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[摘要]
目的 研究药食两用的中药余甘子Phyllanthus emblica的化学成分,并评价其抗炎活性。方法 利用硅胶柱色谱、ODS柱色谱、Sephadex LH-20柱色谱和半制备HPLC以及重结晶方法对余甘子50%乙醇提取物的醋酸乙酯部位进行分离纯化;通过化合物的物理化学性质及其波谱数据等进行结构鉴定;最后利用脂多糖(LPS)诱导的小鼠巨噬细胞RAW264.7炎症反应模型,探究余甘子中含量高的化合物对NO、白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、单核细胞趋化蛋白-1(MCP-1)等炎症因子的影响,以评价其抗炎活性。结果 从余甘子中分离得到14个化合物,分别鉴定为异香草酸(1)、反式肉桂酸(2)、对羟基苯甲醛(3)、松柏醛(4)、槲皮素(5)、山柰酚-3-O-α-L-鼠李糖(6)、柚皮素(7)、2-羟基-3-苯基丙酸甲酯(8)、对苯二酚(9)、杨梅素(10)、2-呋喃甲酸(11)、没食子酸甲酯(12)、原儿茶酸(13)、没食子酸(14)。对含量较高的没食子酸、没食子酸甲酯和槲皮素3个化合物展开抗炎活性研究,结果表明没食子酸和没食子酸甲酯均能不同程度抑制各类炎症因子;槲皮素对炎症因子TNF-α和IL-6无显著抑制作用。结论 化合物1、3、4、8~11和13均为首次从该植物中分离得到。余甘子的抗炎作用可能与其酚酸类化合物相关。
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[Abstract]
Objective To study the chemical constituents and its anti-inflammtory activity effect of Phyllanthus emblica. Methods The chemical constituents of P. emblica were isolated and purified by silica gel column chromatography, ODS column chromatography, Sephadex LH-20 column chromatography, semi-preparative high-performance liquid chromatography and recrystallization method. Through their spectra data, physical and chemical properties analysis, the structures of those compounds with high content were identified. LPS-induced RAW264.7 inflammatory cell model was established to evaluate the effect of compounds in P. emblica on proinflammatory factors (NO, IL-6, TNF-α, and MCP-1) of RAW264.7 inflammatory cells. Results Totally, 14 compounds were isolated from P. emblica. and idetified as isovanillic acid (1), trans-cinnamic acid (2), p-hydroxybenzaldehyde (3), coniferyl aldehyde (4), quercetin (5), kaempferol-3-O-α-L-rhamnose (6), naringenin (7), 2-hydroxy-3-methyl phenylpropiolate (8), hydroquinone (9), myricetin (10), 2-furoic acid (11), methyl gallate (12), protocatechuic acid (13), gallic acid (14). The experiment of anti-inflammatroy effects showed that those compounds had different inhibitory effects on the production of inflammatory factors NO, IL-6, TNF-α and MCP-1. Conclusion Compounds 1, 3, 4, 8-11 and 13 are isolated from P emblica for the first time. The anti-inflammatory effect of P. emblica is related to its phenolic acids.
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[基金项目]
中国中医科学院“十三五”重点领域研究专项(ZZ10-007)