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Title: Synthesis and Biological Evaluation of the 12,12-Dimethyl Derivative of Aplog-1, an Anti-Proliferative Analog of Tumor-Promoting Aplysiatoxin
Authors: NAKAGAWA, Yu
KIKUMORI, Masayuki
TOKUDA, Harukuni
NAGAI, Hiroshi
IRIE, Kazuhiro  kyouindb  KAKEN_id  orcid (unconfirmed)
Author's alias: 入江, 一浩
Keywords: Aplog-1
protein kinase C
tumor promoter
Issue Date: Jun-2011
Publisher: Japan Society for Bioscience, Biotechnology, and Agrochemistry
Journal title: Bioscience, Biotechnology, and Biochemistry
Volume: 75
Issue: 6
Start page: 1167
End page: 1173
Abstract: Aplog-1 is a unique analog of tumor-promoting aplysiatoxin that inhibits tumor-promotion by phorbol diesters and proliferation of tumor cells. While the structural features relevant to the biological activities of Aplog-1 remain to be identified, recent studies by us have suggested that local hydrophobicity around the spiroketal moiety of Aplog-1 is a crucial determinant of its anti-proliferative activity. This hypothesis led us to design 12, 12-dimethyl-Aplog-1 (3), in which a hydrophobic geminal dimethyl group is installed proximal to the spiroketal moiety to improve biological potency. As expected, 3 was more effective than Aplog-1 in inhibiting cancer cell growth and binding to protein kinase Cδ, a putative receptor responsible for the biological response of Aplog-1. Moreover, an induction test on Epstein-Barr virus early antigen demonstrated 3 to be a better anti-tumor promoter than Aplog-1. These results indicate that 3 is a superior derivative of Aplog-1, and thus a more promising lead for anti-cancer drugs.
Rights: © 2011 by Japan Society for Bioscience, Biotechnology, and Agrochemistry
DOI(Published Version): 10.1271/bbb.110130
PubMed ID: 21670518
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