Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Mar Drugs. 2022 May 31;20(6):375. doi: 10.3390/md20060375.
Five novel tyrosine-decahydrofluorene analogues, xenoacremones D−H (1−5), each bearing a fused 6/5/6 tricarbocyclic core and a 13-membered para-cyclophane ring system, were isolated from the endophytic fungus Xenoacremonium sinensis. Compound 1 was a novel polyketide synthase−nonribosomal peptide synthetase (PKS−NRPS) tyrosine-decahydrofluorene hybrid containing a 6/5/6/6/5 ring system. Their structures were elucidated from comprehensive spectroscopic analysis and electronic circular dichroism (ECD) calculations. All compounds were evaluated for their inhibitory activities on LPS-induced NO production in macrophages and their cytotoxicities against the NB4 and U937 cell lines. Compounds 3 and 5 exhibited potent anti-inflammatory activities in vitro. Compounds 1 and 3−5 displayed significant antiproliferative activity against the tumor cell lines (IC50 < 20 µM).
从内生真菌中华地霉菌中分离得到了 5 种新型的酪氨酸-十氢芴类似物，分别为 xenocremones D-H（1-5），它们均具有融合的 6/5/6 三环骨架和 13 元对环芳烷环系。化合物 1 是一种新型的聚酮合酶-非核糖体肽合酶（PKS-NRPS）酪氨酸-十氢芴杂合体，含有 6/5/6/6/5 环系统。通过全面的光谱分析和电子圆二色性（ECD）计算确定了它们的结构。所有化合物均评估了其对 LPS 诱导的巨噬细胞中 NO 产生的抑制活性以及对 NB4 和 U937 细胞系的细胞毒性。化合物 3 和 5 在体外表现出很强的抗炎活性。化合物 1 和 3-5 对肿瘤细胞系显示出显著的增殖抑制活性（IC50<20 μM）。
