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目的对北极真菌Nectriasp.B-13中的酚醛倍半萜烯类化合物进行结构鉴定及生物学活性研究。方法采用硅胶柱层析、Sephadex LH-20凝胶柱层析、高效液相色谱等分离手段对极地真菌Nectriasp.B-13发酵液的乙酸乙酯萃取部位进行了系统的分离,利用1 H-和13 C-NMR、LC-MS等现代波谱解析手段,结合文献对照,鉴定化合物结构;采用MTT法和微量稀释法测试了化合物的细胞毒活性和抗稻瘟霉作用。结果从提取物中分离得到4个化合物,这4个为酚醛倍半萜烯类化合物,分别为dechlorodeacetylchloronectrin(1),LL-Z-1272εacid(2),8’-hydroxyascochlorin(3)和LL-Z 1272β(4)。活性测试的结果表明,化合物2对5种肿瘤细胞株均有一定程度的生长抑制作用,其IC50值的范围在48.67~92.18μmol/L之间;同时,化合物2还可抑制稻瘟霉的生长,MIC值为18.2μg/mL。结论化合物1和化合物2为首次从微生物次级代谢产物中获得的化合物,为新天然产物。化合物2有一定的细胞毒活性和抗稻瘟霉作用。
OBJECTIVE To study the structural identification and biological activity of phenolic sesquiterpenes in Arctic fungi Nectriasp.B-13. Methods The ethyl acetate extract of the polar fermentation broth Nectriasp.B-13 was systematically isolated by silica gel column chromatography, Sephadex LH-20 gel column chromatography and high performance liquid chromatography (HPLC) And 13 C-NMR, LC-MS and other modern spectroscopic analysis methods, combined with the literature control to identify the structure of the compounds; MTT assay and micro-dilution method was used to test the compounds cytotoxic activity and anti-Pyricularia oryzae role. Results Four compounds were isolated from the extracts, which are phenolic sesquiterpenes, dechlorodeacetylchloronectrin (1), LL-Z-1272εacid (2), 8’-hydroxyascochlorin (3) and LL-Z 1272β (4). The results of the activity test showed that compound 2 inhibited the growth of five tumor cell lines to a certain extent with the IC50 values ranging from 48.67 to 92.18 μmol / L. Meanwhile, compound 2 also inhibited the growth of rice blast , MIC value of 18.2μg / mL. Conclusions Compounds 1 and 2 are the first compounds derived from microbial secondary metabolites and are novel natural products. Compound 2 has certain cytotoxic activity and resistance to Pyricularia oryzae.