College of Pharmacy, Kangwon National University, Chunchon, Korea.
College of Pharmacy, Seoul National University, Seoul, Korea.
J Ginseng Res. 2015 Jan;39(1):54-60. doi: 10.1016/j.jgr.2014.06.006. Epub 2014 Jul 2.
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.
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.
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).
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.
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。
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)。
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%)。
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。