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  • 标题:PTP1B Inhibitory and Anti-inflammatory Properties of Constituents from Eclipta prostrata L.
  • 本地全文:下载
  • 作者:Duc Dat Le ; Duc Hung Nguyen ; Eun Sook Ma
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2021
  • 卷号:44
  • 期号:3
  • 页码:298-304
  • DOI:10.1248/bpb.b20-00994
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The white-flowered leaves of Eclipta prostrata L. together with leaves of Scoparia dulcis and Cynodon dactylon are mixedly boiled in water and given to diabetic patients resulting in the significant improvement in the management of diabetes. However, the active constituents from this plant for antidiabetic and anti-obesity properties are remaining unclear. Thus, this study was to discover anti-diabetes and anti-obesity activities through protein tyrosine phosphatases (PTP)1B inhibitory effects. We found that the fatty acids ( 23 , 24 ) showed potent PTP1B inhibition with IC 50 values of 2.14 and 3.21 µM, respectively. Triterpenoid-glycosides ( 12 – 15 ) also exhibited strong to moderate PTP1B inhibitory effects, with IC 50 values ranging from 10.88 to 53.35 µM. Additionally, active compounds were investigated for their PTP1B inhibitory mechanism and docking analysis. On the other hand, the anti-inflammatory activity from our study revealed that compounds ( 1 – 4 , 7 , 8 , 10 ) displayed the significant inhibition nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Especially, compound 9 showed the potent inhibitory effects in LPS-induced NO production on RAW264.7 cell. Therefore, further Western blot analysis was performed to identify the inhibitory expression including heme oxygenase-1 (HO-1) and inhibitor of kappaB (IκB) phosphorylation.
  • 关键词:Eclipta prostrata L.;molecular docking analysis;nitric oxide (NO) inhibition;protein tyrosine phosphatase (PTP)1B;inflammation
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