title: The Rhizomes of Acorus gramineus and the Constituents Inhibit Allergic Response In vitro and In vivo.
abstract: 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.
authors.affiliation: College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
authors.forename: Hyun
authors.initials: H
authors.lastname: Lim
authors.forename: Seung Young
authors.initials: SY
authors.lastname: Lee
authors.forename: Kang Ro
authors.initials: KR
authors.lastname: Lee
authors.forename: Yeong Shik
authors.initials: YS
authors.lastname: Kim
authors.forename: Hyun Pyo
authors.initials: HP
authors.lastname: Kim
keywords: 2; 3-Dihydro-4; 4; 5; 5-Lipoxygenase; 5-trimethoxyphenyl)indene; 7-trimethoxy-1-ethyl-2-methyl-3-(2; Acorus gramineus; Anti-allergy; β-Asarone; β-Hexosaminidase