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Article

A New Ligustrazine Derivative-Selective Cytotoxicity by Suppression of NF-κB/p65 and COX-2 Expression on Human Hepatoma Cells. Part 3

by
Chenze Zhang
1,†,
Wenqiang Yan
1,†,
Bi Li
1,
Bing Xu
1,
Yan Gong
1,
Fuhao Chu
1,
Yuzhong Zhang
2,
Qiuli Yao
3,
Penglong Wang
1,* and
Haimin Lei
1,*
1
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
2
Department of Pathology, Beijing University of Chinese Medicine, Beijing 100102, China
3
School of Nursing, Beijing University of Chinese Medicine, Beijing 100102, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Int. J. Mol. Sci. 2015, 16(7), 16401-16413; https://doi.org/10.3390/ijms160716401
Submission received: 14 May 2015 / Revised: 3 July 2015 / Accepted: 13 July 2015 / Published: 17 July 2015
(This article belongs to the Section Biochemistry)
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Abstract

A new anticancer ligustrazine derivative, 3β-hydroxyolea-12-en-28-oic acid- 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 that 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 the 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 4ʹ,6-diamidino-2-phenylindole (DAPI) staining, acridine orange (AO)/ethidium bromide (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 and are mainly located in the nuclei. Moreover subcellular localization was performed to reveal that T-OA exerts in nuclei of Bel-7402 cells. The result was in accordance with the effects of down-regulating the expression of NF-κB/p65 and COX-2.
Keywords: ligustrazine derivative; selective cytotoxicity; hepatoma; NF-κB/p65 and COX-2 ligustrazine derivative; selective cytotoxicity; hepatoma; NF-κB/p65 and COX-2
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MDPI and ACS Style

Zhang, C.; Yan, W.; Li, B.; Xu, B.; Gong, Y.; Chu, F.; Zhang, Y.; Yao, Q.; Wang, P.; Lei, H. A New Ligustrazine Derivative-Selective Cytotoxicity by Suppression of NF-κB/p65 and COX-2 Expression on Human Hepatoma Cells. Part 3. Int. J. Mol. Sci. 2015, 16, 16401-16413. https://doi.org/10.3390/ijms160716401

AMA Style

Zhang C, Yan W, Li B, Xu B, Gong Y, Chu F, Zhang Y, Yao Q, Wang P, Lei H. A New Ligustrazine Derivative-Selective Cytotoxicity by Suppression of NF-κB/p65 and COX-2 Expression on Human Hepatoma Cells. Part 3. International Journal of Molecular Sciences. 2015; 16(7):16401-16413. https://doi.org/10.3390/ijms160716401

Chicago/Turabian Style

Zhang, Chenze, Wenqiang Yan, Bi Li, Bing Xu, Yan Gong, Fuhao Chu, Yuzhong Zhang, Qiuli Yao, Penglong Wang, and Haimin Lei. 2015. "A New Ligustrazine Derivative-Selective Cytotoxicity by Suppression of NF-κB/p65 and COX-2 Expression on Human Hepatoma Cells. Part 3" International Journal of Molecular Sciences 16, no. 7: 16401-16413. https://doi.org/10.3390/ijms160716401

APA Style

Zhang, C., Yan, W., Li, B., Xu, B., Gong, Y., Chu, F., Zhang, Y., Yao, Q., Wang, P., & Lei, H. (2015). A New Ligustrazine Derivative-Selective Cytotoxicity by Suppression of NF-κB/p65 and COX-2 Expression on Human Hepatoma Cells. Part 3. International Journal of Molecular Sciences, 16(7), 16401-16413. https://doi.org/10.3390/ijms160716401

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