| 新型丹参素衍生物的合成与初步活性研究 |
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| 引用本文： | 许本洪,崔庆彬,朱华,赵增超,单璐琛. 新型丹参素衍生物的合成与初步活性研究[J]. 中南药学, 2013, 0(5): 338-341 |
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| 作者姓名： | 许本洪 崔庆彬 朱华 赵增超 单璐琛 |
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| 作者单位： | 氍南大学新药研究所,广州510632 |
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| 摘 要： | 目的对丹参素进行结构修饰,改善其理化性质和生物活性。方法以丹参素为母核结构,设计并合成丹参素衍生物。建立叔丁基过氧化氢诱导心肌细胞损伤模型,MTT方法检测丹参素及其衍生物对叔丁基过氧化氢诱导的H9c2细胞损伤的保护作用。结果合成了5个全新丹参素衍生物（2、3、4、7、8）,其化学结构经现代波谱学方法确认。结论丹参素羧基部位进行酯键修饰能明显增加其抗氧化活性,结果优于酰胺键。
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| 关 键 词： | 丹参素 衍生物 生物活性 |
Synthesis and preliminary activity of Danshensu derivates |
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| XU Ben-hong,CUI Qing-bin,ZHU Hua,ZHAO Zeng-chao,SHAN Lu-chen. Synthesis and preliminary activity of Danshensu derivates[J]. Central South Pharmacy, 2013, 0(5): 338-341 |
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| Authors: | XU Ben-hong CUI Qing-bin ZHU Hua ZHAO Zeng-chao SHAN Lu-chen |
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| Affiliation: | ＊(Institute of New Drug Research of Jinan University,Guangzhou 510632) |
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| Abstract: | Objective To improve the physicochemical properties and pharmacological activities of Danshensu by structure modification.Methods We synthethized Danshensu derivates and tested their protective effect against oxidative damage induced by t-BHP with MTT method.Results Five new Danshensu derivatives（2,3,4,7 and 8） were synthesized and confirmed by modern spectroscopy.Compared with activities of Danshensu,the activities of compound 2,7 and 8 were not increased,compound 3 and 4 showed potent antioxidant activities.Conclusion Modification in the carboxyl group through ester bond with propargyl can increase the activity significantly,and is better than amide bond. |
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| Keywords: | Danshensu derivative bioactivity |
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