OBJECTIVE:To study the effect of grape seed procyanidins on protein expressions of cysteine aspartic protease 3 (Caspase-3), tumor necrosis factor-related receptors (TRAF6) in renal tissue of rats with renal ischemia-reperfusion injury (RIRI),and explore the protective mechanism of procyanidins on RIRI. METHODS:50 rats were randomly divided into sham op-eration group,model group,Shenfukang capsules group(positive control,600 mg/kg),procyanidins low-dose,high-dose groups (100,150 mg/kg),10 in each group. All rats were intragastrically administrated once a day,for 7 d. After administration,rats in other groups except for sham operation group were established the RIRI model.After the modeling successed of 24 h,levels of creati-nine(Cr),urea nitrogen(BUN)in serum,and protein expressions of Caspase-3,TRAF6 in renal tissue of rats in each group were detected,and apoptotic rate of renal tubular epithelial cells was determined. RESULTS:Compared with sham operation group,lev-els of Cr,BUN in serum in model group were significantly increased(P<0.05);protein expressions of Caspase-3,TRAF6 in re-nal tissue were obviously enhanced (P<0.05);apoptotic rate of renal tubular epithelial cells was obviously increased (P<0.05). Compared with model group,levels of Cr,BUN in serum in each administration group were obviously decreased(P<0.05);pro-tein expressions of Caspase-3,TRAF6 in renal tissue were obviously weakened(P<0.05);apoptotic rate of renal tubular epithelial cells was obviously decreased(P<0.05);and procyanidins high-dose group showed superior effect to low-dose group and Shenfu-kang granules group (P<0.05). CONCLUSIONS:Grape seed procyanidins can relieve the RIRI of rats,which may be achieved by reducing protein expressions of Caspase-3 and TRAF6 to inhibit the apoptotic rate of renal tubular epithelial cells.

OBJECTIVETo study the effect of combination components on pharmacokinetics of Shuxiong tablet to provide evidence for the new recipe.

METHODSix groups of rats (6 for each group) were orally administered with co-extractum of chuanxiong and honghua (CHE), mixed solution of hydroxysafflor yellow A (HSYA) and ferulic acid (FA) (HFM). Panax notoginseng saponins solution (PNS), mixed solution of PNS and CHE (PCHE), mixed solution of PNS and HFM (PHFM) and mixed emulsion of Chuanxiong volatile oil (CVO) and PHFM (CVO-PHFM), respectively. The concentrations of HSYA, FA, ginsnenoside Rg1 and Rb1 in rat plasma were determined by HPLC. Pharmacokinetic parameters (Ka, Kel, Cmax, Tmax and AUC) were calculated by model simulation. The differences of HSYA, FA, Rg1 and Rb1 in pharmacokinetics parameters after administration of six preparations were demonstrated by statistical analysis.

RESULTAfter oral administration of six preparations to rats, the concentration-time curve of HSYA and Rg1 fitted to one-compartment model, and that of FA fitted to double-compartment model. After oral administration of CHE, Kel of FA reduced; Cmax decreased; but K12 increased, significantly, compared with oral administration of HFM. Other parameters were not significant differences. After co-administration of PNS and CHE (PCHE) or PNS and HFM (PHFM), Ka of HSYA increased; Tmax reduced, significantly. After oral administration of PNS and HFM (PHFM), Ka of Rg1 improved, Tmax decreased, significantly. However, the parameters of FA and Rb1 were not significantly changed. After co-administration of CVO and PHFM (CVO-PHFM), Cmax of Rb1 decreased, K12 improved, significantly. Meanwhile, the oral bioavailability of HSYA, FA and Rg1 was improved by 6.056, 2.854 and 2.055 folds, respectively.

CONCLUSIONAfter oral administration of different combinations of Shuxiong tablet constituents, some pharmacokinetics parameters of active ingredients are significantly changed, but the bioavailability is improved only when CVO is co-administered.

Animals ; Biological Availability ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tablets ; administration & dosage ; pharmacokinetics