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| The study on plasma protein binging of glucoside compounds |
| Hits 2445 Download times 1713 Received:June 29, 2013 |
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| DOI
10.11656/j.issn.1672-1519.2013.10.15 |
| Key Words
glucoside compounds;protein binding rate;binding site |
| Author Name | Affiliation | E-mail | | LIU Fei | State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Center for Drug Safety Evaluation and Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China | | | ZHANG Shi-jun | State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Center for Drug Safety Evaluation and Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China | | | XU Wei-ren | State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Center for Drug Safety Evaluation and Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China | xuwr@tjipr.com | | SHEN Xiu-ping | State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Center for Drug Safety Evaluation and Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China | | | SHANG Qian | State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Center for Drug Safety Evaluation and Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China | | | TANG Li-da | State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Center for Drug Safety Evaluation and Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China | |
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| Abstract
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| [Objective] To investigate the relationship between structure and protein binding rate,and explore the possible binding position of dapagliflozin and its derivatives. [Methods] The plasma balance dialysis and HPLC analysis were used to determine the protein binding rate of glucoside compounds. A few representative derivatives were for competitive combination experiment with diazepam and warfarin. The docking calculation was used to explore the binding position to human albumin of glucoside compounds. [Results] The protein binding rate of dapagliflozin was related to plasma volume used. The modification of dapagliflozin structure could change the protein binding rate of glucoside compounds to some degree. The existence of warfarin and diazepam could not change protein binding rate of glucoside compounds too much. [Conclusion] Dapagliflozin and its derivatives showed strong binding ability with serum protein. Their binding site with albumin may be different with that of diazepam and warfarin. The modification of structure could change the binding ability to a certain degree. |
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