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KMID : 1034820170130030271
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Molecular & Cellular Toxicology
2017 Volume.13 No. 3 p.271 ~ p.278
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Effects of triterpenoid Alisol-F on human 5-hydroxytryptamine 3A and α3β4 nicotinic acetylcholine receptor channel activity
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Yeom Hye-Duck
Kim Young-Min
Lee Sung-Bae
Noh Shin-Hwa
Eom Sa-Nung
Kim Hyun-Ah
Kim Won-Kil
Lee Jae-Hwan
Bae Hyun-Su
Lee Jun-Ho
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Abstract
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Alisma Rhizome is a known tradition medication, which has been used for its diuretic, hypolipidemic, anti-diabetic, and anti-inflammatory purposes for thousands of years. The primary compounds of Alisma Rhizome are protostane type triterpenes, such as Alisols A, B or C. We previously demonstrated that Alisol derivatives (Alisols A, B, and C) have inhibitory effects on 5-hydroxytryptamine 3A (5-HT3A) currents1. In this study, we tested the effects of a new triterpene, Alisol-F, on human 5-HT3A and α3β4 nicotinic acetylcholine (nACh) receptor channel currents by using Xenopus oocytes expressing these channels. Co-application of Alisol-F inhibited 5-HT3A and α3β4 nACh receptor-mediated inward peak currents. The inhibitory effect of Alisol-F on 5-HT and ACh-induced inward peak currents occurred in a reversible and concentration- dependent manner. The half maximal inhibitory concentrations (IC50) of Alisol-F were 79.4 ± 11.0 and 21.2 ±6.0 μM for the 5-HT3A and α3β4 nACh receptors, respectively. In addition, the inhibition of I 5-HT and I ACh by Alisol-F occurred noncompetitive and voltage insensitive manner. Taken together, these results show that Alisol-F may regulate 5-HT3A and α3β4 nACh receptors channel expressed in Xenopus oocytes.
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KEYWORD
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Alisma Rhizome, Alisol-F, Ligand-gated ion channel, 5-Hydroxytryptamine 3A receptor, Nicotinic acetylcholine receptor
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