白鹤灵芝化学成分及其体外抗肿瘤与降脂活性研究

Chemical constituents from Rhinacanthus nasutus and their in vitro antitumor and lipid-lowering activities

目的研究白鹤灵芝的化学成分及其体外抗肿瘤与降脂活性。方法白鹤灵芝乙酸乙酯部位采用正相、反相硅胶柱和半制备HPLC分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用MTT法测定体外抗肿瘤活性,采用油酸诱导的HepG2高脂细胞模型评价体外降脂活性。结果从中分离得到20个化合物,分别鉴定为rhinacanthin A(1)、rhinacanthin B(2)、rhinacanthin C(3)、rhinacanthin D(4)、rhinacanthin E(5)、rhinacanthin M(6)、rhinacanthin N(7)、rhinacanthin Q(8)、rhinacanthin T(9)、rhinacanthone(10)、β-谷甾醇(11)、没食子酸(12)、香草酸(13)、丁香酸(14)、拉帕醇(15)、伞形花内酯(16)、sambucunlin A(17)、17α,21-dihydroxy-1,4-pregnadiene-3,11,20-trione,21-acetate(18)、1,8-二羟基蒽醌(19)、2,6-二甲氧基-1,4-苯醌(20)。化合物3、7抑制HepG2、Hela、A549、H22肿瘤细胞增殖的IC_(50)值为(0.66±0.17)~(3.22±0.49)μmol/L,且呈时间和浓度依赖性;化合物3、7、9对油酸诱导的HepG2高脂细胞脂质的清除率高达50%以上。结论化合物16~20为首次从该植物中分离得到。化合物3、7具有良好的体外抗肿瘤活性,3、7、9具有较好的体外降脂活性。

AIM To study the Chemical constituents from Rhinacanthus nasutus(L.)Kurz and their in vitro antitumor and lipid-lowering activities.METHODS The ethyl acetate fraction from R.nasutus was isolated and purified by normal phase,reverse phase silica gel column and semi-preparative HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The in vitro anti-tumor activity was determined by MTT assay,and the in vitro lipid-lowering activity was evaluated by oleic acid-induced HepG2 high-fat cell model.RESULTS Twenty compounds were isolated and identified as rhinacanthin A(1),rhinacanthin B(2),rhinacanthin C(3),rhinacanthin D(4),rhinacanthin E(5),rhinacanthin M(6),rhinacanthin N(7),rhinacanthin Q(8),rhinacanthin T(9),rhinacanthone(10),β-sitosterol(11),gallic acid(12),vanillic acid(13),syringic acid(14),lapachol(15),umbelliferone(16),sambucunlin A(17),17α,21-dihydroxy-1,4-pregnadiene-3,11,20-trione,21-acetate(18),1,8-dihydroxyanthraquinone(19),2,6-dimethoxy-1,4-benzoquinone(20).Compounds 3 and 7 inhibited the proliferation of HepG2,Hela,A549 and H22 tumor cells with IC_(50) values of(0.66±0.17)-(3.22±0.49)μmol/L in a time-and concentration-dependent manner.Compounds 3,7 and 9 had a lipid clearance rate of more than 50%in oleic acid-induced HepG2 high-fat cells.CONCLUSION Compounds 16-20 are isolated from this plant for the first time.Compounds 3 and 7 have good in vitro anti-tumor activities,and 3,7,9 have good in vitro lipid-lowering activities.