青蒿化学成分及其抗补体活性

Chemical constituents from Artemisia annua and their anti-complement activities

目的研究青蒿Artemisia annua L.化学成分及其抗补体活性。方法青蒿75%乙醇提取物采用硅胶、Sephadex LH-20、TLC、半制备HPLC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。采用溶血试验法评价其抗补体活性。结果从中分离得到11个化合物,分别鉴定为chrysosplenetin(1)、artemetin(2)、东莨菪内酯(3)、山柰酚(4)、casticin(5)、芹菜素(6)、木犀草素(7)、青蒿素(8)、loliolide(9)、圣草酚(10)、3,7-dimethylquercetin(11)。化合物4、6~8、10~11对补体的经典和旁路途径均有抑制作用,活性最强的化合物8作用于补体C1q、C3~C5、C9靶点。结论化合物9、11为首次从该植物中分离得到。从青蒿中分离得到的青蒿素抗补体活性最强,可以作为补体抑制剂的候选化合物。

AIM To study the chemical constituents from Artemisia annua L.and their anti-complement activities.METHODS The 75%ethanol extract from A.annua was isolated and purified by silica gel,Sephadex LH-20,TLC and semi-preparative HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their anti-complement activities were evaluated by hemolysis test method.RESULTS Eleven compounds were isolated and identified as chrysosplenetin(1),artemetin(2),scopoletin(3),kaempferol(4),casticin(5),apigenin(6),luteolin(7),artemisinin(8),loliolide(9),eriodictyol(10),3,7-dimethylquercetin(11).Compounds 4,6-8,10-11 exhibited anti-complement activities toward classical and alternative pathway.Compound 8 with the strongest activity acted on C1q,C3-C5,C9 targets.CONCLUSION Compounds 9,11 are isolated from this plant for the first time.Artemisinin isolated from A.annua has the strongest anti-complement activity and can be used as a candidate compound for complement inhibitors.