[Growth inhibition of tanshinones on SPC-A-1 cell line and their structure-activity relationship]

Zhongguo Fei Ai Za Zhi. 2011 Jan;14(1):7-12. doi: 10.3779/j.issn.1009-3419.2011.01.02.
[Article in Chinese]

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。

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abietanes / chemistry*
  • Abietanes / pharmacology*
  • Antineoplastic Agents, Phytogenic / chemistry*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Humans
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / physiopathology
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Abietanes
  • Antineoplastic Agents, Phytogenic
  • tanshinone

Grants and funding

本研究受教育部博士点基金新教师项目(No.20070610050)资助