title: A dioxidovanadium (V) complex of NNO-donor Schiff base as a selective inhibitor of protein tyrosine phosphatase 1B: Synthesis, characterization, and biological activities.
abstract: 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 P21/c. It potently inhibited PTP1B with IC50of 0.13 μM, 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.
authors.affiliation: Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, Taiyuan 030006, Shanxi, People's Republic of China.
authors.forename: Yuqi
authors.initials: Y
authors.lastname: Jia
authors.affiliation: Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, Taiyuan 030006, Shanxi, People's Republic of China. Electronic address: luliping@sxu.edu.cn.
authors.forename: Liping
authors.initials: L
authors.lastname: Lu
authors.affiliation: Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, Taiyuan 030006, Shanxi, People's Republic of China. Electronic address: miaoli@sxu.edu.cn.
authors.forename: Miaoli
authors.initials: M
authors.lastname: Zhu
authors.affiliation: Institute of Molecular Science, Key Laboratory of Chemical Biology and Molecular Engineering of the Education Ministry, Shanxi University, Taiyuan 030006, Shanxi, People's Republic of China.
authors.forename: Caixia
authors.initials: C
authors.lastname: Yuan
authors.affiliation: Edmond H. Fischer Signal Transduction Laboratory, School of Life Sciences, Jilin University, Changchun, 130012, People's Republic of China. Electronic address: xingshu@jlu.edu.cn.
authors.forename: Shu
authors.initials: S
authors.lastname: Xing
authors.affiliation: Edmond H. Fischer Signal Transduction Laboratory, School of Life Sciences, Jilin University, Changchun, 130012, People's Republic of China.
authors.forename: Xueqi
authors.initials: X
authors.lastname: Fu
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects*; D018360:Crystallography, X-Ray; D056945:Hep G2 Cells; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D012545:Schiff Bases / Q000737:chemistry*; D014638:Vanadates / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D012545:Schiff Bases; D014638:Vanadates; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: Cytotoxicity; Dioxidovanadium (V) complex; Inhibitor; Protein tyrosine phosphatase 1B; Selectivity