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40 μmol·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-10水平.结论 芸香通过抑制TNF-α和促进IL-4及IL-10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.
Anti-hepatitis activities of(+)/(-)-Rutabenzofuran A and(+)/(-)-Rutabenzofuran B in traditional Chinese medicine Ruta graveolens L.
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 40 μmol·L-1,the four compounds reduced the levels of alanine aminotransferase,aspartate aminotransferase and tumor necrosis factor α level,and increased interleukin-4 and interleukin-10 levels dose-dependently.Conclusion Ruta graveolens L.can inhibit tumor necrosis factor α and 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.
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