Precursor-Directed Generation of Indolocarbazoles with Topoisomerase IIα Inhibitory Activity

Precursor-Directed Generation of Indolocarbazoles with Topoisomerase IIα Inhibitory Activity

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 elu...

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Bibliographic Details
Main Authors: Cong Wang, Adeep Monger, Liping Wang, Peng Fu, Pawinee Piyachaturawat, Arthit Chairoungdua, Weiming Zhu
Format: Article
Language:English
Published: MDPI AG 2018-05-01
Series:Marine Drugs
Subjects:
marine-derived Streptomyces
Streptomyces sp. OUCMDZ-3118
indolocarbazole
cytotoxicities
topoisomerase IIα enzyme activity
Online Access:http://www.mdpi.com/1660-3397/16/5/168
Description
Summary: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:1660-3397

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