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从花芽中分离得到的六种新达玛烷型三萜皂苷及其细胞毒性

Six new dammarane-type triterpene saponins from flower buds and their cytotoxicity.

作者信息

Li Ke-Ke, Li Sha-Sha, Xu Fei, Gong Xiao-Jie

机构信息

Department of Biological Engineering, College of Life Science, Dalian Minzu University, Dalian, China.

Department of Traditional Chinese Medicine, College of Medical, Dalian University, Dalian, China.

出版信息

J Ginseng Res. 2020 Mar;44(2):215-221. doi: 10.1016/j.jgr.2018.12.008. Epub 2018 Dec 30.

Abstract

BACKGROUND

has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities.

METHODS

Ginsenoside constituents from flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines.

RESULTS

Six ginsenosides, namely 6'-malonyl formyl ginsenoside F (), 3-acetoxyl ginsenoside F (), ginsenoside Rh (), ginsenoside Rh (), 7-hydroxyl ginsenoside Rd () and ginsenoside Rh () were isolated and elucidated as new compounds, together with four known compounds (- and ). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay.

CONCLUSION

The study of chemical constituents was useful for the quality control of flower buds. The study on antitumor activities showed that new Compound exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

摘要

背景

在东方国家,它已被用于多种医疗目的两千多年。从其漫长用药历史中积累的丰富经验以及现代研究中的大量有力证据可知,人参具有多种药理活性,如抗肿瘤、抗糖尿病、抗氧化以及保护心血管系统的作用。人参的活性化学成分人参皂苷,结构多样,展现出广泛的生物活性。

方法

采用多种色谱方法从人参花蕾中分离纯化人参皂苷成分,并通过光谱分析及与报道数据对比鉴定其结构。采用3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2H-溴化四氮唑法检测它们对三种人类癌细胞系的细胞毒性作用。

结果

分离并鉴定出六种人参皂苷,即6'-丙二酰基甲酰人参皂苷F()、3-乙酰氧基人参皂苷F()、人参皂苷Rh()、人参皂苷Rh()、7-羟基人参皂苷Rd()和人参皂苷Rh()为新化合物,同时还有四种已知化合物(-和)。此外,这些分离化合物的细胞毒性以半数抑制浓度值表示,还根据生物测定结果讨论了初步的构效关系。

结论

人参花蕾化学成分的研究有助于其质量控制。抗肿瘤活性研究表明,新化合物对HL-60、MGC80-3和Hep-G2表现出中等细胞毒性活性,半数抑制浓度值分别为16.74、29.51和20.48μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/767a/7031747/33c80cb5fed9/gr1.jpg

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