Interaction of some estrogenic drugs with tubulin. Formation of twisted ribbon structures.
We studied the action of E-diethylstilbestrol (E-DES), erythro-hexestrol (erythro-HES), and E,E-dienestrol (E,E-DIES) on microtubule formation. The three drugs inhibit this formation from microtubular protein; the percentages of inhibition were, respectively, 15% and 45% for 1.25 X 10-s M E-DES and E,E-DIES. With purified tubulin 6S, 7.5 X 10(-6) M E,E-DIES and erythro-HES induced a 20% inhibition. In the case of E-DES, our results are in good agreement with previous ones. These drugs partially disrupt preformed microtubules. Moreover, when E,E-DIES (5 X 10(-5) M) is added to tubulin, loosely organized aggregates composed of twisted ribbon structure are formed. In the case of erythro-HES, similar structures were observed but at higher concentrations. With E-DES, no organized structures are present.
Chaudoreille
M M
MM
Laboratoires de Biophysique, Faculté de Pharmacie, Marseille, France.
Peyrot
V
V
Braguer
D
D
Crevat
A
A
D000818:Animals; D004028:Dienestrol / Q000494:pharmacology*; D004054:Diethylstilbestrol / Q000494:pharmacology*; D006589:Hexestrol / Q000494:pharmacology*; D008854:Microscopy, Electron; D008870:Microtubules / Q000187:drug effects*; D010636:Phenols / Q000494:pharmacology*; D013552:Swine; D014404:Tubulin / Q000378:metabolism*; D014747:Vinblastine / Q000494:pharmacology
D010636:Phenols; D014404:Tubulin; D006589:Hexestrol; D014747:Vinblastine; D004054:Diethylstilbestrol; D004028:Dienestrol