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Journal of Chinese Pharmaceutical Sciences ›› 2016, Vol. 25 ›› Issue (11): 814-820.DOI: 10.5246/jcps.2016.11.090

• Original articles • Previous Articles     Next Articles

Bis(acetylacetonato)-oxidovanadium(IV) inhibits isoproterenol-induced lipolysis in insulin-resistant 3T3-L1 adipocytes by reducing phosphorylation of perilipin and hormone-sensitive lipase

Xia Hu, Jingcheng Liu, You Yu, Weixia Bian, Xiaogai Yang*   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2016-05-13 Revised:2016-07-25 Online:2016-11-26 Published:2016-08-10
  • Contact: Tel.: +86-010-82805956, E-mail: yxg@bjmu.edu.cn
  • Supported by:
    This work was supported by National Natural Science Foundation of China (Grant No. 21171011 and 21671009).

Abstract:

Insulin resistance is characterized as one of crucial pathological changes in type 2 diabetes mellitus (T2DM), and dyslipidaemia is frequently detected in T2DM. A variety of vanadium compounds have been studied as drug candidates for diabetes based on their insulin-like action. However, few studies focus on their antilipolytic effect. In the present study, we established an insulin-resistant model in 3T3-L1 adipocytes to mimic pathological conditions of T2DM according to a well-established method by the treatment of high concentrations of glucose and insulin, which was validated by oil red O staining and the decreased levels of phosphorylated Akt, AS160 and GSK3 after insulin treatment. The results demonstrated that bis(acetylacetonato)-oxidovanadium (IV) (VO(acac)2) could inhibit isoproterenol-stimulated lipolysis through the reduction of the phosphorylated HSL and perilipin levels in both insulin-sensitive and insulin-resistant 3T3-L1 adipocytes. Moreover, although the levels of phosphorylated Akt induced by VO(acac)2 were decreased, the rates of lipolytic inhibition were not significantly altered compared with those under insulin-sensitive condition, indicating that the anti-lipolytic effect of VO(acac)2 might also function in an Akt-independent way in insulin-resistant adipocytes. Our work here help elucidate the anti-diabetic effects of vanadium compounds. It may not only shed light on the utility of vanadium-based compounds as potential anti-diabetic drugs but also serve as a useful screening model for new anti-diabetic drugs.

Key words: Bis(acetylacetonato)-oxidovanadium (IV), Lipolysis, Insulin-resistant 3T3-L1 adipocytes

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