Abstract: A new selaginellin derivative named as selaginellin S (1) was isolated from the whole plants of Selaginella pulvinata (Hook. et Grev.) Maxim. (Selaginellaceae), together with a known one (selaginellin M, 2). Compounds 1 and 2 were separated and purified by silica gel and Sephadex LH-20 column chromatography. Their structures were determined on the basis of extensive spectroscopic analysis including IR, MS, 1D and 2D NMR experiments, as well as ECD calculations. Compound 1 is a key intermidiant in the biosynthesis pathway of selaginellins. Compound 2 is first reported in this plant.

AIM: To elucidate the effect of HPMC on the floating and releasing performances of Zuojin Gastric Floating Sustained-Release Tablets(ZJ-GFST) and to select the optimum matrix adjuvant for ZJ-GFST. METHODS: Seven kinds of ZJ-GFST from pharmaceutical factories as main adjuvant respectively.The floating lag time and the sustained floating time were used to evaluate the floating performance of ZJ-GFST.The accumulative releasing rates of berberine and palmatine in vitro were used to evaluate the releasing efficiency of ZJ-GFST. RESULTS: The tablets prepared with HPMC MK-100000 and MK-15000 disintegrated quickly when contacting with water, and the tablets prepared with HPMC MK-100M and MK-4000 had too long floating lag time and low release speed.The tablets prepared with HPMC 60RT-50、K-4M and MK-1500 all possessed short floating lag time and long sustained floating time and suitable drug releasing rate. CONCLUSION: The selected HPMC is 60RT-50.

To explore the mechanism of the absorption of flavonoids from Abelmoschus manihot flowers, in situ intestinal recirculation was performed to study the effect of the absorption at different concentrations and different intestinal regions. To evaluate the conditions of the absorption of six flavonoids from Abelmoschus manihot flowers, the concentrations of Abelmoschus manihot in the perfusion solution were determined by HPLC at predesigned time. And we have investigated the inhibitory effect of six flavonoids from Abelmoschus manihot flowers on P-glycoprotein (P-gp) drug efflux pump. The results demonstrated that the absorption rates of flavonoids from Abelmoschus manihot flowers are not significantly different (P > 0.05) at various drug concentrations, the absorption of flavonoids from Abelmoschus manihot flowers is a first-order process with the passive diffusion mechanism. The absorption rates of each of flavonoids are significantly different. The absorption rate of flavonoid glycoside was lower than that of aglycone; the flavonoids from Abelmoschus manihot flowers could be absorbed in all of the intestinal segments. The best parts of intestine to absorb hyperoside and myricetin are jejunum and duodenum, separately. Verapamil could enhance the absorption of isoquercitrin, hyperoside, myricetin and quercetin-3'-O-glucoside by inhibiting P-glycoprotein (P-gp) drug efflux pump.

To analyze naringin, naringenin and its metabolites in rat urine and feces after intragastric administration of alcohol extract of Exocarpium Citri Grandis, healthy SD rats were fed with alcohol extract of Exocarpium Citri Grandis for 3 days. On the last day, 0-24 h feces and 0-4 h, 4-8 h, 8-24 h urine were collected and analyzed by UPLC-Q-TOF/MS. The post-acquisition data were processed using Metabolynx The result is that naringin and its 6 metabolites, naringenin and its 4 metabolites were detected in the urine of rat. Meanwhile, naringin and its 3 metabolites, naringenin and its 2 metabolites were detected in the feces of rat.

Aim: To study the synthesis and anti-platelet aggregation activities of ferulic acidic esters so as to search for novel antithrombus agents. Methods: Based on prodrug strategy and combination principles, monoesters were first synthesized by reaction of ferulic acid with alcohols, and then the monoesters were coupled with aspirin to afford bis-esters. The target compounds were assayed for anti-platelet aggregation activities in vitro. Results: Sixteen target compounds and eight sideproducts including 15 new compounds were synthesized and their struc-tures were determined by IR, MS and ~1H NMR. The results demonstrated that some tested compounds exhibited potential anti-platelet aggregation activities. Conclusion: The bis-esters of ferulic esters coupling with aspirin with 4 to 5 carbons in side chain might be used as lead compounds for further study in searching for novel antithrom-bus agents.

Aim: To evaluate the effects of bioactive extracts from Fructus Jujubae in attenuating the inflammation induced by Radix Kansui. Methods: Exoteric splenic lymphocyte ( SPL) of mouse and peritoneal macrophage ( PMψ) of rat were used as cell model to evaluate the anti-inflammatory effects of fractions from Fructus Jujubae. MTT method was used to assay SPL proliferation, and Griess method was used in NO release of PMψ. Firstly, Radix Kansui fraction was applied to induce inflammatory effects of the cells, and then, the anti-inflammatory effects of five extracts of Fructus Jujubae were investigated to determine the active fractions in Fructus Jujubae, which probably contribute to the attenuation of Radix Kansui. The effects of Fructus Jujubae extract in interfering the gastrointestinal acute damages caused by the extract of Radix Kansui were observed according to the pathological sections of mice. Results: The extract RK-3 ( diterpenes) exhibited the most significant pro-inflammatory effect. The bioactive extracts B (micromolecule saccharides and amino acids), D(flavonoid glycosides), and E (triterpenes) of Fructus Jujubae could attenuate the action of RK-3. The effective extract of Fructus Jujubae protected stomach and duodenum of mouse from acute damages caused by the extract of Radix Kansui. Conclusion: Fraction RK-3 (diterpenes) of Radix Kansui had pro-inflammatory effects, and some extracts of Fructus Jujubae could attenuate this effect of Radix Kansui. The results helped to clarify that Fructus Jujubae attenuates the toxic effect of Radix Kansui in certain cases, and the bioactive extracts of Fructus Jujubae discovered in the experiments offer the basis for further research to the active components of Fructus Jujubae.

Aim To study the combined effect Euphor-bia kansui of and Glycyrrhiza uralensis on metabolism of Kansuinine A and Kansuinine B. Methods Control, GU and GU plus EK groups were treated for 10 days, respectively. Then the liver microsomes were pre-pared. KA and KB were incubated with microsomes of each group, and concentrations of KA and KB were measured to reflect the metablism of KA and KB. E-rythromycin, diphenhydramine hydrochloride,benzbro-marone, cimetidine, fluconazole the inhibitors of CYP3 A4 , CYP2 D6 , CYP2 C9 , CYP1 A2 , CYP2 C19 respectively, were incubated with KA and KB. Con-centrations of KA and KB were measured to reveal the cytochrome P450 isoforms which involved in the metab-olism of them. KA and KB were incubated with glycyr-rhizic acid and enoxolone. Then concentrations of KA and KB were measured to reveal the effects of glycyr-rhizic acid and enoxolone to KA and KB. Results Concentrations of KA and KB in GU plus EK group were significantly higher than those in control and EK groups, which showed that the metablisom of KA and KB was inhibited in GU plus EK group. In addition, concentrations of KA and KB were higher in microsomes incubated with erythromycin, diphenhydramine hydrochloride, benzbromarone, cimetidine and fluconazole than in control group, which revealed that the metablism of KA and KB was slowed down when CYP3A4, CYP2D6, CYP2C9, CYP1A2 and CYP2C19 were inhibited. They may participate in the metablisom of KA and KB. After incubation with glycyrrhizic acid and enoxolone, the metablism of KA and KB was slowed down. Conclusions KA and KB may be the substrates of CYP2C19. GU plus EK can inhibit the activity of CYP2C19, which resulted in KA and KB metablism slowing down and accumulation. In addition, glycyrrhizic acid and enoxolone can inhibit the metablism of KA and KB. It may be one of the reasons of increased toxicity of GU plus EK.

AIM:To study the chemical constituents of the roots of Astragalus hoantchy Franch.. METHOD:Isolation and elucidation of the chemical constituents,were conducted by chromatography and spectral evidences. RESULTS and CONCLUSION:Six steroids and four anthraquinones were isolated from the roots of A. hoantchy. Their structures were identified to be stigmastane-3,6-dione (1),5α,8α-epidioxy- (22E,24R)-ergosta-6,22-dien-3β-ol (2),stigmastane-3β,6α-diol (3),daucosterol (4),β-sitosterol (5),stigmasterol (6),chrysophanol (7),emodin (8),physion (9) and aloe-emodin (10) on the basis of spectral data and physical constants. Among them,compounds 1,2,3,7,8,9,10 were isolated from the genus Astragalus for the first time.

Objective:To investigate the ameliorated effects of n-butanol extract from Radix Pseudostellariae(RP) on rat experimental cardiopulmonary Injury induced by acute myocardial infarction.Methods:The experimental rat cardiac and lung injury was reproduced by acute cardiac infraction ligating left coronary artery for 4 weeks.Cardiac function were assayed by hemodynamics,heart index and lung index were detected by weighting,pathologic change was checked out by histophathology,and cardiac infarction size was assayed by image analysis system.Results:After operation 4 weeks,cardiac function was disturbed according to the results of hemodynamics.Cardiac and lung index,and cardiac infarction size was significantly increased in model group.Results of histopathology indicated that cardiac myocyte decrease,cardiac fibrosis functional disorder of the heart,increase of heart index and lun index,inflammatory cell infiltration,and pulmonary congestion and edema and so on indicated the model was succeed.Continued administration of n-butanol extract from RP for 4 weeks can remarkable ameliorate cardiac function,decrease the cardiac and lung index,and attenuate the heart failure pathological change.Conclusion:N-butanol extract from RP can alleviate rat cardiopulmonary injury induced by acute myocardial infarction.The present research provided the pharmacological base of replenishing qi for invigorating the spleen and promoting body fluid production for nourishing lung.

The relationship of dose and effect in TCM formulae was an important subject in the TCM modernization research.Some characteristic properties of TCM dose-effect relationship were proposed in this paper: the dose-effect relationship of TCM had a specifi c regulation from the whole-view idea in traditional medical theories besides common properties,nonlinear character from the compatibility of medicine properties,and multi-effects varied with the different compatibility from the alternation of doses.The subjects of dose-effect relationship included single medicine,drug pair and formulae.The study on the dose-effect relationship of TCM might be helpful to the explanation of conception,connotation,ideas and methods of TCM,provide scientifi c supports and instructions for the TCM clinical practices,and provide research bases for the TCM innovation.