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  • Title: [Growth inhibition of tanshinones on SPC-A-1 cell line and their structure-activity relationship].
    Author: Shi H, Zhang Q, Li H, Chu T, Jin H, Mao S.
    Journal: Zhongguo Fei Ai Za Zhi; 2011 Jan; 14(1):7-12. PubMed ID: 21219824.
    Abstract:
    BACKGROUND AND OBJECTIVE: Numerous studies have shown that Tanshinones have anti-tumor effects in vitro, but few studies were focusing on the anti-tumor activity of Tanshinones against one special cancer cell line. The aim of this study is to investigate the growth inhibition effect of four Tanshinones on SPC-A-1 cell line and the relationship between their structures and cytotoxicity. METHODS: The modified MTT assay was adopted to measure the inhibition effect of Tanshinones on SPC-A-1 cells at different concentrations at 24 h, 48 h and 72 h, and the changes of cell morphology were observed by inverted phase contrast microscope. RESULTS: Tanshinones could inhibit the proliferation of SPC-A-1 cells effectively, and their cytotoxicities on SPC-A-1 cells are all in concentration-dependent and time-dependent manners. The IC50 of dihydro-Tanshinone I, Tanshinone I, Tanshinone IIA and Cryptotanshinone at 24 h were 2.77 μg/mL, 6.01 μg/mL, over 10 μg/mL and over 10 μg/mL, at 48 h were 1.80 μg/mL, 4.04 μg/mL, 8.12 μg/mL, 8.71 μg/mL, at 72 h were 1.36 μg/mL, 1.69 μg/mL, 3.81 μg/mL, 7.35 μg/mL, respectively. CONCLUSIONS: All of the four Tanshinones have proliferation inhibitory effects on SPC-A-1 cell line, among which the Dihydrotanshinone I is the most active one, followed by Tanshinone I, Tanshinone IIA and Cryptotanshinone subsequently. The results showed that the structure of aromatic ring A could enhance the cytotoxicity and the structure of furan ring C would influence the cytotoxicity, but the mechanism is still remained to be further investigated. 背景与目的: 大量研究表明丹参酮类化合物具有体外抗肿瘤作用，但很少有人综合研究丹参酮类化合物对同一种肿瘤细胞的作用情况。本文旨在比较4种丹参酮类化合物对SPC-A-1细胞的增殖抑制作用，并探讨其结构与细胞毒性之间的关联性。 方法: 采用改良MT法测定不同浓度的丹参酮类化合物与细胞共培养预定时间（24 h、48 h和72 h）后对SPC-A-1细胞的增殖抑制作用；倒置显微镜下观察不同药物处理对于SPC-A-1细胞的形态学影响。 结果: 丹参酮类化合物均能有效抑制SPC-A-1细胞增殖，其抑制作用呈明显的时间和剂量依赖性。二氢丹参酮Ⅰ、丹参酮Ⅰ、丹参酮ⅡA、隐丹参酮作用24 h的IC50值分别为2.77 μg/mL、6.01 μg/mL、 > 10 μg/mL和 > 10 μg/mL；作用48 h的IC50值分别为1.80 μg/mL、4.04 μg/mL、8.12 μg/mL、8.71 μg/mL；作用72 h的IC50值分别为1.36 μg/mL、1.69 μg/mL、3.81 μg/mL、7.35 μg/mL。 结论: 4种丹参酮类化合物均对SPC-A-1细胞具有明显的增殖抑制作用，作用强度大小依次为二氢丹参酮Ⅰ、丹参酮Ⅰ、丹参酮ⅡA、隐丹参酮，提示A环为芳环时可增强细胞毒性，C环的呋喃环结构可能影响其细胞毒性，其具体作用机理尚有待探讨。
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