油茶枯乙酸乙酯部位化学成分及其抗炎活性

Chemical Constituents of Ethyl Acetate Extract from Seed Cake of Camellia oleifera and Its Anti-inflammatory Activities

目的:为了深入研究油茶枯化学成分及其药理活性,为其进一步开发利用奠定科学依据。方法:采用各种柱色谱手段对油茶枯醇提取物的乙酸乙酯部位化学成分进行分离,采用现代波谱手段鉴定其结构;并采用脂多糖(LPS)诱导的小鼠巨噬细胞RAW264. 7建立体外炎症筛选模型,评价其抗炎活性,为其进一步开发利用奠定科学依据。结果:从油茶枯醇提取物的乙酸乙酯部位中分离获得10个化合物,其中8个为酚酸类化合物,2个为黄酮类化合物,分别为对羟基苯甲酸(1),原儿茶酸(2),没食子酸(3),没食子酸甲酯(4),没食子酸乙酯(5),异香草酸(6),3,4-二羟基苯甲酸乙酯(7),2-(3’,4’-二羟苯基)-1,3-胡椒环-5-醛(8),槲皮素(9),芦丁(10),其中化合物4~8为首次从该植物中分离获得。上述化合物对LPS诱导巨噬细胞RAW264. 7产生炎症因子NO均具有良好的抑制作用,剂量依赖性明显,其中化合物8的活性最强。结论:油茶枯中的酚酸和黄酮类化合物在抗炎药物的开发、应用上具有良好发展前景。

Objective:To intensively study the chemical constituents from the seed cake of Camellia oleifera and its pharmacological activities,in order to provide scientific basic for its further development and utilization.Method:All kinds of column chromatography and spectral methods were employed to isolate and identify the monomeric compounds from its ethyl acetate portion of ethanol extract.The in vitro anti-inflammatory effects were evaluated by LPS-induced inflammatory model in RAW264.7 macrophages.Result:Eight phenolic acids and two flavonoids were isolated from the ethyl acetate soluble portion and identified as p-hydroxybenzoic acid(1),protocatechuic acid(2),gallic acid(3),methyl gallate(4),ethyl gallate(5),isovanillic acid(6),ethyl 3,4-dihydroxylbenzoate(7),2-(3’,4’-dihydroxyphenyl)-1,3-benzodioxole-5-aldehyde(8),quercetin(9),rutoside(10).Among them,compounds 4-8 were first isolated from this plant.These compounds had good anti-inflammatory activities against NO production in LPS-stimulated RAW264.7 macrophages in an obvious dose-dependent manner.Among them,compound 8 showed a strongest activity.Conclusion:The above results show that the phenolic acids and flavonoids from seed cake of C.oleifera have good prospects for the development and application of anti-inflammatory drugs.