Screening of active substance FS11052 as an inhibitor of neurotransmitter release from PC12 cells |
Yun-Sik Lee1, John Hwa Lee2 |
1Department of Infection Biology, College of Medicine, Wonkwang University 2Bio-Safety Research Institute, College of Veterinary Medicine, Chonbuk National University |
PC12 세포에서 신경전달물질 방출을 저해하는 생리활성물질 FS11052의 탐색 |
이윤식1, 이존화2 |
1원광대학교 의과대학 감염생물학교실 2전북대학교 수의과대학 생체안전성연구소 |
|
Abstract |
We established an in vitro experimental system using the following procedure. We first introduced tritium-labeled norepinephrine ([$^3$H]-NE) into PC12 cells, The [$^3$H]-NE incorporated into PC12 cells were then stimulated by a high concentration (60 mM) of $K^+$ buffer during 12 minutes. Then, we collected $100{mu}l$ supernatant and counted the amount of [$^3$H]-NE release from PC12 cells with a scintillation counter. After screening fungal, Streptomyces spp. or bacterial product using this experimental sytem, we obtained FS11052 from Streptomyces spp. which inhibited [$^3$H]-NE release from PC12 cells. FS11052 also inhibits the release of ATP as a neurotransmitter of PC12 cells and rat cortical neurons, The inhibitory effect was seen even when the PC12 cells were treated with low $K^-$ buffer containing ionomycin ($1{mu}M$) as an ionopore. This result suggests that the inhibitory action of FS11052 on neurotransmitter release appeared after the influx of $Ca^{2+}$. |
Key Words:
exocytosis, inhibitor, neurotransmitter release, PC12 cells, Streptomyces spp |
|