Lin Ping, Tian Chuan, Peng Xiao-Ping, Lou Hong-Xiang, Li Gang
Department of Natural Medicinal Chemistry and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao 266071, People's Republic of China.
Department of Natural Medicinal Chemistry and Pharmacognosy, School of Pharmacy, Qingdao University, Qingdao 266071, People's Republic of China; Department of Natural Product Chemistry, Key Laboratory of Chemical Biology of Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, People's Republic of China.
Steroids. 2023 Apr;192:109188. doi: 10.1016/j.steroids.2023.109188. Epub 2023 Feb 2.
In our process of studying fusidane-type antibiotics, metabolomics-guided chemical investigation on the endophytic Acremonium pilosum F47 led to the isolation of two unique heterodimers, acremonidiols B and C (1 and 2) consisting of a fusidane-type triterpenoid motif and a steroid unit. Four biosynthetically related known natural products including fusidic acid (FA, 3), as well as ergosterol derivatives (4-6) were also obtained. Their structures were determined by the analyses of ESI-HRMS and NMR data. Compounds 1 and 2, as hybrid molecules comprising the fusidane triterpenoid and steroid, are rare in nature. Compared with the clinically used antibiotic FA (3), new compounds 1 and 2 showed no obvious antibiotic activity, indicating the importance of free C-21 carboxyl group for antibacterial activity.
在我们对夫西烷型抗生素的研究过程中，通过代谢组学引导的内生毛枝顶孢霉F47化学研究，分离出了两种独特的杂二聚体，即由夫西烷型三萜基序和甾体单元组成的顶孢二醇B和C（1和2）。还获得了四种生物合成相关的已知天然产物，包括夫西地酸（FA，3）以及麦角甾醇衍生物（4 - 6）。通过电喷雾高分辨质谱（ESI - HRMS）和核磁共振（NMR）数据分析确定了它们的结构。化合物1和2作为包含夫西烷三萜和甾体的杂合分子，在自然界中很罕见。与临床使用的抗生素FA（3）相比，新化合物1和2没有显示出明显的抗生素活性，这表明游离的C - 21羧基对抗菌活性的重要性。
