The synthesis of polyhydroxy sterone 2β,3α,5-trihydroxy-5α-androst-6-one and its neuroprotection

Minyu Xie, Xinhua Li, Li-qiang Yuan, Yiyu Chen, Xiaolei Zhang, Wei Yin, Bing-zheng Lu, Zhu Zhu, Haitao Shi, Jingxia Zhang
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引用次数: 1

Abstract

Neuroactive steroids exhibit better neuroprotective properties in vitro and in vivo, and will be a potential neuroprotective effect. In this study, polyhydroxy sterone 2β,3α,5-trihydroxy-5α- androst-6-one (YC-10) was designed and synthesized from androst-5-en-3-ol by 6 steps reactions. Its absolute structure was characterized by X-SRD and its structure was characterized by NMR, IR, and MS. Its neuroprotective action was determined by MTT assay with two models of neurotoxicity. The maximum protective effect was at a concentration of 40μM for neurotoxicity induced by glutamate, and showing better cell viability in a dose-dependent manner; Moreover it cloud significantly protect the cerebellar granule neurons against neuronal death mediated by low K + , its effective protective concentration was 50μM.
多羟基酮2β,3α,5-三羟基-5α-雄激素-6- 1的合成及其神经保护作用
神经活性类固醇在体内和体外均表现出较好的神经保护作用,具有潜在的神经保护作用。本研究以雄甾-5-烯-3-醇为原料,经6步反应设计合成了多羟基酮2β,3α,5-三羟基-5α-雄甾-6-酮(YC-10)。用X-SRD对其绝对结构进行表征,用NMR、IR、ms对其结构进行表征,用MTT法测定其神经保护作用,采用两种神经毒性模型。在浓度为40μM时,对谷氨酸神经毒性的保护作用最大,且呈剂量依赖性;低K +介导的小脑颗粒神经元死亡具有明显的保护作用,其有效保护浓度为50μM。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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