College of Pharmacy, Kangwon National University, Chunchon, Republic of Korea.
Biol Pharm Bull. 2012;35(9):1581-7. doi: 10.1248/bpb.b110689.
The 70% ethanol extract of the rhizome of Alisma orientale (Alismatis rhizome) (AOE) was prepared and found to significantly inhibit 5-lipoxygenase (5-LOX)-catalyzed leukotriene (LT) production from rat basophilic leukemia (RBL)-1 cells and β-hexosaminidase release by antigen-stimulated RBL-2H3 cells. It also attenuated delayed-type hypersensitivity (DTH) reaction in mice. Among the three major triterpene constituents isolated (i.e., alisol B, alisol B 23-acetate, alisol C 23-acetate) as active principles, alisol B and its 23-acetate strongly and significantly inhibited LT production and β-hexosaminidase release between 1-10 µM. On the other hand, all these alisol derivatives significantly and strongly inhibited DTH response after oral administration. In addition, AOE (200 mg/kg/d) was for the first time found to considerably alleviate hapten-induced dermatitis symptoms in NC/Nga mice, an animal model of atopic dermatitis. These results indicate that alisol derivatives possess inhibitory activities on immediate-type as well as delayed-type hypersensitivity reactions and may contribute to the anti-allergic action of AOE.
泽泻根茎的 70%乙醇提取物（AOE）经制备发现可显著抑制大鼠嗜碱性白血病（RBL）-1 细胞中 5-脂氧合酶（5-LOX）催化的白三烯（LT）产生和抗原刺激的 RBL-2H3 细胞中β-己糖胺酶的释放。它还可减轻小鼠迟发型超敏反应（DTH）。作为活性成分分离的三种主要三萜成分（即泽泻醇 B、泽泻醇 B23-醋酸酯、泽泻醇 C23-醋酸酯）中，泽泻醇 B 和其 23-醋酸酯在 1-10 μM 之间强烈且显著地抑制 LT 产生和β-己糖胺酶释放。另一方面，所有这些泽泻醇衍生物在口服给药后均能显著和强烈地抑制 DTH 反应。此外，AOE（200mg/kg/d）首次被发现可显著减轻变应原诱导的 NC/Nga 小鼠（特应性皮炎的动物模型）的皮炎症状。这些结果表明，泽泻醇衍生物具有抑制即刻型和迟发型超敏反应的活性，可能有助于 AOE 的抗过敏作用。
