鸦胆子中苦木素类成分及其生物活性

Quassins from Brucea javanica and their biological activities

目的 研究鸦胆子Brucea javanica(L.) Merr.苦木素类成分及其生物活性。方法 采用硅胶、大孔吸附树脂HP-20、Sephadex LH-20、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。对化合物抗炎活性、抗补体活性进行评价,利用流式细胞术检测化合物对HepG2细胞凋亡的作用。结果 从中分离得到10个化合物,分别鉴定为javanicoside A(1)、yadanzioside A(2)、yadanzioside G(3)、yadanzioside J(4)、yadanziolide S(5)、desmethyl-brusatol(6)、yadanzioside F(7)、yadanzioside E(8)、javanicoside J(9)、javanicoside B(10)。化合物3和8对RAW267.4、MH-S、HepG2细胞的IC_(50)值分别为(87.8±1.08)、(75.3±0.03)、(32.9±0.89)、(92.9±1.83)、(99.7±0.33)、(38.0±0.45)μmol/L。结论 化合物3和8具有明显的抗炎、抗补体、抗肿瘤活性。

AIM To study quassins from Brucea javanica(L.) Merr. and their biological activities.METHODS The extract from B. javanica was isolated and purified by silica gel, macroporous adsorption resin HP-20, Sephadex LH-20 and HPLC, then the structures of obtained compounds were identified by physicochemical properties and spectral data. The anti-inflammatory activity and anti-complement activity of the compounds were evaluated. The effects of the compounds on apoptosis of HepG2 cells was examined by flow cytometry.RESULTS Ten compounds were isolated and identified as javanicoside A(1), yadanzioside A(2), yadanzioside G(3), yadanzioside J(4), yadanziolide S(5), desmethyl-brusatol(6), yadanzioside F(7), yadanzioside E(8), javanicoside J(9), javanicoside B(10). The IC_(50)values of compound 3 and 8 on RAW267.4, MH-S, HepG2 cells were(87.8±1.08),(75.3±0.03),(32.9±0.89),(92.9±1.83),(99.7±0.33),(38.0±0.45) μmol/L, respectively.CONCLUSION Compounds 3 and 8 have obvious anti-inflammatory, anti-complement and anti-tumor activities.