Synthesis, in silico and in vivo blood brain barrier permeability of ginkgolide B cinnamate.
作者： Yong-Ming Lu , Jian Pan , Wen-Na Zhang , Ai-Ling Hui , Wen-Qiang Guo
DOI: 10.1016/J.FITOTE.2015.08.012
关键词:
摘要: Ginkgolide B, one of the important components Ginkgo biloba extracts, has been revealed to exhibit great potential in therapy cerebrovascular diseases. However lack permeability greatly limited it from further clinical application. Based on prediction model for blood brain barrier (BBB) permeation, herein a brain-targeting analog ginkgolide B cinnamate (GBC) was successfully synthesized and characterized. After intravenous administration GBC or GB, liquid chromatography tandem mass spectrometry (LC-MS/MS) conducted determine rat plasma brain. The results showed that had significant increase BBB permeability. A 1.61-times half-life observed drug targeting index (DTI) value calculated be 9.91. experiment matched well with predicted one, which combined vivo study could used as quick, feasible efficient tool design.
elsevier.com
sci-hub.se 参考文章(41)
Lihong Hu, Zhongliang Chen, Yuyuan Xie, Yuanyin Jiang, Huawu Zhen, Alkyl and alkoxycarbonyl derivatives of ginkgolide B: synthesis and biological evaluation of PAF inhibitory activity. Bioorganic & Medicinal Chemistry. ,vol. 8, pp. 1515- 1521 ,(2000) , 10.1016/S0968-0896(00)00085-7
P Braquet, Proofs of involvement of PAF-acether in various immune disorders using BN 52021 (ginkgolide B): a powerful PAF-acether antagonist isolated from Ginkgo biloba L. Advances in prostaglandin, thromboxane, and leukotriene research. ,vol. 16, pp. 179- 198 ,(1986)
Clive Bate, Mario Salmona, Alun Williams, Ginkgolide B inhibits the neurotoxicity of prions or amyloid-β1-42 Journal of Neuroinflammation. ,vol. 1, pp. 4- 4 ,(2004) , 10.1186/1742-2094-1-4
Stanislav Jaracz, Koji Nakanishi, Anders A. Jensen, Kristian Strømgaard, Ginkgolides and Glycine Receptors: A Structure–Activity Relationship Study Chemistry: A European Journal. ,vol. 10, pp. 1507- 1518 ,(2004) , 10.1002/CHEM.200305473
Hidemi Yoshida, Tadaatsu Imaizumi, Kunikazu Tanji, Hirotaka Sakaki, Norifumi Metoki, Masaharu Hatakeyama, Koji Yamashita, Akira Ishikawa, Kageaki Taima, Yoshihiro Sato, Hiroto Kimura, Kei Satoh, Platelet-activating factor enhances the expression of nerve growth factor in normal human astrocytes under hypoxia. Molecular Brain Research. ,vol. 133, pp. 95- 101 ,(2005) , 10.1016/J.MOLBRAINRES.2004.09.022
Andreas Reichel, The role of blood-brain barrier studies in the pharmaceutical industry. Current Drug Metabolism. ,vol. 7, pp. 183- 203 ,(2006) , 10.2174/138920006775541525
Anna Valeria Vergoni, Giovanni Tosi, Raffaella Tacchi, Maria Angela Vandelli, Alfio Bertolini, Luca Costantino, Nanoparticles as drug delivery agents specific for CNS: in vivo biodistribution. Nanomedicine: Nanotechnology, Biology and Medicine. ,vol. 5, pp. 369- 377 ,(2009) , 10.1016/J.NANO.2009.02.005
Michel Demeule, Anthony Régina, Christian Ché, Julie Poirier, Tran Nguyen, Reinhard Gabathuler, Jean-Paul Castaigne, Richard Béliveau, Identification and Design of Peptides as a New Drug Delivery System for the Brain Journal of Pharmacology and Experimental Therapeutics. ,vol. 324, pp. 1064- 1072 ,(2008) , 10.1124/JPET.107.131318
Yan Chen, Qing-Jun Zhu, Jian Pan, Yi Yang, Xiao-Pei Wu, A prediction model for blood-brain barrier permeation and analysis on its parameter biologically Computer Methods and Programs in Biomedicine. ,vol. 95, pp. 280- 287 ,(2009) , 10.1016/J.CMPB.2009.03.006
P.J. Gaillard, A.G. de Boer, A novel opportunity for targeted drug delivery to the brain. Journal of Controlled Release. ,vol. 116, ,(2006) , 10.1016/J.JCONREL.2006.09.050