Antiproliferative and apoptotic activity of gemcitabine-lauric acid conjugate on human bladder cancer cells

吉西他滨-月桂酸结合物对人膀胱癌细胞的抗增殖和凋亡活性

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作者:Hongxia Wang, Zhiyu Shao, Zhiwen Xu, Binghao Ye, Ming Li, Qiaoqiao Zheng, Xingyuan Ma, Ping Shi

Conclusion

SZY-200 has the same or more advantages as CP-4126 and could be an ideal candidate drug for further in vivo investigation.

Methods

Antiproliferative activities of SZY-200 and lauric acid were evaluated using CCK-8 assay and clonogenic survival assay. The hENT1 inhibitor NBMPR was employed to determine the role of hENT1 in the apoptotic activity of GEM, CP-4126, and SZY-200. RT-qPCR, flow cytometry, fluorescence microscope, western blotting, and wound healing assay were used to study the mechanisms of SZY-200. The target genes were predicted using the BATMAN-TCM database.

Results

Our data showed that SZY-200 could inhibit the proliferation of bladder cancer cells by inducing cell cycle arrest and apoptosis. The inhibitory effects were comparable to gemcitabine and CP-4126. SZY-200 does not rely on hENT1 to help it enter bladder cancer cells. Also, we found that lauric acid could inhibit the proliferation of bladder cancer cells. SZY-200 could down-regulate the expressions of PPARG and PTGS2 which were related to the occurrence and development of bladder cancer.

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