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

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.

• Authors: Ji-Hye Ahn, Jeong-Hwa Woo, Jung-Rae Rho, Jung-Hye Choi
• Journal: Marine drugs (Mar Drugs) Vol. 17 Issue 2 (Feb 21 2019) ISSN: 1660-3397 [Electronic] Switzerland
• PMID: 30795557 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents, Phytogenic
• Terpenes
• gukulenin A
• Caspase 3
• Caspase 8
• Caspase 9

Topics

• Animals
• Antineoplastic Agents, Phytogenic (isolation & purification, pharmacology)
• Apoptosis (drug effects)
• Caspase 3 (metabolism)
• Caspase 8 (metabolism)
• Caspase 9 (metabolism)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• Female
• Humans
• Mice
• Mice, Inbred BALB C
• Mice, Nude
• Ovarian Neoplasms (drug therapy, metabolism, pathology)
• Porifera (chemistry)
• Random Allocation
• Terpenes (isolation & purification, pharmacology)
• Xenograft Model Antitumor Assays