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来自三尖杉内生真菌——炭角菌属CFL5的细胞松弛素

Cytochalasins from Xylaria sp. CFL5, an Endophytic Fungus of Cephalotaxus fortunei.

作者信息

Ma Kai-Liang, Dong Shi-Hui, Li Hang-Ying, Wei Wen-Jun, Tu Yong-Qiang, Gao Kun

机构信息

State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China.

出版信息

Nat Prod Bioprospect. 2021 Feb;11(1):87-98. doi: 10.1007/s13659-020-00279-5. Epub 2020 Nov 4.

DOI:10.1007/s13659-020-00279-5
PMID:33146865
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7933320/
Abstract

Three previously undescribed cytochalasins, named xylariasins A‒C (1‒3), together with six known ones (4‒9) were isolated from Xylaria sp. CFL5, an endophytic fungus of Cephalotaxus fortunei. The chemical structures of all new compounds were elucidated on the basis of extensive spectroscopic data analyses and electronic circular dichroism calculation, as well as optical rotation calculation. Biological activities of compounds 1, 4‒9 were evaluated, including cytotoxic, LAG3/MHC II binding inhibition and LAG3/FGL1 binding inhibition activities. Compounds 6 and 9 possessed cytotoxicity against AGS cells at 5 μM, with inhibition rates of 94% and 64%, respectively. In addition, all tested isolates, except compound 6, exhibited obvious inhibitory activity against the interaction of both LAG3/MHC II and LAG3/FGL1. Compounds 1, 5, 7, and 8 inhibited LAG3/MHC II with IC values ranging from 2.37 to 4.74 μM. Meanwhile, the IC values of compounds 1, 7, and 8 against LAG3/FGL1 were 11.78, 4.39, and 7.45 μM, respectively.

摘要

从三尖杉内生真菌Xylaria sp. CFL5中分离出三种以前未描述过的细胞松弛素，命名为木层孔菌素A‒C（1‒3），以及六种已知的细胞松弛素（4‒9）。所有新化合物的化学结构均通过广泛的光谱数据分析、电子圆二色性计算以及旋光计算得以阐明。对化合物1、4‒9的生物活性进行了评估，包括细胞毒性、LAG3/MHC II结合抑制和LAG3/FGL1结合抑制活性。化合物6和9在5 μM浓度下对AGS细胞具有细胞毒性，抑制率分别为94%和64%。此外，除化合物6外，所有测试的分离物对LAG3/MHC II和LAG3/FGL1的相互作用均表现出明显的抑制活性。化合物1、5、7和8对LAG3/MHC II的抑制IC值范围为2.37至4.74 μM。同时，化合物1、7和8对LAG3/FGL1的IC值分别为11.78、4.39和7.45 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/7cc8ba0c949d/13659_2020_279_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/fb3362256200/13659_2020_279_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/563d0e545081/13659_2020_279_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/8c525b709fb3/13659_2020_279_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/ff3b80dd1569/13659_2020_279_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/b263f0a455e0/13659_2020_279_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/ae64b270852a/13659_2020_279_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/84778da509b0/13659_2020_279_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/7cc8ba0c949d/13659_2020_279_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/fb3362256200/13659_2020_279_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/563d0e545081/13659_2020_279_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/8c525b709fb3/13659_2020_279_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/ff3b80dd1569/13659_2020_279_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/b263f0a455e0/13659_2020_279_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/ae64b270852a/13659_2020_279_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/84778da509b0/13659_2020_279_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/89b8/7933320/7cc8ba0c949d/13659_2020_279_Fig8_HTML.jpg

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