scholarly journals Anti-Inflammatory Effects of 5α,8α-Epidioxycholest-6-en-3β-ol, a Steroidal Endoperoxide Isolated from Aplysia depilans, Based on Bioguided Fractionation and NMR Analysis

Marine Drugs ◽  
2019 ◽  
Vol 17 (6) ◽  
pp. 330 ◽  
Author(s):  
Renato B. Pereira ◽  
David M. Pereira ◽  
Carlos Jiménez ◽  
Jaime Rodríguez ◽  
Rosa M. Nieto ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Selective Inhibition ◽  
Nmr Analysis ◽  
Necrosis Factor Alpha ◽  
Diverse Range ◽  
Protein Levels ◽  
Factor Alpha ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Oxide Synthase

Sea hares of Aplysia genus are recognized as a source of a diverse range of metabolites. 5α,8α-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 5α,8α-epidioxycholest-6-en-3β-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-α) 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.

scholarly journals Caulerpa Cupressoides Var. Flabellata

Marine Drugs ◽  
2019 ◽  
Vol 17 (2) ◽  
pp. 105 ◽  
Author(s):  
Jefferson Da Silva Barbosa ◽  
Mariana Santana Santos Pereira Costa ◽  
Luciana Fentanes Moura De Melo ◽  
Mayara Jane Campos De Medeiros ◽  
Daniel De Lima Pontes ◽  
...  
Keyword(s):  
Gene Expression ◽  
Nitric Oxide ◽  
Sulfated Polysaccharides ◽  
Immunostimulatory Activity ◽  
Necrosis Factor Alpha ◽  
Raw 264.7 Macrophages ◽  
Tnf Α ◽  
Factor Alpha ◽  
Cox 2 ◽  
Oxide Synthase

Green seaweeds are rich sources of sulfated polysaccharides (SPs) with potential biomedical and nutraceutical applications. The aim of this work was to evaluate the immunostimulatory activity of SPs from the seaweed, Caulerpa cupressoides var. flabellata on murine RAW 264.7 macrophages. SPs were evaluated for their ability to modify cell viability and to stimulate the production of inflammatory mediators, such as nitric oxide (NO), intracellular reactive oxygen species (ROS), and cytokines. Additionally, their effect on inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) gene expression was investigated. The results showed that SPs were not cytotoxic and were able to increase in the production of NO, ROS and the cytokines, tumor necrosis factor alpha (TNF-α) and interleukin 6 (IL-6). It was also observed that treatment with SPs increased iNOS and COX-2 gene expression. Together, these results indicate that C. cupressoides var. flabellata SPs have strong immunostimulatory activity, with potential biomedical applications.

scholarly journals Higenamine inhibits IL-1β-induced inflammation in human nucleus pulposus cells

2019 ◽  
Vol 39 (6) ◽  
Author(s):  
Xiaoliang Bai ◽  
Wenyuan Ding ◽  
Sidong Yang ◽  
Xiaohui Guo
Keyword(s):  
Nitric Oxide ◽  
Signaling Pathway ◽  
Nucleus Pulposus ◽  
Inflammatory Activity ◽  
Nucleus Pulposus Cells ◽  
Necrosis Factor Alpha ◽  
Natural Progression ◽  
Anti Inflammatory ◽  
Inflammatory Molecules ◽  
Oxide Synthase

Abstract Intervertebral disc degeneration (IDD) is a natural progression of the aging process associated with inflammation. Higenamine, a plant-based alkaloid, has been identified to possess various pharmacological properties, including anti-inflammatory activity. In the present study, we aimed to evaluate the role of higenamine in interleukin (IL)-1β-induced inflammation in human nucleus pulposus cells (NPCs). The results showed that higenamine improved cell viability in IL-1β-induced NPCs. The IL-1β-dependent up-regulation of inflammatory molecules including inducible nitric oxide synthase (iNOS), nitric oxide (NO), prostaglandin E2 (PGE2), cyclooxygenase-2 (COX-2), tumor necrosis factor alpha (TNF-α), and IL-6 was attenuated by higenamine in NPCs. The increased productions of matrix metalloproteinases (MMP-3 and MMP-13), as well as a disintegrin and metalloprotease with thrombospondin motifs (ADAMTS-4 and ADAMTS-5) were significantly mitigated by higenamine treatment. Furthermore, we also found that higenamine suppressed the IL-1β-induced activation of NF-κB signaling pathway in NPCs. In conclusion, the present study proved that higenamine exhibited anti-inflammatory activity against IL-1β-induced inflammation in NPCs via inhibiting NF-κB signaling pathway. These results suggested that higenamine might be a therapeutic agent for the treatment of IDD.

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