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 anti-proliferation action of aversectin C was not inhibited by bicuculline or picrotoxin, antagonists of the GABAα 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 GABAα- and B1-sensitive neurons whereas the rest, about 45% neurons, were the GABAα-insensitive and the neurotoxic effect of aversectin C was caused mainly by the B2 component.
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December 01 1999
Selective Cytostatic and Neurotoxic Effects of Avermectins and Activation of the GABAα Receptors
Yuri M. Kokoz;
Yuri M. Kokoz
1Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Moscow Region, Pushchino 142292, Russia
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Vera G. Tsyganova;
Vera G. Tsyganova
1Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Moscow Region, Pushchino 142292, Russia
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Antonina F. Korystova;
Antonina F. Korystova
1Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Moscow Region, Pushchino 142292, Russia
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Alexey S. Grichenko;
Alexey S. Grichenko
1Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Moscow Region, Pushchino 142292, Russia
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Konstantin I. Zenchenko;
Konstantin I. Zenchenko
1Institute of Theoretical and Experimental Biophysics, Russian Academy of Sciences, Moscow Region, Pushchino 142292, Russia
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Victor A. Drinyaev;
Victor A. Drinyaev
2NBC Pharmbiomed, 12a Selskokhozyaistvennaya Street, Moscow 129226, Russia
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Vladimir A. Mosin;
Vladimir A. Mosin
2NBC Pharmbiomed, 12a Selskokhozyaistvennaya Street, Moscow 129226, Russia
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Elena B. Kruglyak;
Elena B. Kruglyak
2NBC Pharmbiomed, 12a Selskokhozyaistvennaya Street, Moscow 129226, Russia
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Tatyana S. Sterlina;
Tatyana S. Sterlina
2NBC Pharmbiomed, 12a Selskokhozyaistvennaya Street, Moscow 129226, Russia
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Alexander V. Victorov
Alexander V. Victorov
2NBC Pharmbiomed, 12a Selskokhozyaistvennaya Street, Moscow 129226, Russia
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Publisher: Portland Press Ltd
Online ISSN: 1573-4935
Print ISSN: 0144-8463
© 1999 Plenum Publishing Corporation
1999
Biosci Rep (1999) 19 (6): 535–546.
Citation
Yuri M. Kokoz, Vera G. Tsyganova, Antonina F. Korystova, Alexey S. Grichenko, Konstantin I. Zenchenko, Victor A. Drinyaev, Vladimir A. Mosin, Elena B. Kruglyak, Tatyana S. Sterlina, Alexander V. Victorov; Selective Cytostatic and Neurotoxic Effects of Avermectins and Activation of the GABAα Receptors. Biosci Rep 1 December 1999; 19 (6): 535–546. doi: https://doi.org/10.1023/A:1020262811459
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