Abstract

The peel of Trichosanthes kirilowii Maxim is clinically used to treat cardiovascular diseases in China. In this study, the NF-κB inhibitory activity of the peel of T. kirilowii Maxim extracts was determined by Dual-Luciferase Reporter Assay System, and the results showed 70% ethanol extract could significantly inhibit the activation of NF-κB (p < 0.001). Further, 21 compounds were isolated from 70% ethanol extract. One new compound, namely (2 R)-(2-amino-2-hydroxymethyl-3-[(4-hydroxy-3-methoxybenzoyl)-O-]-propanoic acid (1), and 20 known compounds were elucidated by comprehensive spectroscopic analyses. The isolated compounds were tested in the anti-inflammatory assay, and the results indicated compounds 5, 8, 11, 14, 15, 17 and 21 could inhibit the activation of NF-κB (p <0 .05, p < 0.001) at concentration of 1 μM.

摘要

在我国，天竺葵果皮在临床上用于治疗心血管疾病。本研究采用 Dual-Luciferase Reporter Assay System 测定桐木提取物果皮对 NF-κB 的抑制活性，结果显示 70% 乙醇提取物可显着抑制 NF-κB 的活化（p  < 0.001 ）。此外，从 70% 的乙醇提取物中分离出 21 种化合物。一种新化合物，即 (2  R )-(2-amino-2-hydroxymethyl-3-[(4-hydroxy-3-methoxybenzoyl) -O -]-propanoic acid ( 1)，并通过综合光谱分析阐明了 20 种已知化合物。将分离的化合物中的抗炎测定中测试，结果表明化合物5，8，11，14，15，17和21可以抑制NF-κB的活化（p  <0 0.05，p  <0.001）在浓度为 1 μM。