Simplicilones A and B Isolated from the Endophytic Fungus Simplicillium subtropicum SPC3.

Simplicilones A and B Isolated from the Endophytic Fungus Simplicillium subtropicum SPC3.
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DOI:
10.3390/antibiotics9110753
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发表时间:
2020-10-29
期刊:
Antibiotics (Basel, Switzerland)
影响因子:
--
通讯作者:
Surup F
Surup F
中科院分区:
其他
文献类型:
--
作者:
Anoumedem EGM;Mountessou BYG;Kouam SF;Narmani A;Surup F

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在我们筛选新的生物活性次生代谢物的过程中,从内生真菌亚热带辛普利菌 (SPC3) 的肉汤培养物中分离出两种具有螺中心的新四环聚酮化合物,辛普利酮 A (1) 和 B (2)。这种内生真菌天然存在于喀麦隆药用植物 Duguetia staudtii (Engl. and Diels) Chatrou 的新鲜树皮中。通过 MS 和 1D 以及 2D NMR 光谱技术阐明了 simplicilones 的平面结构。相对构型由 NOESY 实验结合耦合常数确定;随后,通过修改后的Mosher方法分配绝对构型。这些化合物对细胞系 KB3.1 显示出较弱的细胞毒性作用(体外细胞毒性 (IC50) = 1 为 25 µg/mL,2 为 29 µg/mL),但对测试的革兰氏阳性和革兰氏阴性细菌以及真菌没有活性。
Two new tetracyclic polyketides with a spirocenter, simplicilones A (1) and B (2) were isolated from the broth-culture of the endophytic fungus Simplicillium subtropicum (SPC3) in the course of our screening for new bioactive secondary metabolites. This endophytoic fungus is naturally harboured in the fresh bark of the Cameroonian medicinal plant Duguetia staudtii (Engl. and Diels) Chatrou. The planar structures of the simplicilones were elucidated by MS and 1D as well as 2D NMR spectroscopic techniques. The relative configuration was assigned by NOESY experiments in conjunction with coupling constants; subsequently, the absolute configurations were assigned by the modified Mosher’s method. The compounds showed weak cytotoxic effects against the cell line KB3.1 (in vitro cytotoxicity (IC50) = 25 µg/mL for 1, 29 µg/mL for 2), but were inactive against the tested Gram-positive and Gram-negative bacteria as well as fungi.
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