Cytotoxic steroidal glycosides from the underground parts of Hosta ventricosa.

A phytochemical study on the underground parts of Hosta ventricosa yielded one new spirostanol saponin (1), two new furostanol saponins (2 and 3), and one new pregnane glycoside (4), along with three known compounds (5‒7). Their structures were elucidated on the basis of chemical and spectroscopic analysis. All isolated compounds were evaluated for their cytotoxic effects against five human cancer cell lines (HL-60, A-549, SMMC-7721, MCF-7, and SW-480). Compounds 1, 2, and 5‒7 showed cytotoxic activities with IC50 values of 3.21-17.06 µM.

Steroidal glycosides from the underground parts of Hosta ventricosa and their anti-inflammatory activities in mice.

Two new pregnane glycosides, 2α, 3ß-dihydroxy-5α-pregn-16-en-20-one-3-O-{α-L-rhamnopyranosyl-(1→2)-[ß-D-glucopyranosyl-(1→4)]-ß-D-galactopyranoside} (1) and 2α, 3ß-dihydroxy-5α-pregn-16-en-20-one-3-O-{ß-D-glucopyranosyl-(1→2)-[ß-D-xylopyranosyl-(1→3)]-ß-D-glucopyranosyl-(1→4)-ß-D-galactopyranoside}(2), have been isolated along with two known spirostanol saponins from the underground parts of Hosta ventricosa. Their structures were elucidated on the basis of chemical and spectral evidence. The anti-inflammatory activities of these steroidal glycosides were evaluated using a xylene-induced ear edema model. Our results indicated that the compounds exhibited promising anti-inflammatory activities.

Anxiolytic and anti-depressant effects of hydroalcoholic extract from Erythrina variegata and its possible mechanism of action.

BACKGROUND: Erythrina variegata has been widely used as a traditional medicine. OBJECTIVE: The study was designed to evaluate the anxiolytic and anti-depressant effects of an extract from Erythrina variegata. METHODS: The extract was evaluated for anxiolytic and anti-depressant action using the elevated plus maze, light/dark box, open field, forced swimming and tail suspension tests in mice. The mechanism of action was further elucidated using high-performance liquid chromatography with fluorescence detection methods to assay the levels of five neurotransmitters in brain. RESULTS: The extract exhibited significant increase in the percentage of the open arms entries and the time spent in the open arms in the elevated plus maze test. The results of the light/dark box test revealed a significant increase in the amount of time spent in the light chamber. Extract- treated mice also produced significant increase in the number of crossings and rearings in the open field test. In the forced swimming and tail suspension tests, the extract was able to promote significant decrease in the immobility time. In addition, the extract significantly altered the levels of five neurotransmitters in the brain tissue. CONCLUSION: These findings suggest that Erythrina variegata presents potential anxiolytic and anti-depressant activity, and the mechanism may be related to the alteration of neurotransmitter levels.

Content Determination of Phenylpropanoids and Enhancing Exercise Ability of Effective Fractions in Pedicularis densispica.

BACKGROUND: Most researches were focused on chemical constituents and bioactivities of Pedicularis. However, there were a few reports on simultaneous determination of the series phenylpropanoids compounds in Pedicularis by High Performance Liquid Chromatography (HPLC). OBJECTIVE: To establish an HPLC method for simultaneous determination of salidroside, verbascoside, iso-verbascoside, leucoseptoside A, jionoside D and martynoside in Pedicularis densispica (PD), and to assess the enhancing exercise ability of effective fractions of phenylpropanoids (EFP). MATERIALS AND METHODS: The separation was performed on C18 column with step-wise gradient elution with water (A)-methanol (B) as the mobile phase at a flow rate of 1.0 mL/min, with detection wavelength at 275 nm (0-4 min) and 330 nm (4-40 min). The EFP were obtained from extracts of PD by resin gradient dilution. The enhancing exercise ability of EFP was exerted in exhaustive swimming and anoxia endurance tests in vivo. RESULTS: The contents of six marker compounds had good linear relationship in the ranges of 2.10-8.40, 13.60-54.40, 0.93-3.72, 0.53-2.12, 1.50-6.00, 0.37-1.28, respectively, and the average recoveries of the six phenylpropanoids were all in the range of 98-103%. Total contents of phenylpropanoids in EFP were more than 60%. Three medicine groups of exhaustive swimming and anoxia endurance time were higher than those of the water group. CONCLUSION: The analytical method is reliable, simple and accurate, and can be used for the comprehensive quality control of PD. This experiment suggests that PD has the effect of promoting the recovery and elimination of fatigue and improving the exercise capacity. SUMMARY: A simple, practical and low-cost RP-HPLC method has been developed for the simultaneous determination of six marker phenylpropanoids in Pedicularis densispica.Three effective fractions of phenylpropanoids groups of exhaustive swimming and anoxia endurance time were higher than those of the water group.The separation was performed on C18 column with stepwise gradient elution with water-methanol. The enhancing exercise ability was exerted in exhaustive swimming and anoxia endurance tests in vivo.This plant has the effect of promoting the recovery and elimination of fatigue and improving the exercise capacity. Abbreviation used: PD: Pedicularis densispica, EFP: Effective fractions of phenylpropanoids, DAD: Diode array detector, HPLC: High performance liquid chromatography, LOD: Limits of detection, LOQ: Limits of quantification, RSD: Relative standard deviation, BV: Bed volumes.

Central anti-fatigue activity of verbascoside.

In this study, the effects of verbascoside on treadmill exercise endurance, 5-hydroxytryptamine (5-HT) concentrations, the second isoforms of tryptophan hydroxylase (TPH2) and serotonergic type 1B inhibitory autoreceptors (5-HT1B) protein expression in the caudate putamen of exercised rats were investigated. Sixty Sprague-Dawley male rats were randomly divided into six groups: normal group, exercise group, exercise and verbascoside (0.1mg/kg)-treated group, exercise and verbascoside (1mg/kg)-treated group, exercise and verbascoside (10mg/kg)-treated group, exercise and caffeine (10mg/kg)-treated group. In exercise groups, rats were put on treadmill and forced to run for 30min once a day for 6 consecutive days. On the 7th day of the experiment, the time to exhaustion in treadmill exercise was determined for the trained groups. Immediately after the determination of the exhaustion time, all rats were sacrificed. 5-HT concentrations were detected by HPLC analysis. TPH2 and 5-HT1B protein expression were measured by western blot analysis. We found that verbascoside could prolong the time to exhaustion in treadmill exercise and suppress the exercise-induced increase of 5-HT synthesis and TPH2 protein expression, and prevent the exercise-induced decrease of 5-HT1B protein expression in the caudate putamen. Verbascoside was found as effective as caffeine in these effects. Verbascoside at 10mg/kg improved endurance of exercised rats. The mechanism of verbascoside' s anti-fatigue activity might be related to the inhibition of the exercise-induced synthesis of 5-HT and TPH2 expression, and to the increase of the 5-HT1B expression in the caudate putamen of exercised rats.

The effects of Acorus tatarinowii Schott on 5-HT concentrations, TPH2 and 5-HT1B expression in the dorsal raphe of exercised rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Acorus tatarinowii Schott (Shi Chang Pu) belongs to the family of Acoraceae. The plant is used as an important herb for prolonging life many years in traditional Chinese medicine. It is an ancient herbal tonic nutriment and can be used as anti-fatigue medicine. However, the effects of Acorus tatarinowii Schott on the endurance exercise in relation to central nervous system have not yet been clarified. In this study, the effects of Acorus tatarinowii Schott on treadmill running endurance, 5-HT concentrations, TPH2, 5-HT1B expression in the dorsal raphe of exercised rats were investigated. MATERIALS AND METHODS: Sixty adult male Sprague-Dawley rats were randomly divided into six groups: the normal group, the exercise group, the exercise and the rhizomes of Acorus tatarinowii Schott (ATS)(1mg/kg)-treated group, the exercise and ATS (10mg/kg)-treated group, the exercise and ATS (100mg/kg)-treated group, the exercise and caffeine (10mg/kg)-treated group. The effects of Acorus tatarinowii Schott on endurance exercise were determined by the time to exhaustion during treadmill exercise. The detection of 5-HT concentrations in the dorsal raphe was performed by HPLC analysis. The levels of TPH2, 5-HT1A and 5-HT1B expression were measured by western blot analysis and real-time PCR. RESULTS: We found Acorus tatarinowii Schott could prolong the time to exhaustion in treadmill exercise and suppress the exercise-induced increase of 5-HT synthesis, TPH2 mRNA and protein expression and prevent the exercise-induced decrease of 5-HT1B mRNA and protein expression in the dorsal raphe. Acorus tatarinowii Schott was as effective as caffeine in prolonging the exhaustion time in treadmill running and in decreasing the exercise-induced increase of 5-HT synthesis and TPH2 mRNA and protein expression and in preventing the exercise-induced decrease of 5-HT1B mRNA and protein expression in the dorsal raphe. CONCLUSIONS: The results indicated that the effects of Acorus tatarinowii Schott in inhibiting the exercise-induced synthesis of 5-HT and TPH2 expression and in preventing the exercise-induced decrease of 5-HT1B expression in the dorsal raphe might be the anti-fatigue mechanism of Acorus tatarinowii Schott.

Terpene and lignan glycosides from the twigs and leaves of an endangered conifer, Cathaya argyrophylla.

Labdane diterpene glycosides cathargyroside A and cathargyroside B, monoterpene glycosides vervenone-10-O-ß-D-glucopyranoside and vervenone-10-O-ß-D-apiofuranosyl-(1″→6')-ß-D-glucopyranoside, as well as lignan glycosides cedrusinin-4-O-α-L-rhamnopyranoside and (+)-cyclo-olivil-9'-O-ß-D-xylopyranoside, along with 39 known compounds, were obtained from the methanol extract of the twigs and leaves of Cathaya argyrophylla. These compounds were identified mainly by analyzing their NMR and MS data. Almost all of these compounds were hitherto unknown in this genus. The isolated compounds were screened against Candida albicans and Staphylococcus aureus for antimicrobial assay, and against K562, HT-29, BEL-7402, SGC-7901, B16, BGC-823, U251 and A549 cancer cell lines for cytotoxic activities. One compound showed antimicrobial activity against C. albicans, and four of them displayed cytotoxicity. Similarity analysis on the chemical constituents of the genera Cathaya, Picea and Pinus supported their close phylogenetic relationships.

Antimicrobial, cytotoxic lignans and terpenoids from the twigs of Pseudolarix kaempferi.

Seven new compounds, including four lignans, (+)-(8S,8'S)-9,9'-dibenzoylsecoisolariciresinol (1), (+)-(8S*,8'R*)-4,4'-dimethyloxomatairesinol (2), (+)-(7S*,8R*,8'R*,9'S*)-9'-n-butoxytsugacetal (3), and pseudolarkaemin A (4), a pyronane glycoside, pseudolarkaemin B (5), an ent-beyerene glycoside, pseudolarkaemin C (6), and a triterpene, 25-epi-pseudolarolide Q (7), along with 25 known compounds (8­32) were isolated from the twigs of Pseudolarix kaempferi. Their structures were elucidated mainly by the analysis of their NMR and MS data. Pseudolarolide C acid (24) was isolated for the first time as a natural product. All compounds were evaluated for antimicrobial activity against Candida albicans and Staphylococcus aureus, and cytotoxic activity against K562, HT-29, B16, BGC-823, BEL-7402, SGC-7901, U251, and A549 cancer cell lines were assayed. Results indicated that the new compounds 3, 7, and some known compounds showed antimicrobial and cytotoxic activities.

[Flavonoids and nor-sesquiterpenes of Pedicularis densispica].

OBJECTIVE: To study the chemical constituents of the whole plants of Pedicularis densispica. METHOD: The chemical constituents were isolated by various chromatographic methods and their structures were determined by chemical evidences and spectral data. RESULT: Ten compounds were isolated and identified as acacetin (1), apigenin-7-0-beta-glucopyranoside (2), kaempferol-3,7-O-alpha-dirhamnopyranoside (3), scutellarein-7-0-beta-glucopyranoside (4), chrysoeriol-7-O-beta-glucopyranoside (5), pedicutricone A (6), dearabinosyl pneumonanthoside (7), salidroside (8), darendoside B (9), and maltol-beta-D-glucopyranoside (10). CONCLUSION: These compounds were isolated from the titled plant for the first time. Except compounds 6 and 8, the others were obtained for the first time from the genus Pedicularis.

[Progress in research on Pedicularis plants].

Pedicularis comprises about 300 species in China and hemiparasite is its most important characteristic. Many compounds have been isolated from the genus, including phenylpropanoids, iridoids, flavonoids and so on. Among them, some showed antioxidative, antitumor, antifatigue, repairing DNA and antidiabetic activities. This review summarized hemiparasite, chemical constituents and pharmacological activities on Pedicularis plants. The aim was to provide information for the further study of Pedicularis.