Search results for " Oral bioavailability"

showing 2 items of 2 documents

Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Epheephrin system

2015

The Eph receptor-ephrin system is an emerging target for the development of novel anti-angiogenic therapies. Research programs aimed at developing small-molecule antagonists of the Eph receptors are still in their initial stage as available compounds suffer from pharmacological drawbacks, limiting their application in vitro and in vivo. In the present work, we report the design, synthesis and evaluation of structure-activity relationships of a class of Δ(5)-cholenoyl-amino acid conjugates as Eph-ephrin antagonists. As a major achievement of our exploration, we identified N-(3β-hydroxy-Δ(5)-cholen-24-oyl)-L-tryptophan (UniPR1331) as the first small molecule antagonist of the Eph-ephrin syste…

MaleModels MolecularAnti-angiogenic agentsAngiogenesis InhibitorsEpheephrin antagonistsPharmacologyEphA2MiceStructure-Activity RelationshipIn vivoCell Line TumorOral bioavailabilityProteineprotein interaction inhibitorsDrug DiscoveryAnimalsHumansStructure–activity relationshipEphrinAmino AcidsReceptorReceptors Eph Familychemistry.chemical_classificationPharmacologyDose-Response Relationship DrugMolecular StructureAnti-angiogenic agents; Bile acids; EphA2; Epheephrin antagonists; Oral bioavailability; Proteineprotein interaction inhibitors; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryErythropoietin-producing hepatocellular (Eph) receptorEndothelial CellsBiological activityGeneral MedicineEPH receptor A2biological factorsBile acidsAmino acidchemistryBiochemistryEphrins
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In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition.

2017

Recently, we have reported that glycol chitosan (GCS) was able to reverse the P- glycoprotein (P-gp) efflux pump. The objective of the present study was to evaluate the potential of two GCS-based dosage forms (aqueous solution or nanoparticle suspension) for oral administration of the P-gp substrate Rho-123. A further aim of the present study was to assess the effect of the glycol chitosan-4-thiobutylamidine thiomer (GCS-TBA) on P-gp activity considering that the corresponding thiomer of chitosan series is a well-known P-gp inhibitor. Pre-treatment of Caco-2 cell monolayer with a GCS solution or GCS-based nanoparticles increased the absorptive transport of Rho-123 across the monolayer of 1.…

endocrine systemATP Binding Cassette Transporter Subfamily BPolymers and Plastics02 engineering and technologyPharmacologyDosage formChitosan03 medical and health scienceschemistry.chemical_compoundGlycols0302 clinical medicineDrug Delivery SystemsOral administrationhealth services administrationpolycyclic compoundsMaterials ChemistryHumansGlycol chitosan-based formulations P-gp inhibition properties Rhodamine 123 Glycol chitosan-4-thiobutylamidine thiomer Caco-2 cells Oral bioavailabilityChitosanChemistryThiomerOrganic ChemistryGlycol chitosan-based formulations P-gp inhibition properties Rhodamine 123 Glycol chitosan-4-thiobutylamidine thiomer Caco-2 cells Oral bioavailability021001 nanoscience & nanotechnologyBioavailabilityCaco-2Settore CHIM/09 - Farmaceutico Tecnologico Applicativo030220 oncology & carcinogenesisNanoparticlessense organsEffluxCaco-2 Cells0210 nano-technologyhormones hormone substitutes and hormone antagonistsConjugateCarbohydrate polymers
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