两种新硫色满酮衍生物体外抗肿瘤活性研究

Antitumor Activities of Two Novel Thiochromanone Derivatives in Vitro

关键词:  (顺)-3-(氯代亚甲基)-5-氟-硫色满-4-酮  (顺)-3-(氯代亚甲基)-5-甲基-硫色满-4-酮  MTT法  体外抗肿瘤活性

Key words:  (Z)-3-chloromethylene-5-fluoro-thiochroman-4-ketone  (Z)-3-chloromethylene-5- methyl-thiochroman-4-ketone  MTT assay  antitumor effect in vitro

摘要:

目的 研究新合成化合物(顺)-3-(氯代亚甲基)-5-氟-硫色满-4-酮(CFTK)和(顺)-3-(氯代亚甲基)-5-甲基-硫色满-4-酮(CMTK)对人乳腺癌MCF-7细胞、人肝癌HepG-2细胞、人结肠癌LS174T细胞、人肺癌A549细胞、人黑色素瘤A375细胞、人肾癌786-O细胞、人慢性粒细胞白血病K562细胞、人系髓样白血病U937细胞、小鼠肉瘤S180细胞的抗肿瘤活性，为深入研究CFTK和CMTK抗肿瘤作用提供实验依据。方法 以不同浓度的CFTK和CMTK作用于9种癌细胞，应用改良的MTT法检测CFTK和CMTK对9种癌细胞生长的抑制作用。结果 通过检测以上细胞的增殖情况，得出CFTK对9种癌细胞的半数抑制浓度(IC50)在(6.32±1.52)μmol·L^?1~(19.8±4.08)μmol·L^?1之间，CMTK对9种癌细胞的IC50在(7.16±0.76)μmol·L^?1~(18.2±5.28)μmol·L^?1之间；与同浓度的顺铂(CDDP)相比，具有明显的抗肿瘤活性。结论 CFTK和CMTK能够明显抑制肿瘤细胞的生长，具有极高的体外抗肿瘤活性，为进一步研究开发提供依据。

Abstract:

OBJECTIVE To investigate the antitumor effect of (Z)-3-chloromethylene-5-fluoro-thiochroman-4-ketone (CFTK) and (Z)-3-chloromethylene-5-methyl-thiochroman-4-ketone (CMTK) on the growth of human cancer cell lines (MCF-7, HepG-2, LS174T, A549, A375, 786-O, K562, U937) and mouse S180 cell line. METHODS Nine cancer cell lines were subjected to various concentrations of CFTK and CMTK, the inhibitory rates of CFTK and CMTK were measured by MTT assay. RESULTS CFTK and CMTK could dramatically exhibit antitumor activities at a low concentration (IC50 were (6.32±1.52) μmol·L^?1-(19.8±4.08) μmol·L^?1 and (7.16±0.76) μmol·L^?1-(18.2±5.28) μmol·L^?1). Importantly, the inhibition effects of CFTK and CMTK on nine cancer cells were much higher than cisplatin at the same concentration. CONCLUSION The results indicated that CFTK and CMTK can significantly inhibit cell proliferation and show extremely high antitumor activity in vitro, which provides preliminarily valuable data for further drug research and development.