Abstract

Inflammation is a common and important pathological process, and nuclear factor-κB (NF-κB) is a key mediator of it. Moutan Cortex (MC), the dried root cortex of Paeonia suffruticosa Andr., is widely used as a remedy for the treatment of inflammatory diseases in Asian region. However, there are few studies on the systematic identification of NF-κB inhibitors of MC. In this study, the effect of inhibiting NF-κB activation of MC was assessed at the cellular level using a tumor necrosis factor-α (TNF-α) induced inflammatory model. Subsequently, ultra-performance liquid chromatography-quadrupole/time of flight-mass spectrometry (UPLC-Q/TOF-MS) combined with biological activity assay was established to screen and identify potential anti-inflammatory ingredients in MC. The results revealed that MC significantly inhibited the activation of NF-κB. Seven potential NF-κB inhibitors were screened from MC, including oxypaeoniflorin, paeoniflorin, galloylpaeoniflorin, benzoyloxypaeoniflorin, mudanpioside C, gallic acid, and paeonol. Among them, the NF-κB inhibitor activity of galloylpaeoniflorin, benzoyloxypaeoniflorin, and mudanpioside C is first reported here. In conclusion, the anti-inflammatory activity of MC was associated with the seven components mentioned above. And the bioactivity-integrated UPLC-Q/TOF which contains both chemical and bioactive details is suitable for screening active ingredients from natural medicines.

Highlights

  • Inflammation is a multicomponent response to injury, tissue stress, and infection, associated with most diseases, and it can occur in various tissues and organs of the organism [1]

  • The seven potential nuclear factor-κB (NF-κB) inhibitors could be classified into two types according to their chemical structures: monoterpenes

  • The results demonstrated that the antiinflammatory activity of Moutan Cortex (MC) was related to the process of various components acting on multiple targets (Figure 5), which was consistent with the characteristics of traditional Chinese medicine (TCM) with multiple components, multiple pathways, and multiple targets [25, 26]

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Summary

Introduction

Inflammation is a multicomponent response to injury, tissue stress, and infection, associated with most diseases, and it can occur in various tissues and organs of the organism [1]. NSAID is one of the most widely used drugs in the world and are mainly classified into salicylates, propionic acids, indoles, fenamic acids, acetic acids and pyrazolones [3]. It has potential cardiovascular and gastrointestinal bleeding risks [4]. Due to the strong toxic and side effects of many synthetic drugs, and because traditional Chinese medicine (TCM) has the advantages of abundant resources, definite therapeutic effectiveness, and fewer side effects, the discovery of novel anti-inflammatory drugs from natural compounds has gradually become a research hotspot [5]

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