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

中国民间医药，黄芪。作为传统的解热、抗毒、消炎、止血和抗风湿病的药物。本研究用含80%水丙酮（MDL）的全株提取物和从该植物中分离出的化合物，对其抗过敏活性、被动皮肤过敏反应（PCA）活性、体外大鼠腹膜肥大细胞释放组胺和白素（LT）的活性以及被脂多糖（LPS）和干扰素- γ (lfn - γ)激活的小鼠巨噬细胞样细胞系RAW264.7产生一氧化氮（NO）的活性进行了检测。1) MDL抑制大鼠PCA、组胺释放、LT释放和NO生成。2)从mdl中分离到壬烯类化合物，松果素C(1)、木麻黄素(2)、豆黄素(3)、木麻黄素(4)、木麻黄素B(5)、牡荆素(6)、异槲皮素(7)、4- o -[β - d -葡萄糖吡喃基]- 3,3 ‘、4’-三- o -甲基鞣花酸（8)和没食子酸3- o - β - d （6'- o -没食子基）-葡萄糖吡喃苷(9)。3）可水解的单宁酸1、2、3、4和5对PCA有较强的抑制作用，黄酮醇7对PCA也有抑制作用。4)化合物1、2、3、9在组胺释放抑制试验中表现出较强的抑制活性。二聚体可水解单宁5和化合物7、8表现出中等抑制活性，而化合物4不表现出抑制活性。5)化合物1、2、3、4、5和7在LT释放抑制试验中表现出较强的抑制活性。6)化合物5是一种二聚单宁，对LPS和ifn - γ激活的巨噬细胞产生NO的抑制作用强于其他单体单宁2、3和4。然而，化合物1显示细胞毒性活性。

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.