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产气荚膜梭菌外毒素。IV. 类固醇及相关化合物对θ毒素诱导的溶血作用的抑制

Clostridium perfringens exotoxins. IV. Inhibition of the theta-toxin induced hemolysis by steroids and related compounds.

作者信息

Hase J, Mitsui K, Shonaka E

出版信息

Jpn J Exp Med. 1976 Feb;46(1):45-50.

PMID:180313
Abstract
  1. The inhibitory powers of thirty two samples of steroids and their related compounds on the theta-toxin induced hemolysis were assayed. Apparent I50 value of cholesterol, the most potent inhibitor amoung them, was 0.022 muM. 2. Inhibitory powers of sterol acetates were not more than one tenth of those of the corresponding sterol, and steroids without 3-hydroxyl group hardly inhibited the hemolysis. These results suggest that 3-hydroxyl group of sterols plays an important role in the inhibition. 3. The inhibitory power of sterols were strongly affected by steric situation of 3-hydroxyl group for the face of their tetracyclic rings. From these results it is suggested that theta-toxin binds to beta-side of the tetracyclic rings but not to alpha-side. 4. A methylsterol and pentacyclic triterpens with 3-hydroxyl group also inhibited the hemolysis, but steroids and their related compounds either with a hydrophylic or without a hydrophobic group at their ring D had little, if any, inhibitory power.
摘要
  1. 测定了32种甾体及其相关化合物对θ毒素诱导的溶血作用的抑制能力。其中最有效的抑制剂胆固醇的表观I50值为0.022μM。2. 甾醇醋酸酯的抑制能力不超过相应甾醇的十分之一,且无3-羟基的甾体几乎不抑制溶血。这些结果表明甾醇的3-羟基在抑制作用中起重要作用。3. 甾醇的抑制能力受其四环环面上3-羟基空间位置的强烈影响。从这些结果推测,θ毒素与四环环的β面结合,而非α面。4. 具有3-羟基的甲基甾醇和五环三萜也抑制溶血,但在其D环带有亲水基团或无疏水基团的甾体及其相关化合物几乎没有抑制能力(若有也极小)。

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