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

Abstract:

: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.

journal_name

Biosci Rep

journal_title

Bioscience reports

authors

Kokoz YM,Tsyganova VG,Korystova AF,Grichenko AS,Zenchenko KI,Drinyaev VA,Mosin VA,Kruglyak EB,Sterlina TS,Victorov AV

doi

10.1023/a:1020262811459

keywords:

subject

Has Abstract

pub_date

1999-12-01 00:00:00

pages

535-46

issue

6

eissn

0144-8463

issn

1573-4935

journal_volume

19

pub_type

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