1-1-diphenyl-2-picrylhydrazyl and thiazolyl-blue

This research aimed to compare antioxidant and anticancer activities of the essential oil from various habitats of Selaginella doederleinii Hieron. The results showed that antioxidative activities of the essential oil were the best from Guizhou province in 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) radical scavenging, ferric reducing and ferric reducing antioxidant power (FRAP), while those of the essential oil from Sichuan province were the weakest among different habitats. The anticancer results showed that antitumor effects of the essential oil from Guizhou province were the best against A549 cell line and 7721 cell line, while those of the essential oil from Sichuan province were the weakest among different habitats. Proliferative and antioxidant activities were correlated. The correlation coefficients (R2) between antioxidant and anticancer capacities varied from 0.71 to 0.94. The results of tests indicated that the antioxidant and anticancer activities of the essential oil from various habitats were great differences that might be affected by environmental variation, harvest seasons and so on. Investigation in vitro revealed that the essential oil of S. doederleinii were found to be effective in suppressing the oxidative activity and proliferation of cancer cells. This experiment provides scientific foundation for further utilization of S. doederleinii.

Topics: Antineoplastic Agents; Antioxidants; Ascorbic Acid; Benzothiazoles; Biphenyl Compounds; Butylated Hydroxytoluene; Cell Line, Tumor; Cell Proliferation; Cisplatin; Ecosystem; Humans; Oils, Volatile; Picrates; Selaginellaceae; Sulfonic Acids; Tetrazolium Salts; Thiazoles

The essential oil obtained from the fruits of hogweed (Heracleum sphondylium subsp. ternatum) growing in central Apennines (Italy) was analysed for chemical composition by gas chromatographic-flame ionisation detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). The oil was composed mainly of aliphatic esters (86.9-89.5%), among them octyl acetate (54.9-60.2%) and octyl butyrate (10.1-13.4%) were the most abundant. The oil and its two major esters, octyl acetate and octyl butyrate, were tested for in vitro biological activity, namely antibacterial, antioxidant and cytotoxic, by microdilution, DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)) and MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assays. Worthy of mention was only the cytotoxic activity of the oil against two tumour cell lines, i.e. A375 (human malignant melanoma) and HCT116 (human colon carcinoma) cells, with IC50 values of 48.69 and 95.83 μg/mL, respectively; the major compound responsible for this effect was octyl butyrate which displayed IC50 values of 20.19 μg/mL (100.8 μM) and 55.35 μg/mL (276.3 μM) on the same cells, respectively.

Topics: Acetates; Anti-Bacterial Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Benzothiazoles; Biphenyl Compounds; Drug Screening Assays, Antitumor; Enterococcus faecalis; Escherichia coli; Fruit; Gas Chromatography-Mass Spectrometry; HCT116 Cells; Heracleum; Humans; Inhibitory Concentration 50; Italy; Microbial Sensitivity Tests; Molecular Structure; Oils, Volatile; Picrates; Pseudomonas aeruginosa; Staphylococcus aureus; Sulfonic Acids; Tetrazolium Salts; Thiazoles

Resveratrol interacts with the complex III of the respiratory chain, is a radical scavenger and also suppressor of radical formation in the mitochondria. It reduces the intracellular calcium levels in pre- and postsynaptic neurons and also may inhibit the pro-apoptotic factors in glutamate overflow that occurs, e.g. in excitotoxicity. In cell cultures, glutamate overflow leads to formation of free radicals and results in apoptosis. This increase of radical concentration is enhanced by influx of cations like iron or copper ions into the cell. In present study, the beneficial action of resveratrol was investigated in glutamate-affected dissociated cultures of mice mesencephalic primary cultures. On the 10th day in vitro, 5 mM of glutamate was administered for 15 min and the cultures were further maintained in medium containing 0, 0.01, 0.1 or 1 μM of resveratrol. Resveratrol reduced glutamate-induced damages. The number of dopaminergic neurons was increased and their morphology ameliorated when resveratrol followed glutamate treatment. A significant reduction of glutamate-induced radical formation in cultures treated with resveratrol corresponded with a considerable high antioxidative potential of this stilbene determined using the DPPH assay. In addition, ICP-OES was set up to measure the tissues' copper and iron contents in organotypic cortical cultures of glutamate treated (0 or 30 μM) slices and those in which resveratrol (0, 0.01, 0.1 or 1 μM) was co-administered. Levels of copper were dose-dependently increased, and also the concentration of iron was higher in resveratrol-treated organotypic cultures. The hypothesis that resveratrol has beneficial actions against glutamate damages was verified.

Topics: Animals; Antioxidants; Biphenyl Compounds; Brain; Cells, Cultured; Coloring Agents; Copper; Ethidium; Excitatory Amino Acid Antagonists; Female; Fluorescent Dyes; Glutamic Acid; Iron; Mesencephalon; Mice; Mice, Inbred C57BL; Neurites; Neurons; Organ Culture Techniques; Picrates; Pregnancy; Propidium; Resveratrol; Spectrophotometry, Atomic; Stilbenes; Tetrazolium Salts; Thiazoles; Tyrosine 3-Monooxygenase

A potent endophytic fungus, Fusarium solani SD5 was used for exopolysaccharide (EPS) production. The isolated EPS were purified and major EPS fraction (PS-I); rhamno galactan was used to evaluate anti oxidant activities in vitro. EPS (PS-I) showed significant free radical scavenging effect on DPPH (1,1-diphenyl-2-picrylhydrazyl) and scavenging potency is indicated by IC(50) value 578.541 ± 33.256 μg/ml. EPS (PS-I) significantly induced antioxidant parameters of peritoneal macrophage cells at a concentration dependent manner and at 500 μg/ml it showed maximum protective effect against free radicals [malondialdehyde (MDA) 0.178 ± 0.015; super oxide dismutase (SOD) 41.287 ± 1.051; glutathione peroxidase (GPx) 30.182 ± 1.237; reduced glutathione (GSH) 56.892 ± 1.272; oxidized glutathione (GSSG) 8.458 ± 0.768]. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide] cytotoxicity assay indicated that EPS (PS-I) had no significant cytotoxic effect (concentration up to 500 μg/ml) on macrophage cells. Present findings suggested that the EPS (PS-I) may become a potential nontoxic exogenous antioxidant.

Topics: Animals; Ascorbic Acid; Biphenyl Compounds; Cell Survival; Cells, Cultured; Endophytes; Free Radical Scavengers; Free Radicals; Fungal Polysaccharides; Fusarium; Glutathione; Glutathione Peroxidase; Lipid Peroxidation; Macrophages, Peritoneal; Male; Malondialdehyde; Mice; Picrates; Superoxide Dismutase; Tetrazolium Salts; Thiazoles

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

Reactive oxygen species (ROS) are important mediators in a number of neurodegenerative diseases and molecules capable of scavenging ROS may be a feasible strategy for protecting neuronal cells. We previously demonstrated a powerful iron-chelating action of Guttiferone-A (GA), a naturally occurring polyphenol, on oxidative stress injuries initiated by iron overload. Here we addressed the neuroprotective potential of GA in hydrogen peroxide and glutamate-induced injury on rat's primary culture of cortical neurons and PC12 cells, respectively, and antioxidant properties concerning scavenging and anti-lipoperoxidative activities in cell-free models. The decrease in cell viability induced by each of the toxins, assessed by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] (MTT) assay, was significantly attenuated by GA. In addition, GA was found to be a potent antioxidant, as shown by (i) inhibition of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical reduction (EC50=20.0 μM), (ii) prevention against chemically or electrochemically generated superoxide radicals, (iii) inhibition of spontaneous brain lipid peroxidation and (iv) interference with the Fenton reaction. These results indicate that GA exerts neuroprotective effects against H2O2 or glutamate toxicity and its antioxidant activity, demonstrated in vitro, could be at least partly involved. They also suggest a promising potential for GA as a therapeutic agent against neurodegenerative diseases involving ROS and oxidative damage.

Topics: Animals; Benzophenones; Biphenyl Compounds; Cell Survival; Cerebral Cortex; Coloring Agents; Electrochemistry; Free Radical Scavengers; Fruit; Garcinia; Glutamic Acid; Humans; Hydrogen Peroxide; Iron; Lipid Peroxidation; Neurons; Neuroprotective Agents; PC12 Cells; Picrates; Prenylation; Rats; Reactive Oxygen Species; Tetrazolium Salts; Thiazoles

The first glycosylated isoferulic acid, isoferulic acid 3-O-beta-glucopyranoside, together with the new phenolics, tamarixetin 3,3'-di-sodium sulphate and dehydrodigallic acid dimetyl ester have been characterized from a flower extract of Tamarix aphylla. The structures were established on the basis of spectral data. The extract exhibited a distinct radical scavenging effect and to improve the viability of human keratinocytes (HaCaT cells). Also, the known isoferulic acid and ferulic acid which have been determined to be the major components of the investigated extract by HPLC/ESI mass spectrometric screening have been separated, characterized and evaluated as active antioxidants and as cell activity stimulating agents as well.

Topics: Antioxidants; Biphenyl Compounds; Cell Differentiation; Cell Line; Cell Survival; Chromatography, High Pressure Liquid; Cinnamates; Coloring Agents; Coumaric Acids; Flowers; Free Radical Scavengers; Glucosides; Humans; Keratinocytes; Methanol; Phenols; Picrates; Plant Extracts; Solvents; Spectrometry, Mass, Electrospray Ionization; Spectrophotometry, Ultraviolet; Tamaricaceae; Tetrazolium Salts; Thiazoles

The cancer chemopreventive and cytotoxic properties of 50 extracts derived from Twilight Zone (50-150 m) sponges, gorgonians and associated bacteria, together with 15 extracts from shallow water hard corals, as well as 16 fractions derived from the methanol solubles of the Twilight Zone sponge Suberea sp, were assessed in a series of bioassays. These assays included: Induction of quinone reductase (QR), inhibition of TNF-alpha activated nuclear factor kappa B (NFkappaB), inhibition of aromatase, interaction with retinoid X receptor (RXR), inhibition of nitric oxide (NO) synthase, inhibition 2,2-diphenyl-1-picrylhydrazyl radical scavenging (DPPH), and inhibition of HL-60 and MCF-7 cell proliferation. The results of these assays showed that at least 10 extracts and five fractions inhibited NFkappaB by greater than 60%, two extracts and two fractions inhibited DPPH by more than 50%, nine extracts and two fractions affected the survival of HL-60 cells, no extracts or fractions affected RXR, three extracts and six fractions affected quinone reductase (QR), three extracts and 12 fractions significantly inhibited aromatase, four extracts and five fractions inhibited nitric oxide synthase, and one extract and no fractions inhibited the growth of MCF-7 cells by more than 95%. These data revealed the tested samples to have many and varied activities, making them, as shown with the extract of the Suberea species, useful starting points for further fractionation and purification. Moreover, the large number of samples demonstrating activity in only one or sometimes two assays accentuates the potential of the Twilight Zone, as a largely unexplored habitat, for the discovery of selectively bioactive compounds. The overall high hit rate in many of the employed assays is considered to be a significant finding in terms of "normal" hit rates associated with similar samples from shallower depths.

Topics: Animals; Anthozoa; Anticarcinogenic Agents; Antineoplastic Agents; Antioxidants; Aromatase Inhibitors; Bacteria; Biphenyl Compounds; Chromatography, High Pressure Liquid; Coloring Agents; Drug Screening Assays, Antitumor; Guam; Marine Biology; NAD(P)H Dehydrogenase (Quinone); NF-kappa B; Picrates; Porifera; Retinoid X Receptors; Seawater; Tetrazolium Salts; Thiazoles; Water Microbiology

Ten South African Commiphora (Burseraceae) species were investigated to validate their use in traditional healing rites. The leaf and stem extracts of each species were analysed for the anti-oxidant (ABTS and DPPH assays), antimicrobial (MIC and death kinetic assays), anti-inflammatory (5-LOX assay), anticancer (SRB assay) properties, as well as the cytotoxic effects (tetrazolium-based assay). The best anti-oxidant activity (ABTS assay) was observed for the stem extracts of Commiphora tenuipetiolata IC(50)=5.10 microg/ml), Commiphora neglecta (IC(50)=7.28 microg/ml) and Commiphora mollis (IC(50)=8.82 microg/ml). Extracts generally exhibited poor anti-oxidant activity in the DPPH assay, with the exception of Commiphora schimperi (stem), Commiphora neglecta (stem), Commiphora tenuipetiolata (stem and leaf), and Commiphora edulis (stem), with IC(50) values ranging between 7.31 and 10.81 microg/ml. The stem extracts exhibited moderate to good 5-LOX inhibitory activity with Commiphora pyracanthoides (stem) displaying the greatest inhibitory effect (IC(50)=27.86+/-4.45 microg/ml). For the antimicrobial (MIC) assay, a greater selectivity was exhibited by the extracts against the Gram-positive bacteria (0.01-8.00 mg/ml) and the yeasts (0.25-8.00 mg/ml) than against the Gram-negative bacteria (1.00-8.00 mg/ml). Using death kinetic studies (time-kill studies), the rate at which Commiphora marlothii (stem) kills Staphylococcus aureus over a 24h period was determined. Mostly, a concentration-dependent antibacterial activity was observed beginning after ca. 30 min. All concentrations exhibited antibacterial activity, with complete bactericidal effect achieved by the 24(th) hour. The most active Commiphora species against the HT-29 cells (SRB anticancer assay) were Commiphora glandulosa (leaf and stem) and Commiphora marlothii (leaf). The MCF-7 cells (SRB anticancer assay) exhibited the highest sensitivity to indigenous Commiphora species, with Commiphora edulis (leaf and stem), Commiphora glandulosa (leaf and stem), Commiphora marlothii (leaf), Commiphora pyracanthoides (leaf and stem), Commiphora schimperi (stem), and Commiphora viminea (stem) all possessing a percentage inhibition greater than 80% at 100 microg/ml. Commiphora glandulosa (leaf and stem) and Commiphora pyracanthoides (leaf and stem) were the two most active species against the SF-268 cells (SRB anticancer assay), with IC(50) values ranging between 68.55+/-2.01 and 71.45+/-1.24 microg/ml. The majority

Topics: Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Cell Line, Tumor; Commiphora; Drug Screening Assays, Antitumor; Free Radical Scavengers; Humans; Lipoxygenase Inhibitors; Microbial Sensitivity Tests; Picrates; Plant Bark; Plant Extracts; Plant Leaves; South Africa; Tetrazolium Salts; Thiazoles

Danshensu (3-(3,4-dihydroxyphenyl) lactic acid) and salvianolic acid B, two natural phenolic acids of caffeic acid derivatives isolated from Salvia miltiorrhiza root of the most widely used traditional Chinese medicine for the treatment of various cardiovascular diseases, have been reported to have potential protective effects from oxidative injury. To better understand their biological functions, the in vitro radical scavenging and antioxidant activities of danshensu and salvianolic acid B were evaluated along with vitamin C. Both danshensu and salvianolic acid B exhibited higher scavenging activities against free hydroxyl radicals (HO()), superoxide anion radicals (O(2)(-)), 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radicals and 2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radicals than vitamin C. In contrary, danshensu and salvianolic acid B showed weaker iron chelating and hydrogen peroxide (H(2)O(2)) scavenging activities than vitamin C. As expressed as vitamin C equivalent capacity (VCEAC), the relative VCEAC values (mg/100ml) were in the order of salvianolic acid B (18.59) > danshensu (12.89) > vitamin C (10.00) by ABTS radical assay. The protective efficiencies against hydrogen peroxide induced human vein vascular endothelial cell damage were correlated with their antioxidant activities. Analysis of structure-activity relationship of these two compounds showed that the condensation and conjugation of danshensu and caffeic acid appears important for antioxidant activity. These results indicated that danshensu and salvianolic acid B are efficient radical scavengers and antioxidants, and salvianolic acid B is superior to danshensu. Their radical scavenging and antioxidant properties might have potential applications in food and healthcare industry.

Topics: Antioxidants; Ascorbic Acid; Benzofurans; Benzothiazoles; Biphenyl Compounds; Cell Survival; Chelating Agents; Endothelial Cells; Ferrous Compounds; Free Radical Scavengers; Humans; Hydrogen Peroxide; Hydroxyl Radical; Lactates; Oxidants; Picrates; Plant Roots; Salvia; Sulfonic Acids; Tetrazolium Salts; Thiazoles

The protective effects of pine (Pinus morrisonicola Hay.) needle on low-density lipoprotein (LDL) oxidation and nitric oxide production in macrophages as well as its bioactive compounds were investigated. Of the four solvent extracts, the ethyl acetate extract of pine needle (EAE-PN) exhibited the strongest scavenging action on free radicals. EAE-PN significantly inhibited copper-induced LDL oxidation through prolonging the lag phase of conjugated dienes formation and decreasing the relative electrophoretic mobility of LDL. Lipid accumulation and foam cell formation were significantly reduced when EAE-PN (75 microg/mL) was added to the medium co-incubated with macrophages cells and copper-induced LDL. EAE-PN also markedly inhibited reactive oxygen species production in RAW 264.7 cells stimulated with lipopolysaccharide (LPS). As regards NO production in cells, EAE-PN showed dose-dependent inhibitory effect on nitric oxide (NO) production in LPS-stimulated RAW 264.7 cells. The inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) protein expressions in LPS-stimulated RAW 264.7 cells were inhibited by EAE-PN. RT-PCR analysis indicated that the iNOS and COX-2 mRNA expression were suppressed by EAE-PN. The major phenolic compounds in EAE-PN were epicatechin and p-coumaric acid by HPLC analysis. The presence of epicatechin and p-coumaric acid in EAE-PN may be partially responsible for the biological action of EAE-PN. Taken together, these results suggest that EAE-PN may provide potential protective effects against LDL oxidation and attenuating excessive NO generation at inflammatory sites; consequently, this may contribute to anti-atherosclerotic and anti-inflammatory effects of EAE-PN.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Blotting, Western; Cell Line; Chromans; Chromatography, High Pressure Liquid; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Electrophoretic Mobility Shift Assay; Enzyme Inhibitors; Flavonoids; Free Radical Scavengers; Humans; In Vitro Techniques; Lipopolysaccharides; Lipoproteins, LDL; Macrophages; Mice; Nitric Oxide Synthase Type II; Oxidation-Reduction; Phenols; Picrates; Pinus; Polyphenols; Reactive Oxygen Species; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Tetrazolium Salts; Thiazoles

Organic solvent (methanol, ethanol, and acetone) extracts and water extracts of cherry (Prunus serrulata var. spontanea) blossoms were prepared, and antioxidant activities of the extracts were evaluated. Methanolic CBE (100 microg/ml) showed the highest total phenol content (104.30 microM), radical scavenging activity (34.2%), and reducing power (0.391). The effect of CBE on DNA damage induced by H(2)O(2) in human leukocytes was evaluated by Comet assay. All CBE was a potent dose dependent inhibitor of DNA damage induced by 200 microM of H(2)O(2), methanolic CBE showed the most strong inhibition activity. The methanolic CBE of 500 microg/ml showed 38.8% inhibition against growth of human colon cancer cell line HT-29. These results indicated that cherry blossoms could provide valuable bioactive materials.

Topics: Anticarcinogenic Agents; Antioxidants; Biphenyl Compounds; Comet Assay; DNA Damage; Dose-Response Relationship, Drug; Free Radical Scavengers; HT29 Cells; Humans; Hydrazines; Leukocytes; Phenols; Picrates; Plant Extracts; Prunus; Reactive Oxygen Species; Tetrazolium Salts; Thiazoles

Suaeda asparagoides Miq. (Chenopodiaceae: S. asparagoides) is a salt-marsh plant that has long been prescribed in traditional Oriental medicine for the treatment of hypertension and hepatitis. In order to elucidate the pharmacological mechanisms of the herb, we conducted an examination of the anti-oxidative and anti-inflammatory properties of solvent-extracts of S. asparagoides. All of the solvent fractions showed potent anti-oxidative effects, as assessed using a radical generation assay system (xanthine oxidase assay) and an electron-donating activity system (DPPH [2,2-diphenyl-l-picrylhydrazyl radical] assay), with IC50 values ranging from 9 to 42 microg/ml. In agreement with this pattern, the total phenolic contents were widely distributed in the various solvent fractions, and ranged from 36.5 to 50.3 mg/g of dry weight. All of the solvent fractions significantly suppressed NO production in RAW264.7 cells induced by lipopolysaccharide (LPS, 0.1 microg/ml) and of the fractions, only the chloroform (CHC) fraction completely blocked the expression of inducible NO synthase (iNOS). Additionally, the hexane (HEX) and CHC fractions suppressed the mRNA expression of granulocyte/macrophage colony-stimulating factor (GM-CSF) and monocyte chemoattractant protein 1 (MCP-1), respectively, in the LPS-stimulated RAW264.7 cells. Therefore, these results suggest that the pharmacological action of S. asparagoides is due to its potent anti-oxidative effects and anti-inflammatory effects, and that therefore it can be applied to other diseases caused by oxidative stress and inflammation, such as cardiovascular diseases.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Cell Line; Cell Proliferation; Chemokines; Chenopodiaceae; Cytokines; Enzyme Inhibitors; Free Radical Scavengers; Lipopolysaccharides; Macrophages; Mice; Nitric Oxide; Nitric Oxide Synthase Type II; Phenols; Picrates; Plant Extracts; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Solvents; Tetrazolium Salts; Thiazoles; Xanthine Oxidase

Plant phenolic compounds isolated from a 70% aqueous acetone extract of the leaves of Malus doumeri A. CHEV. var. formosana (KAWAK. & KOIDZ.) S. S. YING, a type of Taiwanese indigenous plant, were evaluated for potential application in the field of skin care. A phytochemical investigation of the active fractions resulted in the isolation of seven compounds of which the structures were identified by spectroscopic characterization. In the present study, the isolated phenolic compounds were evaluated for their free radical-scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and the superoxide radicals, anti-elastase, and for their anti-matrix metalloproteinase-1 (MMP-1) activity in human skin fibroblast cells. Of these compounds, 3-hydroxyphloridzin (2), 3-hydroxyphloretin (6), and quercetin (7) exhibited the strongest DPPH and superoxide radical-scavenging activities. The IC50 values of these compounds were 9.2, 7.7, and 15.4 microM, respectively, for the DPPH radical, and 25.0, 19.6, and 42.6 microM, respectively, for the superoxide radical. 3-Hydroxyphloridzin (2) and 3-hydroxyphloretin (6) also showed xanthine oxidase inhibitory activity, with IC(50) values of 52.1 and 22.4 muM, respectively. In the test for elastase inhibitory activity, phloretin (5) and 3-hydroxyphloretin (6) were the most potent compounds. Phloretin (5), 3-hydroxyphloretin (6), and quercetin (7) showed better inhibition of MMP-1 production in fibroblast cells. To the best of our knowledge, this is the first time that the active phenolic compounds from M. doumeri var. formosana have been isolated, reported, and described. The above results suggest that the extract of M. doumeri var. formosana containing phenolic compounds could be suitable naturally occurring active constituents for use in anti-aging or cosmetic products.

Topics: Biphenyl Compounds; Caseins; Cells, Cultured; Chromatography, High Pressure Liquid; Enzyme Inhibitors; Free Radical Scavengers; Kinetics; Malus; Metalloproteases; Phenols; Picrates; Plant Extracts; Skin Care; Superoxides; Tetrazolium Salts; Thiazoles; Xanthine Oxidase

Geum quellyon Sweet, a perennial herb of the Rosaceae family, has been used in the traditional medicine of the Mapuche Amerindians of Chile to treat tooth neuralgia, gastric inflammation, prostatitis and to regulate menstruation, and for its diuretic and aphrodisiac properties. Although many benefits have been claimed for this plant, few scientific studies are available in the literature. In this study, we investigated the antioxidant activity of a methanolic extract of Geum quellyon roots. We also examined the anticancer action of this plant on Caco-2 (colon adenocarcinoma cells), DU-145 (androgen-insensitive prostate cancer cells) and KB (oral squamous carcinoma cells) human tumor cell lines. Our data showed that Geum quellyon extract, containing tannins, exhibits interesting antioxidant properties, expressed by its capacity to scavenge 1,1-diphenyl-2-picryl-hydrazyl radical (DPPH) and superoxide anion (O(2)*-), to inhibit xanthine oxidase activity, to chelate metals, and to protect plasmid DNA from cleavage induced by hydroxyl radicals (*OH) and nitric oxide (NO). These results may explain, at least in part, its use in Mapuche traditional medicine for gastric inflammation and prostatitis. The assays on human tumor cell lines demonstrated that this natural product exhibits a inhibitory effect on all human cancer cells examined, and seem to indicate that necrosis cell death is triggered in KB cells and Caco-2, while apoptotic cell demise appears to be induced in DU-145. The effect evidenced in Caco-2 cells can be in part correlated to a modulation of redox-sensitive mechanisms.

Topics: Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Caco-2 Cells; Cell Line, Tumor; Chelating Agents; Chile; Comet Assay; DNA, Neoplasm; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Free Radical Scavengers; Geum; Humans; Hydrazines; Hydrogen Peroxide; KB Cells; L-Lactate Dehydrogenase; Male; Medicine, Traditional; Picrates; Plant Extracts; Plant Roots; Prostatic Neoplasms; Reactive Oxygen Species; Tannins; Tetrazolium Salts; Thiazoles; Ultraviolet Rays; Xanthine Oxidase

In order to develop new anti-photoaging agents, we examined the antioxidative activity and the inhibition effect of matrix metalloproteinase-1 (MMP-1) on the extracts of a marine product, Zostera marina L., which is known for its potent activity. Three compounds (compounds 1, 2, and 3) were isolated from an ethyl acetate (EtOAc) soluble fraction of the product; they were identified as apigenin-7-O-beta-D-glucoside (1), chrysoeriol (2), and luteolin (3). These compounds were found to scavenge radicals and reactive oxygen species (ROS) and were measured to have SC50 values of 0.18 mM, 0.68 mM, and 0.01 mM against the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and 0.04 mM, 0.03 mM, and 0.01 mM against the superoxide radical in the xanthine/xanthine oxidase system, respectively. Compound 3 suppressed the expression of MMP-1 by up to 44% at 4.0 microM and inhibited the production of interleukin 6 (IL-6), which is known as a cytokine that induces MMP-1 expression. From these results, compound 3 and the other compounds were determined to have antioxidative activity and to inhibit MMP-1 expression. Thus, the three compounds are expected to be useful for preventing the photoaging of skin.

Topics: Antioxidants; Biphenyl Compounds; Cell Line; Cell Survival; Cytokines; Enzyme-Linked Immunosorbent Assay; Humans; Magnetic Resonance Spectroscopy; Matrix Metalloproteinase Inhibitors; Picrates; Plant Leaves; Protease Inhibitors; Superoxides; Tetrazolium Salts; Thiazoles; Ultraviolet Rays; Zosteraceae