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