reveal for the first time that compounds contained in the A. dioica leaves exert anti-inflammatory, hypoglycaemic, antiproliferative, and antioxidant effects. The antioxidant activity may be associated with the presence of flavonoids.

Topics: Animals; Annona; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Biphenyl Compounds; Blood Glucose; Carrageenan; Cell Line, Tumor; Dose-Response Relationship, Drug; Edema; Free Radical Scavengers; Hypoglycemic Agents; Inhibitory Concentration 50; Kaempferols; Male; Mice; Neoplasms; Peroxidase; Phytotherapy; Picrates; Plant Extracts; Quercetin; Rats; Rats, Wistar

The commercial development of plants as sources of antioxidants that can be used to enhance the properties of foods, for nutritional purposes and preservation as well as for prevention of oxidation-related diseases, is currently of major interest. Rosehip (Rosa canina L.) is a rich source of vitamin C and polyphenols.. Phytochemicals in rosehip tea were separated into three fractions: Fr1 (vitamin C, 39.17 mg kg(-1)), Fr2 (flavonoids, 451.05 µg kg(-1)) and Fr3 (phenolic acids, 504.69 µg kg(-1)). Quercetin and ellagic acid were the most abundant polyphenolic compounds. Rosehip fractions, primarily rosehip flavonoids (EC(50) = 49 mg L(-1)), showed high antioxidant activity towards 2,2-diphenyl-1-picrylhydrazyl radicals (DPPH(•)). Cell growth effects of rosehip fractions were assessed in HeLa, MCF7 and HT-29 cell lines, with the lowest IC(50) values being determined for rosehip flavonoids, (80.63, 248.03 and 363.95 mg L(-1) respectively). However, the vitamin C fraction did not inhibit the growth of tested tumour cells.. The results of this study confirm that vitamin C and flavonoids are responsible for the antioxidant activity of rosehip tea, while only polyphenols contribute to its antiproliferative activity.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Ascorbic Acid; Biphenyl Compounds; Cell Line, Tumor; Ellagic Acid; Flavonoids; Free Radicals; Fruit; HeLa Cells; Humans; Inhibitory Concentration 50; Neoplasms; Phytotherapy; Picrates; Plant Extracts; Polyphenols; Quercetin; Rosa

Twenty-nine phenolic compounds were isolated from the root bark of fresh (Yunnan) ginger and their structures fully characterized. Selected compounds were divided into structural categories and twelve compounds subjected to in-vitro assays including DPPH radical scavenging, xanthine-oxidase inhibition, monoamine oxidase inhibition, rat-brain homogenate lipid peroxidation, and rat pheochromocytoma PC12 cell and primary liver cell viability to determine their antioxidant and cytoprotective properties. Isolated compounds were also tested against nine human tumor cell lines to characterize anticancer potency. Several diarylheptanoids and epoxidic diarylheptanoids were effective DPPH radical scavengers and moderately effective at inhibiting xanthine oxidase. An enone-dione analog of 6-shogaol (compound 2) was isolated and identified to be most effective at protecting PC12 cells from H₂O₂-induced damage. Almost all tested compounds inhibited lipid peroxidation. Three compounds, 6-shogaol, 10-gingerol and an enone-diarylheptanoid analog of curcumin (compound 6) were identified to be cytotoxic in cell lines tested, with KB and HL60 cells most susceptible to 6-shogaol and the curcumin analog with IC₅₀<10 μM. QSAR analysis revealed cytotoxicity was related to compound lipophilicity and chemical reactivity. In conclusion, we observed distinct compounds in fresh ginger to have biological activities relevant in diseases associated with reactive oxygen species.

Topics: Animals; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Catechols; Curcumin; Cytoprotection; Fatty Alcohols; HL-60 Cells; Humans; Hydrogen Peroxide; Hydrophobic and Hydrophilic Interactions; KB Cells; Lipid Peroxidation; Neoplasms; PC12 Cells; Phenols; Phytotherapy; Picrates; Plant Bark; Plant Extracts; Plant Roots; Rats; Xanthine Oxidase; Zingiber officinale

The goal of this study was to evaluate the antioxidant and antiproliferative activities of 10 traditional medicinal plants, Asclepias curassavica, Ophiorrhiza mungos Linn., Cynodon dactylon (L.) Pers, Costus speciosus (J. Koenig.) Smith Costaceae, Achyranthes aspera L., Amaranthus tristis Roxb., Blepharis maderaspatensis L., Merremia emerginata Hall.f., Aegle marmelos Corr., and Tabernaemontana heyneana Wall., used in the traditional Indian system of medicine as a cure for cancer. The present study focuses on the anticancer potential of traditional medicinal plants to induce apoptosis in cancer cell lines.. Plants were sequentially extracted with hexane, ethyl acetate, and methanol. The extract was concentrated to yield the crude extract, which was tested for antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl, nitric oxide and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assays on four cancer cell lines and a normal cell line. The anticancer potential of cytotoxic extracts was determined by the Annexin-fluorescein isothiocyanate-conjugated assay in human colon adenocarcinoma cell lines (COLO 320 DM).. All the tested extracts showed significant antioxidant and antiproliferative activities in a concentration- and time-dependant manner in the following descending order: A. curassavica > C. dactylon > C. speciosus root > A. tristis > M. emarginata > O. mungos > T. Heyneana > B. maderaspatensis > A. marmelos > A. aspera.. The results of the present study support the need of further studies to isolate potential anticancer drug with cancer cell-specific cytotoxicity. Additionally, the study supports the anticancer property of medicinal plants used in the traditional Indian medicine system and further evaluation of the selected medicinal plants for an effective anticancer drug with minimal side effects.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Apoptosis; Biphenyl Compounds; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Flow Cytometry; Fluorescein-5-isothiocyanate; Humans; India; Magnoliopsida; MCF-7 Cells; Medicine, East Asian Traditional; Neoplasms; Nitric Oxide; Picrates; Plant Extracts; Tetrazolium Salts; Thiazoles

The in vitro antiproliferative and antioxidant activities of the aqueous, chloroform and methanol extracts of Muntingia calabura leaves were determined in the present study. Assessed using the 3,(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay, the aqueous and methanol extracts of M. calabura inhibited the proliferation of MCF-7, HeLa, HT-29, HL-60 and K-562 cancer cells while the chloroform extract only inhibited the proliferation of MCF-7, HeLa, HL-60 and K-562 cancer cells. Interestingly, all extracts of M. calabura, which failed to inhibit the MDA-MB-231 cells proliferation, did not inhibit the proliferation of 3T3 (normal) cells, indicating its safety. All extracts (20, 100 and 500 μg/ml) were found to possess antioxidant activity when tested using the DPPH radical scavenging and superoxide scavenging assays with the methanol, followed by the aqueous and chloroform, extract exhibiting the highest antioxidant activity in both assays. The total phenolic content for the aqueous, methanol and chloroform extracts were 2970.4 ± 6.6, 1279.9 ± 6.1 and 2978.1 ± 4.3 mg/100 g gallic acid, respectively. In conclusion, the M. calabura leaves possess potential antiproliferative and antioxidant activities that could be attributed to its high content of phenolic compounds, and thus, needs to be further explored.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Cell Line, Tumor; Cell Proliferation; Elaeocarpaceae; HeLa Cells; Humans; Neoplasms; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves

Arctium lappa, known as burdock, is widely used in popular medicine for hypertension, gout, hepatitis and other inflammatory disorders. Pharmacological studies indicated that burdock roots have hepatoprotective, anti-inflammatory, free radical scavenging and antiproliferative activities. The aim of this study was to evaluate total phenolic content, radical scavenging activity by DPPH and in vitro antiproliferative activity of different A. lappa root extracts.. Hot and room temperature dichloromethanic, ethanolic and aqueous extracts; hydroethanolic and total aqueous extract of A. lappa roots were investigated regarding radical scavenging activity by DPPH, total phenolic content by Folin-Ciocalteau method and antiproliferative in vitro activity was evaluated in human cancer cell lines. The hydroethanolic extract analyzed by high-resolution electrospray ionization mass spectroscopy.. Higher radical scavenging activity was found for the hydroethanolic extract. The higher phenolic contents were found for the dichloromethane, obtained both by Soxhlet and maceration extraction and hydroethanolic extracts. The HRESI-MS demonstrated the presence of arctigenin, quercetin, chlorogenic acid and caffeic acid compounds, which were identified by comparison with previous data. The dichloromethane extracts were the only extracts that exhibited activity against cancer cell lines, especially for K562, MCF-7 and 786-0 cell lines.. The hydroethanolic extracts exhibited the strongest free radical scavenging activity, while the highest phenolic content was observed in Soxhlet extraction. Moreover, the dichloromethanic extracts showed selective antiproliferative activity against K562, MCF-7 and 786-0 human cancer cell lines.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Arctium; Biphenyl Compounds; Cell Line, Tumor; Cell Proliferation; Humans; Neoplasms; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Roots

Reactive oxygen species, along with reactive nitrogen species, may play an important role in the pathogenesis and progress of many diseases, including cancer, diabetes and sickle cell disease. It has been postulated that hydroxyurea, one of the main treatments in sickle cell disease, achieves its activity partly also through its antioxidant properties. A series of hydroxyurea derivatives of L- and D-amino acid amides and cycloalkyl-N-aryl-hydroxamic acids was synthesized and investigated for their radical scavenging activity, chelating properties and antioxidant activity. All the compounds showed exceptional antiradical activities. For example, free radical scavenging activities of investigated hydroxyureas were higher than the activity of standard antioxidant, butylated hydroxyanisole (BHA). Moreover, most of the investigated hydroxamic acids were stronger Fe²⁺ ion chelators than quercetin. In addition, the investigated compounds, especially hydroxamic acids, were proven to be excellent antioxidants. They were as effective as BHA in inhibiting β-carotene-linoleic acid coupled oxidation. It is reasonable to assume that the antioxidant activity of the investigated compounds could contribute to their previously proven biological properties as cytostatic and antiviral agents.

Topics: Anemia, Sickle Cell; beta Carotene; Biphenyl Compounds; Butylated Hydroxyanisole; Butylated Hydroxytoluene; Free Radical Scavengers; Humans; Hydroxamic Acids; Hydroxyurea; Iron; Iron Chelating Agents; Linoleic Acid; Magnetic Resonance Spectroscopy; Neoplasms; Oxidation-Reduction; Picrates; Reactive Oxygen Species; Spectrophotometry, Infrared

The aim of this study was to investigate the flavonoid composition of Scutellaria immaculata and S. ramosissima (Lamiaceae) and the in-vitro biological activity of their extracts and flavonoids.. The flavonoid composition of S. immaculata (Si) and S. ramosissima (Sr) were analysed using LC-MS. Antimicrobial activity was studied in vitro against a range of bacteria and fungi using diffusion and microdilution methods. Anti-trypanosomal and cell proliferation inhibitory activity of the extracts and flavonoids was assessed using MTT. The antioxidant activity of the flavonoids and extracts were evaluated using DPPH* test.. LC-MS investigation of Si and Sr plants allowed the identification, for the first time, of an additional 9 and 16 flavonoids, respectively. The methanol, chloroform and water extracts from these plants and six flavonoids (scutellarin, chrysin, apigenin, apigenin-7-O-glucoside, cynaroside and pinocembrine) exhibited significant inhibition of cell growth against HeLa, HepG-2 and MCF-7 cells. The chloroform extract of Sr showed potent cytotoxic effects with IC50 (drug concentration which resulted in a 50% reduction in cell viability) values of 9.25 ± 1.07 µg/ml, 12.83 ± 1.49 µg/ml and 17.29 ± 1.27 µg/ml, respectively. The highest anti-trypanosomal effect against T. b. brucei was shown by the chloroform extract of Sr with an IC50 (drug concentration which resulted in a 50% inhibition of the biological activity) of 61 µg/ml. The pure flavonoids showed an IC50 range between 3 and 29 µm, with cynaroside as the most active compound with an IC50 value of 3.961 ± 0.133 µm. The chloroform extract of Sr has potent antimicrobial activity against Streptococcus pyogenes (minimum inhibitory concentration, MIC = 0.03 mg/ml). Pinocembrine exhibited a strong activity against the all bacteria except Escherichia coli and yeasts. Water extracts of Sr and Si exhibited potent antioxidant activity with IC50 values of 5.62 ± 0.51 µg/ml and 3.48 ± 0.02 µg/ml, respectively. Scutellarin exerted stronger antioxidant activity than other flavonoids.. This is the first study reporting an in-vitro biological investigation for Si and Sr. Especially the chloroform extract of Sr showed potent anticancer and antimicrobial activity. Cynaroside had a highly selective and strong cytotoxicity against T. b. brucei while showing only mild effects against cancer cells.

Topics: Anti-Infective Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Apigenin; Bacteria; Biphenyl Compounds; Flavonoids; Glucosides; Glucuronates; HeLa Cells; Humans; Inhibitory Concentration 50; Luteolin; Neoplasms; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Plant Roots; Scutellaria; Trypanocidal Agents; Trypanosoma brucei brucei; Yeasts

Chemical investigation of the 1-BuOH soluble fraction of the dried fruits of Myrsine seguinii (Myrsinaceae) led to the isolation of five new glycosides, named myrseguinosides A-E (1-5), together with eight known compounds (6-13). The absolute structures of the new glycosides were elucidated by spectroscopic and chemical analyses to be a monoterpene glucoside (1), two flavonol glycosides (2, 3), and two oleanane-type triterpene saponins (4, 5). Myrseguinosides B (2), D (4), and E (5) exhibited 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity and growth inhibitory activity toward human cancer cells, respectively.

Topics: Anticarcinogenic Agents; Biphenyl Compounds; Cell Line, Tumor; Drug Screening Assays, Antitumor; Formazans; Fruit; Glycosides; HL-60 Cells; Humans; Inhibitory Concentration 50; Molecular Structure; Neoplasms; Phytotherapy; Picrates; Plant Extracts; Primulaceae; Structure-Activity Relationship; Tetrazolium Salts

Within a project focusing on the chemopreventive potential of algal phenols, two phloroglucinol derivatives, belonging to the class of fucophlorethols, and the known fucotriphlorethol A were obtained from the ethanolic extract of the brown alga Fucus vesiculosus L. The compounds trifucodiphlorethol A and trifucotriphlorethol A are composed of six and seven units of phloroglucinol, respectively. The compounds were examined for their cancer chemopreventive potential, in comparison with the monomer phloroglucinol. Trifucodiphlorethol A, trifucotriphlorethol A as well as fucotriphlorethol A were identified as strong radical scavengers, with IC(50) values for scavenging of 1,1-diphenyl-2 picrylhydrazyl radicals (DPPH) in the range of 10.0-14.4 microg/ml. All three compounds potently scavenged peroxyl radicals in the oxygen radical absorbance capacity (ORAC) assay. In addition, the compounds were shown to inhibit cytochrome P450 1A activity with IC(50) values in the range of 17.9-33 microg/ml, and aromatase (Cyp19) activity with IC(50) values in the range of 1.2-5.6 microg/ml.

Topics: Animals; Antineoplastic Agents, Phytogenic; Antioxidants; Aromatase Inhibitors; Biphenyl Compounds; Cell Line, Tumor; Cytochrome P-450 Enzyme Inhibitors; Fucus; Humans; Inhibitory Concentration 50; Mice; Neoplasms; Phenyl Ethers; Phloroglucinol; Picrates; Plant Extracts; Terphenyl Compounds

Phenolic compounds, named integracin D (1), (7'R, 8'S, 8S)-8-hydroxyisoguaiacin (3), (2R, 3R) pinobanksin-3-caffeoylate (5) and threo-8S-7-methoxysyringylglycerol (6), respectively, were isolated from the Chinese mangrove plant Laguncularia racemosa (L) Gaertn. f. (Combretaceae), together with 23 known phenolic metabolites. Their structures were elucidated on the basis of extensive spectroscopic analyses including that of IR, UV, MS, CD, 1D and 2D NMR spectra as well as by comparison with literature data. Compound 5 showed significant anti-oxidative activity in the DPPH and TEAC free-radical-scavenging assays, while several of the phenolic compounds were tested for protein kinase inhibitory activity in an assay involving 24 different human tumor related protein kinases. Compounds 5, 7, and 23 showed potential inhibition with IC(50) values between 2.2 and 3.6microg/mL toward individual kinases. The ellagic acid derivatives were tested for insecticidal activity.

Topics: Animals; Antioxidants; Biphenyl Compounds; Cell Line, Tumor; Combretaceae; Humans; Models, Molecular; Molecular Conformation; Neoplasms; Phenol; Picrates; Protein Kinase Inhibitors; Rats; Spodoptera

Blechnum orientale Linn. (Blechnaceae) is used ethnomedicinally for the treatment of various skin diseases, stomach pain, urinary bladder complaints and sterilization of women. The aim of the study was to evaluate antioxidant, anticancer and antibacterial activity of five solvent fractions obtained from the methanol extract of the leaves of Blechnum orientale Linn.. Five solvent fractions were obtained from the methanol extract of B. orientale through successive partitioning with petroleum ether, chloroform, ethyl acetate, butanol and water. Total phenolic content was assessed using Folin-Ciocalteu's method. The antioxidant activity was determined by measuring the scavenging activity of DPPH radicals. Cytotoxic activity was tested against four cancer cell lines and a non-malignant cell using MTT assay. Antibacterial activity was assessed using the disc diffusion and broth microdilution assays. Standard phytochemical screening tests for saponins, tannins, terpenoids, flavonoids and alkaloids were also conducted.. The ethyl acetate, butanol and water fractions possessed strong radical scavenging activity (IC50 8.6-13.0 microg/ml) and cytotoxic activity towards human colon cancer cell HT-29 (IC50 27.5-42.8 microg/ml). The three extracts were also effective against all Gram-positive bacteria tested: Bacillus cereus, Micrococcus luteus, methicillin-susceptible Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA) and Stapylococcus epidermidis(minimum inhibitory concentration MIC 15.6-250 mug/ml; minimum bactericidal concentration MBC 15.6-250 microg/ml). Phytochemical analysis revealed the presence of flavonoids, terpenoids and tannins. Ethyl acetate and butanol fractions showed highest total phenolic content (675-804 mg gallic acid equivalent/g).. The results indicate that this fern is a potential candidate to be used as an antioxidant agent, for colon cancer therapy and for treatment of MRSA infections and other MSSA/Gram-positive bacterial infectious diseases.

Topics: Adenocarcinoma; Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Cell Line; Cell Line, Tumor; Colonic Neoplasms; Ferns; Flavonoids; Free Radical Scavengers; Gram-Positive Bacteria; Humans; Microbial Sensitivity Tests; Neoplasms; Phenols; Picrates; Plant Leaves; Tannins; Terpenes

Pectin was dissolved in deionized distilled water (2%, vol/vol) and irradiated at 20 kGy using a Co-60 gamma ray irradiator. The resulting solution was dialyzed and lyophilized. The samples were separated into three groups to estimate their antioxidant and cancer cell proliferation effects: non-irradiated (0 kGy), irradiated (20 kGy), and dialyzed (20 kGy-F, mol wt <10,000) samples. Antioxidant properties of each treatment was tested by a beta-carotene-linoleic acid bleaching assay and electron donating ability and compared for antioxidant index, which indicated that the activity was higher in the order of 20 kGy-F > 20 kGy > 0 kGy. Spleen cell survival effect of the irradiated pectin (20 kGy) and dialyzed (20 kGy-F) samples was higher than the non-irradiated control (0 kGy). The pectins inhibited growth of the cancer cell in the order of 20 kGy- F > 20 kGy > 0 kGy. The Ames test revealed that none of the fractions was mutagenic, and there was no indication of a dose-dependent response for any of the samples. These results suggest that a functional pectin oligosaccharide can be produced by irradiation for the food industry without any chemical treatment.

Topics: Antioxidants; beta Carotene; Biphenyl Compounds; Cell Division; Cell Line, Tumor; Citrus; Free Radical Scavengers; Fruit; Gamma Rays; Humans; Linoleic Acid; Mutagenicity Tests; Neoplasms; Oligosaccharides; Oxidation-Reduction; Pectins; Picrates