cis-trismethoxy Resveratrol

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Background

IC50: 4 microM for tubulin polymerization cis-trismethoxy Resveratrol is an anti-mitotic drug. A mitotic inhibitor is a drug inhibiting mitosis or cell division. Mitotic inhibitors are widely used in cancer treatment, because cancer cells can grow and eventually spread through the body via continuous mitotic division.In vitro: cis-trismethoxy Resveratrol at 0.3 microM could exert a 80% growth inhibition of human colon cancer Caco-2 cells and arrest growth completely at 0.4 microM. The cis conformation of cis-trismethoxy Resveratrol was also 100-fold more potent than the trans isomer. cis-trismethoxy Resveratrol was able to cause cell cycle arrest at the G2/M phase transition and inhibit tubulin polymerization dose-dependently, leading to the depletion of the polyamines, putrescine and spermidine. In addition, cis-trismethoxy Resveratrol inhibited partially colchicine binding to its binding site on tubulin [1]. In vivo: Previous study found that from the angle of pharmacokinetics, cis-trismethoxy Resveratrol appeared to be a superior analog of resveratrol since it was orally available and showed greater plasma exposure, longer elimination half-life and lower clearance. Due to the superior pharmacokinetic characteristics of cis-trismethoxy Resveratrol had, its potentials as a preventive or therapeutic agent in resveratrol-effective diseases would be considered [2].Clinical trial: So far, no clinical study has been conducted.

[1] Schneider, Y. ,Chabert, P.,Stutzmann, J., et al. Resveratrol analog (Z)-3,5,4'-trimethoxystilbene is a potent anti-mitotic drug inhibiting tubulin polymerization. International Journal of Cancer 107, 189-196 (2003).
[2] Lin, H. S. and Ho, P.C. A rapid HPLC method for the quantification of 3,5,4'-trimethoxy-trans-stilbene (TMS) in rat plasma and its application in pharmacokinetic study. Journal of Pharmaceutical & Biomedical Analysis 49, 387-392 (2009).