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全新抗心肌损伤活性贝叶烷型二萜衍生物的设计合成
首发时间：2024-05-20
摘要：目的：合成系列异甜菊醇衍生物，研究其抗心肌损伤活性。方法：在异甜菊醇的c-15位引入各种氨基酸片段合成系列衍生物，通过阿霉素诱导斑马鱼心肌损伤模型评价其抗心肌损伤活性。结果：合成了35个全新的异甜菊醇衍生物，利用核磁共振、质谱确定结构；衍生物4d，5g，5h表现出显著的体内抗心肌损伤活性，效果与阳性药左西孟旦相当。结论：合成了全新异甜菊醇系列衍生物，体内活性筛选结果证实它们具备一定的抗心肌损伤活性，衍生物5h可作为苗头分子深入研究。
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design and synthesis isosteviol derivatives as new cardioprotective agents
abstract：a series of novel isosteviol derivatives was synthesized by integrating diverse amino acid fragments at the c-15 position of isosteviol. their structures were elucidated through nmr and ms analyses. subsequently, all 32 new derivatives underwent in vivo evaluation in a zebrafish model of doxorubicin-induced cardiomyopathy. among them, compounds 4d, 5g, and 5h exhibited noteworthy cardioprotective effects, comparable to the positive control drug, levosimendan. notably, compound 5h emerged as the most potent derivative, showcasing promising potential as a lead candidate for further investigation.
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全新抗心肌损伤活性贝叶烷型二萜衍生物的设计合成
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