[烯醛胆固醇衍生物对蜕皮激素生物合成的抑制作用]。

J P Roussel, A Burger, C Hetru
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引用次数: 0

摘要

飞蝗胚胎后发育过程中的前胸腺是蜕皮素的生物合成来源。这些腺体在体外产生蜕皮酮的实验已被用来评价四种在C-22侧链上具有异位基因功能的胆固醇衍生物的抑制活性。这些分子被设计为C-22羟基化的潜在抑制剂,这是蜕皮激素生物合成的必要步骤。测试的四种分子中有三种对蜕皮激素的产生有明显的抑制作用。活性较高的化合物具有剂量依赖性和不可逆性。
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[Inhibitory activity of allene cholesteryl derivatives on the biosynthesis of ecdysone].

Prothoracic glands of the migratory locust Locusta migratoria during the postembryonnic development, are the biosynthetic source of ecdysone. The production of ecdysone by these glands in vitro has been used to evaluate the inhibitory activity of four cholesteryl derivatives with an allenic function on the side chain at C-22. These molecules were devised as potential inhibitors of hydroxylation at C-22 which is an obligate step in the biosynthesis of ecdysone. Three of the four molecules tested induce a marked depressory effect of the production of ecdysone. The effect of the compound with the higher activity was dose dependent and irreversible.

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