Inhibitory Activities of Some Oxovanadium Complexes with N-Heterocyclic Ligands against PTP1B/ALP

Acta Chimica Sinica ›› 2009, Vol. 67 ›› Issue (9): 929-936. Previous Articles Next Articles

Original Articles

含氮杂环氧钒配合物对PTP1B和ALP的抑制活性研究

高晓丽a 卢丽萍*,a 朱苗力*,a 袁彩霞a 马俊锋b 付学奇*,b

(a山西大学分子科学研究所化学生物学与分子工程教育部重点实验室太原 030006)
(b吉林大学生命科学学院 Edmond H. Fischer细胞信号传导实验室长春 130023)

投稿日期:2009-01-05 修回日期:2009-03-26 发布日期:2009-05-14
通讯作者: 朱苗力

Inhibitory Activities of Some Oxovanadium Complexes with N-Heterocyclic Ligands against PTP1B/ALP

Gao, Xiaoli ^a Lu, Liping ^*,a Zhu, Miaoli ^*,a Yuan, Caixia ^a
Ma, Junfeng ^b Fu, Xueqi ^*,b

(a Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering, Ministry of Education, Shanxi University, Taiyuan 030006)
(b Edmond H. Fischer Signal Transduction Laboratory, College of Life Sciences, Jilin University, Changchun 130023)

Received:2009-01-05 Revised:2009-03-26 Published:2009-05-14
Contact: Zhu, Miaoli

Abstract

Protein tyrosine phosphatase 1B (PTP1B) has been emerging as an attractive drug target for diabetes disease treatment, and is also associated with the anti-diabetes effects of vanadium complexes. The inhibitory activities against PTP1B and alkaline phosphatase (ALP) by oxovanadium complexes with 2,2’-biimidazole (L1), 2,2’-bipyridine (L2) and 1,10-phenanthroline (L3) have been investigated in vitro. The complexes of [VO(L1～L3)] and [VO(L1～L3)2] have been found to be potent inhibitors against PTP1B (IC50＝120～260 nmol/L). Their inhibitory ability is close to bis(maltolato)oxovanadium (BMOV). Kinetics assays suggest that these complexes inhibit PTP1B in a classical competitive manner (Ki＝20～160 nmol/L). The inhibitory activities of these complexes against PTP1B are 103 fold higher than that against ALP, showing a selectivity against both phosphatases.

Key words: oxovanadium complex, protein tyrosine phosphatase 1B, alkaline phosphatase, inhibitor

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含氮杂环氧钒配合物对PTP1B和ALP的抑制活性研究

Inhibitory Activities of Some Oxovanadium Complexes with N-Heterocyclic Ligands against PTP1B/ALP

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