Gymnopilins, a product of a hallucinogenic mushroom, inhibit the nicotinic acetylcholine receptor
| Autor: | Izumi Shibuya, Tomohiko Kayano, Shunsuke Miyazaki, Naoki Kitamura, Norihiro Shimomura, Tsuyoshi Ichiyanagi, Tadanori Aimi |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Nicotine
Patch-Clamp Techniques Terpenes Chemistry Voltage clamp Receptors Nicotinic Pharmacology Toxicology PC12 Cells Acetylcholine Rats Atropine Nicotinic acetylcholine receptor Nicotinic agonist Ganglion type nicotinic receptor Hallucinogens medicine Animals Calcium Dimethylphenylpiperazinium Iodide Alpha-4 beta-2 nicotinic receptor Agaricales Acetylcholine receptor medicine.drug |
| Zdroj: | Toxicon. 81:23-31 |
| ISSN: | 0041-0101 |
| Popis: | Gymnopilins are substances produced in fruiting bodies of the hallucinogenic mushroom, Gymnopilus junonius. Although, only a few biological effects of gymnopilins on animal tissues have been reported, it is believed that gymnopilins are a key factor of the G. junonius poisoning. In the present study, we found that gymnopilins inhibited ACh-evoked responses in neuronal cell line, PC12 cell, and determine the underlying mechanism. Gymnopilins were purified from wild fruiting bodies of G. junonius collected in Japan. Ca(2+)-imaging revealed that gymnopilins reduced the amplitude of ACh-evoked [Ca(2+)]i rises by about 50% and abolished the ACh responses remaining in the presence of atropine. Gymnopilins greatly reduced the amplitude of [Ca(2+)]i rises evoked by nicotinic ACh receptor agonists, 1,1-Dimethyl-4-phenylpiperazinium iodide (DMPP) and nicotine. In the whole-cell voltage clamp recording, gymnopilins inhibited the DMPP-evoked currents, but did not affect the voltage-gated Ca(2+) channel currents. These results indicate that gymnopilins directly act on nicotinic ACh receptors and inhibit their activity. This biological action of gymnopilins may be one of the causes of the G. junonius poisoning. |
| Databáze: | OpenAIRE |
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