Comparison of intestinal absorption of two insulin-mimic vanadyl complexes using Caco-2 monolayers as model system

被引:0
作者
YANG Xiaogai
National Research Laboratories of Natural and Biomimetic Drugs
Laboratories of Preventive Drugs
Analytical Center of Peking University. Beijing 100083
机构
关键词
vanadyl complex; Caco-2; ADME; intestinal absorption;
D O I
暂无
中图分类号
R965 [实验药理学];
学科分类号
100602 ; 100706 ;
摘要
Intestinal absorption of two oxovanadium complexes, vanadyl acetylacetonate (VO(acac)2) and bis-(maltolato)-oxovanadium (VO(ma)2), has been compared using Caco-2 monolayers as a model system. The two compounds are similar in chemical structures but different in glucose-lowering effects. Our experimental results show that they are both transported via passive diffusion with apparent permeabilty coefficients (apical→basolateral) of (82.0 ± 6.7) ×10-7 and (14.6 ± 0.7) ×10-7 cm·s-1, respectively. This suggests that absorptivity of VO(acac)2 is much higher than that of VO(ma)2. This difference may be related to the metabolism of either compound, or its ligand, or both in the course of the transport. However, This difference in absorption will cause the great difference in bioavailability, which might account for better efficacy of VO(acac)2 than VO(ma)2 as the insulin-mimic agent.
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页码:876 / 881
页数:6
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