桦木醇型三萜类化合物具有人中性粒细胞弹性蛋白酶抑制和抗炎作用。
Iridal-Type Triterpenoids Displaying Human Neutrophil Elastase Inhibition and Anti-Inflammatory Effects from .
机构信息
Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University, Jinju 52828, Korea.
Department of Physiology, College of Medicine and Institute of Health Sciences, Gyeongsang National University, Jinju 52727, Korea.
出版信息
Molecules. 2021 Oct 31;26(21):6602. doi: 10.3390/molecules26216602.
The aim of this study is to explore anti-inflammatory phytochemicals from based on the inhibition of pro-inflammatory enzyme, human neutrophil elastase (HNE) and anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage. Three stereoisomers of iridal-type triterpenoids (-) were isolated from the roots of and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC values of 6.8-27.0 µM. The binding affinity experiment proved that iridal-type triterpenoids had only a single binding site to the HNE enzyme. Among them, isoiridogermanal () and iridobelamal A () displayed significant anti-inflammatory effects by suppressing the expressions of pro-inflammatory cytokines, such as iNOS, IL-1β, and TNF-α through the NF-κB pathway in LPS-stimulated RAW264.7 cells. This is the first report that iridal-type triterpenoids are considered responsible phytochemicals for anti-inflammatory effects of .
本研究旨在基于对促炎酶、人中性粒细胞弹性蛋白酶（HNE）的抑制作用和脂多糖（LPS）刺激的 RAW264.7 巨噬细胞中的抗炎活性，从 中寻找抗炎植物化学物质。从 的根部分离出三种伊达醇型三萜类化合物（-），并通过 NOESY 光谱完全确定其立体化学。这些化合物被证实为可逆的非竞争性 HNE 抑制剂，IC 值为 6.8-27.0 μM。结合亲和力实验证明，伊达醇型三萜类化合物仅与 HNE 酶有一个单一的结合位点。其中，异伊达根烷（）和伊达贝马拉 A（）通过 LPS 刺激的 RAW264.7 细胞中的 NF-κB 通路抑制 iNOS、IL-1β 和 TNF-α 等促炎细胞因子的表达，显示出显著的抗炎作用。这是首次报道伊达醇型三萜类化合物被认为是 的抗炎作用的负责植物化学物质。
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