小叶榕叶中具有抗HSV活性的黄烷成分

Flavans with Anti-HSV Activity from the Leaves of Ficus microcarpa L.

摘要:

从小叶榕(Ficus microcarpa L.)叶的乙醇提取物中首次分离鉴定了(+)(2R,3S)阿夫儿茶素(1)、(-)(2R,3R)表阿夫儿茶素(2)、(-)(2R,3S)阿夫儿茶素-(4α-8)(2R,3S)阿夫儿茶素(3)、(-)(2R,3S)阿夫儿茶素-(4α-8)(2R,3R)表阿夫儿茶素(4) 4个黄烷化合物，其中化合物1和2对兔肾细胞中培养的2型单纯疱疹病毒(HSV-2)具有抑制作用，半数抑制浓度(IC50)分别为0.49 和0.55 mg mL-1，治疗指数(TI)分别为4.31和3.19，可用作小叶榕叶药材质量控制的指标成分。从该提取物中还分离鉴定了另外7个已知成分: 儿茶素(5)、phaseic acid (6)、苯甲酸(7)、4-羟基苯甲酸(8)、间苯三酚(9)、胡萝卜苷(10)和β-谷甾醇(11)。

Abstract:

Four flavans, named as (+)(2R,3S) afzelechin (1), (-)(2R,3R) epiafzelechin (2), (-)(2R,3S)afzelechin-(4α-8)(2R,3S) afzelechin (3) and (-)(2R,3S) afzelechin-(4α-8) (2R,3R)epiafzelechin (4), were isolated from ethanolic extract of the leaves of Ficus microcarpa L. for the first time. These compounds were evaluated antiviral effects in vitro towards herpes simplex virus (HSV). Flavans 1 and 2 exhibited low toxicity to rabbit kidney primary cells, moderate antiviral activity against HSV-1 with IC50 values of 0.49 and 0.55 mg mL-1, and therapeutic indexes (TI) of 4.31 and 3.19, respectively. According to cytotoxity and cytopathic effect (CPE) assays, they can be recommended as reference markers for quality control of Folium Fici microcarpae. Other seven known compounds, such as (+)catechin (5), phaseic acid (6), benzoic acid (7), 4-hydroxy-benzoic acid (8), phloroglucinol (9), daucosterol (10), and β-sitosterol (11), were also identified.