Abstract Acanthopanax leucorrhizus is an endemic medicinal plant growing abundantly in the northwest region of China. The roots and stem barks have been widely used to treat rheumatism, numbness, contracture, quadriplegia, hemiplegia, traumatic injury, edema, and itchy skin, although the anti-inflammatory effects of the extracts of A. leucorrhizus have not been assessed until now. To investigate the anti-inflammatory effects on macrophages of various extracts from A. leucorrhizus stems, alterations in the inducible nitric oxide synthase (iNOS)-mediated cyclooxygenase-2 (COX-2) expression and inflammatory cytokine production were measured in lipopolysaccharide (LPS)-activated RAW264.7 cells. Briefly, the dichloromethane extract prepared from stems of A. leucorrhizus (ALSDC) effectively inhibited NO production in LPS-stimulated cells and significantly reduced the production of pro-inflammatory cytokines IL-6 and TNF-α at a dose of 40 µg/mL. We also confirmed a dose-dependent and significant inhibition of iNOS and COX-2 protein expression. In conclusion, ALSDC exerted strong inhibitory effect on the expression of iNOS and COX-2 protein in LPS-induced RAW 264.7 macrophages and these results provide strong evidence to suggest that ALSDC may be considered as an important candidate for the treatment of inflammatory-related diseases in the future.

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.

Abstract Acanthopanax trifoliatus (L.) Merr. have been used as folk medicine to treat various diseases traditionally and the young leaves and shoots of A. trifoliatus are popularly consumed as vegetables and herbal tea in southern China. In the study, we firstly tested the cytotoxicity and NO production of 18 fractions that extracted from the leaves, stems and roots of A. trifoliatus to select the bioactive fraction. The increasing evidence suggested that the dichloromethane extract prepared from stems of A. trifoliatus (ATSDC) have anti-inflammatory activity. Therefore, the study followed to investigate the effects of ATSDC on the inflammatory response and the molecular mechanisms underpinning this effect in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The manuscript showed that ATSDC effectively inhibited NO production in LPS-stimulated cells and significantly reduced the production of pro-inflammatory cytokines IL-6, at a dose of 40 µg/mL, whereas TNF-α production tended to decrease under ATSDC treatment. We also confirmed a dose-dependent and significant inhibition of iNOS and COX-2 protein expression. In conclusion, ATSDC exerted strong inhibitory effect on the expression of iNOS and COX-2 protein in LPS-induced RAW 264.7 macrophages and could be potentially used in treatment of inflammatory-related diseases in the future.