【作者】 赵芬琴；

【导师】 朴惠善；

【作者基本信息】 延边大学 ， 药物化学， 2005， 硕士

【摘要】 随着全球范围内工业化程度的加深和环境污染的加剧,周围环境中大量存在的致突变、致癌物对人类健康造成的威胁日趋严重。抗突变剂是从基因水平上预防疾病,加强保健,为人类健康长寿作出贡献,因此其开发和应用前景十分广阔,受到各国的普遍重视。从天然植物中寻找抗突变有效成分已成为当今国际生命科学领域的重大课题。 桦褐孔菌（Inonotus obliquus或Fuscoporia obliqua）属于多孔菌科褐卧孔菌属,据文献报道桦褐孔菌的水提取液可以抑制小鼠肉瘤的生长,在Walker 256癌肉瘤细胞、人MCF-7乳腺癌细胞的体外实验和白血病P 388细胞的体内实验中,桦褐孔菌中的inotodiol具有显著的细胞抑制活性,另外,3β,22-dihydroxylanosta-8,24-dien-7-one和3β,22-dihydroxy-lanosta-7,6（11）,24-triene的混合物也具有显著的细胞抑制活性。但对桦褐孔菌的抗突变作用的研究,尚未见报道。为了探索桦褐孔菌中的抗突变活性成分,本实验采用Ames试验测试抗突变活性,以抑制率为活性指标对桦褐孔菌中的抗突变有效部位和活性成分进行了较为系统地研究。 本实验先对桦褐孔菌醇提后的各个萃取部分—石油醚萃取物、乙酸乙酯萃取物、正丁醇萃取物以及桦褐孔菌多糖进行了Ames抗突变试验,筛选出有效部位—石油醚萃取物和乙酸乙酯萃取物,并对有效部位进行了化学成分的分离和单体化合物的抗突变试验。 实验结果表明:（一）桦褐孔菌醇提后的各个萃取部分中,石油醚萃取物和乙酸乙酯萃取物在Ames试验中有较高的抑制率,为抗突变有效部位。（二）采用反复的硅胶柱层析对石油醚萃取物和乙酸乙酯萃取物进行进一步的分离,共得到八个晶体化合物。根据理化性质、以及¹H-NMR、¹³C-NMR和MS等波谱数据分析鉴定了七个已知化合物的结构,它们分别是:lanosta-8,24-dien-3β-ol（lanosterol）（1）、lanosta-8,24-diene-3β, 22R-diol（inotodiol）（2和3）、ergosterol peroxide（5）、lanosta-8,24-diene-3β, 21-diol（uvariol）（6）、3β-hydroxy-lanosta 8,24-dien-21-oic acid（trametenolic acid）（7）、3β, 22, 25-trihydroxy-lanosta-8-ene更多还原

【Abstract】 With the deteriorating of environmental pollution in the more industrialized world, the environment mutagens and carcinogens are threatening our health more seriously. Antimutagents can prevent genemutaion-causing diseases. It has been a hot topic for the scholars at home and abroad to search for antimutagenic comstituents from natural plants.Inonotus obliquus (Pers. :Fr.) Pilat has been used for many kinds of tumors for a long time in many countries. It was reported that the aqueous extract of Inonotus obliquus inhibited the growth of sarcoma in mice. Antitumor activity of some compounds and fractions from an n-hexane extract of I. obliquus was tested against Walker 256 carcinosarcoma and MCF-7 human mammary adenocarcinoma in vitro, and leukemia P 388 in vivo. Inotodiol from I. obliquus was proved to be as strongly active as the mixture of 3 β ,22-dihydroxy-lanosta-8,24-dien-7-one and 3 3 ,22-dihydroxy-lanosta-7,6(11),24-triene. But study of antimutagenic activity of/. obliquus was accordingly not reported.In order to search for and make sure its antimutagenic constituents, petroleum ether extract, ethyl acetate extract, n-Butanol extract and crude polysaccharide of /. obliquus were firstly screened by Ames test. And then the antimutagenic extracts were further chromatographed to obtain the active compounds.The results showed: (1) The petroleum ether and ethyl acetate extracts both showed high inhibition rate to Salmonella typhimurium strains TA100, as the antimutagenic extracts. (2) Seven known compounds (1-3,5-8) and a new one (4) were isolated from the petroleum ether and ethyl acetate extracts by repeated silica gel column chromatography. Their chemical structures were identified as: lanosta-8,24-dien-3 β -ol (lanosterol) (1), lanosta-8,24-diene-3 β ,22R-diol (inotodiol) (2 and 3),ergosterol peroxide (5), lanosta-8,24-diene-3 P ,21-diol (uvariol) (6), 3 P -hydroxy-lanosta-8,24-dien-21-oic acid (trametenolic acid) (7) , 3 3 ,22,25-trihydroxy-lanosta-8-ene (8) by comparison of their ’H-NMR and I3C-NMR spectra and MS data with reported values. (3) The chemical structure of compound 4 was established as lanosta-24-ene-3 P ,21-diol on the basis of spectroscopic methods such as ’ H-NMR, 13C-NMR and MS, as well as DEPT-45.DEPT-90 and DEPT-135. (4) The Ames test of compound 1, 3 and 7 showed compound 1 and 3 had significant antimutagenic activity.更多还原