PDF(Pubmed)
Abstract：
Chemical epigenetic cultivation of the sponge-derived fungus Pestalotiopsis sp. SWMU-WZ04-1 contributed to the identification of twelve polyketide derivatives, including six new pestalotiopols E-J (1-6) and six known analogues (7-12). Their gross structures were deduced from 1D/2D NMR and HRESIMS spectroscopic data, and their absolute configurations were further established by circular dichroism (CD) Cotton effects and the modified Mosher\'s method. In the bioassay, the cytotoxic and antibacterial activities of all compounds were evaluated. Chlorinated benzophenone derivatives 7 and 8 exhibited inhibitory effects on Staphylococcus aureus and Bacillus subtilis, with MIC values varying from 3.0 to 50 μg/mL. In addition, these two compounds were cytotoxic to four types of human cancer cells, with IC50 values of 16.2~83.6 μM. The result showed that compound 7 had the probability of being developed into a lead drug with antibacterial ability.
摘要：
海绵来源的真菌Pestalotiopsissp。的化学表观遗传培养。SWMU-WZ04-1有助于鉴定十二种聚酮衍生物，包括六个新的pestalotiopolE-J（1-6）和六个已知的类似物（7-12）。它们的总体结构是从1D/2DNMR和HRESIMS光谱数据推导出来的，通过圆二色性（CD）棉花效应和改良的Mosher方法进一步确定了它们的绝对构型。在生物测定中，评估了所有化合物的细胞毒性和抗菌活性。氯化二苯甲酮衍生物7和8对金黄色葡萄球菌和枯草芽孢杆菌具有抑制作用，MIC值在3.0至50μg/mL之间变化。此外,这两种化合物对四种人类癌细胞有细胞毒性，IC50值为16.2~83.6μM。结果表明，化合物7有可能发展成为具有抗菌能力的先导药物。
