Selective cytostatic and neurotoxic effects of avermectins and activation of the GABAalpha receptors.

Autor: Kokoz YM; Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Moscow Region. kokoz@venus.iteb.serpukhov.su, Tsyganova VG, Korystova AF, Grichenko AS, Zenchenko KI, Drinyaev VA, Mosin VA, Kruglyak EB, Sterlina TS, Victorov AV
Jazyk: angličtina
Zdroj: Bioscience reports [Biosci Rep] 1999 Dec; Vol. 19 (6), pp. 535-46.
DOI: 10.1023/a:1020262811459
Abstrakt: A natural avermectin complex, aversectin C, was shown to be capable of exerting selective cytostatic and neurotoxic effects on mammalian cells. Specifically, it killed proliferating neuroblastoma B103 cells but was non-toxic for differentiated cells of this culture. The antiproliferation action of aversectin C was not inhibited by bicuculline or picrotoxin, antagonists of the GABAalpha receptors, and was partly due to the action of avermectin A1, a component of aversectin C. Aversectin C irreversibly suppressed activity of 60% neurons in medial septal slices of the rat brain. More than 55% of them were the GABAalpha- and B1-sensitive neurons whereas the rest, about 45% neurons, were the GABAalpha-insensitive and the neurotoxic effect of aversectin C was caused mainly by the B2 component.
Databáze: MEDLINE