山木瓜枝中抑制黄嘌呤氧化酶活性的化学成分研究

Xanthine Oxidase Inhibitors from The Twigs of Garcinia Esculenta

目的:研究山木瓜枝中抑制黄嘌呤氧化酶活性的化学成分。方法:通过活性导向分离,筛选山木瓜枝中具有抑制黄嘌呤氧化酶活性的粗提物及组分,采用多种色谱分离技术对活性部位进行系统分离,通过理化常数和光谱分析,结合相关文献确定所得化合物的结构;并对所得化合物进行黄嘌呤氧化酶抑制活性的研究。结果:从山木瓜枝的乙酸乙酯部位分离得到6个化合物,经鉴定分别为桑橙素(1)、4,6,3',4'-tetrahydroxy-2-methoxybenzophenone(2)、2,4,6,3'-tetrahydroxybenzo-phenone(3)、3,6,7-trihydroxy-1-methoxyxanthone(4)、2S,3S-3,5,7,3',5'-pentahydroxyavane(5)、丁香酸(6);实验研究证实化合物1对黄嘌呤氧化酶具有一定的抑制活性(IC50=28.9μM)。结论:从活性部位鉴定的6个化合物均为首次从该植物中分离得到,其中化合物1是主要的活性成分。

Objective： To study the xanthine oxidase inhibitors from the twigs of Garcinia esculenta,and identify novel xanthine oxidase inhibitors. Methods： Bioassay-guided fractionation was used in the investigation of the extracts from the twigs of Garcinia esculenta,as well as means of column chromatography. The structures of the isolated compounds in the investigation were elucidated by comprehensive NMR and MS spectroscopic data analysis,as well as compared with previously publications. The effects of the isolated compounds on xanthine oxidase have been further investigated. Results： Six compounds were isolated from Et OAc fraction of the twigs of Garcinia esculenta,and their structures were identified to be maclurin（ 1）,4,6,3＇,4＇-tetrahydroxy-2-methoxybenzophenone（ 2）,2,4,6,3＇-tetrahydroxybenzophenone（ 3）,3,6,7-trihydroxy-1-methoxyxanthone（ 4）,2S,3S-3,5,7,3＇,5＇-pentahydroxyavane（ 5）,syringic acid（ 6）. Compound 1 showed moderate inhibition on xanthine oxidase activity with an IC50 value of approximately 28. 9 μM. Conclusion： Compounds 1-6 were isolated from the plant,and the xanthine oxidase inhibitory effect of compound 1 was reported for the first time.