| Comparison of intestinal absorption of two insulinmimic vanadyl complexes using Caco-2 monolayers as model system |
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| 作者单位： | YANG Xiaogai(Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China);Yuan Lan(Analytical Center of Peking University, Beijing 100083, China);WANG Kui,Yang Xiaoda(Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China;National Research Laboratories of Natural and Biomimetic Drugs, School or Pharmaceutical Sciences, Peking University, Beijing 100083, China;Laborat) |
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| 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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| 关 键 词： | 氧矾根络合物 Caco-2 肠内吸收 模型系统 胰岛素模拟物 ADME |
| 收稿时间： | 2002-07-19 |
Comparison of intestinal absorption of two insulin-mimic vanadyl complexes using Caco-2 monolayers as model system |
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| Authors: | Xiaogai Yang Lan Yuan Kui Wang Xiaoda Yang |
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| Institution: | e-mail: xiao-dayang@hotmail.com |
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| Abstract: | 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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| Keywords: | vanadyl complex Caco-2 ADME intestinal absorption |
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