[Protective effects of 3'-methoxy-puerarin on rat brain suffering from ischemia].

OBJECTIVE: To research on the protective effect of 3'-methoxy-puerarin (3'-mo-pue) on rat brain suffering from ischemia and to offer the experimental basis for widening the applied areas of Radix Puerariae. METHOD: All rats were randomly divided into sham operation group, control group, Pue group and 3'-mo-pue group. The influence of different dosage on relevant indexes were measured through cerebral artery occlusion (MCAO) model rat covered by Fecl3, and cerebral ischemia-reperfusion model rat after 2VO. RESULT: The result showed that 3'-mo-Pue could reduce the scores of neurological deficit, cerebral infarcted zone to varying degrees and the water content of brain tissue in MCAO model. It could obviously increase the activity of CAT and GPx in the hippocampus and also increase the activity of CAT and GPx in the cortex in the ischemia field. Moreover, 3'-mo-Pue could decrease the content of LPO, LD in the brain tissue of cerebral ischemia-reperfusion model rat. CONCLUSION: 3'-mo-Pue has favorable protective effect on brain suffering from ischemia. The mechanism is possibly related to its effect of anti-oxidation.

[Pharmacodynamical research of Jingu Tongxiao granule].

OBJECTIVE: To study functions of Jingu Tongxiao granule (JGTXG, treatmenting ache of bones and muscles) in antiphlogistic and antalgic aspect, invigorating the circulation of blood and absorbing clots and antitraumatic soft tissue. METHOD: Animal models of inflammation, ache, gore and traumatic soft tissue were adopted, and pharmacodynamic actions of Jingu Tongxiao granule were observed. RESULT: JGTXG could conspicuously restrain inflammatory reactions of mouse ear tumid model treated by croton oil tumid and rat foot metatarsus tumid model treated by carrageenan, and restrain pain responses of mouse caused with whipping back end method by heat stimulating and of mouse caused with wriggling body method by acetic acid being injected in its abdominal cavity. It could significantly improve petechia degree in traumatic rat blood stasis model, and prominently improve raumatized limb's tumefaction degree and alleviate blood stasis, swelling and phlogistic cell soakage in traumatic rat soft tissue model. At the same time, it could prominently restrain platelet aggregation and improve whole blood viscosity. CONCLUSION: Jingu Tongxiao granule has antiphlogistic and antalgic functions, invigorating the circulation of blood and absorbing clots and antitraumatic soft tissue, and it could keep curative effect of original dosage form.

[A comparison of the protective activity of liver injury induced by D-galact-osamine between huangqin-tang and their metabolites by human intestinal bacteria].

OBJECTIVE: To compare the protective activity of liver injury induced by D-galactosamine (GalN) between Huangqin-Tang and their metabolites by human intestinal bacteria(HIB). METHOD: The liver injuries in conventional and pseudo-germfree mice were induced by GalN. After oral administration of Huangqin-Tang and their metabolites mixtures by HIB, the serum transaminase (ALT and AST) activities were detected. RESULT: In conventional mice, large and medium doses (20 and 10 g.kg-1) of Huangqin-Tang decoction significantly reduced the increase of serum ALT activity after 18 h GalN treatment. In pseudo-germfree mice, metabolites significantly reduced the ALT levels. However, Huangqing-Tang didn't affect the ALT levels in this kind of mice. To all of the animals, AST levels remained the same after oral Huangqin-tang or their metabolites. CONCLUSION: The metabolism by intestinal bacteria plays a role in pharmacological effects of constituents of Chinese herbal medicine. The metabolites of the constituents by intestinal bacteria were the real active components in vivo.

Metabolism of constituents in Huangqin-Tang, a prescription in traditional Chinese medicine, by human intestinal flora.

In the course of studies on the metabolism of active components of Huangqin-Tang by human intestinal flora (HIF), Huangqin-Tang and all individual herbs in the decoctions were incubated with a human fecal suspension separately. By using a high-performance liquid chromatographic (HPLC) method which was previously established in our laboratory, the metabolites in both the compound prescription and all the single herb decoctions were identified and determined both qualitatively and quantitatively. We found that the constituents of Huangqin-Tang, incluing baicalin (baicalein 7-glucuronide; BG), wogonoside (wogoninoglucuronide; WG), oroxylin-A-glucuronide (OG) from Scutellariae Radix, paeoniflorin (PF) from Paeoniae Radix, liquiritin (liquiritigenin 4'-O-glucoside; LG), isoliquirtin (isoliquiritigenin 4-glucoside; ILG) and glycyrrhizic acid (GL) from Glycyhhizea Radix, were converted to their metabolites baicalein (B), wogonin (W), oroxylin-A (O), paeonimetabolin-I (PM-I), liquiritigenin (L), isoliquiritigenin (IL) and glycyrrhetinic acid (GA) by HIF. The contents of the metabolites in Huangqin-Tang and in each single herb decoction increased significantly after incubation with intestinal flora. Comparing with single herb decoctions, the transformation of BG, WG, OG, LG and ILG in the compound prescription was promoted, however, that of PF and GL was inhibited. All the results suggested that the glycosides of many medicinal herbs could be converted to aglycones by HIF, and the metabolism of most glycosides was improved in the compound prescription.

Pharmacokinetic study on the multi-constituents of Huangqin-Tang decoction in rats.

Using a validated high-performance liquid chromatographic (HPLC) method, the pharmacokinetics of multi-constituents in Huangqin-Tang decoction were simultaneously studied both in the compound prescription and in each single herb decoction. At different intervals (0, 1, 2, 4, 8, 12, 24, 36, 48 h) after oral administration of the Huangqin-Tang decoction or a single herb decoction at a dose of 10 g x kg(-1), the concentrations of the constituents and their metabolites: baicalin (BG), wogonoside (WG), oroxylin-A-glucuronide (OG), baicalein (B), wogonin (W), oroxylin-A (O), paeoniflorin (PF), paeonimetabolin-I (PM-I), liquiritin (LG), liquiritigenin (L), glycyrrhizic acid (GL) and glycyrrhetinic acid (GA), were detected in the rat plasma. A new metabolite-3,5,7,2',6'-penta hydroxy flavone (visidulin I, VD-I) was found in rat plasma after oral administration of Huangqin-Tang or a single herb Huangqin decoction, and the quality was identified by HPLC and LC/MS. The pharmacokinetic parameters of the constituents and metabolites in the compound prescription and single herb decoctions were compared. All concentration-time curves corresponded to the one-compartment model. The constituents of BG, WG, OG, VD-I and LG had higher C(max) and AUC(0-lim) in the compound prescription than in the single herb decoction, and WG had significant difference. The constituents of PF, W and O only had a higher AUC(0-lim) in the compound prescription, and O had a significant difference. It was concluded, in brief, that there were obvious differences in the pharmacokinetic parameters of most constituents (especially constituent WG) between the compound prescription and single herb decoction. The constituents in the compound prescription had delayed absorption and elimination, a longer residence time in the body, and higher C(max) and AUC(0-lim), than those in the single herb decoction. Therefore, they were more efficient and durable, making them promising to exerting pharmacological effects in vivo.