{"title":"5α-雄激素-3β，5,6β-三醇衍生物的合成及神经保护作用","authors":"Xinhua Li, Xinying Chen, Jiesi Chen, Shujia Zhou, Jin Wen, Yijun Huang, Guangmei Yan, Jingxia Zhang","doi":"10.14800/TTND.831","DOIUrl":null,"url":null,"abstract":"Neurosteroids have siginificant neuroprotection for damaged neurocell and may be developed a kind of potential neuroprotectant for treatment of ischemic stroke. In the study, twelve analogues of 5α-androst-3β,5,6β-triol were synthesized by the multiple steps of reaction from dehydroepiandrosterone (DHEA), and their structures were characterized by IR, NMR, MS. Their neuroprotective activities was tested by evaluating survival cells. The results showed that 3β,5α,6β-trihydroxy sterols (3,4a-4e,5a-5e,11) exhibited certain neuroprotective effect on rat cerebellar granule neurons (CGN) against apoptosis induced by glutamic acid in vitro, and compound 5d and 5e exhibited better neuroprotection with the dose-response relationship.","PeriodicalId":90750,"journal":{"name":"Therapeutic targets for neurological diseases","volume":"2 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2015-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and neuroprotection of 5α-androst-3β,5,6β-triol derivatives\",\"authors\":\"Xinhua Li, Xinying Chen, Jiesi Chen, Shujia Zhou, Jin Wen, Yijun Huang, Guangmei Yan, Jingxia Zhang\",\"doi\":\"10.14800/TTND.831\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Neurosteroids have siginificant neuroprotection for damaged neurocell and may be developed a kind of potential neuroprotectant for treatment of ischemic stroke. In the study, twelve analogues of 5α-androst-3β,5,6β-triol were synthesized by the multiple steps of reaction from dehydroepiandrosterone (DHEA), and their structures were characterized by IR, NMR, MS. Their neuroprotective activities was tested by evaluating survival cells. The results showed that 3β,5α,6β-trihydroxy sterols (3,4a-4e,5a-5e,11) exhibited certain neuroprotective effect on rat cerebellar granule neurons (CGN) against apoptosis induced by glutamic acid in vitro, and compound 5d and 5e exhibited better neuroprotection with the dose-response relationship.\",\"PeriodicalId\":90750,\"journal\":{\"name\":\"Therapeutic targets for neurological diseases\",\"volume\":\"2 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2015-07-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Therapeutic targets for neurological diseases\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.14800/TTND.831\",\"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.831","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and neuroprotection of 5α-androst-3β,5,6β-triol derivatives
Neurosteroids have siginificant neuroprotection for damaged neurocell and may be developed a kind of potential neuroprotectant for treatment of ischemic stroke. In the study, twelve analogues of 5α-androst-3β,5,6β-triol were synthesized by the multiple steps of reaction from dehydroepiandrosterone (DHEA), and their structures were characterized by IR, NMR, MS. Their neuroprotective activities was tested by evaluating survival cells. The results showed that 3β,5α,6β-trihydroxy sterols (3,4a-4e,5a-5e,11) exhibited certain neuroprotective effect on rat cerebellar granule neurons (CGN) against apoptosis induced by glutamic acid in vitro, and compound 5d and 5e exhibited better neuroprotection with the dose-response relationship.
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