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Evidence-Based Complementary and Alternative Medicine
Volume 2017, Article ID 2749643, 8 pages
Research Article

Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC–MS

1Guangzhou Key Laboratory of Chinese Medicine Prevention and Treatment of Chronic Heart Failure, The First Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong 510407, China
2Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 28163, USA
3School of Pharmaceutical Sciences, Peking University, Beijing 100191, China

Correspondence should be addressed to Shaoxiang Xian; moc.liamtoh@xgnaixoahs

Received 22 November 2016; Revised 15 February 2017; Accepted 12 March 2017; Published 23 March 2017

Academic Editor: Hyunsu Bae

Copyright © 2017 Zichen Liu et al. 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.


The cyclic nucleotide phosphodiesterase (PDE) plays an important role in regulating the levels of second messenger molecules cAMP and cGMP. Various PDE inhibitors have been successfully developed into drugs for targeted diseases. In addition, PDE inhibitors can also be found in different foods and natural medicines. In this study, ultrafiltration liquid chromatography–diode-array detector–electrospray ionization–ion-trap–time-of-flight–mass spectrometry (ultrafiltration LC–DAD–ESI–IT–TOF–MS) was applied to screen PDE inhibitors from the roots of Ilex pubescens Hook. et Arn. As a result, 11 major compounds were identified in I. pubescens roots, with nine compounds as potential PDE inhibitors, among which five were further confirmed to be active against PDEI and PDE5A dose-dependently in vitro, with ilexsaponin A1 and ilexsaponin being the strongest. HPLC quantification of these bioactive compounds suggested that they are major components in the plant. The results demonstrate that ultrafiltration LC–DAD–ESI–IT–TOF–MS is an efficient method for rapid screening of PDE inhibitors from natural medicines.