蟾皮化学成分的分离与结构鉴定

Isolation and structure identification of chemical constituents from the skin of Bufo bufo gargarizans

蟾皮为蟾蜍科动物中华大蟾蜍Bufo bufo gargarizansCantor的干燥皮,在我国民间多用来治疗原发性肝癌、肺癌、肠癌等,其水溶性成分制剂华蟾素注射液临床上用于消化道中晚期癌症,疗效确切,体外抗肿瘤活性筛选也表明蟾皮水提取物对结肠癌细胞HCT-8、肺癌细胞A-549生长均有明显的抑制作用。为了阐明其活性成分,对其水溶性成分进行了系统研究,采用Sephadex LH-20、硅胶柱色谱结合结晶法,从其水提物中分离得到6个化合物,分别鉴定为4-氨基-3-羟甲基-环辛酰胺骈四氢-α-呋喃酮(蟾蜍环酰胺B,I)、蟾蜍环酰胺C(II)、蟾蜍噻咛(III)、去氢蟾蜍色氨氢溴酸盐(IV)、辛二酸(V)和丁二酸(VI),其中化合物I和II为新化合物。

The skin of Bufo bufo gargarizans,originated from Bufo bufo gargarizans Cantor(Bufonidae),is widely used in traditional Chinese medicine for the treatment of hepatoma,lung cancer and etc.The preparation of the aqueous components has significant therapeutic effect against the digestive tract cancer.The water-soluble chemical constituents in the skin of Bufo bufo gargarizans were then investigated to make clear the active compounds.Six compounds were isolated and purified by recrystallization and column chromatography on silica gel and ODS,their structures were elucidated as(4-amido-3-hydroxymethyl-cyclooctylamidezotetra-α-furanone)(I),bufogargarizanine C(II),bufothionine(III),dehydrobufotenine hydrobromide(IV),suberic acid(V) and succinic acid(VI) on the basis of physicochemical properties and spectral data((UV,IR,()~1H NMR,()^(13)C NMR and MS).Of the above compounds,compounds I and II are new compounds and named bufogargarizanine B and C,respectively.