Abstract

The fruit of Chaenomeles sinensis has been traditionally used in ethnomedicine for the treatment of various human ailments, including pneumonia, bronchitis, and so on, but the pharmacological applications of the leaf part of the plant have not been studied. In this study, we evaluated the various radical scavenging activities and anti-inflammatory effects of different Chaenomeles sinensis leaf (CSL) extracts. The water extract showed a higher antioxidant and radical scavenging activities. However the ethanolic extracts showed higher NO scavenging activity than water extract, therefore the ethanolic extract of CSL was examined for anti-inflammatory effects on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. The 70% ethanol extract of CSL (CSLE) has higher anti-inflammatory activity and significantly inhibited the production of nitric oxide (NO), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α). In addition, CSLE suppressed LPS-stimulated inducible nitric oxide synthase (iNOS) and NO production, IL-1β and phospho-STAT1 expression. In this study, we investigated the effect of CSLE on the production of inflammatory mediators through the inhibition of the TRIF-dependent pathways. Furthermore, we evaluated the role of CSLE on LPS-induced expression of pro-inflammatory cytokines, such as TNF-α, IL-1β and IL-6. Our results suggest that CSLE attenuates the LPS-stimulated inflammatory responses in macrophages through regulating the key inflammatory mechanisms, providing scientific support for its traditional uses in treating various inflammatory diseases.

Highlights

  • Chaenomeles sinensis (C. sinensis) is an important medicinal plant species of the family Rosacea.It has been traditionally used in Japan, Korea, China, Bhutan, and Burma to treat various human ailments

  • To determine the potential effects of on the production of pro-inflammatory cytokines, IL-6 and pro-IL-1β (Figures 3 and 4). These data suggest that CSLE has the ability to downregulate we examined the accumulation of tumor necrosis factor-α (TNF-α), IL-6 and IL-1β

  • These results indicate that CSLE inhibited STAT1 phosphorylation via the attenuation of IFN-β production

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Summary

Introduction

Chaenomeles sinensis (C. sinensis) is an important medicinal plant species of the family Rosacea. It has been traditionally used in Japan, Korea, China, Bhutan, and Burma to treat various human ailments. The medicinal properties of C. sinensis have been validated through the identification of bioactive components related to its pharmacological applications [1]. Molecules 2016, 21, 422 derived from C. sinensis potentially inhibited hemolysis caused by streptolysin O [2]; the anti-inflammatory effect of an epicatechin polymer derived from C. sinensis was deduced from its hindrance of both the histamine release from rat mast cells and the activation of hyaluronidase [3,4]. The ethanol extracts of C. sinensis has been reported for its potent antipruritic effects.

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