桦褐孔菌抗病毒活性成分的分离及结构鉴定

Isolation and Identification of the Antiviral Active Ingredients of Inonotus obliquus

摘要:

本文研究了桦褐孔菌乙酸乙酯提取物的化学成分、结构鉴定及其抗病毒活性。桦褐孔菌为一种食药型真菌，对人体毐性小，并且含有丰富的、结构复杂多样的和广泛的生物活性的次生代谢产物。桦褐孔菌子实体经干燥、粉碎，依次采用乙酸乙酯、甲醇、水进行常温浸提；采用各种分离手段，从桦褐孔菌乙酸乙酯提取物中分离出10个化合物单体；通过现代各种波谱分析方法及结合文献，最终确定: 白桦醇(1)、桦褐孔菌醇(2)、3-羟基羊毛甾-8,24-二烯-21-醛(3)、3β-羟基甘遂酸(4)、过氧麦角甾醇(5)、3β-羟基-5,8-环氧麦角甾醇-6,9,22-三烯(6)、邻苯二甲酸二正丁酯(7)、5-脱氢麦角甾醇(8)、二十五烷酸(9)、二十四烷酸(10)，其中化合物6和化合物7首次从桦褐孔菌中分离得到。对化合物1-8分别进行了细胞毒性和抗HSV-1病毒活性研究，其中化合物3的抗HSV-1病毒活性最强，其IC50值为98 μM；化合物7的细胞毒性最强，其CC50为24 μM，为后期桦褐孔菌开发成抗疱疹病毒药物提供科学依据。

Abstract:

The chemical composition, structure, and antiviral activity of ethyl acetate extracts of Inonotus obliquus was identified and analyzed. Inonotus obliquus is an edible and medical fungus with diverse and complex structures and a wide range of biological activities; in addition, this fungus has a low toxicity to humans and is rich in secondary metabolites. Inonotus obliquus fruit bodies were dried, ground, and sequentially extracted at room temperature using ethyl acetate, methanol, and water. Ten compounds were isolated from the ethyl acetate extract of Inonotus obliquus using various chromatographic techniques. Various modern spectroscopic methods of analysis and the data available in literature were used to identify the following compounds: betulin (1), inotodiol (2), 3-hydroxy-lanosta-8,24-dien-21-al (3), 3β-hydroxytirucallic acid (4), ergosterol-5,8-peroxide (5), 3β-hydroxy-5α,8α-epidioxyergosta-6,9,22-triene (6), di(n-butyl) phthalate (7), 5-dehydroergosterol (8), pentacosanoic acid (9), and lignoceric acid (10). Among these, compounds 6 and 7 were isolated from Inonotus obliquus for the first time. Furthermore, the cytotoxicity and anti-HSV-1 activity of the isolated compounds 1–8 were also investigated. Compound 3 showed the strongest anti-HSV-1 activity, with a half maximal inhibitory concentration (IC50) of 98 μM; on the other hand, compound 7 exhibited the strongest cytotoxicity, with a 50% cytotoxic concentration (CC50) of 24 μM. This study provides a scientific basis for the future development of anti-HSV drugs from Inonotus obliquus.