中药芸香中(+)/(-)-Rutabenzofuran A和(+)/(-)-Rutabenzofuran B的抗肝炎活性评价

Anti-hepatitis activities of(+)/(-)-Rutabenzofuran A and(+)/(-)-Rutabenzofuran B in traditional Chinese medicine Ruta graveolens L.

目的研究中药芸香中分离鉴定的两对Z/E异构化的苯并呋喃香豆素对映异构体(+)/(-)-Rutabenzofuran A和(+)/(-)-Rutabenzofuran B对肝脏的保护作用。方法以(+)/(-)-Rutabenzofuran A和(+)/(-)-Rutabenzofuran B为研究对象,采用脂多糖(LPS)100 ng·mL^(-1)建立HepG2细胞的炎症模型,对4个化合物的抗肝炎活性进行初步评估。结果在浓度10、20和40μmol·L^(-1)下,4个化合物可以剂量依赖性地降低谷丙转氨酶(ALT)和谷草转氨酶(AST)水平及肿瘤坏死因子(TNF)-α水平,升高白细胞介素(IL-4)和IL^(-1)0水平。结论芸香通过抑制TNF-α和促进IL-4及IL^(-1)0的产生发挥抗肝炎活性,且具有剂量依赖性,本研究为中药芸香的临床应用及药用开发提供充分的理论依据。

Objective To determine the hepatoprotective effect of two Z/E isomerized enantiomers of benzofuran coumarin(+)/(-)-Rutabenzofuran A and(+)/(-)-Rutabenzofuran B isolated from Rutabenzofuran.Methods(+)/(-)-Rutabenzofuran A and(+)/(-)-Rutabenzofuran B were used to establish the inflammation model of HepG2 cells with lipopolysaccharide(100 ng·mL^(-1)).The anti-hepatitis activities of the 4 compounds were preliminatively evaluated.Results At the concentrations of 10,20 and 40μmol·L^(-1),the four compounds reduced the levels of alanine aminotransferase,aspartate aminotransferase and tumor necrosis factorαlevel,and increased interleukin-4 and interleukin-10 levels dose-dependently.Conclusion Ruta graveolens L.can inhibit tumor necrosis factorαand promote interleukin-4 and interleukin-10 to produce anti-hepatitis activity in a dose-dependent manner,providing theoretical basis for clinical application and medicinal development of traditional Chinese medicine ruta.