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来源于内生真菌 的玉红菇衍生物对结直肠癌细胞的体外抗增殖活性。

In Vitro Antiproliferative Activity of Echinulin Derivatives from Endolichenic Fungus sp. against Colorectal Cancer.

机构信息

LABCiS, UR 22722, Faculté de Pharmacie, Univ. Limoges, F-87000 Limoges, France.

Univ. Limoges, CNRS, Inserm, CHU Limoges, BISCEm, UAR 2015, US 42, F-87025 Limoges, France.

出版信息

Molecules. 2024 Aug 30;29(17):4117. doi: 10.3390/molecules29174117.

Abstract

The endolichenic fungus sp. was isolated from the lichen harvested in France. sp. was grown on a solid culture medium to ensure the large-scale production of the fungus with a sufficient mass of secondary metabolites. The molecular network analysis of extracts and subfractions enabled the annotation of 22 molecules, guiding the purification process. The EtOAc extract displayed an antiproliferative activity of 3.2 ± 0.4 µg/mL at 48 h against human colorectal cancer cells (HT-29) and no toxicity at 30 µg/mL against human triple-negative breast cancer (TNBC) cells (MDA-MB-231) and human embryonic kidney (HEK293) non-cancerous cells. Among the five prenylated compounds isolated, of which four are echinulin derivatives, compounds and showed the most important activity, with IC values of 1.73 µM and 8.8 µM, respectively, against HT-29 cells.

摘要

从法国采集的地衣中分离出内生真菌 sp.。 sp. 在固体培养基上生长,以确保大规模生产具有足够质量的次生代谢产物的真菌。提取物和亚组分的分子网络分析使 22 种分子得以注释,指导了其分离过程。在 48 小时内,乙酸乙酯提取物对人结直肠癌细胞(HT-29)的增殖活性为 3.2±0.4μg/mL,在 30μg/mL 时对人三阴性乳腺癌(TNBC)细胞(MDA-MB-231)和人胚肾(HEK293)非癌细胞没有毒性。分离出的五种倍半萜化合物中,有四种是玉红菇素衍生物,化合物 和 表现出最重要的活性,对 HT-29 细胞的 IC 值分别为 1.73μM 和 8.8μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/09f1/11397142/9ccbf99e9ad3/molecules-29-04117-g001.jpg

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