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[丹参酮对K562细胞系增殖的抑制作用及其构效关系]

[Inhibitory effect of tanshinones on proliferation of K562 cell line and its structure-activity relationship].

作者信息

Li Hui, Zhang Qing, Shi Hua-Yue, Chu Ting, Mao Sheng-Jun

机构信息

Department of Hematology, Sichuan Academy of Medical Sciences, Chengdu 610072, Sichuan Province, China.

出版信息

Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2010 Dec;18(6):1469-73.

PMID:21176353
Abstract

The study was purposed to investigate the growth inhibitory effect of tanshinones on K562 cell line and the relationship between their structures and cytotoxicity. The modified MTT assay was adopted to measure the inhibitory effect of tanshinones at different concentrations and chemical structures on K562 cells, and the changes of cell morphology were observed by inverted phase contrast microscopy. The results indicated that the tanshinones could inhibit the proliferation of K562 cells effectively, and their cytotoxicities on K562 cells showed concentration- and time-dependent manners. The IC(50) of dihydrotanshinone I, tanshinone I, tanshinone IIA and cryptotanshinone at 24 hours were 0.91, 4.04, 5.95, 13.85 µg/ml at 48 hours were 0.37, 1.35, 1.71, 6.71 µg/ml; at 72 hours were 0.33, 0.46, 0.82, 6.02 µg/ml, respectively. It is concluded that all of the four tanshinones have proliferation inhibitory effect on K562 cell line, among them the dihydrotanshinone I is the most active one, followed by tanshinone I, tanshinone IIA and cryptotanshinone subsequently, indicating that the chemical structure of aromatic ring A of tanshinones can enhance their cytotoxicity and the structure of furan ring C may influence the cytotoxicity, but their mechanism is still remained to be further investigated.

摘要

本研究旨在探讨丹参酮对K562细胞系的生长抑制作用及其结构与细胞毒性之间的关系。采用改良MTT法测定不同浓度和化学结构的丹参酮对K562细胞的抑制作用,并用倒置相差显微镜观察细胞形态变化。结果表明,丹参酮能有效抑制K562细胞的增殖,其对K562细胞的细胞毒性呈浓度和时间依赖性。二氢丹参酮I、丹参酮I、丹参酮IIA和隐丹参酮在24小时的IC50分别为0.91、4.04、5.95、13.85μg/ml;在48小时分别为0.37、1.35、1.71、6.71μg/ml;在72小时分别为0.33、0.46、0.82、6.02μg/ml。结论:四种丹参酮对K562细胞系均有增殖抑制作用,其中二氢丹参酮I活性最强,其次为丹参酮I、丹参酮IIA和隐丹参酮,提示丹参酮A环的化学结构可增强其细胞毒性,C环的结构可能影响细胞毒性,但其作用机制仍有待进一步研究。

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