Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent

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.

Cytotoxicity and radiosensitizing potency of Moscatilin in cancer cells at low radiation doses of X-ray and UV-C

“…To improve the cytotoxic activity and antiproliferative efficacy of Resveratrol, scientists have attempted to create structural analogs of the compound by adding methyl groups, modifying either the olefinic bridge or aromatic ring structure, which has improved the activity of the compound (Xin et al 2020 ). The improved cytotoxicity of Moscatilin over Resveratrol as observed in the present study is due to the inherent nature of rotatory bridge connecting the benzyl rings and the presence of methyl groups.…”

Multiple Effects of Resveratrol on Osteosarcoma Cell Lines

“…In pathological conditions, RSV exerts the anti-inflammatory, antioxidant effects [ 14 ] and anticancer activities via targeting oxidative systems, inducing cell-cycle arrest, apoptosis, or autophagy [ 15 ]. Indeed, many articles have reported the effects of RSV on various cancer models, highlighting its role in the suppression of the development and progression of cancer cells by the modulation of several cellular mechanisms, including apoptosis, cell cycle arrest, and the activation of transcription factors.…”

Co-delivery of chemotherapeutic drugs and cell cycle regulatory agents using nanocarriers for cancer therapy

“…Thus, the division and proliferation of tumor cells would be prevented [16]. Tetramethylated hydroxydiethylene 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 [17].…”