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A Molecular Basis for the Inhibition of Transient Receptor Potential Vanilloid Type 1 by Gomisin A
Lee, Sung Bae,Noh, Shinhwa,Yeom, Hye Duck,Jo, Heejin,Eom, Sanung,Kim, Yoon Suh,Nam, Sangsoo,Bae, Hyunsu,Lee, Jun-Ho Oxford University Press 2017 Evidence-based Complementary and Alternative Medic Vol.2017 No.-
<P> Transient receptor potential (TRP) channel has critical actions as conditional sensors in primary afferent neurons.We studied the regulatory action of gomisin A on TRPV1 channel current in this report. Schisandra chinensis contains bioactive compounds such as the gomisin derivatives and their related compounds. Coapplication with gomisin A inhibited the capsaicin-mediated inward peak current. This inhibitory effect of gomisin A on capsaicin-induced inward current showed concentration-dependence and was reversible. The half maximal inhibitory concentration of gomisin A was 62.7 ± 8.4 μM. In addition, this inhibition occurred in a noncompetition regulation mode and voltage insensitivemanner. Furthermore, molecular docking studies of gomisin A on TRPV1 showed that it interacted predominantly with residues at cavities in the segments 1 and 2 of each subunit. Four potential binding sites for this ligand in the extracellular region at sensor domain of TRPV1 channel were identified. Point mutagenesis studies were undertaken, and gomisin A potency decreased for both the Y453A and N467A mutants.The double mutation of Y453 and N467 significantly attenuated inhibitory effects by gomisin A. In summary, this study revealed the molecular basis for the interaction between TRPV1 and gomisin A and provides a novel potent interaction ligand. </P>
Lee, Sung Bae,Noh, Shinhwa,Yeom, Hye Duck,Kim, Hyunah,Kim, Wonkil,Kim, Yoon Suh,Bae, Hyunsu,Lee, Jun-Ho Kyung Hee Oriental Medicine Research Center, Kyung 2016 Oriental Pharmacy and Experimental Medicine Vol.16 No.4
Alisma Rhizomes is used as a diuretic, hypolipidemic, anti-diabetic and anti-inflammatory agent in traditional East-Asian medicine. In this study, we tested the effect of Alisma Rhizomes on the <TEX>${\alpha}3{\beta}4$</TEX> nicotinic acetylcholine (nACh) receptor channel current in Xenopus oocytes. The acetylcholine-induced inward peak current (<TEX>$I_{ACh}$</TEX>) was measured with the two-electrode voltage-clamp technique. This experiment shows that the <TEX>${\alpha}3{\beta}4$</TEX> nACh receptor cRNA injected into oocytes followed by co-application with Alisma Rhizomes inhibited <TEX>$I_{ACh}$</TEX> in a noncompetitive or voltage insensitive condition. The half maximal inhibitory concentration (<TEX>$IC_{50}$</TEX>) of Alisma Rhizomes was <TEX>$12.5{\pm}3.4{\mu}g/ml$</TEX> and the Vmax was <TEX>$55.4{\pm}4.7$</TEX>. Protostane-type triterpenoids are the main active ingredient of Alisma Rhizomes (Alisol A, Alisol B, Alisol B 23-acetate, Alisol C 23-acetate). The respective IC50 values of Alisol A, Alisol B, Alisol B 23-acetate, and Alisol C 23-acetate were <TEX>$1.7{\pm}0.1$</TEX>, <TEX>$2.8{\pm}0.5$</TEX>, <TEX>$2.6{\pm}0.7$</TEX> and <TEX>$3.5{\pm}0.3{\mu}M$</TEX> in the <TEX>${\alpha}3{\beta}4$</TEX> nACh receptor expressed in Xenopus oocytes. Altogether, our research shows that protostane-type triterpenoids may modulate the <TEX>${\alpha}3{\beta}4$</TEX> nACh receptors expressed in oocytes in a reversible, concentration dependent and non-competitive manner. Furthermore, this modulation of the nACh receptor activity by protostane-type triterpenoids could underlie the pharmaceutics actions of Alisma rhizome.
Sung Bae Lee,배현수,Jun-Ho Lee,Shinhwa Noh,Hye Duck Yeom,Wonkil Kim,Yoon Suh Kim 경희대학교 융합한의과학연구소 2016 Oriental Pharmacy and Experimental Medicine Vol.31 No.4
Alisma Rhizomes is used as a diuretic, hypolipidemic, anti-diabetic and anti-inflammatory agent in traditional East-Asian medicine. In this study, we tested the effect of Alisma Rhizomes on the α3β4 nicotinic acetylcholine (nACh) receptor channel current in Xenopus oocytes. The acetylcholine-induced inward peak current (IACh) was measured with the two-electrode voltage-clamp technique. This experiment shows that the α3β4 nACh receptor cRNA injected into oocytes followed by co-application with Alisma Rhizomes inhibited IACh in a noncompetitive or voltage insensitive condition. The half maximal inhibitory concentration (IC50) of Alisma Rhizomes was 12.5 ± 3.4 μg/ml and the Vmax was 55.4 ± 4.7. Protostane-type triterpenoids are the main active ingredient of Alisma Rhizomes (Alisol A, Alisol B, Alisol B 23-acetate, Alisol C 23-acetate). The respective IC50 values of Alisol A, Alisol B, Alisol B 23-acetate, and Alisol C 23-acetate were 1.7 ± 0.1, 2.8 ± 0.5, 2.6 ± 0.7 and 3.5 ± 0.3 μM in the α3β4 nACh receptor expressed in Xenopus oocytes. Altogether, our research shows that protostane-type triterpenoids may modulate the α3β4 nACh receptors expressed in oocytes in a reversible, concentration dependent and non-competitive manner. Furthermore, this modulation of the nACh receptor activity by protostane-type triterpenoids could underlie the pharmaceutics actions of Alisma rhizome.
Hye Duck Yeom,Young-Min Kim,Sung Bae Lee,Shinhwa Noh,Sanung Eom,Hyunah Kim,Wonkil Kim,Jae Hwan Lee,Hyunsu Bae,Jun-Ho Lee,H. Bae,J. H. Lee 대한독성 유전단백체 학회 2017 Molecular & cellular toxicology Vol.13 No.3
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 I5-HT and IACh 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.