A novel small molecule compound diaporine inhibits breast cancer cell proliferation via promoting ROS generation.

Diaporine is a novel fungal metabolic product and has an unprecedented symmetric polyketide with a novel framework from diaporthe sp. In the current study, we researched the anti-cancer role of this natural compound. Firstly, we evaluate the sensitivities of diaporine in several cancer cells and the results show that diaporine has proliferation-inhibitory effect against cancer cells via MTT assay, especially on breast cancer cells. In addition, we find that diaporine can disrupt the morphology and viability of breast cancer cells and their migration and invasion capacities are also impaired tested by using wound healing method and transwell. Further investigation show that diaporine can efficiently induce an intensive breast cancer cell cycle arrest especially in G2 phase and finally leads to cancer cell apoptosis by flow cytometer analysis. For the mechanism by which mediated the breast cancer cell death, we find that diaporine can induce an increase of ROS level in breast cancer cells. When depressing ROS generation by using anti-oxidant agent N-acetyl-l-cysteine or Vitamin C, the apoptosis effects of breast cancer cells are disrupted. Collectively, our results suggest that diaporine can act as an anti-cancer agent and this function is dependent on promoting high level ROS release of cancer cells.