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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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Abstract

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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  1. These authors contributed equally to this work.

Authors and Affiliations

  1. Department of Biotechnology, Chonnam National University, Gwangju, 61886, Republic of Korea

    Hye Duck Yeom, Sung Bae Lee, Shinhwa Noh, Sanung Eom, Hyunah Kim, Wonkil Kim & Jun-Ho Lee

  2. Department of Food Science and Technology, Chonnam National University, Gwangju, 61886, Republic of Korea

    Young-Min Kim

  3. College of Korean Medicine, Kyung Hee University, Seoul, 02447, Republic of Korea

    Jae Hwan Lee & Hyunsu Bae

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  1. Hye Duck Yeom
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Correspondence to Hyunsu Bae or Jun-Ho Lee.

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Yeom, H.D., Kim, YM., Lee, S.B. et al. Effects of triterpenoid Alisol-F on human 5-hydroxytryptamine 3A and α3β4 nicotinic acetylcholine receptor channel activity. Mol. Cell. Toxicol. 13, 271–278 (2017). https://doi.org/10.1007/s13273-017-0030-9

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