Anti-inflammatory and antinociceptive potential of major phenolics from Verbascum salviifolium Boiss

The potential effects of flavonoids, phenylethanoid and neolignan glycosides from the aerial parts of Verbascum salviifolium Boiss. were studied in the p-benzoquinone-induced writhing reflex, for the assessment of the antinociceptive activity, and in carrageenan- and PGE1-induced hind paw edema and 12-O-tetradecanoyl-13-acetate (TPA)-induced ear edema models in mice, for the assessment of the anti-inflammatory activity. Through bioassay-guided fractionation and isolation procedures ten compounds from the aqueous extract of the plant, luteolin 7-O-glucoside (1), luteolin 3'-O-glucoside (2), apigenin 7-O-glucoside (3), chrysoeriol 7-O-glucoside (4), beta-hydroxyacteoside (5), martynoside (6), forsythoside B (7), angoroside A (8), dehydrodiconiferyl alcohol-9'-O-beta-D-glucopyranoside (9) and dehydrodiconiferyl alcohol-9-O-beta-D-glucopyranoside (10), were isolated and their structures were elucidated by spectral techniques. Results have shown that 1, 2, 3 and 5 significantly inhibited carrageenan-induced paw edema at a 200 mg/kg dose, while 1, 2 and 5 also displayed anti-inflammatory activity against the PGE1-induced hind paw edema model. However, all the compounds showed no effect in the TPA-induced ear edema model. The compounds 1 and 2 also exhibited significant antinociceptive activity.     

Acylated flavonoids and phenol glycosides from Veronica thymoides subsp. pseudocinerea

A new acylated flavone glucoside, 3'-hydroxyscutellarein 7-O-(6'-O-protocatechuoyl)-beta-glucopyranoside (1), and a new phenol glucoside, 3,5-dihydroxyphenethyl alcohol 3-O-beta-glucopyranoside (6) were isolated from Veronica thymoides subsp. pseudocinerea together with seven known flavone, phenol and lignan glycosides; 3'-hydroxyscutellarein 7-O-(6'-O-trans-feruloyl)-beta-glucopyranoside (2), 3'-hydroxy, 6-O-methylscutellarein 7-O-beta-glucopyranoside (3), luteolin 7-O-beta-glucopyranoside (4), isoscutellarein 7-O-(6'-O-acetyl)-beta-allopyranosyl (1' --> 2')-beta-glucopyranoside (5), 3,4-dihydroxyphenethyl alcohol 8-O-beta-glucopyranoside (7), benzyl alcohol 7-O-beta-xylopyranosyl (1" --> 2')-beta-glucopyranoside (8), and (+)-syringaresinol 4'-O-beta-glucopyranoside (9). Compounds 2, 3 and 7-9 were reported for the first time in the genus Veronica. The structures of the isolates were determined by means of spectroscopic (UV, IR, 1D and 2D NMR, HR ESI-MS) methods. Isolated compounds (1-7) exhibited potent radical scavenging activity against the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical.     

Antioxidant and anticancer activity of extract from Betula platyphylla var. japonica

The antioxidant and anticancer properties of a medicinal plant, Betula platyphylla var. japonica were investigated. The total methanol extract of B. platyphylla var. japonica had protective effects against hydrogen peroxide (H2O2) in the Chinese hamster lung fibroblast (V79-4) cell line and induced apoptotic cell death in human promyelocytic leukemia (HL-60) cells, a cancer cell line. B. platyphylla var. japonica extract significantly increased cell viability against H2O2. The extract also showed high 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (IC50 2.4 microg/ml) and lipid peroxidation inhibitory activity (IC50 below 4.0 microg/ml). Furthermore, B. platyphylla var. japonica extract reduced the number of V79-4 cells arrested in G2/M in response to H2O2 treatment and increased the activities of several cellular antioxidant enzymes, including superoxide dismutase, catalase and glutathione peroxidase. Treatment with B. platyphylla var. japonica extract induced cytotoxicity and apoptosis in HL-60 cells, as shown by nucleosomal DNA fragmentation, increases in the subdiploid cell population, and fluorescence microscopy. B. platyphylla var. japonica extract gradually increased the expression of pro-apoptotic Bax and led to the activation of caspase-3 and cleavage of PARP. These findings suggest that B. platyphylla var. japonica exhibits potential antioxidant and anticancer properties.     

Antioxidant properties and protective effects of a standardized extract of Hypericum perforatum on hydrogen peroxide-induced oxidative damage in PC12 cells

Free radical scavenging and antioxidant activities of a standardized extract of Hypericum perforatum (SHP) were examined for inhibition of lipid peroxidation, for hydroxyl radical scavenging activity and interaction with 1,1-diphenyl-2-picrylhydrazyl stable free radical (DPPH). Concentrations between 1 and 50 microg/ml of SHP effectively inhibited lipid peroxidation of rat brain cortex mitochondria induced by Fe2+/ascorbate or NADPH system. The results showed that SHP scavenged DPPH radical in a dose-dependent manner and also presented inhibitory effects on the activity of xanthine oxidase. In contrast, hydroxyl radical scavenging occurs at high doses. The protective effect of the standardized extract against H2O2-induced oxidative damage on the pheochromocytoma cell line PC 12 was investigated by measuring cell viability via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), lactate dehydrogenase (LDH) assays, caspase-3-enzyme activity and accumulation of reactive oxygen species [2',7'-dichlorofluorescin (DCF) assay]. Following 8-h cell exposure to H2O2 (300 microM), a marked reduction in cell survival was observed, which was significantly prevented by SHP (pre-incubated for 24 h) at 1-100 microg/ml. In a separate experiment, different concentrations of the standardized extract (0.1-100 microg/ml) also attenuated the increase in caspase-3 activity and suppressed the H2O2 -induced reactive oxygen species generation. Taken together, these results suggest that SHP shows relevant antioxidant activity both in vitro and in a cell system, by means of inhibiting free radical generation and lipid peroxidation.     

Bioactive deoxypreussomerins and dimeric naphthoquinones from Diospyros ehretioides fruits: deoxypreussomerins may not be plant metabolites but may be from fungal epiphytes or endophytes

Deoxypreussomerin derivatives, palmarumycins JC1 (1) and JC2 (2), and two dimeric naphthoquinones, isodiospyrin (3) and its new derivative isodiospyrol A (4), were isolated from dried fruits of Diospyros ehretioides. Structures of the isolated compounds were elucidated by spectroscopic analyses. Palmarumycins were not found in the extract of freshly collected fruits; however, they were present in dried fruit extract. The absence of palmarumycins in fresh fruits of D. ehretioides, together with the chemotaxonomic point of view, we proposed that palmarumycins JC1 (1) and JC2 (2) are more likely to be fungal metabolites, i.e., endophytes or epiphytes. The isolation of palmarumycins 1 and 2 from dried D. ehretioides fruits could be reproducible; both plant samples collected in the years 2002 and 2004 provided the same result, and, therefore, symbiont fungal strains should be specific to the plant host, D. ehretioides, and they can grow on the fruits during drying the sample. Palmarumycin JC1 (1) did not exhibit antimalarial, antifungal, antimycobacterial, and cytotoxic activities. Palmarumycin JC2 (2) exhibited antimalarial (IC50 4.5 microg/ml), antifungal (IC50 12.5 microg/ml), antimycobacterial (MIC 6.25 microg/ml), and cytotoxic (IC50 11.0 microg/ml for NCI-H187 cell line) activities. In our bioassay systems, isodiospyrin (3) did not exhibit antimycobacterial, antifungal, antimalarial, and cytotoxic activities. Isodiospyrol A (4) exhibited antimalarial (IC50 2.7 microg/ml) and antimycobacterial (MIC 50 microg/ml) activities, but was inactive towards Candida albicans. Compound 4 also exhibited cytotoxicity against BC cells (IC50 12.3 microg/ml), but not towards KB and Vero cell lines.     

Triterpenic acids and flavonoids from Satureja parvifolia. Evaluation of their antiprotozoal activity

Bioassay-guided fractionation of a Satureja parvifolia MeOH extract led to the isolation of eriodictyol, luteolin and ursolic and oleanolic acids as its active components against Plasmodium falciparum K1. This is the first time these compounds are reported as constituents of S. parvifolia. Ursolic acid showed an IC50 of 4.9 microg/ml, luteolin 6.4 microg/ml, oleanolic acid 9.3 microg/ml and eriodictyol 17.2 microg/ml. Antiplasmodial activity of eriodictyol and luteolin is reported here for the first time. Besides, the four compounds showed activity against P. falciparum 3D7 strain and Trypanosoma brucei rhodesiense. Eriodictyol showed moderate activity on all the parasites but was the most selective compound as a result of its rather low cytotoxicity (IC50 174.2 microg/ml) on the mammalian KB cell line.     

Mitracarpus frigidus aerial parts exhibited potent antimicrobial, antileishmanial, and antioxidant effects

The crude extract and the hexane, CH(2)Cl(2), EtOAc, n-BuOH, and hydromethanolic fractions of the aerial parts of Mitracarpus frigidus were evaluated against promastigote forms of two species of Leishmania (L. chagasi and L. amazonensis), 11 strains of bacteria (Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella enterica sorovar Tythimurium, Shigella sonnei, Klebsiella pneumoniae, Escherichia coli, Micrococcus luteus, Enterococcus faecalis, Enterobacter cloacae, Streptococcus pyogenes and Bacillus cereus) and two yeasts (Candida albicans and Cryptococcus neoformans). The antioxidant activity (DPPH radical scavenging activity and reducing power), cytotoxicity against mammalian cells, and the contents of phenolics and flavonoids were determined. Phytochemical analysis of the major groups of phytoconstituents is also reported. All samples showed antioxidant activity which was positively correlated to the content of phenolic compounds. S. sonnei, B. cereus and C. neoformans were susceptible to all extracts tested, except for the n-BuOH and hydromethanolic fractions, which demonstrated no antimicrobial activity. The lowest MIC was recorded for the CH(2)Cl(2) fraction against C. neoformans (MIC of 10 microg/ml), followed by B. cereus, S. sonnei, and E. cloacae (MIC of 20, 39 and 39 microg/ml, respectively). The CH(2)Cl(2) fraction was the most effective against L. chagasi (IC(50) of 6.7 microg/ml), and the hydromethanolic fraction exhibited the best activity against L. amazonensis (IC(50) of 9 microg/ml). A cytotoxic effect on mammalian cells was observed only for the crude extract and CH(2)Cl(2) fraction at the concentrations of 130 and 31 microg/ml, respectively. These results suggest that M. frigidus has interesting antimicrobial, antileishmanial and antioxidant activities.     

Novel biologically active bibenzyls from Bauhinia saccocalyx Pierre

Four new bibenzyls, bauhinols A-D (1-4), together with the two known bibenzyls 5 and 6, were isolated from the roots of Bauhinia saccocalyx, and their structures were elucidated by analyses of spectroscopic data. Bauhinol A (1) exhibits significant cytotoxicity towards NCI-H187 (small-cell lung cancer), BC (breast cancer), and KB (oral-cavity cancer) cell lines, with IC50 values of 2.7-4.5 microg/ml. Bauhinol B (2) is cytotoxic against NCI-H187 (IC50 = 1.1 microg/ml) and BC (IC50 = 9.7 microg/ml) cell lines, but inactive toward the KB cell line (at 20 microg/ml). Compound 2 also is mildly antifungal towards Candia albicans (IC50 = 28.9 microg/ml). Bibenzyl 6 is active against NCI-H187 (IC50 = 14.1 microg/ml) and BC (IC50 = 4.0 microg/ml) cells, but inactive (at 20 microg/ml) toward the KB cell line. Compounds 1, 2, and 6 show mild antimycobacterial activities, with MIC values of 25-50 microg/ml, but are inactive at 20 microg/ml against the K1 malarial parasite strain (Plasmodium falciparum). While bauhinol A (1) is inactive against cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), compounds 2 and 6 inhibit both COX-1 and COX-2, with IC50 values comparable to those of the standard drug, aspirin (Table 3).     

Chemopreventive effects of minor dietary constituents in common foods on human cancer cells

Epidemiological evidence has suggested that vegetables and fruits may have a role in cancer prevention. The aim of the present study was to examine the anti-proliferative activity of ten related pure compounds from common vegetables and fruits. Studies were conducted on a series of carcinoma cells derived from eight human organs. The results show that linalool possessed the strongest activity against nine carcinoma cells, and that baicalein and luteolin also exhibited a broad spectrum of anti-proliferative activities. Among them, linalool showed the strongest activity against carcinoma of the cervix (IC50: 0.37 microg/ml), stomach (IC50: 14.1 microg/ml), skin (IC50: 14.9 microg/ml), lung (IC50: 21.5 microg/ml) and bone (IC50: 21.7 microg/ml). As for the flavonoids, luteolin exhibited the strongest activity against carcinoma of the stomach (IC50: 7.1 microg/ml), cervix (IC50: 7.7 microg/ml), lung (IC50: 11.7 microg/ml) and bladder (IC50: 19.5 microg/ml), whereas baicalein possessed the strongest anti-proliferative activity against carcinoma of the cervix (IC50: 9.8 microg/ml), stomach (IC50: 16.1 microg/ml) and skin (IC50: 19.5 microg/ml). The present study indicates that linalool possessed the strongest activity against a broad spectrum of carcinoma cells, especially cervical carcinoma cells, suggesting that linalool and flavonoids are partially responsible for the cancer prevention of common vegetables and fruits.     

Antioxidant effects of an aqueous extract of Ilex paraguariensis

In this work we investigate the antioxidant properties of an aqueous extract prepared from an infusion of Ilex paraguariensis (Aquifoliaceae) using free radical-generating systems. The extract inhibited the enzymatic and nonenzymatic lipid peroxidation in rat liver microsomes in a concentration-dependent fashion, with IC(50) values of 18 microg/ml and 28 microg/ml, respectively. The extract also inhibited the H(2)O(2)-induced peroxidation of red blood cell membranes with an IC(50) of 100 microg/ml and exhibited radical scavenging properties toward superoxide anion (IC(50) = 15 microg/ml) and 2,2-diphenyl-1-picrylhydrazyl radical. In the range of concentrations used, the extract was not a scavenger of the hydroxyl radical. Our results suggest that ingestion of extracts of Ilex paraguariensis could contribute to increase the antioxidant defense of an organism against free radicals attack.     

Neuroprotection and free radical scavenging effects of <Emphasis Type="Italic">Osmanthus fragrans</Emphasis>

The ethanol extract of dried flowers Osmanthus fragrans (OFE) was assessed for free radical scavenging effects measured by the bleaching of the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical, scavenging of the hydroxyl anion, investigation of the ferric reducing/antioxidant power (FRAP) and lipid-peroxidation inhibition in rat tissues. OFE contained a high amount of total flavonoid and polyphenol. OFE presented the effects in the metal reducing power, FRAP assay with IC₅₀ values of 0.23 μg/ml, and 7.74 μg/ml, respectively. OFE presented similar activities toward the DPPH and hydroxyl anion scavenging ability with IC₅₀ values of 10 μg/ml. OFE with IC₅₀ values between 46 and 97 μg/ml inhibited lipid peroxidation initiated by ferrous chloride in rat brain, liver, heart and kidney mitochodrias. Moreover, the neuroprotective activity of OFE was investigated under different insults (glutamate, arachidonic acid, and 6-hydroxydopamine) in Wistar rat primary cortical neurons. OFE with EC₅₀ values between 66 and 165 μg/ml attenuated the neurotoxicity on MTT and LDH assays. In addition, the AKT protein expression of excitotoxicity and oxidative stress was displayed by western blotting analysis. OFE could up-regulate the glutamate and 6-OHDA decreased AKT expression. This is the first demonstration of the neuroprotective, free radical scavenging and anti-oxidative effects of O. fragrans.     

Increase of Bax/ Bcl-XL ratio and arrest of cell cycle by luteolin in immortalized human hepatoma cell line

Luteolin is a common constituent of many kinds of fruits and vegetables. It possesses the anti-neoplastic activities against several human cancers, but its activity against hepatocellular carcinoma (HCC) is seldom mentioned. To evaluate the activity against HCC and to provide information about the mechanism, we tested luteolin against five human hepatoma cell lines, namely HepG2, SK-Hep-1, PLC/PRF/5, Hep3B, and HA22T/VGH, with XTT assay and flow cytometry. The results showed that luteolin inhibited PLC/PRF/5, Hep3B and HA22T/VGH at a concentration of 1 microg/ml, but it needed 5 microg/ml to inhibit HepG2 and 10 microg/ml for SK-Hep1 (P <0.05). The inhibitive concentrations of 50% (IC50) of luteolin were between 7.29 microg/ml and 32.59 microg/ml, which were comparable with those of 5-FU (15.35 microg/ml to 32.84 microg/ml). The least effective cell line as affected by luteolin (SK-Hep1) was the most effective one when treating with 5-FU. The least effective cell line as affected by 5-FU (HA22T/VGH) was effectively affected by luteolin. It seemed that luteolin had some complementary activity to 5-FU against these HCC cell lines. The luteolin-treated PLC/PRF/5 cells exhibited typical changes of apoptosis with a characteristic DNA laddering pattern on gel electrophoresis. Luteolin also activated casepase-3, increased Bax protein with a concomitant decrease in Bcl-XL level. Increase in Bax/ Bcl-XL ratio and activation of caspase-3 supported the apoptotic finding on gel electrophoresis. Luteolin also induced cell cycle arrest at G0/G1 phase. We suggested that luteolin might exhibit anti-HCC activity as efficient as 5-FU by the mechanism of not only cell cycle arrest but also apoptosis.     

Functional properties of dioscorin, a soluble viscous protein from Japanese yam (Dioscorea opposita thunb.) tuber mucilage Tororo

A soluble viscous protein was purified from yam (Dioscorea opposita Thunb.) tuber mucilage tororo by chromatographic steps, and its functional properties were estimated. The purified dioscorin having the molecular weight of about 200 kDa exhibited high scavenging activities against hydroxyl radicals (IC50 = 195.1 microg/ml) and superoxide anion radicals (IC50 = 92.7 microg/ml). Moreover, it showed extremely high angiotensin I-converting enzyme inhibitory activity (IC50 = 41.1 microg/ml). The results suggested that yam D. opposita tuber has a wide spectrum of strong antioxidative and antihypertensive activities and it could be utilized as a source of natural antioxidant.     

Antibacterial and antioxidant activity and essential oil composition of Grammosciadium scabridum Boiss. from Iran

The in vitro antibacterial and antioxidant activity of the essential oil and its two main components of Grammosciadium scabridum Boiss. (Apiaceae) growing wild in Iran, as well as the composition of its essential oil were studied. A total of 19 compounds representing 99.9% of the oil has been identified. Gamma-Terpinene (73.5%), p-cymene (14.2%) and (E)-beta-farnesene (5.3%) were characterized as the main components. The oil showed remarkable activity against three Gram-negative and four Gram-positive test bacteria, with minimal inhibitory concentration (MIC) values ranging from 0.31 to 10.00 mg/ml. The oil and its two main components were also subjected to screening for their possible antioxidant activity by using the 2,2-diphenyl-l-picrylhydrazyl (DPPH) assay. The free radical scavenging capacity of the oil was determined with an IC50 value of 6.6 mg/ml.     

Triterpene saponins from Silphium radula

Nine triterpene saponins (1-9) were isolated from leaves and stems of Silphium radula Nutt. (Asteraceae). Their structures were determined by extensive 1D ((13)C, (1)H, DEPT, TOCSY) and 2D NMR (NOESY, HSQC, HMBC) and ESI-MS studies. The compounds were identified as 3beta,6beta,16beta-trihydroxyolean-12-en-23-al-3-O-beta-glucopyranosyl-16-O-beta-glucopyranoside (1), urs-12-ene-3beta,6beta,16beta-triol-3-O-beta-galactopyranosyl-(1-->2)-beta-glucopyranoside (2), 3beta,6beta,16beta-trihydroxyolean-12-en-23-oic acid-3-O-beta-glucopyranosyl-16-O-beta-glucopyranoside (3), urs-12-ene-3beta,6beta,16beta,21beta-tetraol-3-O-beta-glucopyranoside (4), olean-12-ene-3beta,6beta,16beta,21beta-tetraol-3-O-beta-glucopyranoside (5), olean-12-ene-3beta,6beta,16beta,21beta,23-pentaol-3-O-beta-glucopyranosyl-16-O-beta-glucopyranoside (6), olean-12-ene-3beta,6beta,16beta-triol-3-O-beta-glucopyranosyl-16-O-alpha-arabinopyranosyl-(1-->2)-beta-glucopyranoside (7), olean-12-ene-3beta,6beta,16beta,23-tetraol-3-O-beta-glucopyranosyl-16-O-alpha-arabinopyranosyl-(1-->2)-beta-glucopyranoside (8), 3beta,6beta,16beta,21beta-tetrahydroxyolean-12-en-23-al-3-O-beta-glucopyranoside (9). The presence of a 6beta-hydroxyl function was not common in the oleanene or ursene class and the aglycones of these compounds were not found previously in the literature. Moreover, the cytotoxic activities of the isolated compounds were tested against human breast cancer cell line MDA-MB-231. Results showed that compound 2 decreased cell proliferation in a statistically significant manner at 25 microg/ml.     

Antioxidant potential of n-butanol fraction from extract of Jasminum mesnyi Hance leaves

Methanolic extract of Jasminum mesnyi Hance leaves having antidiabetic activity was subjected to fractionation to obtain antioxidant and antihyperglycemic rich fraction. Different concentrations of ethyl acetate and n-butanol fractions were subjected to antioxidant assay by DPPH method, nitric oxide scavenging activity and reducing power assay. The fractions showed dose dependent free radical scavenging property in all the models. IC50 values for ethyl acetate and n-butanol fractions were 153.45 +/- 6.65 and 6.22 +/- 0.25 microg/ml, respectively, as compared to L-ascorbic acid and rutin (as standards; IC50 values 6.54 +/- 0.24 and 5.43 +/- 0.21 microg/ml, respectively) in DPPH model. In nitric oxide scavenging activity, IC50 values were 141.54 +/- 9.95 microg/ml, 35.12 +/- 1.58 microg/ml, 21.06 +/- 0.95 microg/ml and 29.93 +/- 0.32 microg/ml for ethyl acetate, n-butanol fractions, L-ascorbic acid and rutin, respectively. n-Butanol fraction showed a good reducing potential and better free radical scavenging activity as compared to ethyl acetate fraction. Potent antioxidant n-butanol fraction showed better oral glucose tolerance test (antihyperglycemic) at par with metformin (standard drug), n-Butanol fraction contained secoiridoid glycosides which might be responsible for both antioxidant and antihyperglycemic activity.     

Antioxidant activity of extract from Polygonum aviculare L

Free radicals induce numerous diseases by lipid peroxidation, protein peroxidation, and DNA damage. It has been reported that numerous plant extracts have antioxidant activities to scavenge free radicals. Whether Polygonum aviculare L. (Polygonaceae) has antioxidant activity is unknown. In this study, dried Polygonum aviculare L. was extracted by ethanol, and the extract was lyophilized. The antioxidant activities of extract powder were examined by free radical scavenging assays, superoxide radical scavenging assays, lipid peroxidation assays and hydroxyl radical-induced DNA strand scission assays. The results show that the IC50 value of Polygonum aviculare L. extract is 50 microg/ml in free radical scavenging assays, 0.8 microg/ml in superoxide radical scavenging assays, and 15 microg/ml in lipid peroxidation assays, respectively. Furthermore, Polygonum aviculare L. extract has DNA protective effect in hydroxyl radical-induced DNA strand scission assays. The total phenolics and flavonoid content of extract is 677.4 +/- 62.7 microg/g and 112.7 +/- 13 microg/g. The results indicate that Polygonum aviculare L. extract clearly has antioxidant effects.     

Antioxidant and anti-inflammatory activity of extract obtained from Aspergillus candidus MTCC 2202 broth filtrate

Antioxidant potential of Aspergillus candidus MTCC 2202 broth filtrate extract was studied using different antioxidant models, whereas anti-inflammatory potential was studied using carrageenan-induced rat paw oedema model. The ethyl acetate extract at 1000 microg/ml showed maximum scavenging activity of the stable radical 1,1-diphenyl,2-picryl hydrazyl upto 96.65% (IC50=430.36 microg/ml) and scavenging of the radical cation, 2,2-azinobis-(3-ethylbenzothiazoline-6-sulphonate) upto 92.25% (IC50=606.29 microg/ml) at the same concentration. The extract had good reducing power, however showed moderate inhibition for conjugated dienes and thiobarbituric acid reactive acid substances (59.56 and 51.45%). The total phenolic content of various extracts of A. candidus broth filtrate was measured and a correlation between radical scavenging activities of extracts with total phenolic content was observed. The ethyl acetate extract (125 mg/kg ip) showed significant anti-inflammatory activity in carrageenan-induced rat paw oedema model. The exhibited antioxidant activity of ethyl acetate extract of A. candidus broth filtrate was comparable with BHA and ascorbic acid, while anti-inflammatory activity was comparable with standard diclofenac sodium.     

Antioxidant activities of cultured Armillariella mellea

This study aimed to evaluate the antioxidant activities of a cultured medicinal fungus--Armillariella mellea (Vahl. ex Fr.) Karst. (AM). Three antioxidant assay systems, namely cytochrome c, xanthine oxidase inhibition and FeCl2-ascorbic acid stimulated lipid peroxidation in rat tissue homogenate tests, were used. Total flavonoid and phenol contents of AM extracts were also analyzed. Results showed that both aqueous (AM-H2O) and ethanolic (AM-EtOH) extracts of solid state cultured AM showed antioxidant activities in a concentration-dependent manner. At concentrations 1-100 microg/ml, the free radical scavenging activity was 73.7-92.1% for AM-H2O, and 60.0-90.8% for AM-EtOH. These extracts also showed an inhibitory effect on xanthine oxidase activity, but with a lesser potency (IC50 - 9.17 microg/ml for AM-H2O and 7.48 microg/ml for AM-EtOH). In general, AM-H2O showed a stronger anti-lipid peroxidation activity on different rat's tissues than AM-EtOH. However, both AM extracts displayed a weak inhibitory effect on lipid peroxidation in plasma. Interestingly, the anti-lipid peroxidation activity of AM-H2O (IC50 - 6.66 microg/ml) in brain homogenate was as good as alpha-tocopherol (IC50 - 5.42 microg/ml). AM-H2O (80.0 mg/g) possessed a significant higher concentration of total flavonoids than AM-EtOH (30.0 mg/g), whereas no difference was noted in the total phenol content between these two extracts. These results conclude that AM extracts possess potent free radical scavenging and anti-lipid peroxidation activities, especially the AM-H20 in the brain homogenate.     

Free radical scavenging properties of sulfinpyrazone

Sulfinpyrazone, a potent uricosuric drug, was tested in vitro for its scavenging action against oxygen free radicals. In this study, sulfinpyrazone was able to scavenge 1,1-diphenyl-2-picrylhydrazyl radical with IC 50 value of 29.82 μg/ml compared to butylated hydroxytoluene (BHT, IC 50 value=20.15 μg/ml) and Trolox (IC 50 value=16.01 μg/ml). It was able to scavenge superoxide anion with IC 50 value of 27.72 μg/ml compared to Trolox (IC 50 value=22.08 μg/ml) and ascorbic acid (IC 50 value=14.65 μg/ml). The hydroxyl radical scavenging activity of sulfinpyrazone is in a concentration-dependent fashion. In the range of concentrations used, sulfinpyrazone was not a scavenger toward H 2 O 2 . However, the intracellular H 2 O 2 -induced 2',7'-dichlorofluorescin diacetate (DCF-DA) fluorescence in HL-60 cells was significantly reduced by sulfinpyrazone during 30-60 min of incubation. Finally, phorbol-12-myristate-13-acetate induced-lucigenin chemiluminescence in whole blood was markedly inhibited by sulfinpyrazone. Our results suggest a new direction for the pharmacological actions of sulfinpyrazone in free radical scavenging properties.