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KMID : 1200820160160040303
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Oriental Pharmacy and Experimental Medicine
2016 Volume.16 No. 4 p.303 ~ p.309
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The regulatory effect of Alisma Rhizomes and their triterpenoids on α3β4 nicotinic acetylcholine receptor activity
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Lee Sung-Bae
Noh Shin-Hwa
Yeom Hye-Duck
Kim Hyun-Ah
Kim Won-Kil
Kim Yoon-Suh
Bae Hyun-Su
Lee Jun-Ho
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Abstract
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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.
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KEYWORD
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Alisma Rhizomes, Protostane-type triterpenoids, Nicotinic acetylcholine receptor, Ligand-gated ion channel
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