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含铋类药物的生物化学和药物化学研究进展

Basis of Bismuth Antiulcer Drugs: Biological Chemistry and Pharmacology

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【作者】 孙红哲张丽司徒嘉怡

【Author】 SUN Hong-ZHe ZHANG Li SZETO Ka-Yee(Department of Chemistry, University of Hong Kong, Pokfulam Road, Hong Kong, P. R. China)

【机构】 香港大学化学系香港大学化学系 香港香港香港

【摘要】 铋的化合物在医学中应用已超过二百年,但其生物化学并没有深入系统的研究,直到近年来才逐渐引起重视。枸椽酸铋的结构表明其治疗溃疡有赖于在酸性条件下的超分子结构,枸椽酸铋超分子和溃疡膜表面的相互作用对其生物活性起着重要作用,同样重要的是铋和蛋白质及酶的相互作用。铋可以结合在蛋白中铁和锌的位置,和其传输及抑制细菌生长有关,详细机理仍有待进一步研究。铋在人体中的吸收极低,大部分是由肾脏通过尿液排出。“幽门螺杆菌”(Helicobacter pylori)基因组的测定,将有助于了解铋剂的作用机理,并为设计新型铋剂奠定基础。

【Abstract】 Bismuth compounds have been used in medicine for centuries and there is potential for the design of new bismuth drugs. The biological chemistry of bismuth was not attracted attention until recently. The widely used bismuth citrate antiulcer drugs are polymers, which could be deposited on the ulcer crater forming a protective coating. The major biological target for bismuth appears to be proteins and enzymes. It can bind to both zinc(II) and iron(III) sites in proteins and the mechanism of antimicrobial activity may therefore involve interference with zinc and iron(III) pathways. There have been no documented cases of bismuth toxicity with the recommended acute dosage of either bismuth citrate (CBS or RBC) or bismuth subsalicylate. The complete genome sequence of Helicobacter Pylori will facilitate the understanding of the mechanism of action of bismuth and also provide a basis for the design of new bismuth antiulcer drugs.

【关键词】 幽门螺杆菌
【Key words】 BismuthHelicobacter Pylori
  • 【文献出处】 中国临床药理学杂志 ,The Chinese Journal of Clinical Pharmacology , 编辑部邮箱 ,2002年04期
  • 【分类号】R914
  • 【被引频次】31
  • 【下载频次】474
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