期刊
PHYTOTHERAPY RESEARCH
卷 31, 期 10, 页码 1564-1570出版社
WILEY
DOI: 10.1002/ptr.5885
关键词
4,5-Di-O-caffeoylquinic acid; TRPV1; COX-2; Ligularia fischeri (Ledeb) Turcz
资金
- National Research Foundation of Korea [NRF-2017R1A2B2008527]
- Korea Food Research Institute [E0143043494, KFRI-E0143043494]
- National Research Council of Science & Technology (NST), Republic of Korea [E0143043494] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Ligularia fischeri (Ledeb.) Turcz., a perennial plant native to northeastern Asia, has long been used as folk remedies for the alleviation of inflammatory symptoms. We investigated whether the extract of L. fischeri (LFEx) and caffeoylquinic acid (CQA) derivatives, the pharmacologically active ingredients identified from L. fischeri, regulate inflammation via a transient receptor potential vanilloid 1 (TRPV1)-mediated pathway. Changes in intracellular Ca2+ levels to the LFEx and trans-5-O-CQA, 3,4-Di-O-CQA, 3,5-Di-O-CQA, and 4,5-Di-O-CQA were monitored in TRPV1-expressing human embryonic kidney cell HEK 293T. LFEx and 4,5-Di-O-CQA (EC50=69.34 +/- 1.12M) activated TRPV1, and these activations were significantly inhibited by ruthenium red, a general blocker of TRP channels, and capsazepine, a specific antagonist of TRPV1. 4,5-Di-O-CQA has been determined having antiinflammatory effect under hypoxic conditions by detecting the expression of cyclooxygenase-2 (COX-2), a representative inflammatory marker, and cellular migration in human pulmonary epithelial A549 cells. 4,5-Di-O-CQA suppressed COX-2 expression and cell migration, and this inhibition was countered by co-treatment with capsazepine. This study provides evidence that L. fischeri is selective to inflammatory responses via a TRPV1-mediated pathway, and 4,5-Di-O-CQA might play a key role to create these effects. Copyright (C) 2017 John Wiley & Sons, Ltd.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据