A dioxidovanadium (V) complex of NNO-donor Schiff base as a selective inhibitor of protein tyrosine phosphatase 1B: Synthesis, characterization, and biological activities

Jia Yuqi; Lu Liping; Zhu Miaoli; Yuan Caixia; Xing Shu; Fu Xueqi

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A dioxidovanadium (V) complex of NNO-donor Schiff base as a selective inhibitor of protein tyrosine phosphatase 1B: Synthesis, characterization, and biological activities

机译：NNO-供体Schiff碱的二氧化维蒽铵（V）复合物作为蛋白酪氨酸磷酸酶1B的选择性抑制剂：合成，表征和生物活性

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A new dioxidovanadium (V) complex, VO2(HPPCH) (1) (H2PPCH = N'-picolinoylpyridin-1-ium-2-carbohydrazonate) has been synthesized and characterized by elemental analysis, IR, X-ray diffraction analysis and electrospray ionization mass spectra. Complex 1 crystallized in the monoclinic system with space group P2(1)/c. It potently inhibited PTP1B with IC50 of 0.13 mu M, about 7, 15 and 125-fold stronger against PTP1B than over TCPTP, SHP-1 and SHP-2, displaying obvious selectivity against PTP1B. Western blotting analysis indicated that complex 1 effectively increased the phosphorylation of PTP1B substrates, especially the phosphorylation of IR/IGF 1R and IRS-1. It exhibited lower cytotoxicity than positive control VOSO4. These results make complex 1 a promising candidate for novel anti-diabetic drug development. (C) 2017 Elsevier Masson SAS. All rights reserved.

机译：已经合成了一种新的二氧化二氧化钒（V）复合物，VO2（HPPCH）（1）（H2PPCH = N'-PICOLINOYLPYRIDIN-1-IUM-2-碳水化合物），其特征在于元素分析，IR，X射线衍射分析和电喷雾电离质谱。复合物1在具有空间组P2（1）/ c的单斜晶体系中结晶。它易于抑制PTP1B，IC50较小，对PTP1B的IC50较强，而不是在TCPTP，SHP-1和SHP-2上，显示对PTP1B的明显选择性。蛋白质印迹分析表明复合物1有效地增加了PTP1B基材的磷酸化，尤其是IR / IGF 1R和IRS-1的磷酸化。它表现出比阳性对照效率低的细胞毒性。这些结果使复合体成为新型抗糖尿病药物发育的有希望的候选者。（c）2017年Elsevier Masson SAS。版权所有。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2017年第2017期|共6页
作者
Jia Yuqi; Lu Liping; Zhu Miaoli; Yuan Caixia; Xing Shu; Fu Xueqi;
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作者单位

Shanxi Univ Inst Mol Sci Key Lab Chem Biol &

Mol Engn Educ Minist Taiyuan 030006 Shanxi;

Shanxi Univ Inst Mol Sci Key Lab Chem Biol &

Mol Engn Educ Minist Taiyuan 030006 Shanxi;

Shanxi Univ Inst Mol Sci Key Lab Chem Biol &

Mol Engn Educ Minist Taiyuan 030006 Shanxi;

Shanxi Univ Inst Mol Sci Key Lab Chem Biol &

Mol Engn Educ Minist Taiyuan 030006 Shanxi;

Jilin Univ Sch Life Sci Edmond H Fischer Signal Transduct Lab Changchun 130012 Peoples R China;

Jilin Univ Sch Life Sci Edmond H Fischer Signal Transduct Lab Changchun 130012 Peoples R China;

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正文语种 eng
中图分类药学;
关键词
Dioxidovanadium (V) complex; Protein tyrosine phosphatase 1B; Inhibitor; Selectivity; Cytotoxicity;

机译：二氧化维蒽铵（V）复合物;蛋白酪氨酸磷酸酶1b;抑制剂;选择性;细胞毒性;

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1. A dioxidovanadium (V) complex of NNO-donor Schiff base as a selective inhibitor of protein tyrosine phosphatase 1B: Synthesis, characterization, and biological activities [J] . Jia Yuqi, Lu Liping, Zhu Miaoli, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2017,第期

机译：NNO-供体Schiff碱的二氧化维蒽铵（V）复合物作为蛋白酪氨酸磷酸酶1B的选择性抑制剂：合成，表征和生物活性
2. Ternary oxovanadium(IV) complexes of ONO-donor Schiff base and polypyridyl derivatives as protein tyrosine phosphatase inhibitors: synthesis, characterization, and biological activities [J] . Yuan CX, Lu LP, Gao XL, Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry . 2009,第6期

机译：作为蛋白质酪氨酸磷酸酶抑制剂的ONO供体Schiff碱和聚吡啶基衍生物的三价氧钒（IV）配合物：合成，表征和生物学活性
3. Ternary oxovanadium(IV) complexes of ONO-donor Schiff base and polypyridyl derivatives as protein tyrosine phosphatase inhibitors: synthesis, characterization, and biological activities [J] . Caixia Yuan, Liping Lu, Xiaoli Gao, JBIC Journal of Biological Inorganic Chemistry . 2009,第6期

机译：作为蛋白质酪氨酸磷酸酶抑制剂的ONO供体Schiff碱和聚吡啶基衍生物的三价氧化钒（IV）配合物：合成，表征和生物学活性
4. Synthesis, Characterization and Biological Activity of Cis-Dioxomolybdenum(VI) Schiff base Complex MoO2(L)2 [C] . Qian Liu, Yisi Yang, Weidong Hao International Conference on Agricultural and Natural Resources Engineering . 2014

机译：CIS-DIOxomolomboldenum（VI）Schiff碱基复合物的合成，表征和生物活性MOO2（L）2
5. Isolation and partial identification of a polysaccharide from Symphytum officinale L. as a potent inhibitor of protein tyrosine phosphatase 1B (PTP1 B). [D] . Chen, I-Ching Sandy. 2016

机译：从Syphytum officinale L.分离并部分鉴定为蛋白质酪氨酸磷酸酶1B（PTP1 B）的有效抑制剂的多糖。
6. Design Synthesis Biological Activity and Molecular Dynamics Studies of Specific Protein Tyrosine Phosphatase 1B Inhibitors over SHP-2 [O] . Su-Xia Sun, Xiao-Bo Li, Wen-Bo Liu, 2013

机译：SHP-2上特定蛋白酪氨酸磷酸酶1B抑制剂的设计合成生物学活性和分子动力学研究
7. Design, Synthesis, Biological Activity and Molecular Dynamics Studies of Specific Protein Tyrosine Phosphatase 1B Inhibitors over SHP-2 [O] . Wei Liu, Xian-Chao Cheng, Shu-Qing Wang, 2013

机译：SHP-2上特定蛋白酪氨酸磷酸酶1B抑制剂的设计，合成，生物学活性和分子动力学研究

A dioxidovanadium (V) complex of NNO-donor Schiff base as a selective inhibitor of protein tyrosine phosphatase 1B: Synthesis, characterization, and biological activities

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