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Mar. Drugs 2018, 16(5), 168; https://doi.org/10.3390/md16050168

Precursor-Directed Generation of Indolocarbazoles with Topoisomerase IIα Inhibitory Activity

1
Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
2
Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi University for Nationalities, Nanning 530006, China
3
Toxicology Graduate Program, Department of Physiology, Faculty of Science, Mahidol University, Bangkok 10400, Thailand
4
Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, China
5
Toxicology Graduate Program, Excellent Center for Drug Discovery (ECDD), Faculty of Science, Mahidol University, Bangkok 10400, Thailand
6
Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266003, China
These authors contributed equally to this paper.
*
Authors to whom correspondence should be addressed.
Received: 19 April 2018 / Revised: 7 May 2018 / Accepted: 11 May 2018 / Published: 17 May 2018
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Abstract

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. View Full-Text
Keywords: marine-derived Streptomyces; Streptomyces sp. OUCMDZ-3118; indolocarbazole; cytotoxicities; topoisomerase IIα enzyme activity marine-derived Streptomyces; Streptomyces sp. OUCMDZ-3118; indolocarbazole; cytotoxicities; topoisomerase IIα enzyme activity
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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. (CC BY 4.0).

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Wang, C.; Monger, A.; Wang, L.; Fu, P.; Piyachaturawat, P.; Chairoungdua, A.; Zhu, W. Precursor-Directed Generation of Indolocarbazoles with Topoisomerase IIα Inhibitory Activity. Mar. Drugs 2018, 16, 168.

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