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从台湾柳珊瑚Briareum excavatum的培养型中分离出的海洋来源化合物Excavatolide B的抗炎和镇痛作用

Anti-Inflammatory and Analgesic Effects of the Marine-Derived Compound Excavatolide B Isolated from the Culture-Type Formosan Gorgonian Briareum excavatum.

作者信息

Lin Yen-You, Lin Sung-Chun, Feng Chien-Wei, Chen Pei-Chin, Su Yin-Di, Li Chi-Min, Yang San-Nan, Jean Yen-Hsuan, Sung Ping-Jyun, Duh Chang-Yih, Wen Zhi-Hong

机构信息

Department of Marine Biotechnology and Resources, Asia-Pacific Ocean Research Center, National Sun Yat-sen University, Kaohsiung 80424, Taiwan.

Department of Orthopaedic Surgery, Ping-Tung Christian Hospital, Ping-Tung 90059, Taiwan.

出版信息

Mar Drugs. 2015 Apr 27;13(5):2559-79. doi: 10.3390/md13052559.

DOI:10.3390/md13052559
PMID:25923315
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4446594/
Abstract

In recent years, several marine-derived compounds have been clinically evaluated. Diterpenes are secondary metabolites from soft coral that exhibit anti-inflammatory, anti-tumor and cytotoxic activities. In the present study, we isolated a natural diterpene product, excavatolide B, from cultured Formosan gorgonian Briareum excavatum and investigated its anti-inflammatory activities. We found that excavatolide B significantly inhibited the mRNA expression of the proinflammatory mediators, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), in lipopolysaccharide (LPS)-challenged murine macrophages (RAW 264.7). We also examined the anti-inflammatory and anti-nociceptive effects of excavatolide B on intraplantar carrageenan-induced inflammatory responses. Excavatolide B was found to significantly attenuate carrageenan-induced nociceptive behaviors, mechanical allodynia, thermal hyperalgesia, weight bearing deficits and paw edema. In addition, excavatolide B inhibited iNOS, as well as the infiltration of immune cells in carrageenan-induced inflammatory paw tissue.

摘要

近年来，几种海洋来源的化合物已进行了临床评估。二萜类化合物是软珊瑚产生的次生代谢产物，具有抗炎、抗肿瘤和细胞毒性活性。在本研究中，我们从养殖的台湾柳珊瑚Briareum excavatum中分离出一种天然二萜产物——掘扁柳珊瑚内酯B，并研究了其抗炎活性。我们发现，掘扁柳珊瑚内酯B能显著抑制脂多糖（LPS）刺激的小鼠巨噬细胞（RAW 264.7）中促炎介质诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）的mRNA表达。我们还研究了掘扁柳珊瑚内酯B对角叉菜胶诱导的足底内炎症反应的抗炎和抗伤害感受作用。结果发现，掘扁柳珊瑚内酯B能显著减轻角叉菜胶诱导的伤害感受行为、机械性异常性疼痛、热痛觉过敏、负重缺陷和爪肿胀。此外，掘扁柳珊瑚内酯B抑制了角叉菜胶诱导的炎症爪组织中的iNOS以及免疫细胞浸润。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/860d480ef71e/marinedrugs-13-02559-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/9caaedd753b7/marinedrugs-13-02559-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/151368b1b400/marinedrugs-13-02559-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/7e01c2627447/marinedrugs-13-02559-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/5d679b266abe/marinedrugs-13-02559-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/b66c6541b5f8/marinedrugs-13-02559-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/860d480ef71e/marinedrugs-13-02559-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/9caaedd753b7/marinedrugs-13-02559-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/151368b1b400/marinedrugs-13-02559-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/7e01c2627447/marinedrugs-13-02559-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/5d679b266abe/marinedrugs-13-02559-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/b66c6541b5f8/marinedrugs-13-02559-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba56/4446594/860d480ef71e/marinedrugs-13-02559-g006.jpg

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