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基质金属蛋白酶-13 的下调和高丽红参制剂的潜在软骨保护作用。

Matrix metalloproteinase-13 downregulation and potential cartilage protective action of the Korean Red Ginseng preparation.

机构信息

College of Pharmacy, Kangwon National University, Chunchon, Korea.

College of Pharmacy, Seoul National University, Seoul, Korea.

出版信息

J Ginseng Res. 2015 Jan;39(1):54-60. doi: 10.1016/j.jgr.2014.06.006. Epub 2014 Jul 2.

DOI:10.1016/j.jgr.2014.06.006
PMID:25535477
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4268559/
Abstract

BACKGROUND

The present study was designed to prepare and find the optimum active preparation or fraction from Korea Red Ginseng inhibiting matrix metalloproteinase-13 (MMP-13) expression, because MMP-13 is a pivotal enzyme to degrade the collagen matrix of the joint cartilage.

METHODS

From total red ginseng ethanol extract, n-BuOH fraction (total ginsenoside-enriched fraction), ginsenoside diol-type-enriched fraction (GDF), and ginsenoside triol-type-enriched fraction (GTF) were prepared, and ginsenoside diol type-/F4-enriched fraction (GDF/F4) was obtained from Panax ginseng leaf extract.

RESULTS

The n-BuOH fraction, GDF, and GDF/F4 clearly inhibited MMP-13 expression compared to interleukin-1β-treated SW1353 cells (human chondrosarcoma), whereas the total extract and ginsenoside diol-type-enriched fraction did not. In particular, GDF/F4, the most effective inhibitor, blocked the activation of p38 mitogen-activated protein kinase (p38 MAPK), c-Jun-activated protein kinase (JNK), and signal transducer and activator of transcription-1/2 (STAT-1/2) among the signal transcription pathways involved. Further, GDF/F4 also inhibited the glycosaminoglycan release from interleukin-1α-treated rabbit cartilage culture (30.6% inhibition at 30 μg/mL).

CONCLUSION

Some preparations from Korean Red Ginseng and ginseng leaves, particularly GDF/F4, may possess the protective activity against cartilage degradation in joint disorders, and may have potential as new therapeutic agents.

摘要

背景

本研究旨在制备并寻找抑制基质金属蛋白酶-13（MMP-13）表达的韩国红参活性制剂或有效部位，因为 MMP-13 是降解关节软骨胶原基质的关键酶。

方法

从红参乙醇提取物中制备正丁醇（总人参皂苷富集部分）、二醇型人参皂苷富集部分（GDF）和三醇型人参皂苷富集部分（GTF），并从人参叶提取物中制备二醇型/F4 人参皂苷富集部分（GDF/F4）。

结果

与白细胞介素-1β处理的 SW1353 细胞（人软骨肉瘤）相比，正丁醇部分、GDF 和 GDF/F4 明显抑制 MMP-13 表达，而总提取物和二醇型人参皂苷富集部分则没有。特别是最有效的抑制剂 GDF/F4 阻断了 p38 丝裂原活化蛋白激酶（p38 MAPK）、c-Jun 激活蛋白激酶（JNK）和信号转导和转录激活因子-1/2（STAT-1/2）等参与的信号转导途径的激活。此外，GDF/F4 还抑制了白细胞介素-1α处理的兔软骨培养物中糖胺聚糖的释放（在 30μg/mL 时抑制率为 30.6%）。

结论

韩国红参和人参叶的一些制剂，特别是 GDF/F4，可能具有预防关节疾病软骨降解的保护活性，并有作为新的治疗剂的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/a16416fe1df8/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/670570b07bb2/gr1ac.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/ffdcaaf6783c/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/43cc61ee4c53/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/1de99dba0c2a/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/a16416fe1df8/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/670570b07bb2/gr1ac.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/ffdcaaf6783c/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/43cc61ee4c53/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/1de99dba0c2a/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/87ea/4268559/a16416fe1df8/gr5.jpg

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