Abstract

Plant polyphenols are widely used to treat various inflammatory diseases, owing to their ability to suppress reactive oxygen species production and the expression of inflammatory cytokines. Herein, we investigated phenolic compounds from Calystegia soldanella using UPLC Q-TOF MS/MS and their antioxidative and anti-inflammatory activities were analyzed. The C. soldanella ethyl acetate fraction (CsEF) had the strongest antioxidative activity, given its high polyphenol compound content. It also exhibited anti-inflammatory effects, inhibiting the production of inflammatory cytokines such as NO, PGE2, IL-1β, IL-6, and TNF-α in LPS-stimulated mouse macrophages. CsEF activated the nuclear transcription factor Nrf-2, thereby upregulating antioxidant enzymes such as HO-1 and NQO-1 and inhibiting NF-κB expression, which in turn, suppressed the expression of COX-2, iNOS, and inflammatory cytokines, ultimately exerting anti-inflammatory effects. Further, UPLC-Q-TOF-MS/MS was used to analyze the polyphenol compound contents in CsEF. The quercetin glycosides isoquercitrin and quercitrin were the primary flavonoid compounds, while the caffeic acid derivatives, chlorogenic acid and dicaffeoylquinic acid, were the primary phenolic acids. Thus, C. soldanella, which had only a limited use thus far as a medicinal plant, may serve as a natural medicinal resource for treating inflammatory diseases.

Highlights

  • Accepted: 13 October 2021Reactive oxygen species (ROS), which are generated when aerobic organisms use oxygen to produce energy, play various roles in cells, including intracellular signaling and the regulation of homeostasis

  • Macrophages are known to play a role in host defense during the early stage of an infection by producing inflammatory mediators, such as nitric oxide (NO), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) [5]

  • In the present study, which was regarding the development of a natural medicinal ingredient with anti-inflammatory effects, we examined C. soldanella, which has not been studied extensively far

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Summary

Introduction

Accepted: 13 October 2021Reactive oxygen species (ROS), which are generated when aerobic organisms use oxygen to produce energy, play various roles in cells, including intracellular signaling and the regulation of homeostasis. ROS are electron-deficient radicals that are highly reactive; as a result, they can cause oxidative damage to cellular components including the cell membrane, DNA, and proteins. When such oxidative damage persists, intracellular signaling pathways are activated, causing chronic systemic inflammatory responses by exacerbating various pathological conditions, including cardiovascular disease and cancer [1,2]. Excessive or prolonged inflammatory responses may cause chronic inflammatory diseases, such as arthritis, asthma, multiple sclerosis, chronic enteritis, and psoriasis [4] In such inflammatory responses, macrophages are known to play a role in host defense during the early stage of an infection by producing inflammatory mediators, such as nitric oxide (NO), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) [5]

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