Ethnopharmacological Relevance: Acanthopanax koreanum (Araliaceae) has been used in traditional medicine for enhancing vitality, rheumatism, and bone-related pains. But its activity on cartilage protection has not been known yet.
Aim Of The Study: Matrix metalloproteinase (MMP)-13 has an important role in degrading cartilage materials under pathologic conditions such as arthritis. The present study was designed to find the inhibitory activity of impressic acid on MMP-13 expression and cartilage protective action.
Materials And Methods: 70% ethanol extract of Acanthopanax koreanum leaves and impressic acid, a major constituent isolated from the same plant materials, were examined on MMP-13 down-regulating capacity in IL-1β-treated human chondrocyte cell line (SW1353) and rabbit cartilage explants.
Results: In IL-1β-treated SW1353 cells, impressic acid significantly and concentration-dependently inhibited MMP-13 expression at 0.5-10μM. Impressic acid was found to be able to inhibit MMP-13 expression by blocking the phosphorylation of signal transducer and activator of transcription-1/-2 (STAT-1/-2) and activation of c-Jun and c-Fos among the cellular signaling pathways involved. Further, impressic acid was found to inhibit the expression of MMP-13 mRNA (47.7% inhibition at 10μM), glycosaminoglycan release (42.2% reduction at 10μM) and proteoglycan loss in IL-1-treated rabbit cartilage explants culture. In addition, a total of 21 lupane-type triterpenoids structurally-related to impressic acid were isolated from the same plant materials and their suppressive activities against MMP-13 expression were also examined. Among these derivatives, compounds 2, 3, 16, and 18 clearly down-regulated MMP-13 expression. However, impressic acid was more potent than these derivatives in down-regulating MMP-13 expression.
Conclusions: Impressic acid, its related triterpenoids, and A. koreanum extract have potential as therapeutic agents to prevent cartilage degradation by inhibiting matrix protein degradation.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.jep.2017.07.034 | DOI Listing |
Fitoterapia
April 2022
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
Three unprecedented 23-nor-3,4-seco-3-acetallupane triterpenoids, gracilistylacid A-C (1-3), along with three known lupanoids (4-6), were isolated from the aerial parts of Acanthopanax gracilistylus W.W. Smith var.
View Article and Find Full Text PDFAnn N Y Acad Sci
October 2021
OncoWitan, Lille (Wasquehal), Wasquehal, France.
Acankoreagenin (ACK, also known as acankoreanogenin and HLEDA) and impressic acid are two lupane-type triterpenes that can be isolated from various Acanthopanax and Schefflera species. They efficiently block activation of the NF-κB signaling pathway and the release of proinflammatory cytokines and/or the action of inflammation mediators (HMGB1, iNOS, and NO). These effects are the basis for the antiviral and anticancer activities reported with these pentacyclic compounds or their various glycoside derivatives.
View Article and Find Full Text PDFIn Silico Pharmacol
April 2021
OncoWitan, Wasquehal, 59290 Lille, France.
Acankoreagenin (ACK) is a lupane triterpene found in several and plant species. ACK, also known as acankoreanogenin or HLEDA, bears a major structural analogy with other lupane triterpenoids such as impressic acid (IA) and the largely used phytochemical betulinic acid (BA). These compounds display marked anti-inflammatory, anti-diabetes, and anti-cancer properties.
View Article and Find Full Text PDFInt J Mol Sci
February 2021
College of Pharmacy, Chungnam National University, Daejeon 34134, Korea.
Impressic acid (IPA), a lupane-type triterpenoid from , has many pharmacological activities, including the attenuation of vascular endothelium dysfunction, cartilage destruction, and inflammatory diseases, but its influence on atopic dermatitis (AD)-like skin lesions is unknown. Therefore, we investigated the suppressive effect of IPA on 2,4-dinitrochlorobenzene (DNCB)-induced AD-like skin symptoms in mice and the underlying mechanisms in cells. IPA attenuated the DNCB-induced increase in the serum concentrations of IgE and thymic stromal lymphopoietin (TSLP), and in the mRNA levels of thymus and activation regulated chemokine(TARC), macrophage derived chemokine (MDC), interleukin-4 (IL-4), interleukin-5 (IL-5), interleukin-13 (IL-13), tumor necrosis factor-alpha (TNF-α) and interferon-gamma (IFN-γ) in mice.
View Article and Find Full Text PDFInt J Mol Sci
January 2021
College of Pharmacy, Chungnam National University, Daejeon 34134, Korea.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!