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Resveratrol analog ( Z )‐3,5,4′‐trimethoxystilbene is a potent anti‐mitotic drug inhibiting tubulin polymerization by Yann Schneider; Philippe Chabert; Jeanne Stutzmann; David Coelho; André Fougerousse; Francine Gossé; Jean‐François Launay; Raymond Brouillard; Francis Raul is a Medicine article available to read on EtoBox.

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## Abstract Resveratrol (3,5,4′‐trihydroxystilbene) a natural polyphenol present in medicinal plants, grapes and wines, has potent chemopreventive properties on intestinal carcinogenesis. A methylated derivative (__Z__‐3,5,4′‐trimethoxystilbene: R3) was synthesized. R3 at 0.3 μM exerted a 80% growth inhibition of human colon cancer Caco‐2 cells and arrested growth completely at 0.4 μM (R3 was 100‐fold more active than resveratrol). The __cis__ conformation of R3 was also 100‐fold more potent than the __trans__ isomer. R3 (0.3 μM) caused cell cycle arrest at the G2/M phase transition. The drug inhibited tubulin polymerization in a dose‐dependent manner (IC~50~= 4 μM), and it reduced also by 2‐fold ornithine decarboxylase and s‐adenosylmethionine decarboxylase activities. This caused the depletion of the polyamines, putrescine and spermidine, which are growth factors for cancer cells. R3 inhibited partially colchicine binding to its binding site on tubulin, indicating that R3 either partially overlaps with colchicine binding or that R3 binds to a specific site of tubulin that is not identical with the colchicine binding site modifying colchicine binding by allosteric influences. The

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Author

Yann Schneider; Philippe Chabert; Jeanne Stutzmann; David Coelho; André Fougerousse; Francine Gossé; Jean‐François Launay; Raymond Brouillard; Francis Raul

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley; Research Square; Test accounts (ISSN 0020-7136)

Published

2003

Language

EN

Field

Medicine (Health Sciences)