Selective cytotoxicity of T-OA on human hepatoma cells by inhibiting the expression of NF-κB/p65 and COX-2
A new anticancer ligustrazine derivative,3-hydroxyolea-12-en-28-oicacid-3, 5, 6-trimethylpyrazin-2-methylester (T-OA,C38H58O3N2), was previously reported.It was synthesized via conjugating hepatoprotective and anticancer ingredients of traditional Chinese medicine.We found T-OA exerted its anticancer activity by preventing the expression of nuclear transcription factor NF-κB/p65 and COX-2 in S180 mice.However, the selective cytotoxicity of T-OA on various kinds of cell lines has not been studied sufficiently.In present study, compared with Cisplatin, T-OA was more toxic to human hepatoma cell line Bel-7402 (IC50 =6.36±1.56 μM) than other three cancer cell lines (HeLa,HT-29, BGC-823), and no toxicity was observed toward Madin-Darby canine kidney cell line MDCK (IC50 > 150 μM).The morphological changes of Bel-7402 cells demonstrated that T-OA had an apoptosis-inducing effect which had been substantiated using DAPI staining, AO/EB staining, flow cytometry and mitochondrial membrane potential assay.Combining the immumohistochemical staining, we found T-OA could prevent the expression of NF-κB/p65 and COX-2 in Bel-7402 cells.Both of the proteins have been known to play roles in apoptosis.The result can indicate that T-OA can induce Bel-7402 cells apoptosis by inhibiting the expression of NF-κB/p65 and COX-2.
ligustrazine derivative selective cytotoxicity hepatoma NF-κB/p65 and COX-2
Chenze Zhang Wenqiang Yan Bi Li Bing Xu Yan Gong Fuhao Chu Yuzhong Zhang Penglong Wang Haimin Lei
School of Chinese Pharmacy,Beijing University of Chinese Medicine,Beijing 100102,China Department of Pathology,Beijing University of Chinese Medicine,Beijing 100102,China
国内会议
吉林延吉
英文
317-326
2015-08-01（万方平台首次上网日期，不代表论文的发表时间）