膜融合测定法在快速药物筛选中的应用。
Application of a membrane fusion assay for rapid drug screening.
作者信息
Vogel S S, Beushausen S, Lester D S
机构信息
Laboratory of Theoretical and Physical Biology, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland 20892, USA.
出版信息
Pharm Res. 1995 Oct;12(10):1417-22. doi: 10.1023/a:1016258615076.
PURPOSE
The purpose of this study is to develop an in vitro assay for screening drug and their effects on membrane fusion and lysis of intracellular organelles.
METHODS
A 96-well microtiter-dish turbidimetric assay using membrane components of the eggs of sea urchins, a marine invertebrate, was applied to monitor granule fusion and/or lysis.
RESULTS
Of 18 drugs screened, 16 had no effect. One antineoplastic drug, tamoxifen, disrupted intracellular membranes in a calcium independent manner. Taxol, another antineoplastic drug, specifically inhibited calcium triggered exocytosis.
CONCLUSIONS
This assay is inexpensive, simple, rapid, and does not require the sacrifice of animal life. It has the potential to identify drugs that are membrane active, as well as those which specifically perturb events involved in the secretion process.
目的
本研究的目的是开发一种体外检测方法，用于筛选药物及其对细胞内膜融合和细胞器裂解的影响。
方法
采用一种96孔微量滴定板比浊法，利用海洋无脊椎动物海胆卵的膜成分来监测颗粒融合和/或裂解。
结果
在筛选的18种药物中，16种没有效果。一种抗肿瘤药物他莫昔芬以不依赖钙的方式破坏细胞内膜。另一种抗肿瘤药物紫杉醇特异性抑制钙触发的胞吐作用。
结论
该检测方法成本低、操作简单、快速，且无需牺牲动物生命。它有潜力识别具有膜活性的药物，以及那些特异性干扰分泌过程中相关事件的药物。
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