Protein Tyrosine Phosphatase 1B Inhibitors from the Root Bark Pseudolarix amabilis (Nelson) Rehd. (Pinaceae)
| Autor: | Rui Zhou, Zhi-Shu Tang, Jinao Duan, Yalei Pan, Pei Xie, Lei Liyan, Hongbo Xu, Yihan He, Zhenggang Yue |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
ptp1b inhibitors
phenolic compounds Plant Science Pseudolarix lcsh:Chemistry lcsh:QD241-441 lcsh:Organic chemistry lcsh:Botany Drug Discovery Botany isolation and identification Pharmacology oleanolic acid 3-o-β-d-glucuronyl-6′-ethyl ester biology Chemistry Organic Chemistry pseudolarix amabilis biology.organism_classification Protein Tyrosine Phosphatase 1B lcsh:QK1-989 lcsh:QD1-999 Pinaceae visual_art oleanane-type compounds visual_art.visual_art_medium Bark |
| Zdroj: | Records of Natural Products, Vol 13, Iss 6, Pp 475-482 (2019) |
| ISSN: | 1307-6167 |
| Popis: | Pseudolarix amabilis (Nelson) Rehd, is a monotypic genus plant belonging to the family Pinaceae. The root bark , known as “Tu-Jin-Pi” has been used for the treatment of skin diseases. During our activity screening, the water-soluble part of the 70% EtOH extract of P. amabilis bark showed excellent inhibitory bioactivities on PTP1B enzyme, leading to the phytochemical isolation of the root bark of P. amabilis. Three oleanane-type compounds (1-3) and seven phenolic compounds (4-10) were isolated, in which oleanolic acid 3-O-β-D-glucuronyl-6′-ethyl ester (1) was identified as a new saponin. The chemical structures of these compounds were elucidated by 1D/2D nuclear magnetic resonance and high resolution mass spectra. In addition, their pharmacological inhibitory bioactivities on PTP1B enzyme were evaluated, and the three oleanane-type compounds 1-3 exhibited inhibitory bioactivities with IC50 values of 1.90 ± 0.37, 19.15 ± 0.10 and 10.44 ± 0.59 μM, respectively. |
| Databáze: | OpenAIRE |
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