In vitro cytotoxicity of salvicine, a novel diterpenoid quinone.

C Qing, J S Zhang, J Ding
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引用次数: 0

Abstract

Aim: To study the in vitro cytotoxicity of 4,5-seco-5,10-friedo-abieta-3,4-dihydroxy-5(10),6,8,13-tetraene-11, 12-dione (salvicine), a novel diterpenoid quinone compound on human tumor cell lines and its effect on cell cycle progression.

Methods: Growth inhibition of human tumor cells was measured by microculture tetrazolium assay (MTT). Cell cycle was analyzed by flow cytometry.

Results: Exposing tumor cell lines tested to salvicine for 72 h, in comparison with reference drugs vincristine (VCR) and etoposide (VP-16), salvicine was as cytotoxic as VP-16 and weaker than VCR in 3 leukemia cell lines. For 12 solid tumor cell lines, salvicine exhibited cytotoxic activities and was over 5.41- and 4.15-fold stronger than VCR and VP-16, respectively. Salvicine presented better activities especially against gastric and lung carcinoma cell lines. Exposing K562 leukemia cells to 9 graded concentrations of salvicine (from 0.39 to 100 mumol.L-1) for 24 h and to salvicine 10 mumol.L-1 for 7 different periods (from 1 to 48 h), the growth inhibition of cells was enhanced along with increased concentration or prolonged exposure. Cell cycle analysis demonstrated that salvicine arrested K562 cells in G1 phase and this effect was also heightened with increased concentration or extended exposure.

Conclusion: Salvicine exhibited potent cytotoxic activities against various human tumor cell lines, and blocked K562 leukemia cells in G1 phase of cell cycle.

新型二萜醌丹参的体外细胞毒性研究。
目的:研究新型二萜类醌类化合物4,5-seco-5,10-friedo- abieda -3,4-二羟基-5(10,6,8,13 -tetraene- 11,12 -dione (salvicine))对人肿瘤细胞株的体外细胞毒性及其对细胞周期进程的影响。方法:采用微培养四氮唑法(MTT)检测肿瘤细胞的生长抑制作用。流式细胞术分析细胞周期。结果:salvicine对肿瘤细胞株暴露72h,与对照药物长春新碱(VCR)和依托泊苷(VP-16)相比,salvicine对3株白血病细胞株的细胞毒性与VP-16相当,弱于VCR。对12种实体瘤细胞株,salvicine表现出细胞毒活性,分别比VCR和VP-16强5.41倍和4.15倍。丹参碱对胃癌和肺癌细胞系有较好的抑制作用。将K562白血病细胞暴露于9种不同浓度的萨尔维辛(0.39至100 μ mol. l -1)中24小时,并暴露于萨尔维辛10 μ mol. l -1中。L-1处理7个不同时期(1 ~ 48 h),随着浓度的增加或暴露时间的延长,细胞的生长抑制作用增强。细胞周期分析表明,salvicine在G1期阻滞K562细胞,这种作用随着浓度的增加或暴露时间的延长而增强。结论:丹参素对多种人肿瘤细胞系具有较强的细胞毒活性,对K562白血病细胞处于细胞周期G1期的阻断作用。
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