强效细菌诱变剂3-氯-4-（二氯甲基）-5-羟基-2（5H）-呋喃酮（MX）与牛血清白蛋白的结合
Binding of the strong bacterial mutagen, 3-chloro-4-(dichloromethyl)-5-hydroxy-2(5H)-furanone (MX) to bovine serum albumin.
作者信息
Haataja L, Vartiainen T, Lampelo S, Lötjönen S, Tuomisto J
机构信息
National Public Health Institute, Department of Environmental Hygiene and Toxicology, Kuopio, Finland.
出版信息
Toxicol Lett. 1991 Dec;59(1-3):187-95. doi: 10.1016/0378-4274(91)90071-d.
Binding of 3-chloro-4-(dichloromethyl)-5-hydroxy-2(5H)-furanone (MX) to bovine serum albumin (BSA) was studied. MX bound mainly reversibly to BSA but, for a minor part, also irreversibly. It was possible to extract the main part of the reversibly bound MX with ethyl acetate and the extractable compound was chromatographically identical to MX. The affinity-binding characteristics of the interaction with albumin were K = 1.6 x 10(7) M-1, n = 3.4. Furthermore, mutagenicity studies indicated that reversibly bound MX remained mutagenic but that irreversibly bound MX was no longer mutagenic in the Ames test. These results suggest that the binding of MX to albumin is an important factor for both the toxicological effects and the toxicokinetics of MX.
研究了3-氯-4-（二氯甲基）-5-羟基-2（5H）-呋喃酮（MX）与牛血清白蛋白（BSA）的结合情况。MX主要以可逆方式与BSA结合，但也有一小部分是不可逆结合。用乙酸乙酯可以提取出大部分可逆结合的MX，且提取物经色谱分析与MX相同。与白蛋白相互作用的亲和结合特性为K = 1.6×10⁷ M⁻¹，n = 3.4。此外，致突变性研究表明，在艾姆斯试验中，可逆结合的MX仍具有致突变性，但不可逆结合的MX不再具有致突变性。这些结果表明，MX与白蛋白的结合对于MX的毒理学效应和毒代动力学都是一个重要因素。
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