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从……中分离出的未折叠蛋白反应的呫吨酮抑制剂

Xanthone Inhibitors of Unfolded Protein Response Isolated from .

作者信息

Chambaud Marine, Le Ray Anne-Marie, Hamzi Racha, Charpentier Thomas, Blon Nadège, Bréard Dimitri, Le Pogam Pierre, Litaudon Marc, Dumontet Vincent, Bataillé-Simoneau Nelly, Guillemette Thomas, Simoneau Philippe, Schinkovitz Andreas, Guilet David, Viault Guillaume, Richomme Pascal

机构信息

SONAS | Substances d'Origine Naturelle et Analogues Structuraux Univ Angers, SONAS, SFR QUASAV, F-49000 Angers, France.

BioCIS | Biomolécules: conception, isolement, synthèse, CNRS, UMR 8076, Université Paris-Saclay, 91400 Orsay, France.

出版信息

J Nat Prod. 2024 Jun 28;87(6):1628-1634. doi: 10.1021/acs.jnatprod.4c00328. Epub 2024 Jun 13.

DOI:10.1021/acs.jnatprod.4c00328
PMID:38869194
Abstract

The unfolded protein response (UPR) is a key component of fungal virulence. The prenylated xanthone γ-mangostin isolated from (Clusiaceae) fruit pericarp, has recently been described to inhibit this fungal adaptative pathway. Considering that (Calophyllaceae) is known for its high prenylated xanthone content, its stem bark extract was fractionated using a bioassay-guided procedure based on the cell-based anti-UPR assay. Four previously undescribed xanthone derivatives were isolated, caledonixanthones N-Q (, , , and ), among which compounds and showed promising anti-UPR activities with IC values of 11.7 ± 0.9 and 7.9 ± 0.3 μM, respectively.

摘要

未折叠蛋白反应(UPR)是真菌毒力的关键组成部分。最近有研究表明,从藤黄科植物果实果皮中分离出的异戊烯基化氧杂蒽酮γ-山竹黄酮可抑制这种真菌适应性途径。鉴于红厚壳科植物以其高含量的异戊烯基化氧杂蒽酮而闻名,因此采用基于细胞的抗UPR检测的生物测定指导方法对其茎皮提取物进行了分级分离。分离出了四种先前未描述的氧杂蒽酮衍生物,即喀里多尼亚氧杂蒽酮N-Q(、、和),其中化合物和表现出有前景的抗UPR活性,IC值分别为11.7±0.9和7.9±0.3μM。

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