期刊
MARINE DRUGS
卷 17, 期 6, 页码 -出版社
MDPI
DOI: 10.3390/md17060330
关键词
Aplysia depilans; 5 alpha; 8 alpha-epidioxycholest-6-en-3 beta-ol; iNOS; COX-1; COX-2; IL-6; TNF-alpha
资金
- FCT/MCTES through national funds [UID/QUI/50006/2019]
- [PD/BD/113565/2015]
- Fundação para a Ciência e a Tecnologia [PD/BD/113565/2015] Funding Source: FCT
Sea hares of Aplysia genus are recognized as a source of a diverse range of metabolites. 5 alpha ,8 alpha -Endoperoxides belong to a group of oxidized sterols commonly found in marine organisms and display several bioactivities, including antimicrobial, anti-tumor, and immunomodulatory properties. Herein we report the isolation of 5 alpha ,8 alpha -epidioxycholest-6-en-3 beta -ol (EnP(5,8)) from Aplysia depilans Gmelin, based on bioguided fractionation and nuclear magnetic resonance (NMR) analysis, as well as the first disclosure of its anti-inflammatory properties. EnP(5,8) revealed capacity to decrease cellular nitric oxide (NO) levels in RAW 264.7 macrophages treated with lipopolysaccharide (LPS) by downregulation of the Nos2 (inducible nitric oxide synthase, iNOS) gene. Moreover, EnP(5,8) also inhibited the LPS-induced expression of cyclooxygenase-2 (COX-2), interleukin 6 (IL-6), and tumor necrosis factor alpha (TNF-alpha) at the mRNA and protein levels. Mild selective inhibition of COX-2 enzyme activity was also evidenced. Our findings provide evidence of EnP(5,8) as a potential lead drug molecule for the development of new anti-inflammatory agents.
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