Triterpenoid saponins from Bupleurum marginatum and their anti-liver fibrotic activities.

A new triterpenoid saponin (1), along with five known compounds (2-6), was isolated from Bupleurum marginatum Wall. ex DC, of which compounds 2-4 were obtained for the first time from this plant. The structures were confirmed by the analysis of 1D, 2D NMR, and HR-ESIMS data, and comparison with previous spectral data. Anti-liver fibrotic activities of the isolates were determined as proliferation inhibition of LPS-induced activation of HSC-T6 in vitro.

Two new triterpenoid saponins from Bupleurum marginatum Wall. ex DC.

Two new triterpenoid saponins (1 and 2), together with two known saponins (3 and 4) were isolated from Bupleurum marginatum Wall. ex DC. Their structures were elucidated by the comprehensive spectroscopic analysis. Compounds 1 and 2 represented the rare example of an oleanane-type triterpenoid with two sugar moieties at C-3 and C-28. The cytotoxic activity of four compounds was evaluated against normal heptocell BRL-3A in vitro.

Rapid identification and structural characterization of polyoxypregnane glycosides in Dregea sinensis by HPLC-MSn and HRMS.

By HPLC-MSn and HRMS analyses, the structures of 52 polyoxypregnane glycosides were rapidly inferred from Dregea sinensis Hemsl on the basis of their sodium-cationized molecules [M + Na]+ and predominant diagnostic ions resulting from the saccharic chain on C3 and the neutral loss of substituent on C11 and C12. Compounds 1 and 7 significantly inhibited LPS-stimulated splenocyte proliferation in vitro.[Formula: see text].

Six new C-21 steroidal glycosides from Dregea sinensis Hemsl.

Six new C-21 steroidal glycosides (1-6) were separated from the root of Dregea sinensis Hemsl. and their structures were elucidated using extensive nuclear magnetic resonance, mass spectrometry, and infrared spectral analyses. Isolated compounds were evaluated for antitumor activity, which showed that compound 3 had moderate activity in Jurkat cells (IC50 19.54 ± 0.91 µM), and compounds 1-4 had significant effects against IL-2R and TNFR2 (IC50 1.518 ± 0.06 µM to 5.9 ± 0.07 µM).

C-21 steroidal glycosides from Dregea sinensis.

Two new C-21 steroidal glycosides, dregeosides D (1) and E (2), were isolated from the roots of Dregea sinensis. The structures of the isolated compounds were elucidated on the basis of 1D and 2D NMR spectra and HR-ESI-MS analysis. Finally, the inhibited effects of the isolated compounds on interleukin 2 receptor were evaluated by enzyme-linked immunosorbent assay.

Dragon's blood dropping pills have protective effects on focal cerebral ischemia rats model.

Dragon's blood is a bright red resin obtained from Dracaena cochinchinensis (Lour.) S.C.Chen (Yunnan, China). As a traditional Chinese medicinal herb, it has great traditional medicinal value and is used for wound healing and to stop bleeding. Its main biological activity comes from phenolic compounds. In this study, phenolic compounds were made into dropping pills and their protective effects were examined by establishing focal cerebral ischemia rats model used method of Middle Cerebral Artery Occlusion (MCAO), and by investigating indexes of neurological scores, infarct volume, cerebral index, cerebral water content and oxidation stress. Compared to model group, high, middle and low groups of Dragon's blood dropping pills could improve the neurological function significantly (p<0.01) and reduce cerebral infarct volume of focal cerebral ischemia rats remarkably (p<0.05-0.01). Meanwhile, each group could alleviate cerebral water content and cerebral index (p<0.05-0.01) and regulate oxidative stress of focal cerebral ischemia rats obviously (p<0.05-0.01). Activities of middle group corresponded with that treated with positive control drug. The results obtained here showed that Dragon's blood dropping pills had protective effects on focal cerebral ischemia rats.

Dragon's blood may have radioprotective effects in radiation-induced rat brain injury.

Dragon's blood is a bright red resin obtained from Dracaena cochinchinensis. It is a traditional medicinal that is used for wound healing and to stop bleeding. Its main biological activity appears to be from phenolic compounds found in Dragon's blood. In this study, the radioprotective effects of Dragon's blood were examined after whole brain irradiation of rats with either 100 MeV/u Carbon (12)C(6+) heavy ions or (60)Co γ-rays. The amounts of radiation-induced oxidative stress, inflammatory cytokines and apoptosis in irradiated rat brains were compared with and without Dragon's blood treatment. Compared to the "irradiation only" control group, the Dragon's blood treatment group significantly decreased malondialdehyde and hydrogen peroxide levels, and increased superoxide dismutase activity and glutathione levels induced by oxidative stress in radiation exposed rats (P < 0.05). Dragon's blood also significantly reduced radiation-induced inflammatory cytokines of tumor necrosis factor-α, interferon-γ and interleukin-6 levels (P < 0.05) and inhibited hippocampal neuronal apoptosis in (60)Co γ-ray irradiated rats. Furthermore, Dragon's blood significantly increased expression of brain-derived neurophic factor and inhibited the expression of pro-apoptotic caspase 3 (P < 0.05-0.01). Finally, Dragon's blood significantly inhibited expression of the AP-1 transcription factor family members c-fos and c-jun proteins (P < 0.05-0.01). The results obtained here suggest that Dragon's blood has radioprotective properties in rat brains after both heavy ions and (60)Co γ-ray exposure.

Dragon's Blood extract has antithrombotic properties, affecting platelet aggregation functions and anticoagulation activities.

ETHNOPHARMACOLOGICAL RELEVANCE: Dragon's Blood from Dracaena cochinchinensis (Lour.) S.C. Chen (Yunnan, China), as a traditional Chinese medicinal herb, was shown to have certain antithrombotic effects. A new preparation process was used to extract effective components from Dragon's Blood. A 95% ethanol extract A (EA) and a precipitate B (PB) fraction were obtained and compared. Reliability of the preparation process was validated by pharmacodynamic experiments. MATERIALS AND METHODS: A rat/mouse thrombosis and blood stasis model was developed for this study, and EA and PB effects on thrombosis, platelet functions and blood coagulation activities were analyzed. RESULTS: It was observed that the EA fraction had significantly better inhibitory effects than the PB fraction on thrombosis (p<0.05), platelet aggregation function (p<0.01) and anticoagulation activity (p<0.05-0.01). CONCLUSIONS: The results obtained here showed that EA fraction from Dragon's Blood contained pharmacologically effective compounds with antithrombotic effects, partially improving platelet function and anticoagulation activity.

Combination of HPLC chromatogram and hypoglycemic effect identifies isoflavones as the principal active fraction of Belamcanda chinensis leaf extract in diabetes treatment.

In previous study, we demonstrated the hypoglycemic effect of aqueous extract of Belamcanda chinensis leaves in rats. Here, we separated the aqueous extract of B. chinensis leaves and investigated the spectrum-effect relationships between HPLC chromatograms and hypoglycemic activities of different isolates from B. chinensis leaf extract. Sequential solvent extraction with petroleum ether, chloroform, acetic ester and n-butanol provided several isolates showing similar hypoglycemic activities, making it difficult to discriminate the active fractions. Stepwise elution through HP20 macroporous resin by water, 40% and 95% ethanol provided isolates with distinct hypoglycemic activities, representing a simple, rapid and efficient preparative separation method. Combination of HPLC chromatogram and pharmacological effect targeted a hypoglycemic activity-related region in HPLC chromatogram. Each peak in this region was analyzed by UV spectrum scan. Most of them were flavonoids in which tectoridin and swertisin were known flavonoids with anti-diabetic activities. In together, this work provides a general model of combination of HPLC chromatography and pharmacological effect to study the spectrum-effect relationships of aqueous extract from B. chinensis leaves, which can be used to find principle components of B. chinensis on pharmacological activity.

[Suitable oxygen concentration for rat model's hypoxic preconditioning].

OBJECTIVE: To study the suitable oxygen concentration in hypoxic preconditioning. METHODS: Short-term and long-term intermittent hypoxia modes were designed and the effects of various oxygen concentrations on body weight, blood oxygen saturation, swimming capability were analyzed. RESULTS: The rate of body weight gain in rat model decreased gradually when exposed to hypoxia environment for long time. When the concentration of oxygen changed from 15% to 8%, accompanied with the decreasing of oxygen concentration, a platform was observed in blood oxygen saturation of rat model after hypoxic preconditioning training. Rat swimming capability improved significantly. After trained in 10% hypoxia environment, the swimming capability of kunming mice improved obviously. CONCLUSION: Proper level of hypoxic preconditioning training could improve hypoxia tolerance and enhance the rat sport capability significantly. 15%-10% oxygen concentration range could be regarded as a helpful effective area for hypoxic preconditioning, 10% oxygen concentration might be the eligible concentration for hypoxic preconditioning training.

Superparamagnetic lysozyme surface-imprinted polymer prepared by atom transfer radical polymerization and its application for protein separation.

Molecular imprinting as a promising and facile separation technique has received much attention because of their high selectivity for target molecules. In this study, the superparamagnetic lysozyme surface-imprinted polymer was prepared by a novel fabricating protocol, the grafting of the imprinted polymer on magnetic particles in aqueous media was done by atom transfer radical polymerization (ATRP), and the properties of the imprinted polymer were characterized in detail. Its high selective adsorption and recognition to lysozyme demonstrated the separation ability of the magnetic imprinted material to template molecule, and it has been used for quick and direct separation of lysozyme from the mixture of standard proteins and real egg white samples under an external magnetic field. Furthermore, the elution of lysozyme from the imprinted material was achieved by PEG/sulphate aqueous two-phase system, which caused lysozyme not only desorption from the imprinted materials but also redistribution in the top and bottom phase of aqueous two-phase system. The aqueous two-phase system exhibited some of the extraction and enrichment effect to desorbed lysozyme. Our results showed that ATRP is a promising method for the protein molecularly imprinted polymer preparation.

[Study on the flavonoids compounds of Thesium chinese].

OBJECTIVE: To study the flavonoids compounds from the effective fraction of Thesium chinese in anti-inflammation. METHODS: The isolation and purification were carried out by many kinds of column chromatographic techniques. The flavonoids were analyzed by HPLC-DAD, and elucidated by 1H-NMR, 13C-NMR and ESI-MS. RESULTS: Five compounds were obtained and therir structures were determined as kaempferol-3-O-glucoside (I), rutinoside (II), luteolin-7-O-glucoside (III), kaempferyl 5-methyl ether (IV), apigenin-5-O-neohesperidoside (V). CONCLUSION: Compounds IV and V are isolated from this plant for the first time.

Antihyperglycemic effect of Cephalotaxus sinensis leaves and GLUT-4 translocation facilitating activity of its flavonoid constituents.

The objectives of this study were to investigate the antihyperglycemic effect of Cephalotaxus sinensis leaves and to identify the active components. The antihyperglycemic effect of various fractions (FA, FB, FC, FD) of the 80% ethanol extract of the leaves was evaluated in streptozotocin (STZ)-induced diabetic rats. Among the tested fractions, FC was the most active. FC (0.48 g/kg) given orally for 10 d reduced significantly (p<0.001) the blood glucose of STZ-induced diabetic rats. The food and water intakes of FC (0.48 g/kg)-treated diabetic rats were reduced significantly (p<0.001) when compared to the 0.5% carboxymethyl cellulose (CMC)-treated diabetic rats. The activity-guided fractionation of the ethanol extract of C. sinensis leaves furnished three flavonoid compounds, apigenin-5-O-[alpha-L-rhamnopyranosyl-(1-->4)-6-O-beta-D-acetylglucopyranoside] (1), apigenin (2), and apigenin-5-O-[alpha-L-rhamnopyranosyl-(1-->4)-6-O-beta-D-glucopyranoside] (3). The elevation of GLUT-4 protein level in membrane preparations from mice adipocytes was detected by Western blot analysis after adipocytes were pre-incubated with FC (0.1, 1, 10 mg/ml), apigenin (0.1, 2 mg/ml) and apigenin-5-O-[alpha-L-rhamnopyranosyl-(1-->4)-6-O-beta-D-acetylglucopyranoside] (0.1, 2 mg/ml), respectively. Phytochemical investigation and HPLC-DAD analysis of FC indicated that the flavonoids were the major constituents in this fraction. These results suggest that the fraction from C. sinensis leaves is a promising drug for the treatment of diabetes, and that the flavonoids from this plant are the active constituents.

[Determination of astragulin in Thesium chinese by RP-HPLC].

OBJECTIVE: To establish a determination method of astragulin in Thesium chinese. METHOD: RP-HPLC analytical method was established using a Polaris C18 column and acetonitrile-water (23:77) as the mobile phase, with a flow rate of 10 mL x min(-1), detected at 346 nm. The method of sample is refluxing exation by 50% alcohol for 2 times. RESULT: The content of astragulin was from 0. 120% to 0. 155%, in different groups of T. chinese collected from the same location. CONCLUSION: The method was validated to show convenient and reliable.