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专利菌丝体的乙醇提取物:具有抗增殖活性的生物活性化合物来源及潜在的PPAR-γ天然配体

Ethanolic Extract of Pat. Mycelium: A Source of Bioactive Compounds with Antiproliferative Activity and Potential PPAR-γ Natural Ligands.

作者信息

Angulo-Sanchez Lucia T, Vidal-Gutiérrez Max, Torres-Moreno Heriberto, Esqueda Martín, Gutiérrez Aldo, Vargas Georgina, Monribot-Villanueva Juan Luis, Guerrero-Analco José A, Muñoz-Bacasehua César, Robles-Zepeda Ramón Enrique

机构信息

Centro de Investigación en Alimentación y Desarrollo, A.C. Carretera Gustavo Enrique Astiazarán Rosas 46, La Victoria, Hermosillo 83304, Sonora, Mexico.

Departamento de Ciencias Químico, Biológicas y Agropecuarias, Campus Navojoa, Universidad de Sonora, Lázaro Cárdenas del Río 100, Francisco Villa, Navojoa 85880, Sonora, Mexico.

出版信息

Pharmaceuticals (Basel). 2025 Jun 18;18(6):909. doi: 10.3390/ph18060909.

Abstract

spp. have long been studied for their bioactive pharmacological properties, and their biomass and extracts have been obtained from various sources. This study adopts a novel approach: enriching a liquid culture of with a vineyard pruning waste extract to identify bioactive compounds with antiproliferative activity through enriched chromatographic fractions. The ethanolic extract from a mycelial culture was separated following a partitioning process, and the hexane fraction was subsequently separated in a chromatographic column. The fractions were evaluated for their antiproliferative properties against cancer cell lines. The interactions of the molecules identified with peroxisome proliferator-activated receptor gamma (PPAR-γ) were analyzed via molecular docking. Three chromatographic fractions (FH11-FH13) exhibited antiproliferative activity which was significantly more effective against non-small lung cancer cells (A549). The cells treated with the crude extract and fractions presented a balloon-like morphology. A chemical analysis of the active fractions allowed us to identify four compounds: one fatty acid (9-Hydroxy-10E,12Z-octadecadienoic acid) and three triterpenes (ganoderic acids DM, TQ, and X). These compounds showed interactions with the PPAR-γ receptor through molecular docking. : is a promising source of compounds with antiproliferative activity that could serve as natural ligands for PPAR-γ and has possible applications in lung cancer therapy.

摘要

长期以来,人们一直在研究葡萄孢属的生物活性药理特性,并且已经从各种来源获得了它们的生物质和提取物。本研究采用了一种新方法:用葡萄园修剪废料提取物富集葡萄孢属的液体培养物,以通过富集的色谱馏分鉴定具有抗增殖活性的生物活性化合物。对菌丝体培养物的乙醇提取物进行分配分离,随后在色谱柱中分离己烷馏分。评估这些馏分对癌细胞系的抗增殖特性。通过分子对接分析鉴定出的分子与过氧化物酶体增殖物激活受体γ(PPAR-γ)的相互作用。三个色谱馏分(FH11 - FH13)表现出抗增殖活性,对非小细胞肺癌细胞(A549)的作用明显更有效。用粗提取物和馏分处理的细胞呈现出气球样形态。对活性馏分的化学分析使我们鉴定出四种化合物:一种脂肪酸(9-羟基-10E,12Z-十八碳二烯酸)和三种三萜(灵芝酸DM、TQ和X)。这些化合物通过分子对接显示出与PPAR-γ受体的相互作用。葡萄孢属是具有抗增殖活性的化合物的一个有前景的来源,这些化合物可以作为PPAR-γ的天然配体,并且在肺癌治疗中可能有应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5bf9/12195858/4380c5e17cf7/pharmaceuticals-18-00909-g001.jpg

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