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- Title
Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei.
- Authors
Zhang, Yongli; Chen, Guilin; Ma, Hong; Guo, Mingquan
- Abstract
Engleromyces goetzei P. Henn. (E. goetzei) has been widely used as a traditional herb for many years in Kenya due to its diverse biological effects. Although engleromycin was first isolated from E. goetzei in 1980, its pharmacological activity is still unknown. In this study, engleromycin from E. goetzei was identified by spectroscopic analyses, and subsequently examined for its antiproliferative activity using human cancer cell lines of SGC-7901, HT-29, HeLa and A549. As a result, it was revealed that engleromycin strongly inhibited the growth of SGC-7901, HT-29, HeLa and A549 cells with IC50 values at 26.77 ± 1.69 µM, 7.73 ± 0.18 µM, 7.00 ± 0.12 µM and 3.14 ± 0.03 µM, respectively. The results of topoisomerase II (Top II) inhibition assay in vitro implied that engleromycin might be a Top II inhibitor. Further insights into the potential mechanism of antiproliferative activity displayed that engleromycin could dock into the binding pockets of Top II, like the clinical inhibitor doxorubicin, and then inhibit the biological activity of Top II. Taken together, our findings suggest that engleromycin has an anticancer potential, and may serve as a leading compound for the development of antitumor agents.
- Subjects
KENYA; HERBAL medicine; CANCER cells; DNA topoisomerase II; DOXORUBICIN; ANTINEOPLASTIC agents; TRADITIONAL medicine
- Publication
Molecules, 2019, Vol 24, Issue 1, p166
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules24010166