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.
Subject(s)
Humans , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Absorption , Biological Transport , Caco-2 Cells , Flavanones , Pharmacology , Glucosides , Pharmacology , Glycyrrhiza uralensis , Chemistry , Hydrogen-Ion Concentration , Permeability , Plants, Medicinal , Chemistry , Strychnine , Pharmacokinetics , Strychnos nux-vomica , Chemistry , Verapamil , PharmacologyABSTRACT
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.
Subject(s)
Humans , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Absorption , Biological Transport, Active , Caco-2 Cells , Drugs, Chinese Herbal , Pharmacology , Hydrochlorothiazide , Pharmacokinetics , Hydrogen-Ion Concentration , Indole Alkaloids , Pharmacology , Isoflavones , Pharmacology , Plants, Medicinal , Chemistry , Time Factors , Vasodilator Agents , Pharmacology , Verapamil , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To investigate the relationship between adiponectin and beta-cell function in abdominal visceral obesity women.</p><p><b>METHODS</b>Nine abdominal visceral obesity women (VO), 9 normal subjects (C) and 7 patients with type 2 diabetes mellitus (T2DM) were enrolled in the study. Beta-cell function and insulin sensitivity were determined by hyperglycemic clamp, fasting serum adiponectin was assayed by ELISA and regional body fat was measured by MRI.</p><p><b>RESULT</b>The levels of first phase insulin release (FPIR), glucose disposal rates (GDR), insulin sensitivity index (ISI) and adiponectin were significantly elevated in control group compared with VO group and T2DM group. As compared with T2DM group, the levels of adiponectin, FPIR, second phase insulin release (SPIR) and maximum insulin release (INS(max)) increased significantly in VO group. Multiple stepwise regression analysis showed that age, FPIR and GDR were positively correlated to adiponectin (B=0.145, 0.194, 0.277 respectively, all P<0.05), while waist-hip ratio was negatively correlated with adiponectin (B=-7.424, P<0.05).</p><p><b>CONCLUSION</b>The visceral obesity women have lower adiponectin levels, and hyperadiponectinemia may be the link with insulin secretion.</p>
Subject(s)
Adult , Female , Humans , Middle Aged , Abdominal Fat , Adiponectin , Blood , Glucose Clamp Technique , Insulin-Secreting Cells , Physiology , Obesity , BloodABSTRACT
The plasma visfatin,endothelium-dependent artery dilation and intima-media thickness of common carotid arteries were measured in first-degree relatives of type 2 diabetes,obese patients and control subjects.Regional body fat were detected by MRI.The result suggested that plasma visfatin levels were significantly higher in obese subjects than those in non-obese subjects,and hypervisfatinemia is independently associated with fasting blood glucose.