Abstract
Vanadium compounds are promising anti-diabetic agents. Although BEOV was not able to succeed in phase II clinical trial, great progresses have been made in the past three decades on the discovery and development of anti-diabetic vanadium compounds. A vast of knowledge has been obtained on the molecular mechanisms of both the pharmacological and toxicological effects of vanadium complexes. It has been revealed that vanadium compounds exert insulin enhancement effects and cell protection via a multiple mechanism involving inhibition of PTP1B, activation of PPARs- AMPK signaling, regulation of unfolded protein responses (UPRs), and stimulation of antioxidant enzymes, while vanadium-induced oxidative stress and inflammatory response could primarily be attributed to vanadium toxicity. Based on the present results concerning the relationship between structures, biological activities and biochemical properties, the rationale for future design of anti-diabetic vanadium compounds has been discussed.
Keywords: Vanadium, Diabetes, Structure-activity relationship, β-cells, PTP1B, PPAR.
Current Topics in Medicinal Chemistry
Title:The Molecular Mechanisms and Rational Design of Anti-Diabetic Vanadium Compounds
Volume: 16 Issue: 8
Author(s): Xia Niu, Ruyue Xiao, Na Wang, Ziwei Wang, Yue Zhang, Qing Xia and Xiaoda Yang
Affiliation:
Keywords: Vanadium, Diabetes, Structure-activity relationship, β-cells, PTP1B, PPAR.
Abstract: Vanadium compounds are promising anti-diabetic agents. Although BEOV was not able to succeed in phase II clinical trial, great progresses have been made in the past three decades on the discovery and development of anti-diabetic vanadium compounds. A vast of knowledge has been obtained on the molecular mechanisms of both the pharmacological and toxicological effects of vanadium complexes. It has been revealed that vanadium compounds exert insulin enhancement effects and cell protection via a multiple mechanism involving inhibition of PTP1B, activation of PPARs- AMPK signaling, regulation of unfolded protein responses (UPRs), and stimulation of antioxidant enzymes, while vanadium-induced oxidative stress and inflammatory response could primarily be attributed to vanadium toxicity. Based on the present results concerning the relationship between structures, biological activities and biochemical properties, the rationale for future design of anti-diabetic vanadium compounds has been discussed.
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Cite this article as:
Niu Xia, Xiao Ruyue, Wang Na, Wang Ziwei, Zhang Yue, Xia Qing and Yang Xiaoda, The Molecular Mechanisms and Rational Design of Anti-Diabetic Vanadium Compounds, Current Topics in Medicinal Chemistry 2016; 16 (8) . https://dx.doi.org/10.2174/1568026615666150827094652
DOI https://dx.doi.org/10.2174/1568026615666150827094652 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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