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Anticancer Activity of Gukulenin A Isolated from the Marine Sponge Phorbas gukhulensis In Vitro and In Vivo

1
College of Pharmacy, Kyung Hee University, Seoul 02447, Korea
2
Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul 02447, Korea
3
Department of Biochemistry and Molecular Genetics, University of Virginia School of Medicine, Pinn Hall 1232, Charlottesville, VA 22908, USA
4
Department of Oceanography, Kunsan National University, Jeonbuk 54150, Korea
*
Author to whom correspondence should be addressed.
Mar. Drugs 2019, 17(2), 126; https://doi.org/10.3390/md17020126
Received: 11 January 2019 / Revised: 16 February 2019 / Accepted: 18 February 2019 / Published: 21 February 2019
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Abstract

Gukulenin A is a bis-tropolone tetraterpenoid isolated from the marine sponge Phorbas gukhulensis. In this study, we examined the anticancer activities of gukulenin A in ovarian cancer cell lines (A2780, SKOV3, OVCAR-3, and TOV-21G) and in an ovarian cancer mouse model generated by injecting A2780 cells. We found that gukulenin A suppressed tumor growth in A2780-bearing mice. Gukulenin A markedly inhibited cell viability in four ovarian cancer cell lines, including the A2780 cell line. Gukulenin A treatment increased the fraction of cells accumulated at the sub G1 phase in a dose-dependent manner and the population of annexin V-positive cells, suggesting that gukulenin A induces apoptotic cell death in ovarian cancer cells. In addition, gukulenin A triggered the activation of caspase-3, -8, and -9, and caspase inhibitors attenuated gukulenin A-induced A2780 cell death. The results suggest that gukulenin A may be a potential therapeutic agent for ovarian cancer. View Full-Text
Keywords: gukulenin A; Phorbas gukhulensis; ovarian cancer; apoptosis; tumor xenograft model gukulenin A; Phorbas gukhulensis; ovarian cancer; apoptosis; tumor xenograft model
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Ahn, J.-H.; Woo, J.-H.; Rho, J.-R.; Choi, J.-H. Anticancer Activity of Gukulenin A Isolated from the Marine Sponge Phorbas gukhulensis In Vitro and In Vivo. Mar. Drugs 2019, 17, 126.

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