Protein Tyrosine Phosphatase 1B Inhibitors from the Roots of Cudrania tricuspidata

Molecules

Tran Hong Quang²  Nguyen Thi Thanh Ngan²  Chi-Su Yoon²  Kwang-Ho Cho²  Dae Gill Kang¹  Ho Sub Lee¹  Youn-Chul Kim²  Hyuncheol Oh² 

[1] Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea; E-Mails:;College of Pharmacy, Wonkwang University, Iksan 570-749, Korea; E-Mails:

关键词: Moraceae;    Cudrania tricuspidata;    xanthones;    flavonoids;    PTP1B;   

DOI  :  10.3390/molecules200611173

来源: mdpi

【 摘 要 】

A chemical investigation of the methanol extract from the roots of Cudrania tricuspidata resulted in the isolation of 16 compounds, including prenylated xanthones 1–9 and flavonoids 10–16. Their structures were identified by NMR spectroscopy and mass spectrometry and comparisons with published data. Compounds 1–9 and 13–16 significantly inhibited PTP1B activity in a dose dependent manner, with IC₅₀ values ranging from 1.9–13.6 μM. Prenylated xanthones showed stronger PTP1B inhibitory effects than the flavonoids, suggesting that they may be promising targets for the future discovery of novel PTP1B inhibitors. Furthermore, kinetic analyses indicated that compounds 1 and 13 inhibited PTP1B in a noncompetitive manner; therefore, they may be potential lead compounds in the development of anti-obesity and -diabetic agents.

【 授权许可】

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© 2015 by the authors; licensee MDPI, Basel, Switzerland.