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KMID : 0606920120200050477
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Biomolecules & Therapeutics
2012 Volume.20 No. 5 p.477 ~ p.481
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The Rhizomes of Acorus gramineus and the Constituents Inhibit Allergic Response In vitro and In vivo
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Lim Hyun
Lee Seung-Young
Lee Kang-Ro
Kim Yeong-Shik
Kim Hyun-Pyo
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Abstract
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The rhizomes of Acorus gramineus have frequently been used in traditional medicine mainly for sedation as well as enhancing brain function. In this study, the anti-allergic activity of A. gramineus was investigated. The 70% ethanol extract of the rhizomes of A. gramineus was found to inhibit the allergic response against 5-lipoxygenase (5-LOX)-catalyzed leukotriene (LT) production from rat basophilic leukemia (RBL)-1 cells and β-hexosaminidase release from RBL-2H3 cells with IC50’s of 48.9 and >200 μg/ml, respectively. Among the 9 major constituents isolated, β-asarone, (2R,3R,4S,5S)-2,4-dimethyl-1,3-bis (2',4',5'-trimethoxyphenyl)tetrahydrofuran (AF) and 2,3-dihydro-4,5,7-trimethoxy-1-ethyl-2-methyl-3-(2,4,5-trimethoxyphenyl)indene (AI) strongly inhibited 5-LOX-catalyzed LT production in A23187-treated RBL-1 cells, AI being the most potent (IC50=6.7 μM). Against β-hexosaminidase release by antigen-stimulated RBL-2H3 cells, only AI exhibited strong inhibition (IC50=7.3 μM) while β-asarone and AF showed 26.0% and 39.9% inhibition at 50 μM, respectively. In addition, the ethanol extract of A. gramineus showed significant inhibitory action against the hapten-induced delayed hypersensitivity reaction in mice by oral administration at 200 mg/kg. Therefore, it is suggested that A. gramineus possesses anti-allergic activity and the constituents including β-asarone and AI certainly contribute to the anti-allergic activity of the rhizomes of A. gramineus.
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KEYWORD
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Acorus gramineus, β-Asarone, 2, 3-Dihydro-4, 5, 7-trimethoxy-1-ethyl-2-methyl-3-(2, 4, 5-trimethoxyphenyl)indene, 5-Lipoxygenase, β-Hexosaminidase, Anti-allergy
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