Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS.
机构：[1]Guangzhou 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深圳市中医院深圳医学信息中心[2]Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 28163, USA[3]School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
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 B2 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.
基金：
This work was supported by the National Natural Science
Foundation of China (Grant nos. 81473621 and 30873397).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2016]版：
大类|4 区医学
小类|3 区全科医学与补充医学
最新[2025]版：
无
第一作者：
第一作者机构：[1]Guangzhou 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
共同第一作者：
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推荐引用方式(GB/T 7714)：
Zichen Liu,Zongtao Lin,Shizhong Chen,et al.Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS.[J].Evidence-based complementary and alternative medicine : eCAM.2017,2017:2749643.doi:10.1155/2017/2749643.
APA：
Zichen Liu,Zongtao Lin,Shizhong Chen,Lingjun Wang&Shaoxiang Xian.(2017).Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS..Evidence-based complementary and alternative medicine : eCAM,2017,
MLA：
Zichen Liu,et al."Rapid Screening of Potential Phosphodiesterase Inhibitors from the Roots of Ilex pubescens Hook. et Arn. Using a Combination of Ultrafiltration and LC-MS.".Evidence-based complementary and alternative medicine : eCAM 2017.(2017):2749643
