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Suppressive effects of coumarins from Mammea siamensis on inducible nitric oxide synthase expression in RAW264.7 cells

机译:暹罗香豆素类香豆素对RAW264.7细胞诱导型一氧化氮合酶表达的抑制作用

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摘要

A methanol extract of the flowers of Mammea siamensis (Calophyllaceae) was found to inhibit nitric oxide (NO) production in lipopolysaccharide-activated RAW264.7 cells. From the extract, two new geranylated coumarins, mammeasins A (1) and B (2), were isolated together with 17 known compounds including 15 coumarins. The structures of 1 and 2 were determined on the basis of their spectroscopic properties as well as of their chemical evidence. Among the isolates, 1 (IC 50 = 1.8 μM), 2 (6.4 μM), surangins B (3, 5.0 μM), C (4, 6.8 μM), and D (5, 6.2 μM), kayeassamins E (7, 6.1 μM), F (8, 6.0 μM), and G (9, 0.8 μM), mammea A/AD (11, 1.3 μM), and mammea E/BB (16, 7.9 μM) showed NO production inhibitory activity. Compounds 1, 9, and 11 were found to inhibit induction of inducible nitric oxide synthase (iNOS). With regard to mechanism of action of these active constituents (1, 9, and 11), suppression of STAT1 activation is suggested to be mainly involved in their suppression of iNOS induction.
机译:发现棉麻花(Calamphyllaceae)的甲醇提取物可抑制脂多糖激活的RAW264.7细胞中一氧化氮(NO)的产生。从提取物中分离出两种新的香兰素化香豆素,mammeasins A(1)和B(2),以及17种已知化合物,其中包括15种香豆素。 1和2的结构是根据其光谱性质和化学证据确定的。在分离物中,有1种(IC 50 = 1.8μM),2种(6.4μM),surangins B(3、5.0μM),C(4、6.8μM)和D(5、6.2μM),kayeassamins E(7, F(8,6.0μM)和F(8,6.0μM),G(9,0.8μM),A / AD(11,1.3μM)和E / BB(16,7.9μM)表现出NO产生抑制活性。发现化合物1、9和11抑制诱导型一氧化氮合酶(iNOS)的诱导。关于这些活性成分(1、9和11)的作用机理,建议抑制STAT1激活主要涉及抑制iNOS诱导。

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