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Int. J. Mol. Sci. 2015, 16(7), 16401-16413; doi:10.3390/ijms160716401

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

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
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Maurizio Battino
Received: 14 May 2015 / Revised: 3 July 2015 / Accepted: 13 July 2015 / Published: 17 July 2015
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [5165 KB, uploaded 17 July 2015]   |  

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. View Full-Text
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.

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