PEG-amino acid-przewaquinone a conjugations: Synthesis,physicochemical properties and protective effect in a rat model of brain ischemia-reperfusion |
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| Affiliation: | 1. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, PR China;2. Department of Chemistry, University of South Florida, Florida 33620, USA;1. Center for Ultrasound Molecular Imaging and Therapeutics, University of Pittsburgh Medical Center, Heart and Vascular Institute, Pittsburgh, Pennsylvania, USA;2. Department of Cardiology and Institute for Cardiovascular Research (ICaR-VU), VU University Medical Center, Amsterdam, The Netherlands;3. Interuniversity Cardiology Institute of the Netherlands (ICIN), Utrecht, The Netherlands;1. Jiangsu Key Laboratory for Functional Substance of Chinese Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, State Key Laboratory Cultivation Base for TCM Quality and Efficacy, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China;2. Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Shanghai 201203, China;1. Key Lab of Eco-chemical Engineering, Ministry of Education, College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology, Qingdao 266042, PR China;2. College of Science, China University of Petroleum (East China), Qingdao 266580, PR China;1. College of Chemistry and Chemical Engineering, Fujian Normal University, Fuzhou, Fujian 350007, China;2. Fujian Key Laboratory of Polymer Materials, College of Material Science and Engineering, Fujian Normal University, Fuzhou, Fujian 350007, China;1. Department of Chemistry, Faculty of Arts and Sciences, Eskişehir Osmangazi University, 26480 Eskişehir, Turkey;2. Vocational School of Health Services, Bartın University, Bartın, Turkey |
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| Abstract: | A total of 21 PEG-przewaquinone A conjugations with high drug loading ability, good water solubility and in vivo slow-release quality were obtained by conjugating przewaquinone A with PEG through amino acids and tripeptides spacers respectively. Notably, compound 3a can obviously reduce the brain ischemia-reperfusion damage dose-dependently in a rat model, which indicated the efficacy of our PEG prodrug strategy. |
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| Keywords: | PEG Conjugation Przewaquinone A Tanshinone IIA Brain ischemia-reperfusion Neuro-protective effect Pharmacokinetic properties |
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