RESUMO
The effects of Cinnamon granules on pharmacokinetics of berberine in Rhizoma Coptidis granules in healthy male volunteers, and the compatibility mechanism of Jiao-Tai-Wan (JTW) composed of Rhizoma Coptidis granules and Cinnamon granules were investigated. The concentration of berberine in plasma of healthy male volunteers was determined directly by high performance liquid chromatography (HPLC) after an oral administration of Rhizoma Coptidis granules alone or combined with Cinnamon granules (JTW). The plasma concentration-time curves of berberine were plotted. The data were analyzed with Drug and Statistics (DAS) 2.0 pharmacokinetic program (Chinese Pharmacology Society) to obtain the main pharmacokinetic parameters. The results showed that the plasma concentration-time curve of berberine was described by a two-compartment model. The C(max), T(max), t(1/2) and CLz/F of berberine in Rhizoma Coptidis granules were 360.883 μg/L, 2.0 h, 3.882 h, 119.320 L·h(-1)·kg(-1) respectively, and those of berberine in JTW were 396.124 μg/L, 1.5 h, 4.727 h, 57.709 L·h(-1)·kg(-1) respectively. It was suggested that Rhizoma Coptidis granules combined with Cinnamon granules could increase the plasma concentration of berberine, promote berberine absorption and lengthen the detention time of berberine in healthy male volunteers.
RESUMO
This study investigated the effects and molecular mechanisms of genistein in improving insulin resistance induced by free fatty acids (FFAs) in HepG2 hepatocytes. A model of insulin resistance in HepG2 cells was established by adding palmitic acid (0.5 mmol/L) to the culture medium and the cells were treated by genistein. Glucose consumption of HepG2 cells was determined by glucose oxidase method. The levels of c-jun N-terminal kinase (JNK) phosphorylation, insulin receptor substrate-1 (IRS-1) Ser307 phosphorylation, JNK, IRS-1, phosphatidylinositol-3-kinase p85 (PI-3K p85) and glucose transporter 1 (GLUT1) proteins were detected by Western blotting. The results showed that after the treatment with palmitic acid for 24 h, the insulin-stimulated glucose transport in HepG2 cells was inhibited, and the glucose consumption was substantially reduced. Meanwhile, the expressions of IRS-1, PI-3K p85 protein and GLUT1 were obviously reduced, while the levels of JNK phosphorylation and IRS-1 Ser307 phosphorylation and the expression of JNK protein were significantly increased, as compared with cells of normal control. However, the aforementioned indices, which indicated the existence of insulin resistance, were reversed by genistein at 1-4 μmol/L in a dose-dependent manner. It was concluded that insulin resistance induced by FFAs in HepG2 hepatocytes could be improved by genistein. Genistein might reverse FFAs-induced insulin resistance in HepG2 cells by targeting JNK.
RESUMO
Objective: To study the mechanism and effect of Chinese medicine Yiqi Tongyang Huatan prescription(益气通阳化痰方,YQTYHT) on hyperlipidemia and atherosclerosis(AS).Methods: The rabbit′s model was established by feeding the food containing high cholesterol,and 32 rabbits were randomly divided into four groups(each n=8): normal group,model group,Huoxue Huayu prescription treatment group(活血化瘀方,HXHY group) and YQTYHT treatment group(YQTYHT group).Before the experiment,at the end of 6 th and 12 th weeks after the experiment,the following items were measured: blood lipids platelet aggregation rate,platelet adhesion rate,malondialdehyde(MDA),endothelin-1(ET-1),nitric oxide(NO),the ratio of the lipid plaque area and the thickness of the endothelial plaque.Results: After feeding the food containing high cholesterol,the blood lipids,platelet aggregation rate,platelet adhesion rate,MDA,ET1,the ratio of lipid plaque area and the thickness of plaque were elevated significantly,while serum NO3-/NO2-decreased significantly in model group.Compared with the model group,the blood lipids were lower in the two treatment groups,and the blood lipid regulating effect in YQTYHT group was significantly better than that in HXHY group.Platelet aggregation rate and platelet adhesion rate of YQTYHT group and HXHY group were lower than those in the model group,but the degree of lowering in YQTYHT group and HXHY group had no significant differences.The serum MDA of YQTYHT group and HXHY group was lower than that in model group,and the lowering effect in YQTYHT group was better than that in HXHY group.YQTYHT group and HXHY group had a significant increase on the level of serum NO3-/NO2-and a decrease on the content of plasma ET-1,furthermore,the effects in the former group were significantly better than those of the latter group.The area of atherosclerotic plaque coverage in aorta and the thickness of plaque of HXHY group were larger than those in YQTYHT group(both P