Anti-inflammatory effects of two lupane-type triterpenes from leaves of Acanthopanax gracilistylus on LPS-induced RAW264.7 macrophages

Jiao Luo,Xiao-Jun Li,Chang-Soo Yook,Xiang-Qian Liu,Geon-Ho Lee,Xiao-Dan Zhang,Jian-Jun Huang,Wan-Kyunn Whang

doi:10.1590/fst.89721

Abstract

Acanthopanax gracilistylus W.W.Smith (AGS) is an traditional Chinese medicine and its leaves that have rich biological activities has been long used as a fresh vegetable in Chinese folk. There are two lupane-type triterpenoids, 3α,11α-dihydroxy-23-oxo-lup-20(29)-en-28-oic acid (1) and 3α,11α,23-trihydroxy-lup-20(29)-en-28-oic acid (2), were isolated as the active constituents from leaves of AGS. However, the anti-inflammatory effects and potential mechanisms of 1 and 2 on LPS-induced RAW264.7 Macrophages have not been evaluated. In this study, the results shown that compounds 1 and 2 reduced the levels of early pro-inflammatory cytokines TNF-α, IL-1β, the secretion of late pro-inflammatory cytokine HMGB1, as well as the activation of transcription factor NF-κB in RAW 264.7 macrophages induced by LPS. In conclusion, two lupane-type triterpenes (1 and 2) have anti-inflammatory activities in LPS-induced RAW264.7 cells through inhibiting expression of proinflammatory cytokines and NF‐κB activation and could be potentially used in treatment of inflammatory-related diseases in the future.

Highlights

Macrophages are immune cells that can response to stimuli and secrete inflammatory mediators, as well as proinflammatory cytokines (Han et al, 2021)
LPS-induced RAW264.7 macrophages were used to evaluate the inhibitory action of compounds 1 and 2 on the production of tumor necrosis factor (TNF)-α and IL-1β
To confirm whether the inhibition of TNF-α and IL-1β production was due to the decreased gene expression, we examined the mRNA levels of IL-1β and TNF-α in the LPSstimulated RAW 264.7 cells

Summary

Introduction

Macrophages are immune cells that can response to stimuli and secrete inflammatory mediators, as well as proinflammatory cytokines (Han et al, 2021). Recent studies have shown that acute and uncontrolled chronic inflammation is associated with multiple diseases, including rheumatoid arthritis, metabolic syndrome, inflammatory bowel disease, diabetes, and various types of cancer (Ahn et al, 2018; Xu et al, 2021a, b). Activation of NF-κB plays a central role in inflammation through its ability to induce production and release of multiple pro-inflammatory cytokines and chemokines (Lin et al, 2021). These factors mediate and amplify the inflammatory response

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Conclusion