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Oxidative Medicine and Cellular Longevity
Volume 2017, Article ID 8392035, 13 pages
Research Article

Cytotoxicity Study of Cyclopentapeptide Analogues of Marine Natural Product Galaxamide towards Human Breast Cancer Cells

1Department of Chemistry, College of Chemistry and Materials Science, Jinan University, 510632 Guangzhou, China
2Institute of Biomineralization and Lithiasis Research, Jinan University, 510632 Guangzhou, China

Correspondence should be addressed to Bingxin Zhao; moc.361@226048xbz and Shihai Xu; nc.ude.unj@hsuxt

Received 3 June 2017; Revised 18 October 2017; Accepted 26 October 2017; Published 19 December 2017

Academic Editor: Felipe Dal Pizzol

Copyright © 2017 Jignesh Lunagariya et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Herein, we report the cytotoxicity of cyclopentapeptide analogues of marine natural product galaxamide towards breast carcinoma cells and the underlying mechanisms. We examined the effect of the novel galaxamide analogues on cancer cell proliferation by MTT assay and also further examined the most active compound for morphological changes using Hoechst33342 staining technique, induction of apoptosis, cell cycle phases, mitochondrial membrane potential (MMP), and reactive oxygen species (ROS) generation using flow cytometry in human breast cancer MCF-7 cells in vitro. Galaxamide and its analogues effectively induced toxicity in human hepatocellular carcinoma HepG2, human breast carcinoma MCF-7, human epitheloid cervix carcinoma HeLa, and human breast carcinoma MB-MDA-231 cell lines. Amongst them, compound 3 exhibited excellent toxicity towards MCF-7 cells. This galaxamide analogue significantly induced apoptosis in a dose-dependent manner in MCF-7 cells involves cell cycle arrest in the G1 phase, a reduction of MMP, and a marked increase in generation of ROS. Particularly, compound 3 of galaxamide analogues might be a potential candidate for the treatment of breast cancer.