Synthesis, in silico and in vivo blood brain barrier permeability of ginkgolide B cinnamate

Fitoterapia
Yong-Ming LuYan Chen

Abstract

Ginkgolide B, one of the important components of Ginkgo biloba extracts, has been revealed to exhibit great potential in therapy of cerebrovascular diseases. However the lack of permeability greatly limited it from further clinical application. Based on the prediction model for blood brain barrier (BBB) permeation, herein a potential brain-targeting analog ginkgolide B cinnamate (GBC) was successfully synthesized and characterized. After intravenous administration of GBC or GB, liquid chromatography tandem mass spectrometry (LC-MS/MS) was conducted to determine the analog in rat plasma and brain. The results showed that GBC had a significant increase in BBB permeability. A significant 1.61-times increase in half-life was observed for GBC and the drug targeting index (DTI) value was calculated to be 9.91. The experiment results matched well with the predicted one, which revealed that BBB permeability prediction model combined with in vivo study could be used as a quick, feasible and efficient tool for brain-targeting drug design.

References

Jun 1, 1985·Journal of Neurochemistry·W M PardridgeJ Yang
Jul 28, 1995·International Journal of Cancer. Journal International Du Cancer·L LiuD Samid
May 12, 2000·Archives of Physical Medicine and Rehabilitation·B J DiamondN E Schoenberger
Jan 22, 2003·Advanced Drug Delivery Reviews·Alexander V KabanovDonald W Miller
Mar 23, 2004·Chemistry : a European Journal·Stanislav JaraczKristian Strømgaard
Jan 22, 2005·Brain Research. Molecular Brain Research·Hidemi YoshidaKei Satoh
May 18, 2005·International Journal of Pharmaceutics·E Garcia-GarciaP Couvreur
Feb 14, 2006·Current Drug Metabolism·Andreas Reichel
Jun 15, 2007·Ultrasound in Medicine & Biology·Feng-Yi YangWin-Li Lin
Aug 28, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·P J Gaillard, A G de Boer
Jun 19, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Barbara PavanSilvia Vertuani
Apr 4, 2009·Nanomedicine : Nanotechnology, Biology, and Medicine·Anna Valeria VergoniLuca Costantino
May 29, 2009·Computer Methods and Programs in Biomedicine·Yan ChenXiao-Pei Wu
Oct 17, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Weirong FangLishun Mao
Mar 10, 2010·Current Pharmaceutical Design·Javed Ali Bhavna
Nov 23, 2010·Journal of Controlled Release : Official Journal of the Controlled Release Society·Inge van RooyRaymond M Schiffelers
Jul 26, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Huali ChenQin He
Aug 30, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Gow-Chin YenChia-Jui Weng
Dec 14, 2011·Advanced Drug Delivery Reviews·Yan Chen, Lihong Liu
Nov 20, 2012·Fitoterapia·Preeti SinghVipin Kumar Garg
Aug 8, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Chi ZhangQizhi Zhang

❮ Previous
Next ❯

Related Concepts

Related Feeds

Blood Brain Barrier

The blood brain barrier is a border that separates blood from cerebrospinal fluid. Discover the latest search on this highly selective semipermeable membrane here.

Blood Brain Barrier Regulation in Health & Disease

The blood brain barrier is essential in regulating the movement of molecules and substances in and out of the brain. Disruption to the blood brain barrier and changes in permeability allow pathogens and inflammatory molecules to cross the barrier and may play a part in the pathogenesis of neurodegenerative disorders. Here is the latest research in this field.

Blood Brain Barrier Chips

The blood brain barrier (BBB) is comprised of endothelial cells that regulate the influx and outflux of plasma concentrations. Lab-on-a-chip devices allow scientists to model diseases and mechanisms such as the passage of therapeutic antibodies across the BBB. Discover the latest research on BBB chips here.