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Synthesis and structure-activity relationships of bioactive compounds using sterols

机译：生物活性化合物使用甾醇的合成与结构 - 活性关系

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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且大量分布。利用它们方便地用于制备有用的化合物，例如用类固醇和脱硫骨骼制备药物。本文介绍了天然存在的维生素D类似物，甾醇具有神经突生长活性的合成和结构 - 活性关系，以及肝X受体激动剂。活性形式的维生素D（4）显示出类似的生物活性，但与相应的维生素D（2）和D（3）相比，对维生素D末结合蛋白具有更高的亲和力。这表明活性形式的维生素D（4）是药剂的良好候选者，用于替代维生素D（2）和D（3）的活性形式。在筛选培养肉汤中具有神经沸石产物的低分子量化合物的筛选过程中，我们发现天然产物Dictyosterol醇表现出强烈的活性。从筛选类似物中，发现甾醇侧链中C22和C23之间的双键对于其活性至关重要。发现ERGOST-22-ENE-1ALPHA，3beta-DIOL作为较强的肝X受体激动剂，比24（S），25-环氧胆固醇调节脂质代谢的表达。结构 - 函数研究表明，α-羟基，饱和类固醇结构和C22和C23之间的双键是用作肝X受体激动剂的作用。

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