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目的:探讨并评价羟基氯喹(HCQ)体外抗肿瘤活性。方法:采用CCK-8法测定不同浓度HCQ(4.78,9.55,19.10,38.20,76.40μg·ml~(-1))对A549细胞、HepG2细胞、HT-29细胞、K562细胞、Hela细胞和B16细胞的抑制作用。用酶标仪检测吸光度(A)值并计算肿瘤细胞抑制率和IC_(50)。结果:与阴性对照组相比,不同浓度HCQ对6株肿瘤细胞的增殖抑制率均明显升高,且呈剂量依赖性(P<0.01)。浓度达到38.20μg·ml~(-1)的HCQ对6株肿瘤细胞的抑制率均在60%以上。HCQ对肿瘤细胞的IC_(50)值分别为26.70(A549)、27.47(Hep G2)、5.72(HT-29)、14.03(K562)、20.21(Hela)、13.62(B16)μg·ml~(-1)。结论:HCQ对多种肿瘤细胞具有一定的体外抗肿瘤作用,在治疗肺癌、直肠腺癌、肝癌、宫颈癌、黑色素瘤和红白血病方面可能有良好的应用前景。
Objective: To investigate and evaluate the antitumor activity of hydroxychloroquine (HCQ) in vitro. Methods: The effects of different concentrations of HCQ (4.78,9.55,19.10,38.20,76.40μg · ml -1) on A549 cells, HepG2 cells, HT-29 cells, K562 cells, Hela cells and B16 cells were determined by CCK- Inhibition. The absorbance (A) value was detected by microplate reader and the tumor cell inhibitory rate and IC50 (50) were calculated. Results: Compared with the negative control group, the inhibitory rates of HCQ on the proliferation of 6 tumor cells were significantly increased in a dose-dependent manner (P <0.01). HCQ concentration of 38.20μg · ml ~ (-1) on six tumor cells were more than 60% inhibition rate. The IC 50 values of HCQ against tumor cells were 26.70 (A549), 27.47 (Hep G2), 5.72 (HT-29), 14.03 (K562), 20.21 (Hela), 13.62 (B16) μg · ml ~ (- 1). CONCLUSION: HCQ has a certain anti-tumor activity against various tumor cells in vitro and may have a good application prospect in the treatment of lung cancer, rectal adenocarcinoma, liver cancer, cervical cancer, melanoma and erythroleukemia.