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Molecules 2015, 20(6), 11173-11183; doi:10.3390/molecules200611173

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

1
College of Pharmacy, Wonkwang University, Iksan 570-749, Korea
2
Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam
3
Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea
4
Professional Graduate School of Oriental Medicine and College of Oriental Medicine, Wonkwang University, Iksan 570-749, Korea
*
Authors to whom correspondence should be addressed.
Academic Editor: Pascal Richomme
Received: 20 April 2015 / Revised: 11 June 2015 / Accepted: 12 June 2015 / Published: 17 June 2015
(This article belongs to the Special Issue Coumarins, Xanthones and Related Compounds)
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Abstract

A chemical investigation of the methanol extract from the roots of Cudrania tricuspidata resulted in the isolation of 16 compounds, including prenylated xanthones 19 and flavonoids 1016. Their structures were identified by NMR spectroscopy and mass spectrometry and comparisons with published data. Compounds 19 and 1316 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. View Full-Text
Keywords: Moraceae; Cudrania tricuspidata; xanthones; flavonoids; PTP1B Moraceae; Cudrania tricuspidata; xanthones; flavonoids; PTP1B
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Quang, T.H.; Ngan, N.T.T.; Yoon, C.-S.; Cho, K.-H.; Kang, D.G.; Lee, H.S.; Kim, Y.-C.; Oh, H. Protein Tyrosine Phosphatase 1B Inhibitors from the Roots of Cudrania tricuspidata. Molecules 2015, 20, 11173-11183.

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