Ye Chun-Lin, Liu Jian-Wen, Wei Dong-Zhi, Lu Yan-Hua, Qian Feng
State Key Laboratory of Bioreactor Engineering, Institute of Biochemistry, East China University of Science and Technology, Shanghai 200237, PR China.
Pharmacol Res. 2004 Nov;50(5):505-10. doi: 10.1016/j.phrs.2004.05.004.
2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), isolated from the buds of Cleistocalyx operculatus, was investigated in its cytotoxicity and its influence on six human cancer cell lines. Among SMMC-7721, 8898, HeLa, SPC-A-1, 95-D and GBC-SD cell lines, SMMC-7721 cells was the most sensitive one in these tested cell lines, with IC50 equal to 32.3 +/- 1.13 microM, EC50 equal to 9.00 +/- 0.36 microM and the therapeutic index equal to 3.59. Staining with Hoechst 33258 showed fragmentation and condensation of chromatin in the cells treated with 9 microM DMC for 48 h. Flow cytometric analysis was performed to determine hypodiploid cells. The results of flow cytometry assay indicated that the percentage of hypodiploid SMMC-7721 cells were 49.44 +/- 1.06% after 48 h treatment with 18.0 microM DMC. The treatment resulted in the appearance of a hypodiploid peak (A0 region), probably due to the presence of apoptosing cells and/or apoptotic bodies with DNA content less than 2n. To our knowledge, this is the first report on anti-tumor activity by DMC.
从水翁花的芽中分离出的2',4'-二羟基-6'-甲氧基-3',5'-二甲基查耳酮（DMC），对其细胞毒性及其对六种人类癌细胞系的影响进行了研究。在SMMC-7721、8898、HeLa、SPC-A-1、95-D和GBC-SD细胞系中，SMMC-7721细胞是这些测试细胞系中最敏感的，其半数抑制浓度（IC50）等于32.3±1.13微摩尔，半数有效浓度（EC50）等于9.00±0.36微摩尔，治疗指数等于3.59。用Hoechst 33258染色显示，用9微摩尔DMC处理48小时的细胞中染色质出现碎片化和凝聚。进行流式细胞术分析以确定亚二倍体细胞。流式细胞术检测结果表明，用18.0微摩尔DMC处理48小时后，SMMC-7721亚二倍体细胞的百分比为49.44±1.06%。该处理导致出现一个亚二倍体峰（A0区域），这可能是由于存在凋亡细胞和/或DNA含量小于2n的凋亡小体。据我们所知，这是关于DMC抗肿瘤活性的首次报道。
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