Abstract
With the improvement and advance in cancer diagnosis and treatment, the cancer is still a major cause of morbidity and mortality throughout the world. Obviously, new breakthroughs in therapies remain be urgent needed. In this work, we designed and synthesized the compound 1–4, namely resveratrol analogues with methylation of hydroxy distyrene, to further explore its new anti-cancer potential. Encouragingly, compound 1 ((E)-4,4′-(ethene-1,2-diyl)bis(3,5-dimethylphenol)) exhibited cytotoxicity superior to resveratrol in MCF 7 cells. More importantly, the compound 1 showed greater toxicity to tumor cells than that to normal cells, which proved that it could selectively kill tumor cells. The favorable results encouraged us to explore the inhibitory mechanism of compound 1 on MCF 7 cells. The research finding indicated the compound 1 inhibited tumor cell proliferation by both arresting cell cycle in S phase and apoptosis via a prooxidant manner. In addition, the results further verified compound 1 caused cell cycle arrest in S phase and apoptosis by down-regulation of the cycling A1/cycling A2 expression and the rise of Bax/Bcl-2 ratio in a p21-dependant pathway in MCF 7 cells. Therefore, these results are helpful for the effective design of anticancer reagents and the better understanding of their mechanism of action.
Highlights
Cancer, as a global public health and social problem, is a major cause of morbidity and mortality, affecting all of humankind [1]
A large body of research has shown that carcinogenesis is associated with the cell cycle control, signal transduction or apoptosis leading to abnormal proliferation of cancer cells, which may provide the potential drug targets for cancer therapies [2,3,4,5]
Cytotoxic activities of the resveratrol and compound 1–4 Firstly, we investigated the anti-proliferative activities of resveratrol and compound 1–4 by MTT assay in various cell lines
Summary
As a global public health and social problem, is a major cause of morbidity and mortality, affecting all of humankind [1]. A large body of research has shown that carcinogenesis is associated with the cell cycle control, signal transduction or apoptosis leading to abnormal proliferation of cancer cells, which may provide the potential drug targets for cancer therapies [2,3,4,5]. Molecules with the potential of an anti-proliferation and pro-apoptotic effect on tumor cells, but not on normal cells, may be appropriate anti-cancer agents. Reactive oxygen species (ROS), as the intracellular second messengers, are closely involved in various physiology processes in normal cells. Once the redox homeostasis is disrupted, ROS will present heterogeneous effects depending on the different levels [6]. ROS may display the carcinogenic effect at low levels
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