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FS145 exerts anti-inflammatory and analgesic effects through blocking integrin αvβ3 on macrophages
Jianxi Yang1, Yihan Gao2, Junfang Liu2
1NMPA Key Laboratory for Research and Evaluation of Drug Metabolism & Guangdong Provincial Key Laboratory of New Drug Screening & Guangdong-Hongkong-Macao Joint Laboratory for New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Abstract:
Macrophages exert a crucial role in the initiation and regulation of inflammation, and certain proteins derived from the saliva of blood-feeding arthropods have been proven to have potent anti-inflammatory and analgesic properties by regulating macrophages' functions. We previously identified and characterized FS145, a disintegrin from the saliva of the flea Xenopsylla cheopis, which was demonstrated as an antiangiogenesis factor in vivo and in vitro by specific blockage of the integrin αvβ3 function. Here, we investigated its anti-inflammatory and analgesic effects as well as the molecular mechanism of action of this ectoparasitic peptide. FS145 could bind to RAW264.7 cells at a concentration-dependent manner and significantly attenuate the adhesion of LPS-activated RAW264.7 cells to fibrinogen, fibronectin, and vitronectin but not to laminin. Furthermore, FS145 was shown to inhibit macrophage migration and the production of NO, TNF-α, IL-1β and IL-6 by suppressing MAPK/NF-κB signaling cascades in LPS-induced macrophages. Notably, FS145 was also exhibited the potent anti-inflammatory and anti-nociceptive effects in vivo. These findings suggest that FS145 may exert a therapeutic effect by blocking integrin αvβ3 and suppressing MAPK/NF-κB ing pathways and the subsequent inflammatory response of macrophages. Therefore, FS145 holds promise as a novel anti-inflammatory and analgesic agent, warranting further investigation into its potential clinical applications.
Insights
FS145, a flea saliva protein, reduces inflammation and pain by blocking macrophage activity and key signaling pathways. This peptide shows promise as a novel anti-inflammatory and analgesic therapeutic agent.
Area of Science:
- Immunology
- Pharmacology
- Molecular Biology
Background:
- Macrophages play a key role in inflammation.
- Saliva proteins from blood-feeding arthropods can possess anti-inflammatory properties.
- FS145 is a disintegrin from flea saliva with previously identified antiangiogenesis effects.
Purpose of the Study:
- To investigate the anti-inflammatory and analgesic effects of FS145.
- To elucidate the molecular mechanisms underlying FS145's action.
- To evaluate FS145's therapeutic potential.
Main Methods:
- Assessed FS145 binding to RAW264.7 cells.
- Measured the effect of FS145 on LPS-activated macrophage adhesion to extracellular matrix proteins.
- Quantified macrophage migration and production of inflammatory mediators (NO, TNF-α, IL-1β, IL-6).
- Investigated the impact of FS145 on MAPK/NF-κB signaling pathways.
- Evaluated in vivo anti-inflammatory and anti-nociceptive effects.
Main Results:
- FS145 concentration-dependently bound to RAW264.7 cells.
- FS145 significantly inhibited LPS-induced macrophage adhesion to fibrinogen, fibronectin, and vitronectin.
- FS145 suppressed macrophage migration and the production of nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6).
- FS145 inhibited the MAPK/NF-κB signaling cascades in LPS-induced macrophages.
- FS145 demonstrated potent anti-inflammatory and anti-nociceptive effects in vivo.
Conclusions:
- FS145 exerts anti-inflammatory and analgesic effects by blocking integrin αvβ3 and suppressing MAPK/NF-κB signaling pathways.
- FS145 modulates macrophage inflammatory responses.
- FS145 holds promise as a novel therapeutic agent for inflammatory conditions and pain management.
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