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蛋白酪氨酸磷酸酶1B(protein tyrosine phosphatase 1B,PTP1B)是当前开发治疗糖尿病药物的优秀靶标,也是钒配合物抗糖尿病作用相关的重要靶蛋白.研究了三种含氮平面杂环螯合配体2,2’-联咪唑(L1),2,2’-联吡啶(L2),1,10-邻菲咯啉(L3)的氧钒配合物对PTP1B以及碱性磷酸酶(alkaline phosphatase,ALP)的体外抑制作用.结果表明,1∶1和2∶1型配位的氧钒化合物均表现出对PTP1B较强的抑制活性,IC50值在120～260nmol/L间,抑制能力接近双麦芽酚氧钒配合物(BMOV).抑制动力学实验表明这些氧钒配合物对PTP1B的抑制模式均为竞争性抑制,抑制常数在20～160nmol/L.其对PTP1B抑制活性较ALP高103倍,表明氧钒配合物对两种磷酸酶的抑制具有一定的选择性.
Protein tyrosine phosphatase 1B (PTP1B) is an excellent target for the current development of drugs for the treatment of diabetes mellitus, and is also an important target protein for the anti-diabetic effect of vanadium complexes. Three nitrogen-containing planar heterocyclic chelates Oxygen-vanadium complex of 2,2’-biimidazole (L1), 2,2’-bipyridine (L2) and 1,10-phenanthroline (L3) PTP1B and alkaline phosphatase ALP) in vitro.The results showed that the 1: 1 and 2: 1 coordination vanadyl compounds all showed strong inhibitory activity against PTP1B with the IC50 value of 120 ~ 260nmol / L, the inhibition ability close to double malt The results of inhibition kinetics showed that the inhibition mode of PTP1B was competitively inhibited by these vanadyl complexes with the inhibition constant of 20 ~ 160nmol / L. The inhibitory activity of PTP1B was 103-fold higher than that of ALP, It is indicated that the oxygen-vanadium complex has a certain selectivity for the inhibition of two phosphatases.