赤芝子实体化学成分研究和细胞毒活性测试  

Chemical constituents from the fruiting body of Ganoderma lucidum with cytotoxicity investigations

作　　者：程纯儒[1] 杨义[1] 丁杰[1] 关树宏[2] 果德安[2] 

机构地区：[1]四川理工学院化学与制药工程学院制药工程与技术应用研究所,四川自贡643000 [2]中国科学院上海药物研究所中药现代化研究中心,上海201203

出　　处：《沈阳药科大学学报》2014年第2期102-106,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的研究赤芝子实体石油醚部位的化学成分,寻找具有抗肿瘤活性的先导化合物。方法采用硅胶、Sephadex LH-20等柱色谱以及半制备高效液相色谱等手段分离纯化,并通过理化性质和波谱数据鉴定化合物的结构;采用MTT法测试分离化合物对人宫颈癌细胞的细胞毒活性。结果从赤芝子实体石油醚部位分离得到9个化合物,分别鉴定为3,7-二羟基-12-乙酰氧基-11,15,23-三羰基羊毛甾-8,22-二烯-26-酸(12-acetoxy-3,7-dihydroxy-11,15,23-trioxolanost-8,22-dien-26-oic acid,1)、灵芝三醇M(ganoderitriol M,2)、亚油酸乙酯[(10E,13E)-ethyl octadeca-10,13-dienoate,3]、亚油酸[(10E,13E)-octadeca-10,13-dienoic acid,4]、二十四碳酸(tetracosanoic acid,5)、3β-羟基-5α,8α-过氧麦角甾-6,9,22-三烯(3β-hydroxy-5α,8α-epidioxyergosta-6,9,22-triene,6)、麦角甾-7,22-二烯-3-酮(ergosta-7,22-dien-3-one,7)、过氧麦角甾醇(ergosterol peroxide,8)和麦角甾醇(ergosterol,9)。结论化合物1的波谱数据为首次报道,化合物3、4、7为首次从赤芝中分离得到。化合物2显示出中等强度的癌细胞抑制活性,其IC50为12μmol·L-1。Objective To study the chemical constituents of the petroleum ether extract of Ganoderma lucid- um and find compounds with anti-tumor activity. Methods Silica gel column chromatography, Sephadex LH- 20 and semi-preparative high performance liquid chromatography were applied for the isolation and pur- ification of the constituents. The structures were elucidated by their physicochemical properties and spectral methods. The inhibitory activity against the human HeLa cervical cancer cell lines was evaluated by MTT as- say. Results Nine compounds were isolated, including 12-acetoxy-3,7-dihydroxy-11,15,23-trioxolanost-8, 22-dien-26-oic acid （1）, ganoderitriol M （2）, （ 10E, 13E）-ethyl octadeca-10, 13-dienoate （3）, （ 10E, 13 E） -octadeca- 10,13 -dienoic acid （ 4 ）, tetracosanoic acid （ 5 ）, 3β-hydroxy -5 α, 8 α-epidioxyergosta-6,9,22- triene （6）, ergosta-7,22-dien-3-one （ 7 ）, ergosterol peroxide （ 8 ） and ergosterol （ 9 ）. Conclusions Com- pound 1 is first separated from fungus and its NMR spectral data are first reported. Compounds 3,4 and 7 are obtained from G. lucidum for the first time. Compound 2 exhibited moderate cytotoxicity （IC50 = 12 μmol.L-1 ）.

关 键 词：赤芝 三萜 甾醇 细胞毒活性 化学成分 结构鉴定 

分 类 号：R914[医药卫生—药物化学]