Development of na HPLC-MS/MS method for the determination of ginsenosides Rg1 and Rb1 from 'Shenmai' Injection in beagle dogs after single and multiple doses and application in pharmacokinetics.

Shenmai Injection (SMI), which tonifies Qi and prevents exhaustion, nourishes Yin and generates body fluid, is usually used in the treatment of shock with deficiency of Qi and Yin, coronary artery disease, viral myocarditis, granulocytopenia and chronic pulmonary heart disease clinically. Ginsenosides Rg1 and Rb1 are the main active ingredients of SMI. In this study, high-performance liquid chromatography tandem mass spectrometry methods for quantification of Rb1 and Rg1 in beagle dogs were developed and validated according to international regulatory guidelines. The methods were applied to measure the pharmacokinetics parameters of the two ginsenoside after intravenous administration. The linear ranges of the analytes were 3.9-1,000 ng/ml for Rg1 and Rb1. After injection of single and multiple doses of SMI (1 ml/kg), the plasma concentration-time profiles of Rg1 and Rb1 met the characteristics of one-compartment and typical two-compartment intravenous injection.

Bioactive constituents from Salacia cochinchinensis.

Two new isopimarane diterpenoids, named 1α-hydroxy-7-oxoisopimara-8, 15-diene (1), 11ß-hydroxy-7-oxoisopimara-8(14), 15-diene (2), together with six known compounds (3-8), were isolated from the medicinal plant Salacia cochinchinensis. All isolates were assayed for their cytotoxicity and α-glucosidase inhibitory activity. Results suggested compounds 1, 3 possessed significant cytotoxic activity against HepG2, HL60, and Hela cell lines with IC50 values ranging from 0.23 to 0.35 µM, and compounds 7, 8 exhibited noticeable α-glucosidase inhibitory ability with IC50 values of 0.25 and 0.31 µM, respectively.

[A new guaiane-type sesquiterpenoid from Croton yunnanensis].

Five sesquiterpenoids were isolated from 90% ethanol extract of Croton yunnanensis by silica gel,Sephadex LH-20 column chromatography,as well as prep-HPLC methods. Based on MS,1 D and 2 D NMR spectral analyses,the structures of the five compounds were identified as 11-methoxyl alismol(1),6ß,7ß-epoxy-4α-hydroxyguaian-10-ene(orientalol C,2),multisalactone D(3),arvestonol(4),and 4,5-dihydroblumenol A(5). Compound 1 was a new guaiane-type sesquiterpenoid. Compounds 2-4 were isolated from the Croton genus for the first time,and compound 5 was obtained from this plant for the first time.

Bioactive glycosides from Salacia cochinchinensis.

Four new triterpene glycosides, named salaciacochinosides A-D (1-4) were isolated from the 90% ethanol extract of Salacia cochinchinensis, together with five known compounds 2α,3ß,23-trihydroxyurs-12,18-dien-28-oic acid 28-O-ß-d-glucopyranoside (5), racemiside (6), alangiplatanoside (7), acantrifoside E (8), and syringin (9). The structures of the four new triterpenoids were characterized by chemical methods and MS, IR, 1D and 2D NMR spectral analyses. The α-glucosidase inhibitory activities of the nine compounds were assessed, compounds 6 and 7 showed remarkable α-glucosidase inhibitory activities, with IC50 values of 0.44 and 0.75 µM, respectively. Compounds 1-5 exhibited moderate α-glucosidase inhibitory activities, and compounds 8 and 9 showed none α-glucosidase inhibitory activity in our current experiments.

Triterpenoid saponins from the roots of Cyathula officinalis and their inhibitory effects on nitric oxide production.

The present study was designed to investigate the chemical constituents of the roots of Cyathula officinalis. Compounds were isolated by silica gel, Sephadex LH-20, ODS column chromatography, and preparative HPLC. Their structures were determined on the basis of 1D and 2D NMR techniques, mass spectrometry, and chemical methods. One new oleanane-type triterpenoid saponin, 28-O-[α-L-rhamnopyranosyl-(1→3)-ß-D-glucuronopyranosyl-(1→3)-ß-D-glucopyranosyl] hederagenin (1), was isolated from the roots of Cyathula officinalis. The anti-inflammatory activities of the isolates were evaluated for their inhibitory effects against LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages cells. Compounds 2, 4, and 6 exhibited moderate anti-inflammatory activities.

[The impact of Yishenqinghuo recipe on alveolar bone reconstruction of rats with experimental periodontitis].

PURPOSE: To evaluate the impact of Yishenqinghuo recipe on alveolar bone reconstruction of rats with experimental periodontitis. METHODS: 12-months old Spague-Dawley rats were selected for the study. All rats were randomly divided into 4 groups. Group A: control group (with no periodontitis model, fed with the same dosage of saline as Group D); Group B: model group (with periodontitis model, fed with the same dosage of saline as Group D); Group C: high-dosage group (with periodontitis model, fed with doubling dosage of medicine as Group D); Group D: equivalent-dosage group (with periodontitis model, fed with clinical equivalent effective dosage of medicine). After being gavaged with medicine/saline for 3 months, the alveolar bone were collected to make undecalcified histological slices and evaluate the changes of alveolar bone histomorphometric parameters. All the results were analyzed by ANOVA, with the use of SAS 6.04 software package. RESULTS: Compared with group B, the formation of osteoid were increased and had less free ending trabecular in group C and D. The percent age of trabecular area (%Tb.Ar) and node-terminus ratio (NTR) of alveolar bone for this 4 groups were 75.24+/-3.82/1.49+/-0.12, 45.78+/-6.70/0.48+/-0.08, 73.33+/-4.20/1.33+/-0.06 and 67.69+/-2.83/1.26+/-0.10,respectively. This two parameters of group B were much lower than that in other three groups (P<0.01). At the same time, the NTR in group D was significantly lower than that in group A (P<0.01). The osteoid area (Os.Ar) of different groups were (88.44+/-7.52) microm(2), (145.37+/-13.91) microm(2), (211.10+/-22.96) microm(2) and (201.22+/-24.75) microm(2) (transformation variables), respectively. The Os.Ar of group A was lowest, and that in group B was lower than group C and D, there were significant differences(P<0.01). CONCLUSIONS: From this study, we conclude that Yishenqinghuo recipe is in favor of enhancing alveolar bone quantity, improving bone structure and reconstructing bone loss of rats with experimental periodontitis. Supported by National Key Technologies R&D Program (Grant No.2004BA726) and Natural Science Foundation of Shanghai Municipality (Grant No.03ZR14081).