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伊拉地平与拉西地平:体内外对克氏锥虫前鞭毛体的作用

Isradipine and lacidipine: effects in vivo and in vitro on Trypanosoma cruzi epimastigotes.

作者信息

Núñez-Vergara L J, Squella J A, Bollo-Dragnic S, Marín-Catalán R, Pino L, Díaz-Araya G, Letelier M E

机构信息

Facultad De Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago, Chile.

出版信息

Gen Pharmacol. 1998 Jan;30(1):85-7. doi: 10.1016/s0306-3623(97)00077-3.

Abstract
  1. Isradipine and lacidipine, two new drugs that are members of the nitro-aryl-1,4-dihydropyridine family, produced inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. 2. Isradipine was found to be the most potent derivative in both, in growth cultures (I50 = 20.8 microM) and in vivo oxygen uptake (I50 = 31.1 microM). 3. Diltiazem and verapamil, two well-known calcium channel antagonists, lacked inhibitory activity, even at a 100 microM concentration. 4. The present findings indicate that the trypanocide effects exerted by isradipine and lacidipine are not related with a disruption of the calcium homeostasis of the parasite.
摘要
  1. 伊拉地平(isradipine)和拉西地平(lacidipine)是硝基芳基-1,4-二氢吡啶家族的两种新药,在微摩尔浓度下对克氏锥虫图拉亨株(Trypanosoma cruzi Tulahuen strain)的前鞭毛体的生长培养和氧气消耗均产生抑制作用。2. 发现在生长培养(半数抑制浓度I50 = 20.8微摩尔)和体内氧气摄取(I50 = 31.1微摩尔)方面,伊拉地平都是最有效的衍生物。3. 两种著名的钙通道拮抗剂地尔硫䓬(diltiazem)和维拉帕米(verapamil)即使在100微摩尔浓度下也缺乏抑制活性。4. 目前的研究结果表明,伊拉地平和拉西地平发挥的杀锥虫作用与寄生虫钙稳态的破坏无关。

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