目的:研究黄酮类化合物木犀草素(Luteolin)对体外抗肿瘤细胞增殖,以及其与抗肿瘤药联用的增敏作用。方法:选用5μmol/L或10μmol/L木犀草素与不同浓度抗肿瘤药联合作用肿瘤细胞24 h后,用MTS法检测其体外抗增殖作用。结果:5μmol/L木犀草素对人非小细胞肺癌细胞(A549)、人子宫颈癌细胞(Hela)、人乳腺癌细胞(MCF-7)、人胃腺癌细胞(AGS)、人胃癌细胞(MGC-803)的抗增殖作用均〈20%,对人结肠癌细胞(Caco2)和人肝癌细胞(HepG2)的抗增殖作用约20%。Bexarotene单一用药时对Hela细胞抑制率达50%(IC50)的浓度约为2μmol/L,与5μmol/L木犀草素联用后IC50约0.2μmol/L,5μmol/L木犀草素与0.1μmol/L Bexarotene联用对Hela细胞的抗增殖作用达44%,Bexarotene与木犀草素联用在MGC-803、HepG2、A549细胞中增敏较小,在Caco2和MCF-7细胞中无增敏作用;顺铂单一用药时对Hela细胞的IC50〉30μmol/L,与5μmol/L木犀草素联用后IC50约3μmol/L,联用后在MGC-803、HepG2和A549中增敏较小;博来霉素单一用药时对Hela细胞的IC50〉100μmol/L,对A549细胞的IC50约为100μmol/L,与5μmol/L木犀草素联用后Hela细胞的IC50约为1μmol/L,与10μmol/L木犀草素联用后A549细胞的IC50约为10μmol/L。木犀草素与格列卫联用在MGC-803、HepG2、A549和AGS中增敏较小。结论:木犀草素在低于10μmol/L浓度时,对肿瘤细胞体外抗增殖作用较小。低浓度(5μmol/L~10μmol/L)的木犀草素在不同的肿瘤细胞中对抗肿瘤药的增敏作用强度不同,在Hela细胞中增敏作用最显著。
Objective: To investigate the effect of Luteolin alone or combination with chemotherapentic drugs on the cytoxicity of cancer cells.Methods: Cultured A549,Hela,MCF-7,AGS,MGC-803,Caco2 and HepG2 cells were treated with Luteolin or the combination of Luteolin with other chemotherapeutic agents(Bexarotene,Cisplatin and Bleomycin).Cell viability was measured by MTS assay and IC50 was calculated.Results: The IC50 of Bexarotene to Hela cells was 2 μmol/L,but with the combination of 5 μmol/L of Luteolin that reduced to 0.2 μmol/L.However,the combination of Bexarotene and Luteolin did not show significant benefit in MGC-803,HepG2 cells,Caco2 and MCF-7 cells.The IC50 of Cisplatin to Hela cells was over 30 μmol/L,but it decreased to 3 μmol/L in the presence of 5 μmol/L Luteolin;Luteolin also sensitized Cisplatin in MGC-803,HepG2 and A549 cells studied.The IC50 of Bleomycin to Hela cells was over 100 μmol/L,but it was about 1 μmol/L in the presence of 5 μmol/L Luteolin.A549 cells were resistant to Bleomycin with an IC50 of 100 μmol/L,10 μmol/L Luteolin greatly enhanced the cytotoxicity of Bleomycin to the cells with the IC50 of about 10 μmol/L.The inhibitions of MGC-803,HepG2,A549 and AGS cells didn't change by combination of Luteolin.Conclusion: Low concentration of Luteolin has little toxic effect on the cancer cell lines tested in the study,but it can sensitize chemotherapeutic drugs in various cancer cell lines.