Abstract

Aralia continentalis (A. continentalis) is a medicinal plant belonging to Araliaceae, it has been reported to exert anti-cancer, anti-bacterial, anti-inflammatory, anti-platelet and anti-oxidative activities. But the potential mechanism for the anti-inflammatory effect of compounds isolated from the roots of A. continentalis is still insufficient. So, we evaluated whether compounds isolated from the roots of A. continentalis exert anti-inflammatory effects and elucidated its potential mechanism in RAW264.7 cells. The concentrated residue was subsequently suspended in H2O and partitioned with n-hexane, methylene chloride (CH2Cl2), ethyl acetate (EtOAc) and n-butanol (n-BuOH). The fractions were subjected to sequential column chromatography over silica-gel, RP-18, MPLC, recycling and preparative HPLC to isolated the novel compound. The novel compound was identified as 18-nor-ent-pimara-9(11),15-diene-4β-ol and confirmed anti-inflammatory activity. The 18-nor-ent-pimara-9(11),15-diene-4β-ol dose-dependently blocked NO production and inhibited iNOS, COX-2, TNF-α and IL-1β expression in LPS-stimulated RAW264.7 cells. The 18-nor-ent-pimara-9(11),15-diene-4β-ol inhibited LPS-stimulated degradation of IκB-α and nuclear accumulation of p65, which resulted in the suppression of NF-κB activation in RAW264.7 cells. Also, the 18-nor-ent-pimara-9(11),15-diene-4β-ol attenuated the phosphorylation of p38 and ERK1/2 in LPS-induced RAW264.7 cells. These results suggest that the nor-ent-pimara-9(11),15-diene-4β-ol isolated from the roots of A. continentalis may have grate potential for the development of anti-inflammatory drugs.

Highlights

  • In recent years, interest and expectations for medicinal resource plants have been increased, and many studies have been conducted to extract effective ingredients from natural resources and find functional materials because compounds present in medicinal resource plants have a Inflammatory reactions are reported to be involved in various pathological mechanisms, such as the introduction of bacteria and viruses into the body, in which the immune cells recognize and protect the body by secreting various inflammatory intermediaries, thereby promoting the growth of cancer cells, increasing insulin resistance, and worsening arteriosclerosis

  • The nuclear factor kappaB (NF-κB) activation is significantly associated with inflammatory diseases and much attention is focused on developing anti-inflammatory drugs targeting Nuclear factor kappa-B (NF-κB)

  • The mitogen-activated protein kinases (MAPK) cascade is one of the important signaling pathways in immune responses, and several recent studies reported that inhibition of MAPKs in mast cells can be an suitable target for pharmacological treatment of inflammatory diseases [7, 8]

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Summary

Introduction

Interest and expectations for medicinal resource plants have been increased, and many studies have been conducted to extract effective ingredients from natural resources and find functional materials because compounds present in medicinal resource plants have a Inflammatory reactions are reported to be involved in various pathological mechanisms, such as the introduction of bacteria and viruses into the body, in which the immune cells recognize and protect the body by secreting various inflammatory intermediaries, thereby promoting the growth of cancer cells, increasing insulin resistance, and worsening arteriosclerosis. The mitogen-activated protein kinases (MAPK) cascade is one of the important signaling pathways in immune responses, and several recent studies reported that inhibition of MAPKs in mast cells can be an suitable target for pharmacological treatment of inflammatory diseases [7, 8]. We investigated antiinflammatory activity of 18-nor-ent-pimara-9(11),15diene-4β-ol isolated from the ethanol extract of the roots A. continentalis.

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