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Local anesthetics affect pore-forming activity of cyclic lipopeptide syringomycin E. Abstracts of 42th FEBS Congressтезисы доклада Тезисы
Информация о цитировании статьи получена из
Web of Science
Дата последнего поиска статьи во внешних источниках: 29 марта 2018 г.
- Авторы: Zakharova A.A., Efimova S.S., Ostroumova O.S.
- Сборник: FEBS J
- Серия: Suppl. 1
- Том: 284
- Тезисы
- Год издания: 2017
- Место издания: Jerusalem, Israel
- Первая страница: 108
- Аннотация: Syringomycin E is a well-studied CLP which forms anion-selective voltage-dependent ion channels in model lipid membranes. Here the effects of local anesthetics (LAs) on the conductance and dwell time of SRE-channels have been studied. Planar lipid bilayers composed of DOPC and bathed in 0.1 M or 2 M KCl have been formed by the Montall and Müller technique. It has been shown that at 0.1 M KCl aminoamides, lidocaine (LDC), mepivacaine (MPV), and prilocaine (PLC), have increased the conductance of the SRE-channels (g) on 15% via alteration in the membrane surface potential. The effects of aminoesters, tetracaine (TTC), procaine (PC), and benzocaine (BZC), have been in accordance to their effects on the dipole potential of lipid bilayers. TTC has enhanced g on 30%, PC has not changed it, while BZC has reduced g on 50%. Aminoamides and PC have not affected the dwell time of SRE-channels (τ), while TTC and BZC have significantly reduced it by about 4 times. This effect might be related to uncoupling action of TTC and BZC on the lipid bilayer. Effects of aminoesters were practically independent on the concentration of electrolyte in the bathing solution, while aminoamides have significantly influenced the shape of current-voltage curve of SRE-channels and have drastically reduced τ at 2 M KCl contrary to 0.1 M KCl. We have hypothesized that in the conditions of LA’s and SRE’s charges screening by high concentration of counter ions in bathing solution, aminoamides are able to interact with channel-forming SRE-molecules. Measuring the cooperativity of binding it has been shown that two LA molecules interact with single SRE-channel. The possible structural determinates of the interaction are discussed.
- Добавил в систему: Ефимова Светлана Сергеевна