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Synthesis and structure-activity relationships of bioactive compounds using sterols

机译：使用甾醇的生物活性化合物的合成及其构效关系

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摘要

Sterols are widely and abundantly distributed in nature. It is convenient to utilize them for the preparation of useful compounds such as pharmaceuticals with steroid and secosteroid skeletons. This paper describes the synthesis and structure-activity relationships of naturally occurring active forms of vitamin D analogues, sterols having neurite outgrowth activity, and liver X receptor agonist. The active form of vitamin D(4) showed similar biological activities but had higher affinity to the vitamin D-binding protein compared with the corresponding vitamins D(2) and D(3). This shows that the active form of vitamin D(4) is a good candidate for an agent to replace the active forms of vitamins D(2) and D(3). In the course of screening for low molecular-weight compounds that exhibit neurite outgrowth activity in the culture broth, we found that the natural product dictyosterol showed strong activity. From screening of the analogues, it was found that the double bond between C22 and C23 in the side chain of the sterol is essential for its activity. Ergost-22-ene-1alpha,3beta-diol was found to serve as a stronger liver X receptor agonist than 24(S), 25-epoxycholesterol, which regulates the expression of genes involved in lipid metabolism. Structure-function study showed that the 1alpha-hydroxyl group, the saturated steroid structure, and the double bond between C22 and C23 are needed to function as a liver X receptor agonist.
机译：甾醇在自然界中广泛而丰富地分布。方便地将它们用于制备有用的化合物，例如具有类固醇和类固醇骨架的药物。本文描述了天然存在的维生素D类似物，具有神经突向外生长活性的固醇和肝X受体激动剂的活性形式的合成与构效关系。维生素D（4）的活性形式具有相似的生物活性，但与相应的维生素D（2）和D（3）相比，对维生素D结合蛋白的亲和力更高。这表明维生素D（4）的活性形式是替代维生素D（2）和D（3）的活性形式的良好候选者。在筛选在培养液中表现出神经突生长活性的低分子量化合物的过程中，我们发现天然产物dictyosterol具有很强的活性。通过类似物的筛选，发现固醇侧链中的C22和C23之间的双键对其活性至关重要。与24（S），25-环氧胆固醇相比，Ergost-22-ene-1alpha，3beta-diol被发现是更强的肝X受体激动剂，后者调节参与脂质代谢的基因的表达。结构功能研究表明，1alpha-羟基，饱和类固醇结构以及C22和C23之间的双键需要用作肝X受体激动剂。

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