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学科主题药学
Synthesis, characterization and anti-diabetic therapeutic potential of novel aminophenol-derivatized nitrilotriacetic acid vanadyl complexes
Wang, Na; Wang, Ziwei; Niu, Xia; Yang, Xiaoda
关键词Vanadium Diabetes Aminophenol Ppar Alpha Ppar Gamma
刊名JOURNAL OF INORGANIC BIOCHEMISTRY
2015-11-01
DOI10.1016/j.jinorgbio.2015.07.012
152期:SI页:104-113
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Inorganic & Nuclear
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]INSULIN-MIMETIC AGENT ; OXIDATIVE STRESS ; VANADIUM(IV) COMPLEXES ; DIABETIC-RATS ; PPAR-GAMMA ; CHEMISTRY ; ACTIVATION ; CELLS ; OXIDOVANADIUM(IV) ; MECHANISMS
英文摘要

In the present work, we synthesized three novel aminophenol-derivatized nitrilotriacetic acid vanadyl complexes (VOohpada, VOmhpada, VOphpada) using the strategy of rational incorporation of antioxidant groups in ligand in order to balance the side effects with the therapeutic properties. The complexes were characterized by IR, UV-VIS, ESI-MS and elemental analysis. The biological evaluations in vitro revealed that the position of the hydroxyl group of aminophenol moiety regulated the antioxidant activity of the complexes as well as the cytotoxicity on HK-2 cells. The vanadyl complex of p-hydroxyl aminophenol derivative (VOphpada) exhibited better antioxidant activity and lower cytotoxicity than other analogs. In type II diabetic db/db mice, VOphpada (0.1 mmol/kg/day) effectively reduced blood glucose level, improved glucose tolerance, and alleviated stresses induced by hyperglycemia and hyperlipidemia. VOphpada treatment significantly increased expression of PPARa and activated Akt, and inactivated JNK in muscle and adipose tissues. The insulin enhancement effects of VOphpada were observed more potent than BMOV. Moreover, VOphpada decreased the level of kidney injury molecule-1 marker (KIM-1), suggesting a potentially lower renal toxicity. In overall, the present results suggest VOphpada as a novel hypoglycemic agent with improved efficacy-over-toxicity index. (C) 2015 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000367127800010
项目编号21271012
资助机构NNSFC
引用统计
被引频次:8[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51860
专题北京大学第三临床医学院_儿科
北京大学药学院_化学生物学系
作者单位Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Hlth Sci Ctr,State Key Labs Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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Wang, Na,Wang, Ziwei,Niu, Xia,et al. Synthesis, characterization and anti-diabetic therapeutic potential of novel aminophenol-derivatized nitrilotriacetic acid vanadyl complexes[J]. JOURNAL OF INORGANIC BIOCHEMISTRY,2015,152(SI):104-113.
APA Wang, Na,Wang, Ziwei,Niu, Xia,&Yang, Xiaoda.(2015).Synthesis, characterization and anti-diabetic therapeutic potential of novel aminophenol-derivatized nitrilotriacetic acid vanadyl complexes.JOURNAL OF INORGANIC BIOCHEMISTRY,152(SI),104-113.
MLA Wang, Na,et al."Synthesis, characterization and anti-diabetic therapeutic potential of novel aminophenol-derivatized nitrilotriacetic acid vanadyl complexes".JOURNAL OF INORGANIC BIOCHEMISTRY 152.SI(2015):104-113.
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