土曲霉内酯S，一种从内生真菌土曲霉中分离得到的新型抗利什曼原虫丁烯内酯。
Terrenolide S, a new antileishmanial butenolide from the endophytic fungus Aspergillus terreus.
作者信息
Elkhayat Ehab S, Ibrahim Sabrin R M, Mohamed Gamal A, Ross Samir A
机构信息
a Faculty of Pharmacy, Department of Pharmacognosy , Al-Azhar University, Assiut Branch , Assiut , Egypt.
b Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy , Taibah University , Al Madinah Al Munawwarah , Saudi Arabia.
出版信息
Nat Prod Res. 2016;30(7):814-20. doi: 10.1080/14786419.2015.1072711. Epub 2015 Aug 24.
Terrenolide S, a new butenolide derivative (6), together with six known compounds: (22E,24R)-stigmasta-5,7,22-trien-3-β-ol (1), stigmast-4-ene-3-one (2), stigmasta-4,6,8(14),22-tetraen-3-one (3), terretonin A (4), terretonin (5) and butyrolactone VI (7) have been isolated from the endophytic fungus Aspergillus terreus isolated from the roots of Carthamus lanatus (Asteraceae). Their structures were established by extensive spectroscopic analyses (1D, 2D NMR and HRESIMS), as well as optical rotation measurement and comparison with literature data. Compound 1 displayed a potent activity towards methicillin-resistant Staphylococcus aureus (MRSA) and Cryptococcus neoformans with IC50 values of 2.29 and 10.68 µM, respectively. Moreover, 1, 2 and 6 exhibited antileishmanial activity towards Leishmania donovani with IC50 values of 11.24, 15.32 and 27.27 µM, respectively and IC90 values of 14.68, 40.56 and 167.03 µM, respectively.
从菊科植物刺苞菜蓟根部分离得到的内生真菌土曲霉中，分离出了一种新的丁烯内酯衍生物——特雷诺内酯S（6），以及六种已知化合物：（22E，24R）-豆甾-5，7，22-三烯-3-β-醇（1）、豆甾-4-烯-3-酮（2）、豆甾-4，6，8（14），22-四烯-3-酮（3）、土曲霉毒素A（4）、土曲霉毒素（5）和丁内酯VI（7）。通过广泛的光谱分析（一维、二维核磁共振和高分辨电喷雾电离质谱）以及旋光度测量，并与文献数据进行比较，确定了它们的结构。化合物1对耐甲氧西林金黄色葡萄球菌（MRSA）和新型隐球菌显示出较强活性，其半数抑制浓度（IC50）值分别为2.29和10.68 μM。此外，化合物1、2和6对杜氏利什曼原虫均表现出抗利什曼活性，其IC50值分别为11.24、15.32和27.27 μM，IC90值分别为14.68、40.56和167.03 μM。
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