BLT2拮抗剂的体外抗肿瘤效应

In vitro anti-tumor effect of BLT2 receptor antagonist LY255283

目的:探讨白三烯B4受体BLT2拮抗剂LY255283对培养肿瘤细胞增殖的抑制作用。方法:RT-PCR法检测9种人源肿瘤细胞(SMMC7721、A549、Bel7402、BGC823、Eca109、HeLa、HL60、MCF7和Pc3细胞)中BLT2的表达情况;MTT法分析LY255283对上述体外培养肿瘤细胞的增殖抑制作用;流式细胞术及荧光显微镜分析LY255283对MCF7细胞凋亡的影响。结果:9种肿瘤细胞均检测到BLT2 mRNA的表达;LY255283明显抑制上述不同肿瘤细胞的增殖,其IC_(50)值分别为0.21、11.17、1.28、5.9、7.9、1.59、0.14、1.25和31.28μmol/L;在1.0和10.0μmol/L两个作用浓度,LY255283诱导MCF7细胞凋亡的发生率分别为20.47%和37.47%,均明显高于空白对照组(8.66%)和DMSO溶剂对照组(11.71%)(P均<0.01)。结论:BLT2在9种人源肿瘤细胞均有表达,其特异拮抗剂LY255283具有抑制肿瘤细胞增殖效应,诱导细胞凋亡可能是其抗肿瘤的机制之一。

OBJECTIVE：To study the inhibition effect of LY255283,a BLT2 receptor antagonist,on different human cancer cell lines.METHODS：The expressions of BLT2 receptor in SMMC7721、A549、Bel7402、BGC823、Eca109、HeLa、HL60、MCF7 and Pc3 cell were evaluated by RT-PCR.The inhibition effect of LY255283 on the nine tumor cell lines was analyzed by MTT assay.Apoptotic cells were evaluated by flow cytometry and fluorescence microscopy.RESULTS：All nine tumor cell lines expressed BLT2 receptors.LY255283 inhibited the proliferation of all nine tumor cell lines,the IC_（50） values were 0.21,11.17,1.28,5.9,7.9,1.59,0.14,1.25 and 31.28μmol/L, respectively.The apoptotic rates of MCF-7 cells induced by LY255283 at 1 and 10μmol/L were 20.47%and 31.28%,respectively,which were significantly increased compared with blank control group（8.66%） and DMSO control group（11.71%）（P0.01）.CONCLUSION：BLT2 receptor was expressed in nine human tumor cell lines,and the specific antagonist LY255283 could inhibit the proliferation of tumor cells probably by inducing apoptosis.