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.
References:
[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).