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目的考察咪唑类离子液体[C_(12)mim]Cl、[C_(12)mim]Br、[C_(12)mim]PF_6;[C_(10)mim]Cl、[C_(10)mim]Br、[C_(10)mim]PF_6;[C_8mim]Cl、[C_8mim]Br、[C_8mim]PF_6;[C_6mim]Cl、[C_6mim]Br、[C_6mim]PF_6体外对非小细胞肺癌A549及肝癌HepG2细胞的增殖抑制作用。方法磺酰罗丹明B比色法检测咪唑类离子液体对A549及HepG2细胞的增殖抑制作用,以阳离子烷基链长度及阴离子种类分析构效关系。结果 1.25～40μmol/L离子液体阳离子咪唑环N-3位烷基链为6个碳,阴离子为Cl~-、Br~-和PF_6的咪唑类离子液体对A549细胞的生长均无明显影响,对HepG2细胞的生长有一定抑制作用,但最大浓度为40μmol/L作用72h,抑制作用也未达50%;而N-3位烷基链为8、10、12个碳,阴离子为Cl~-、Br~-和PF_6的咪唑类离子液体,对A549和HepG2细胞的生长均有明显抑制作用(P<0.05),呈明显的时效和量效关系,咪唑类离子液体对HepG2细胞的敏感性高于A549细胞。构效关系表明,N-3位烷基链的碳原子数是决定咪唑类离子液体抗肿瘤活性的关键,碳原子数越多,抗肿瘤活性越强,而阴离子的类型如Cl~-、Br~-和PF_6~-对咪唑类离子液体的抗肿瘤活性影响不明显。结论咪唑类离子液体阳离子N-3位烷基链长度>6时能明显抑制A549和HepG2细胞生长,而阴离子种类不影响其抗肿瘤活性。
Objective To investigate the effect of imidazole ionic liquid [C_ (12) mim] Cl, [C_ (12) mim] Br, [C_ (12) mim] PF_6, [C_ (10) [C_6mim] Cl, [C_6mim] Cl, [C_6mim] PF_6 in vitro on non-small cell lung cancer A549 and hepatoma HepG2 cells Inhibition of proliferation. Methods The inhibitory effect of imidazole ionic liquids on the proliferation of A549 and HepG2 cells was determined by sulforhodamine B colorimetric assay. The structure-activity relationship was analyzed based on the length of cationic alkyl chains and the anionic species. Results Imidazolium ionic liquids with 1.25 ~ 40μmol / L ionic liquid cationic imidazole ring N-3 alkyl chain of 6 carbons, Cl ~ -, Br ~ - and PF_6 had no significant effect on the growth of A549 cells. HepG2 cells could inhibit the growth of HepG2 cells, but the maximal concentration was 40μmol / L for 72h and the inhibitory effect was less than 50%. The N-3 alkyl chains were 8,10,12 carbons and the anions were Cl ~ -, The imidazole ionic liquids of Br ~ - and PF_6 significantly inhibited the growth of A549 and HepG2 cells (P <0.05), showing a significant effect of aging and dose-response. The sensitivity of imidazole ionic liquid to HepG2 cells was higher than that of A549 cells. The structure-activity relationship shows that the number of carbon atoms in the N-3 alkyl chain is the key factor that determines the antitumor activity of the imidazole ionic liquid. The more the carbon number, the stronger the antitumor activity. The types of the anion such as Cl ~ -, Br ~ - and PF_6 ~ - had no obvious effect on the antitumor activity of imidazole ionic liquids. Conclusions Imidazole ionic liquid cationic N-3 alkyl chain length> 6 can significantly inhibit the growth of A549 and HepG2 cells, while the anionic species does not affect its antitumor activity.