ABSTRACT
To study the effect of liquiritin (Liq) on the transport of strychnine (Str) in Caco-2 cell monolayer model, the transport parameters of Str, such as apparent permeability coefficient (P app (B-->A) and P app (A-->B)) and cumulative transport amount (TRcum), were determined and comparatively analyzed when Str was used solely and co-used with Liq. The effect of drug concentrations, conveying times, P-glycoprotein (P-gp) inhibitor verapamil and conveying liquor pH values on the transport of Str were also investigated. The results indicated that the absorption of Str in Caco-2 cell monolayer model was well and the passive transference was the main intestinal absorption mechanism of Str in the Caco-2 monolayer model, along with the excretion action mediated by P-gp. Liq enhanced the absorption of Str. Meanwhile, conveying liquor pH value had significant influence on the excretion transport of Str.
ABSTRACT
To study the effects of major components of Maijunan tablets, puerarin (Pue) and rhynchophylline (Rhy) on the transport of hydrochlorothiazide (Hct) Caco-2 cell monolayer model, the transport parameters of Hct, such as apparent permeability coefficient (P(app) (B --> A) and P(app) (A --> B)) and the ratio of P(app) (B --> A) versus P(app) (A --> B), were studied and compared when Hct was used solely and co-used with Pue and/or Rhy. The effects of drug concentrations, conveying times, P-glyprotein (P-gp) inhibitor verapamil and conveying Liq pH values on the transport of Hct in the above conditions were also investigated. The results indicated that the absorption of Hct in Caco-2 cell monolayer model could be a carrier-mediated active transport, along with the excretion action mediated by P-gp. Pue can decrease the excretion action of Hct mediated by P-gp, and Rhy had no significant effect on the transport of Hct. The co-use of Hct, Pue and Rhy enhanced the absorption of Hct. Meanwhile, conveying Liq pH value had significant influence on the transport of Hct. The absorption of Hct at pH 6.0 was higher than that at pH 7.4.
ABSTRACT
Objective To investigate the adiponectin levels in non-obese first-degree relatives (FDR)of type 2 diabetic subjects and its relation to insulin sensitivity and the intima-media thickness of the common carotid artery (IMT) during 5-year follow-up. Methods Fifty-three FDR subjects and 37 control subjects who were free of type 2 diabetes were enrolled. Plasma adipenectin, lipid profile, blood glucose, fasting insulin, and blood pressure were determined at baseline and after 5-year follow-up. IMT and endothelial-dependent vasodilation (EDVD) were measured by high-resolution B-mode ultrasound imaging. Homeostasis model assessment was used to evaluate insulin resistance (HOMA-IR)and β-cell function (HOMA-β). 29 FDR subjects and 20 control subjects completed the follow-up. Results Comparing with the control, plasma adiponectin levels in non-obese FDR subjects were lower at baseline [(10.06±5.79)vs (14.43±7.91) mg/L, P< 0.05]. Plasma adiponectin were decreased 24.0% in non-obese FDR and 36.7% in control duning 5 year follow-up (both P<0.05). Adiponectin levels were negatively correlated with waist-to-hip ratio (r = -0. 397), fasting blood glucose (r = -0. 373), IMT (r = -0. 372), and HOMA-IR (r=-0. 40)in the non-obese FDR. After adjusting other relevant risk factors,adiponectin was associated with age, high-density lipoprotein-cholesterol, and IMT in multiple regression analyses in non-obese FDR group. In the control group, a similar analysis revealed that low-density lipoprotein-cholesterol and IMT explained 25% of the variability in the adiponectin concentration. Conclusion Plasma adiponectin levels were decreased after 5 years in both non-obese FDR and control subjects. Decreased adiponectin level may be related to IMT increment.