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二咖啡酰基丁醚和环烯醚萜苷二元混合物协同作用和加和性,来源于对 NF-κB/AP-1 抑制活性的抑制作用。

Synergism and Subadditivity of Verbascoside-Lignans and -Iridoids Binary Mixtures Isolated from Benth. on NF-κB/AP-1 Inhibition Activity.

机构信息

Centro de Desarrollo de Productos Bióticos, Instituto Politécnico Nacional, Yautepec, Morelos 62731, Mexico.

Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social, Xochitepec, Morelos 62790, Mexico.

出版信息

Molecules. 2021 Jan 21;26(3):547. doi: 10.3390/molecules26030547.

Abstract

Pharmacodynamic interactions between plant isolated compounds are important to understand the mode of action of an herbal extract to formulate or create better standardized extracts, phytomedicines, or phytopharmaceuticals. In this work, we propose binary mixtures using a leader compound to found pharmacodynamic interactions in inhibition of the NF-κB/AP-1 pathway using RAW-Blue™ cells. Eight compounds were isolated from , four were new furofuran-type lignans for the species magnolin, eudesmin, sesamin, and kobusin. Magnolin (60.97%) was the most effective lignan inhibiting the NF-κB/AP-1 pathway, followed by eudesmin (56.82%), tenuifloroside (52.91%), sesamin (52.63%), and kobusin (45.45%). Verbascoside, a major compound contained in wild showed an inhibitory effect on NF-κB/AP-1. This polyphenol was chosen as a leader compound for binary mixtures. Verbacoside-aucubin and verbascoside-kobusin produced synergism, while verbascoside-tenuifloroside had subadditivity in all concentrations. Verbascoside-kobusin is a promising mixture to use on NF-κB/AP-1 related diseases and anti-inflammatory -based phytomedicines.

摘要

植物中分离化合物的药效学相互作用对于理解草药提取物的作用方式非常重要,这样可以用来制定或创造更好的标准化提取物、植物药或植物药制剂。在这项工作中,我们使用先导化合物提出二元混合物,以使用 RAW-Blue™细胞发现 NF-κB/AP-1 通路抑制中的药效学相互作用。从 中分离出 8 种化合物,其中 4 种是新的呋喃型木脂素,分别为木兰脂素、木香烃内酯、芝麻素和柯巴素。木兰脂素(60.97%)是抑制 NF-κB/AP-1 通路最有效的木脂素,其次是木香烃内酯(56.82%)、特女贞苷(52.91%)、芝麻素(52.63%)和柯巴素(45.45%)。桃叶珊瑚苷,一种 中含有的主要化合物,对 NF-κB/AP-1 具有抑制作用。该多酚被选为二元混合物的先导化合物。桃叶珊瑚苷-桃叶珊瑚苷和桃叶珊瑚苷-柯巴素在所有浓度下均表现出协同作用,而桃叶珊瑚苷-特女贞苷则表现出相加作用。桃叶珊瑚苷-柯巴素是一种有前途的混合物,可用于治疗与 NF-κB/AP-1 相关的疾病和抗炎植物药。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55bb/7865359/dfb8632d6dd7/molecules-26-00547-g001a.jpg

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