Publication: Precursor-directed generation of indolocarbazoles with topoisomerase IIα inhibitory activity
2
Issued Date
2018-05-01
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ISSN
16603397
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2-s2.0-85047176616
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Mahidol University
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SCOPUS
Bibliographic Citation
Marine Drugs. Vol.16, No.5 (2018)
Suggested Citation
Cong Wang, Adeep Monger, Liping Wang, Peng Fu, Pawinee Piyachaturawat, Arthit Chairoungdua, Weiming Zhu Precursor-directed generation of indolocarbazoles with topoisomerase IIα inhibitory activity. Marine Drugs. Vol.16, No.5 (2018). doi:10.3390/md16050168 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/47312
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Title
Precursor-directed generation of indolocarbazoles with topoisomerase IIα inhibitory activity
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.