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

• Main Authors: Ji-Hye Ahn, Jeong-Hwa Woo, Jung-Rae Rho, Jung-Hye Choi
• Format: Article
• Language: English
• Published: MDPI AG 2019-02-01
• Series: Marine Drugs
• Subjects: gukulenin A; <i>Phorbas gukhulensis</i>; ovarian cancer; apoptosis; tumor xenograft model
• Online Access: https://www.mdpi.com/1660-3397/17/2/126

Gukulenin A is a bis-tropolone tetraterpenoid isolated from the marine sponge <i>Phorbas gukhulensis</i>. 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.