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Title: Precursor-directed generation of indolocarbazoles with topoisomerase IIα inhibitory activity
Authors: Cong Wang
Adeep Monger
Liping Wang
Peng Fu
Pawinee Piyachaturawat
Arthit Chairoungdua
Weiming Zhu
Guangxi University for Nationalities
Ocean University of China
Chinese Academy of Sciences
Mahidol University
Qingdao National Laboratory for Marine Science and Technology
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-May-2018
Citation: Marine Drugs. Vol.16, No.5 (2018)
Abstract: © 2018 by the authors. One new indolocarbazole, 3-hydroxy-K252d (3), together with the recently reported 3-hydroxyholyrine A (1) and 3-N-acetyl-3-hydroxyholyrine A (2), were obtained by feeding a culture of the marine-derived Streptomyces strain OUCMDZ-3118 with 5-hydroxy-L-tryptophan. Their structures were elucidated on the basis of spectroscopic analysis. Compound 1 potently induced apoptosis of gastric cancer cells by inhibiting topoisomerase IIα enzyme activity and reducing the expression of antiapoptosis protein level. Compound 3 displayed moderate cytotoxicity against the A549 and MCF-7 cell lines with IC50 values of 1.2 ± 0.05 µM, 1.6 ± 0.09 µM, respectively.
ISSN: 16603397
Appears in Collections:Scopus 2018

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