杨桃根化学成分及其体外生物活性

Chemical constituents from the roots of Averrhoa carambola and their in vitro biological activities

目的研究杨桃Averrhoa carambola L.根的化学成分及其体外生物活性。方法杨桃根95%乙醇提取物采用硅胶、Rp-18、Diol、MCI、TLC进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用酶标板法评价体外生物活性。结果从中分离得到15个化合物,分别鉴定为2,2′-氧代双(1,4-二叔丁苯)(1)、5-methoxy-3-undecylphenol(2)、2-dodecyl-6-methoxycyclohexa-2,5-diene-1,4-dione(3)、5-O-methylembelin(4)、鲨烯(5)、豆甾-4-烯-3-酮(6)、邻苯二甲酸二正戊酯(7)、邻苯二甲酸二正丁酯(8)、油酸(9)、β-谷甾醇-3-O-棕榈酸酯(10)、2-tridecyl-6-methoxycyclohexa-2,5-diene-1,4-dione(11)、(±)-lyoniresinol(12)、5α,6β-dihydroxysitosterol(13)、6′-O-棕榈酰-β-胡萝卜苷(14)、10-eicosenoic acid(15)。化合物2~3对α-葡萄糖苷酶的抑制活性强于阿卡波糖,在浓度为180μmol/L时对DPP-Ⅳ酶的抑制活性大于50%。结论化合物1、5~7、10、12~14为首次从阳桃属植物中分离,化合物2、9为首次从杨桃根中分离得到。化合物2~3具有较强的体外α-葡萄糖苷酶和DPP-Ⅳ酶抑制活性。

AIM To study the chemical constituents from the roots of Averrhoa carambola L.and their in vitro biological activities.METHODS The 95%ethanol extract from the roots of A.carambola was isolated and purified by silica gel,Rp-18,Diol,MCI and TLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their biological activities in vitro were evaluated by enzyme plate method.RESULTS Fifteen compounds were isolated and identified as 2,2′-oxybis(1,4-di-tert-butylbenzene)(1),5-methoxy-3-undecylphenol(2),2-dodecyl-6-methoxycyclohexa-2,5-diene-1,4-dione(3),5-O-methylembelin(4),squalene(5),stigmastan-4-en-3-one(6),dipentyl phthalate(7),dibutyl phthalate(8),oleic acid(9),β-sitosterol palmitate(10),2-tridecyl-6-methoxycyclohexa-2,5-diene-1,4-dione(11),(±)-lyoniresinol(12),5α,6β-dihydroxysitosterol(13),β-sitosteryl-3β-glucopyranoside-6′-O-palmitate(14),10-eicosenoic acid(15).Compounds 2 and 3 showed stronger in vitro inhibitory activities againstα-glucosidase than acarbose,whose inhibitory rates against DPP-Ⅳenzyme were more than 50%at the concentration of 180μmol/L.CONCLUSION Compounds 1,5-7,10,12-14 are first isolated from genus Averrhoa.Compounds 2 and 9 are isolated from the roots of A.carambola for the first time.Compounds 2-3 show strong in vitro inhibitory activities againstα-glucosidase and DPP-Ⅳ.