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Int. J. Mol. Sci. 2017, 18(3), 544; doi:10.3390/ijms18030544

d-Amino Acid Position Influences the Anticancer Activity of Galaxamide Analogs: An Apoptotic Mechanism Study

College of Pharmacy, Jinan University, Guangzhou 510632, China
Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Department of Biomedical Engineering, Jinan University, Guangzhou 510632, China
Department of Chemistry, College of Chemistry and Materials Science, Jinan University, Guangzhou 510632, China
Authors to whom correspondence should be addressed.
Academic Editor: Anthony Lemarié
Received: 5 December 2016 / Revised: 10 February 2017 / Accepted: 27 February 2017 / Published: 10 March 2017
(This article belongs to the Section Bioactives and Nutraceuticals)
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Galaxamide, an extract from Galaxaura filamentosa, is a cyclic pentapeptide containing five l-leucines. Due to the particular cyclic structure and the excellent anticancer activity, synthesis of Galaxamide and its analogs and their subsequent bio-applications have attracted great attention. In the present work, we synthesized six Galaxamide analogs by replacing one of the l-leucines with phenylalanine and varying the d-amino acid position. The anticancer effect of the synthesized Galaxamide analogs was tested against four in vitro human cancer cell lines, human hepatocellular cells (HepG2), human breast cancer cell (MCF-7), human breast adenocarcinoma cells (MDA-MB-435) and a human cervical carcinoma cell line (Hela). Results showed that Galaxamide analogs with different d-amino acid positions displayed distinct anticancer potential. The Galaxamide analog containing d-amino acid at position 5 (Analog-6) presented the strongest anticancer activity. The mechanism study revealed that Analog-6 could cause the early apoptosis of HepG2 cells by inhibiting their growth in the sub-G1 stage of the cell cycle and induce the chromatin condensation and fragmentation, which can be seen as 68% of HepG2 cells inhibited in the sub-G1 stage. Moreover, a mitochondria-mediated pathway was found to be involved in the apoptotic process of Analog-6 on HepG2 cells. View Full-Text
Keywords: Galaxamide analogs; cyclopeptide; d-amino acid; anticancer; mechanism Galaxamide analogs; cyclopeptide; d-amino acid; anticancer; mechanism

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Bai, D.; Yu, S.; Zhong, S.; Zhao, B.; Qiu, S.; Chen, J.; Lunagariya, J.; Liao, X.; Xu, S. d-Amino Acid Position Influences the Anticancer Activity of Galaxamide Analogs: An Apoptotic Mechanism Study. Int. J. Mol. Sci. 2017, 18, 544.

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