{"title":"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","authors":"Minyu Xie, Xinhua Li, Li-qiang Yuan, Yiyu Chen, Xiaolei Zhang, Wei Yin, Bing-zheng Lu, Zhu Zhu, Haitao Shi, Jingxia Zhang","doi":"10.14800/TTND.1559","DOIUrl":null,"url":null,"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.","PeriodicalId":90750,"journal":{"name":"Therapeutic targets for neurological diseases","volume":" ","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2017-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"The synthesis of polyhydroxy sterone 2β,3α,5-trihydroxy-5α-androst-6-one and its neuroprotection\",\"authors\":\"Minyu Xie, Xinhua Li, Li-qiang Yuan, Yiyu Chen, Xiaolei Zhang, Wei Yin, Bing-zheng Lu, Zhu Zhu, Haitao Shi, Jingxia Zhang\",\"doi\":\"10.14800/TTND.1559\",\"DOIUrl\":null,\"url\":null,\"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.\",\"PeriodicalId\":90750,\"journal\":{\"name\":\"Therapeutic targets for neurological diseases\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2017-06-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Therapeutic targets for neurological diseases\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.14800/TTND.1559\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Therapeutic targets for neurological diseases","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.14800/TTND.1559","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
The synthesis of polyhydroxy sterone 2β,3α,5-trihydroxy-5α-androst-6-one and its neuroprotection
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.
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