STUDIES ON TYPE I ALLERGIC INHIBITORY EFFECTS TOWARD IMMUNE CELLS ON FOLK MEDICIN "TINEN"

中国民间草药，野牡丹。野牡丹科植物为传统的解热、解毒、利尿、止血、抗风湿药物。用80%丙酮水提物(MDL)和从该植物中分离出的化合物对被动皮肤过敏反应(PCA)活性以及对体外培养的大鼠腹膜肥大细胞释放组胺和白三烯(LT)以及小鼠巨噬细胞样细胞系RAW264.7产生一氧化氮(NO)的作用进行了研究。1)MDL抑制大鼠PCA、组胺释放、LT释放和NO的产生。2)烯类化合物，白三烯C(1)、木麻黄素(2)、马钱子素(3)、木麻黄素(4)、从水解性单宁中分离得到诺博单宁B(5)、牡荆素(6)、异槲皮苷(7)、4-O-[β-D-葡萄糖基]-3，3‘，4’-三O-甲基没食子酸(8)和没食子酸3-O-β-D(6‘-O-没食子酰基)-葡萄糖苷(9)。5)化合物1、2、3、4、5和7对LT释放抑制试验表现出较强的抑制活性。6)化合物5是一种二聚体单宁，对脂多糖和干扰素-γ激活的巨噬细胞产生NO的抑制作用比其他单体单宁2、3和4更强。然而，化合物I显示出细胞毒性活性。

Chinese folk mecicine, Melastoma dodecandum Lour. (Melastomaceae) has been used as a traditional antipyretic, antitoxic, ciuretic, hemostatic and anti-rheumatic medcine. An extract of the whole plant with 80% aqueous acetone (MDL)and compounds isolated from this plantwereexamined foranti-allergic activety in the Passive Cutaneous Anaphylaxis (PCA) activity, and toward histamine and leukottiene (LT) release from rat peritoneal mast cells in vitro and nitric oxide (NO) production by a murine macrophage-like cell line, RAW264.7, activated with lipopolysaccharide (LPS) and interferon-gamma (lFN-gamma).1) MDL inhibited rat PCA, histamine release, LT release and NO production.2) Nene compounds, plerocarinin C (1), casuarictin (2), pedunculagin (3), casuarinin (4), nobotannin B(5), vitexin (6), isoquercitrin (7), 4-O-[beta-D-glucopyranosyl]-3, 3', 4'-tri-O-methyl ellagic acid (8) and gallic acid 3-O-beta-D(6'-O-galloyl)-glucopyranoside (9) were isolated from MDL.3) Major inhibitory compounds on PCA were considered by hydrolyzable tannins because hydolyzable tannins 1, 2, 3, 4 and 5 inhibited strongly PCA and a flavonol 7 inhibited also it.4) Compounds 1, 2, 3 and9 showed strong inhibitory activities on histamine releasinhibitory test. Dimeric hydrolyzable tannin 5 and compounds 7 and 8 showed moderate inhibitory activities, but compound 4 did not show such inhibitory activity.5) Compounds 1, 2, 3, 4, 5 and 7 showed strong inhibitory activities on LT release inhibitory test.6) Compound 5, a dimeric tannin, was a stronger inhibitor than yhe other monomeric tannins 2, 3 and 4 in NO production by macrophages activated with LPS and IFN-gamma. However, compound I showed cytoloxic activity.