Preliminary evaluation of antinephritis and radical scavenging activities of glabridin from Glycyrrhiza glabra

Antinephritis activity of glabridin, a pyranoisoflavan isolated from Glycyrrhiza glabra, was evaluated after its oral administration to mice with glomerular disease (Masugi-nephritis) by measuring the urinary protein excretion, total cholesterol, serum creatinine and blood urea nitrogen levels. Administration of glabridin for 10 days (30 mg kg(-1) day(-1)) reduced the amount of urinary protein excretion from control level (100+/-23 mg/day) to a significantly lower level (47+/-4 mg/day). ESR spectroscopy demonstrated that glabridin neither produced radical, nor affected the radical intensity of sodium ascorbate, suggesting the lack of correlation between the antinephritis activity and radical scavenging activity.     

Stilbenes and flavonoids from Artocarpus nitidus subsp. lingnanensis

The first stilbene possessing a γ-aminobutyric acid lactam function, artocarpene (1), and a new flavanone, 2-hydroxynaringenin 4′-O-β-d-glucopyranoside (2), were isolated from the stems of Artocarpus nitidus subsp. lingnanensis along with four known compounds, 2-hydroxynaringenin (3), oxyresveratrol (4), 3,4′,5-trihydroxy-3′-prenylstilbene (5) and norartocarpetin (6). Their structures were elucidated on the basis of spectroscopic data. Compounds 1 exhibited weak antioxidant activity and 2 displayed weak cytotoxicity against human lung cancer A549 cell line.     

A new norlignan from Taxodium ascendens

A new norlignan, (2R,3R,4S,5S)-2,4-bis(4-hydroxyphenyl)-3,5-dihydroxy-tetrahydropyran (1), together with 9 known compounds were isolated from the branches and leaves of Taxodium ascendens. Their structures were mainly determined on the basis of MS, IR, 1D and 2D NMR spectral evidences. Methanol extract showed inhibitory activity on carbonic anhydrase II with an IC₅₀ value of 4.27 µg/ml, acetone extract and methanol extract inhibited activity of cathepsin B with IC₅₀ values of 2.12 and 3.71 µg/ml, respectively.     

Anti-inflammatory, antioxidant and antifungal furanosesquiterpenoids isolated from Commiphora erythraea (Ehrenb.) Engl. resin

The topical anti-inflammatory, free radical scavenging and antifungal activities of essential oils and extracts of Commiphora erythraea (Ehrenb.) Engl. resin were investigated. The hexane extract significantly inhibited oedema when applied topically in Croton oil-induced ear oedema assay in mice. The same extract showed antioxidant activity in DPPH radical scavenging assay. A bioguided separation of the hexane extract led to the isolation of furanosesquiterpenoids 1 and 2 that showed a weak antifungal activity, while compounds 3-5 resulted to be antioxidant (EC₅₀ 4.28, 2.56 and 1.08 mg/mL, respectively) and anti-inflammatory (30, 26 and 32% oedema reduction, respectively).     

A new flavonoid glycoside from the leaf of Cephalotaxus koreana

A new flavone glycoside, apigenin 5-O-alpha-L-rhamnopyranosyl-(1-->3)-beta-D-glucopyranoside (1), along with four known flavonol glycosides (2-5), were isolated from the leaf of Cephalotaxus koreana. The new glycoside 1 showed inhibitory activity in superoxide radical scavenging assay with IC(50) value of 13.0 microM, while it showed weak activity in 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay. Compounds 2-5 exhibited antioxidant activity in scavenging DPPH and superoxide radicals with IC(50) values ranging from 5.7 to 22.3 microM.     

Effects of Erigeron breviscapus ethanol extract on neuronal oxidative injury induced by superoxide radical

Antioxidant activity of the ethanol extract of Erigeron breviscapus (EEEB) were studied by using neuron oxidative injury model induced by superoxide radical. EEEB at the dose of 10-140 mug/ml reduced significantly the lipid peroxidation levels and lactic dehydrogenase (LDH) release from neuron exposed to superoxide radical (generated by xanthine and xanthine oxidase). These results suggest that neuroprotective actions of EEEB may be due to its antioxidant or radical scavenging activity.     

Preliminary antinociceptive, antioxidant and cytotoxic activities of Leucas aspera root

The ethanolic extract of Leucas aspera root was subjected to acetic acid induced writhing inhibition, 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay and brine shrimp lethality bioassay for screening of antinociceptive, antioxidant and cytotoxic activity, respectively. The extract produced significant writhing inhibition in acetic acid induced writhing in mice at the doses of 250 and 500 mg/kg. The extract showed a significant free radical scavenging activity with an IC(50) of 8 microg/ml. The extract showed significant lethality to brine shrimp with an LC(50) value.     

In vivo antidepressant activity of sesquiterpenes from the roots of Valeriana fauriei Briq

Antidepressant activity-guided fractionation of the MeOH extract of Valeriana fauriei Briq. roots resulted in the isolation of two new germacrane-type sesquiterpenes (1-2) in addition to seven known ones (3-9). Their structures were elucidated as 1β,10α-dihydroxyl-8α-acetoxyl-10β,11,11-trimethyl-4-formyl-bicyclogermacren-E-4(5)-ene (1), 1β-hydroxyl-8α-acetoxyl-11,11-dimethyl-4-formyl-bicyclogermacren-E-4(5),10(14)-diene (2), bicyclo[8,1,0]5β-hydroxyl-7β-1acetoxyl-5α,11,11'-trimethyl -E-1(10)-ene-4α,15-olide (3), 8α-acetoxyl-3α,4α,10-trihydroxyl-guaia-1(2)-ene-12,6α-olide (4), 2-Ethylhexyl-4-hydroxybenzoate (5), 11αH-gemacra-1(10)E,4Z-diene-3-one-12,6α-olide (6), β-Sitoterol (7), isovaleric acid (8), isoborneol acetate (9), using a combination of UV, IR, mass spectroscopy, 1D and 2D NMR spectroscopy. The antidepressant activity of compounds 1-4 was investigated by the FST on mice. Among them, compounds 3 and 4 showed the significant antidepressant activity (*, P<0.01).     

Effect of Spirulina fusiformis on cyclophosphamide and mitomycin-C induced genotoxicity and oxidative stress in mice

Spirulina fusiformis was tested for its possible in vivo protective effects against cyclophosphamide (CP) and mitomycin-C (MMC) induced genotoxicity and oxidative stress in mice. Pre-treatment with S. fusiformis (250, 500 and 1000 mg kg(-1), p.o., daily for 5 days) significantly reduced the chromosomal damage and lipid peroxidation with concomitant changes in antioxidants and detoxification systems. All the three tested doses were effective in exerting a protective effect against CP and MMC.     

New phenolic esters from the resinous exudate of Haplopappus taeda

Two new phenolic esters 9-trans-p-coumaroyloxy-alpha-terpineol (1) and 7-trans-p-coumaroyloxy-taedol (2), both endowed with free radical scavenger activity and cleroda-3,13 (E)-dien-15,18-diol (3) for which a cis stereochemistry at the decalin junction was found, were isolated from the resinous exudate from Haplopappus taeda upper parts.     

Comparison of bioactive compounds content, free radical scavenging and anti-acne inducing bacteria activities of extracts from the mangosteen fruit rind at two stages of maturity

Contents of bioactive components, free radical scavenging and anti-acne producing bacteria activities of young and mature fruit rind extracts of mangosteen were compared. The young fruit rind extract contained significantly higher contents of phenolics and tannins and promoted higher free radical scavenging activity than the mature fruit rind extract, while the later extract contained higher contents of flavonoids and α-mangostin xanthone and gave higher anti-acne producing bacteria activity than the young fruit rind extract. Thus, the young and mature stages of mangosteen fruit rind should be beneficial for further development of antioxidant and anti-acne pharmaceutical preparations, respectively.     

The antiplasmodial activity of spermine alkaloids isolated from Albizia gummifera

In the present study the methanolic extract of Albizia gummifera was fractionated into various fractions. These fractions were tested against choroquine sensitive (NF54) and resistant (ENT30) strains of Plasmodium falciparum. All other fractions apart from the alkaloidal fraction showed low activity with IC 50 above 3 microg/ml. The alkaloidal fraction exhibited strong activity against NF54 and ENT30 with IC 50 of 0.16+/-0.05 and 0.99+/-0.06 microg/ml, respectively. Five known spermine alkaloids were isolated from the alkaloidal fraction. These alkaloids exhibited activities against NF54 and ENT30 with IC 50 ranging from 0.09+/-0.02 to 0.91+/-0.10 microg/ml. Four of the alkaloids were further evaluated for in vivo activity against rodent malaria parasite Plasmodium berghei. The alkaloids showed percentage chemosuppression of parasitaemia in mice ranging from 43 to 72%. The use of the extracts A. gummifera for treatment of malaria in traditional medicine seems to have a scientific basis.     

Irbic acid, a dicaffeoylquinic acid derivative from Centella asiatica cell cultures

3,5-O-dicaffeoyl-4-O-malonilquinic acid (1) (irbic acid) has been isolated for the first time from cell cultures of Centella asiatica and till now it has never been reported to be present in the intact plant. Evidence of its structure was obtained by spectroscopic analyses (MS/NMR). Besides 1, cell cultures produce also the known 3,5-O-dicaffeoylquinic acid, chlorogenic acid, and the triferulic acid 2 (4-O-8′/4′-O-8″-didehydrotriferulic acid). Biological activities were evaluated for compound 1, which showed to have a strong radical scavenging capacity, together with a high inhibitory activity on collagenase. This suggests a possible utilization of this substance as a topical agent to reduce the skin ageing process.     

A new cardenolide from the roots of Streptocaulon tomentosum

A new cardenolide, (17 alpha)-H-periplogenin-3-O-beta-D-glucopyranosyl-(1-4)-2-O-acetyl-3-O-methyl-beta-fucopyranoside (1), was isolated from the roots of Streptocaulon tomentosum.     

Anticancer activities of two sesquiterpene lactones, millerenolide and thieleanin isolated from Viguiera sylvatica and Decachaeta thieleana

The present study was carried out in order to examine the anticancer properties of two sesquiterpene lactones, millerenolide and thieleanin, isolated from Viguiera sylvatica and Decachaeta thieleana, against cell lines in vitro, and on the growth B16/BL6 melanoma tumors in C57BL/6 mice. Millerenolide and thieleanin showed a similar pattern of cytotoxicity with the greatest effect on viability being evident with A549 human lung cancer cells (IC(50) - 40 and 32 microM respectively), and with the 3T3/HER2 cell line which are 3T3 mouse fibroblasts transfected with the HER2 oncogene (IC(50) - 16 and 28 microM respectively). The parent 3T3 cells and the B16/BL6 mouse melanoma cells were less sensitive to these compounds, with thieleanin showing an IC(50) with B16/BL6 greater than the highest dose tested (203 microM). Treatment with millerenolide (8 mg/kg, i.p. on days 0, 2 and 4 post-inoculation) significantly inhibited the growth of subcutaneous B16/BL6 tumors in C57BL/6 mice, (50% inhibition at day 25, P=0.015), as well as retarding the appearance of detectable tumor (millerenolide - day 15.2+/-0.4 vs control - day 12.8+/-0.5, mean+/-SEM, P=0.011). In contrast, treatment with thieleanin (8 mg/kg every other day up to the day of kill) neither retarded the appearance of the tumor nor its growth.     

12个楸树无性系叶片多酚含量与抗氧化活性

自由基具有强氧化性,机体衰老及多种疾病如肿瘤、炎症、神经退行性疾病、动脉粥样硬化等的诱发促进机制都与自由基有关[1]。自由基的减少,不仅要靠自身的清除系统,还需要外部抗氧化剂的协助。近年来,关于合成抗氧化剂的副作用受到人们更多的关注,因此,寻找安全、高效的植物源类抗氧化剂,已成为食品领域研究的热点。楸树(Catalpa bungei C.A.Mey.)为紫葳科(Bignoniaceae)梓属植物,落叶乔木,《本草纲目》记载楸树树皮、叶具有药     

Minor pregnanes from Caralluma adscendens var. gracilis and Caralluma pauciflora

Phytochemical investigation of Caralluma adscendens var. gracilis and Caralluma pauciflora (Asclepiadaceae) whole plant extracts allowed to isolate one pregnane glycoside and two pregnanes characterized as 12β,20-O-dibenzoyl-5α,6-dihydrosarcostin β-oleandropyranosyl-(1→4)-β-cymaropyranosyl-(1→4)-β-digitoxypyranosyl-(1→4)-β-cymaropyranosyl-(1→4)-β-cymaropyranoside (1), 12β-O-benzoyl-3β,11α,14β,20R-pentahydroxy-pregn-5-ene (2), and 11α-O-benzoyl-3β,12β,14β,20R-pentahydroxy-pregn-5-ene (3), respectively. Their structural characterization was obtained on the basis of extensive NMR spectral studies. Three known pregnane glycosides along with lupeol and β-sitosterol were also isolated and characterized.     

The effect of furanoheliangolides from Tithonia diversifolia on superoxide anion generation in human neutrophils

Four known lactones were isolated from Tithonia diversifolia: furanoheliangolides 1,3-dihydroxy-3,10-epoxy-8-(-2-methylpropanoyloxy)-germacra-11(13)-ene-6,12-olide (1), 1,3-dihydroxy-3,10-epoxy-8-(2-methylpropanoyloxy)-germacra-4,11(13)-diene-6,12-olide (2), 1,3-dimethoxy-3,10-epoxy-8-(2-methylpropanoyloxy)-germacra-4,11(13)-diene-6,12-olide (3) and, observed in natural source for the first time, furanoheliangolide 1-hydroxy-3-methoxy-3,10-epoxy-8-(2-methylpropanoyloxy)-germacra-4,11(13)-diene-6,12-olide (4). The activity of sesquiterpene lactones on superoxide anion (O(2)(o)(-)) generation from PMA-activated neutrophils was evaluated. Compound 1 did not show a full dose dependent behavior. The IC(100) was 8+/-1, 12+/-1, and 17+/-3 microM for 2 to 4, respectively.     

A new benzophenanthridine alkaloid from Zanthoxylum buesgenii

A new benzophenanthridine alkaloid, 6-[2'-ethoxy-2'-(2',4',5'-trimethoxyphenyl)] ethyl-7,8-dimethoxy-5-methyl-2,3-methylenedioxy-5,6-dihydrobenzo[c]phenanthridine named buesgeniine (1), as well as the known decarine, were isolated from the extract of the stem bark of Zanthoxylum buesgenii. In addition, three known lignans, sesamine, matairesinol dimethylether, and methylpluviatilol, were also identified. The structure of 1 was elucidated using spectroscopic methods.     

Constituents of aromatic plants: teucrin A

Teucrium chamaedrys L. (Labiatae), a herb used to combat obesity, can occasionally cause hepatitis. All mutagenicity tests done were negative. After 13 weeks of administration by oral route in Sprague Dawley rats T. chamaedrys proved to be well tolerated at 0.056 g kg(-1) day(-1) (i.e. 0.4 mg kg(-1) day(-1) of teucrin A). At this dose the compound induced minor effects on body weight of both males and females and slight, reversible liver changes, confined to females, which mainly consisted of hepatocellular hypertrophy. This modification, in absence of other morphological findings can be considered an adaptative metabolic, rather than toxic effect.