College of Pharmacy, Kyung Hee University, Seoul 02447, Korea.
Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul 02447, Korea.
Mar Drugs. 2019 Feb 21;17(2):126. doi: 10.3390/md17020126.
Gukulenin A is a bis-tropolone tetraterpenoid isolated from the marine sponge . 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.
古库林 A 是一种从海洋海绵中分离出来的双 - 三羟酮四萜类化合物。在这项研究中，我们研究了古库林 A 在卵巢癌细胞系（A2780、SKOV3、OVCAR-3 和 TOV-21G）和通过注射 A2780 细胞生成的卵巢癌小鼠模型中的抗癌活性。我们发现古库林 A 抑制了 A2780 荷瘤小鼠的肿瘤生长。古库林 A 显著抑制了包括 A2780 细胞系在内的四种卵巢癌细胞系的细胞活力。古库林 A 处理以剂量依赖性方式增加了亚 G1 期细胞的比例和膜联蛋白 V 阳性细胞的群体，表明古库林 A 诱导了卵巢癌细胞的凋亡性细胞死亡。此外，古库林 A 触发了 caspase-3、-8 和 -9 的激活，并且 caspase 抑制剂减弱了古库林 A 诱导的 A2780 细胞死亡。结果表明，古库林 A 可能是治疗卵巢癌的潜在治疗剂。
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