Ginkgolide B, one of the important components of Ginkgo biloba exts., has been revealed to exhibit great potential intherapy of cerebrovascular diseases. However the lack of permeability greatly limited it from further clin. application.Based on the prediction model for blood brain barrier (BBB) permeation, herein a potential brain-targeting analogginkgolide B cinnamate (GBC) was successfully synthesized and characterized. After i.v. administration of GBC or GB,liq. chromatog. tandem mass spectrometry (LC-MS/MS) was conducted to det. the analog in rat plasma and brain. Theresults showed that GBC had a significant increase in BBB permeability. A significant 1.61-times increase in half-life wasobsd. for GBC and the drug targeting index (DTI) value was calcd. to be 9.91. The expt. results matched well with thepredicted one, which revealed that BBB permeability prediction model combined with in vivo study could be used as aquick, feasible and efficient tool for brain-targeting drug design
Ginkgolide B, one of the important components of Ginkgo biloba exts., has been revealed to exhibit great potential intherapy of cerebrovascular diseases. However the lack of permeability greatly limited it from further clin. application.Based on the prediction model for blood brain barrier (BBB) permeation, herein a potential brain-targeting analogginkgolide B cinnamate (GBC) was successfully synthesized and characterized. After i.v. administration of GBC or GB,liq. chromatog. tandem mass spectrometry (LC-MS/MS) was conducted to det. the analog in rat plasma and brain. Theresults showed that GBC had a significant increase in BBB permeability. A significant 1.61-times increase in half-life wasobsd. for GBC and the drug targeting index (DTI) value was calcd. to be 9.91. The expt. results matched well with thepredicted one, which revealed that BBB permeability prediction model combined with in vivo study could be used as aquick, feasible and efficient tool for brain-targeting drug design<br>
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