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钒化合物的生物学作用及作为药理学制剂的潜力。

Vanadium compounds biological actions and potential as pharmacological agents.

机构信息

Department of Medicine, Mount Sinai Hospital,Toronto, Ontario, M5G 1X5,Canada; Department of Physiology and Banting and Best Diabetes Centre, University of Toronto,Toronto, Ontario, M5G 1X5,Canada.

出版信息

Trends Endocrinol Metab. 1997 Mar;8(2):51-8. doi: 10.1016/s1043-2760(96)00262-7.

DOI:10.1016/s1043-2760(96)00262-7
PMID:18406786
Abstract

Vanadium is an element found in low concentrations in mammals, for which a function remains to be discovered. Over the past century, vanadium compounds have been suggested anecdotally as therapeutic agents for a variety of diseases. The discovery that vanadate inhibits various enzymes, in particular protein tyrosine phosphatases, and mimics many of the biological actions of insulin suggested a potential role in the therapy of diabetes mellitus. Successful use and an enhancement of insulin sensitivity in rodents and human diabetic subjects, as well as the finding that these agents are capable of stimulating metabolic effects while bypassing the insulin receptor and the early steps in insulin action, target these agents preferentially toward type II diabetes mellitus. Long-term safety remains a major concern, as tissue accumulation and relative nonspecificity of enzyme inhibition may result in adverse effects. Continued research into mechanism of action, consequences of chronic administration, and improvement of specificity is warranted. Regardless of their ultimate success or failure as therapeutic agents, vanadium compounds continue to be useful probes of enzyme structure and function in various biological processes. (Trends Endocrinol Metab 1997;8:51-58). (c) 1997, Elsevier Science Inc.

摘要

钒是哺乳动物中含量较低的一种元素,其功能尚待发现。在过去的一个世纪中,钒化合物被偶然发现可作为多种疾病的治疗剂。钒酸盐抑制各种酶,特别是蛋白质酪氨酸磷酸酶的发现,以及模仿胰岛素的许多生物学作用,提示其在治疗糖尿病方面具有潜在作用。在啮齿动物和人类糖尿病患者中成功地使用和增强胰岛素敏感性,以及发现这些药物能够在绕过胰岛素受体和胰岛素作用的早期步骤的情况下刺激代谢作用,使这些药物优先针对 2 型糖尿病。长期安全性仍然是一个主要问题,因为组织积累和酶抑制的相对非特异性可能导致不良反应。有必要继续研究作用机制、长期给药的后果以及提高特异性。无论作为治疗剂最终成功与否,钒化合物仍然是研究各种生物过程中酶结构和功能的有用探针。(Trends Endocrinol Metab 1997;8:51-58)。(c)1997,Elsevier Science Inc.

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