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New cytotoxic natural products from the marine sponge-derived fungus Pestalotiopsis sp. by epigenetic modification

机译:来自海绵衍生的真菌植物的新细胞毒性天然产物。通过表观遗传修饰

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摘要

Four new polyketide derivatives, pestalotiopols A–D ( 1–4 ), together with seven known compounds ( 5–11 ), were isolated from a chemical-epigenetic culture of Pestalotiopsis sp. The structures and absolute configurations of the new compounds ( 1–4 ) were determined by spectroscopic analyses, Mo _(2) -induced CD, and electronic circular dichroism (ECD) calculations. All the isolated compounds ( 1–11 ) were tested for their cytotoxic activities. Among these compounds, compounds 1 , 2 , 6 and 7 exhibited cytotoxicity against four human cancer cell lines with IC _(50) values of 16.5–56.5 μM. The structure–activity relationships of compounds ( 1–11 ) were examined. The results indicated that both the diol system of the side chain and the aldehyde group might contribute to the cytotoxic activity. The possible biosynthetic pathways for compounds ( 1–4 ) were also postulated.
机译:四种新的聚酮化合物A-D(1-4)与七种已知化合物(5-11)一起分离出四种新的聚酮衍生物,与Pestalotiopsis sp的化学 - 表观培养物中分离出来。通过光谱分析,Mo _(2)诱导的CD和电子圆形二色性(ECD)计算来确定新化合物(1-4)的结构和绝对构型。所有分离的化合物(1-11)被检测其细胞毒性活性。在这些化合物中,化合物1,2,6和7表现出对四种人癌细胞系的细胞毒性,IC _(50)值为16.5-56.5μm。检查化合物(1-11)的结构 - 活性关系。结果表明,侧链和醛基的二醇体系都可能有助于细胞毒性活性。还假定化合物(1-4)的可能的生物合成途径。

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