College of Pharmacy, Kangwon National University, Chunchon 200-701, Korea.
Arch Pharm Res. 2009 Nov;32(11):1509-14. doi: 10.1007/s12272-009-2102-4.
To assess the anti-inflammatory activity of constituents from the rhizomes of Anemarrhena asphodeloides, (-)-nyasol {cis-hinokiresinol, 4,4-[1Z,3R]-3-ethenyl-1-propene-1,3-diyl]bisphenol} was isolated and its anti-inflammatory activity was examined in lipopolysaccharide (LPS)-treated RAW 264.7 cells and A23187-treated RBL-1 cells. In vivo activity was measured using carrageenan-induced paw edema assay. At > 1 microM, (-)-nyasol significantly inhibited cyclooxygenase-2 (COX-2)-mediated PGE2 production and inducible nitric oxide synthase (iNOS)-mediated NO production in LPS-treated RAW 264.7 cells, a mouse macrophage-like cell line, but did not affect the expression levels of COX-2 and iNOS. (-)-Nyasol also inhibited 5-lipoxygenase (5-LOX)-mediated leukotriene production in A23187-treated RBL-1 cells. Furthermore, (-)-nyasol potently inhibited carrageenan-induced paw edema in mice (28.6-77.1% inhibition at 24-120 mg/kg). Therefore, (-)-nyasol is a potential new lead compound and may contribute to the anti-inflammatory action of A. asphodeloides, possibly by inhibiting COX-2, iNOS and 5-LOX.
为了评估知母根茎成分的抗炎活性，分离出了（-）-nyasol（顺式-辛可醇，4,4-[1Z，3R]-3-乙烯基-1-丙烯-1,3-二基]双酚），并在脂多糖（LPS）处理的 RAW 264.7 细胞和 A23187 处理的 RBL-1 细胞中检查了其抗炎活性。体内活性通过角叉菜胶诱导的爪肿胀测定法进行测量。在>1μM时，（-）-nyasol 显著抑制了 LPS 处理的 RAW 264.7 细胞（一种小鼠巨噬细胞样细胞系）中环氧合酶-2（COX-2）介导的 PGE2 产生和诱导型一氧化氮合酶（iNOS）介导的 NO 产生，但不影响 COX-2 和 iNOS 的表达水平。（-）-nyasol 还抑制了 A23187 处理的 RBL-1 细胞中 5-脂氧合酶（5-LOX）介导的白三烯产生。此外，（-）-nyasol 强烈抑制了角叉菜胶诱导的小鼠爪肿胀（在 24-120mg/kg 时抑制率为 28.6-77.1%）。因此，（-）-nyasol 是一种有潜力的新型先导化合物，可能通过抑制 COX-2、iNOS 和 5-LOX 来发挥知母的抗炎作用。
