桦褐孔菌抗肿瘤活性部位的筛选及化学成分研究

Screening of antitumor fractions and chemical constituents from Inonotus obliquus

目的研究桦褐孔菌抗肿瘤活性部位及化学成分。方法将桦褐孔菌乙醇提取物(FT)、石油醚萃取物(FA)、乙酸乙酯萃取物(FB)、正丁醇萃取物(FC)以及水层萃余物(FD)作用于人肝癌Hep G2、胃癌SGC-7901及肺癌A549细胞,检测各提取部位对肿瘤细胞的生长抑制活性,并进一步对活性部分进行化学成分研究。结果活性数据分析表明FT、FA及FB均有抑制肿瘤活性,IC50值分别为56、28、47mg/L。从活性部位FA及FB分离得到10个化合物,分别鉴定为羊毛甾醇(1)、3β-羟基8,24-羊毛甾二烯-21-醛(2)、桦褐孔菌醇(3)、白桦脂醇(4)、5α,8α-表二氧-6,22-麦角甾二烯-3-醇(5)、4,6,8(14),22-麦角甾四烯-3-酮(6)、豆甾-4-烯-3-酮(7)、Inonotsuoxides B(8)、Inonotsutriols A(9)、胡萝卜苷(10)。结论 FA及FB是桦褐孔菌的抗肿瘤活性部位,从活性部位分离鉴定10个化合物,其中6、7、10首次在桦褐孔菌中发现。

Objective To screen the antitumor fractions of Inonotus obliquus and to study chemical constituents from the active fractions. Methods Ethanol extract （FT）, petroleum ether extract （FA）, ethyl acetate extract （FB）, n-butanol extract（FC） and aqueous extract（FD） from Inonotus obliquus were screened by inhibiting the growth of tumor cells（HepG2, SGC-7901, A549）. The constituentsfrom active fractions were further isolated and structurally elucidated by spectral analysis. Results FT, FA and FB exhibited antitumor activity, with ICs0 value of no more than 56, 28 and 47 rag/L, respectively. Ten known compounds were elucidated as lanosterol（ 1 ） , 313-hy- droxy-lanosta-8, 24-dien-21-al （2）, Inotodiol （ 3 ）, betulin （4）, 5c~, 8~x-Epidioxy ergosta-6, 22-dien-313-ol （ 5 ）, ergosta-4, 6, 8 （ 14 ）, 22-Tetraene-3-one （6）, stigmast4-en-3-one （7）, Inonotsuoxides B （ 8 ）, Inonotsutriols A （9）, daucosterol （10）. Conlusion Two fractions, FA and FB, are antitumor fractions, from which 10 compounds were separated and elucidated. Compoud 6, 7 and 10 are reported for the first time from Inonotus obliquus.