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从 L. 中提取的抗炎成分:一种基于生物测定的分级分离研究。

Anti-Inflammatory Principles from L.: A Bioassay-Guided Fractionation Study.

机构信息

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.

Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Kom 32511, Egypt.

出版信息

Molecules. 2020 Jun 30;25(13):2994. doi: 10.3390/molecules25132994.

Abstract

Natural products have served as primary remedies since ancient times due to their cultural acceptance and outstanding biodiversity. To investigate whether L. modulates an inflammatory process, we carried out bioassay-guided isolation where the extracts and isolated compounds were tested for their modulatory effects on several inflammatory indicators, such as nitric oxide (NO), reactive oxygen species (ROS), proinflammatory cytokine; tumour necrosis factor (TNF-), as well as the proliferation of the lymphocyte T-cells. The aqueous ethanolic extract of the plant inhibited the intracellular ROS production, NO generation, and T-cell proliferation. The aqueous ethanolic crude extract was partitioned by liquid-liquid fractionation using -hexane (-CH), dichloromethane (DCM), ethyl acetate (EtOAc), -butanol (-BuOH), and water (HO). The DCM and -BuOH extracts showed the highest activity against most inflammatory indicators and were further purified to obtain compounds -. The structures of 3,5-dihydroxy-4',7-dimethoxyflavone () and 3,5-dihydroxy-4-methoxybenzoic acid methyl ester () from the DCM extracts; and kaempferol (), and 3-hydroxy-4-methoxy-()-cinnamic acid () from the -BuOH extract were elucidated by different spectroscopic tools, including MS, NMR, UV, and IR. Compound inhibited the production of ROS and TNF-, whereas compound showed inhibitory activity against all the tested mediators. A better understanding of the potential aspect of L. derivatives as anti-inflammatory agents could open the door for the development of advanced anti-inflammatory entities.

摘要

天然产物因其文化接受度和突出的生物多样性,自古以来一直是主要的治疗药物。为了研究 L. 是否调节炎症过程,我们进行了基于生物测定的分离,其中提取物和分离的化合物被测试对几种炎症指标的调节作用,如一氧化氮 (NO)、活性氧 (ROS)、促炎细胞因子;肿瘤坏死因子 (TNF-),以及淋巴细胞 T 细胞的增殖。植物的水醇提取物抑制细胞内 ROS 的产生、NO 的生成和 T 细胞的增殖。植物的水醇粗提取物通过液-液分馏用正己烷 (-CH)、二氯甲烷 (DCM)、乙酸乙酯 (EtOAc)、正丁醇 (-BuOH) 和水 (HO) 进行分离。DCM 和 -BuOH 提取物对大多数炎症指标显示出最高的活性,并进一步纯化以获得化合物 -。从 DCM 提取物中获得的 3,5-二羟基-4',7-二甲氧基黄酮 () 和 3,5-二羟基-4-甲氧基苯甲酸甲酯 ();以及来自 -BuOH 提取物的山柰酚 (), 和 3-羟基-4-甲氧基-()-肉桂酸 () 通过不同的光谱工具,包括 MS、NMR、UV 和 IR 进行阐明。化合物 抑制 ROS 和 TNF-的产生,而化合物 对所有测试的介质均显示出抑制活性。更好地了解 L. 衍生物作为抗炎剂的潜在方面可能为开发先进的抗炎实体打开大门。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c0cc/7411813/70998df44d7f/molecules-25-02994-g001.jpg

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