桃仁凝血因子Xa抑制活性部位分析

Coagulation Factor Xa Inhibition Activities of Semen Persicae

目的：研究中药桃仁的化学成分及其对凝血因子Xa（FXa）的抑制活性。方法：采用生色底物法和连续速率法进行FXa抑制活性测定,利用多种柱色谱技术对活性部位进行分离纯化,并通过波谱分析方法鉴定各化合物的结构。结果：桃仁乙酸乙酯萃取部位对FXa的抑制率高达60.27%,为抑制FXa的活性部位;从活性部位中分离鉴定出10个化合物,分别鉴定为9-十八碳烯酸-2＇,3＇-二羟基丙酯（1）,胡萝卜苷（2）,扁桃酰胺（3）,苯甲酸（4）,2-羟基-9-十八碳烯酸（5）,正十七烷酸（6）,9-十八碳烯酸甲酯（7）,对羟基苯甲酸（8）,棕榈酸（9）,苦杏仁苷（10）。结论：桃仁乙酸乙酯萃取部位为抑制FXa的活性部位,从活性部位中分离得到的化合物1和3首次从该科植物中分离得到,化合物5~8首次从该植物中分离得到。

Objective： To study the chemical constituents and coagulation Factor Xa （FXa） inhibition activities of Semen Persicae. Method： Chromogenic-substrates and continuous rate methods were used to assess the FXa inhibition activities. Various chromatographic techniques were used to isolate and purify the major active compounds, and their structures were identified by spectral analysis. Result： The ethyl acetate part possessed inhibition of 60.27% to FXa, and ten compounds were isolated and identified as 9-octadecenoic acid-2, 3- dihydroxypropyl ester （ 1 ）, daucosterol （2）, 2-hydroxy-2-phenylacetamide （3）, benzoic acid （ 4 ）, 2-hydroxy-9- octadecenoic acid （5）, n-heptadecanoic acid （6）, methyl elaidate （7）, p-hydroxybenzoic acid （8）, palmitic acid （9） and amygdalin （10）. Conclusion： The ethyl acetate part was the major FXa inhibition active site. Compounds 1 and 3 were isolated from the family of Rosaceae for the first time, and compounds 5-8 were first reported in this plant.