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Xanthones as P-glycoprotein modulators and their impact on drug bioavailability
- Publication Year :
- 2021
- Publisher :
- Taylor & Francis, 2021.
-
Abstract
- Introduction: P-glycoprotein (P-gp) is an important efflux pump responsible for the extruding of many endogenous and exogenous substances out of the cells. P-gp can be modulated by different molecules – including xanthone derivatives – to surpass the multidrug resistance (MDR) phenomenon through P-gp inhibition, or to serve as an antidotal strategy in intoxication scenarios through P-gp induction/activation. Areas covered: This review provides a perspective on P-gp modulators, with particular focus on xanthonic derivatives, highlighting their ability to modulate P-gp expression and/or activity, and the potential impact of these effects on the pharmacokinetics, pharmacodynamics and toxicity of P-gp substrates. Expert opinion: Xanthones, of natural or synthetic origin, are able to modulate P-gp, interfering with its protein synthesis or with its mechanism of action, by decreasing or increasing its efflux capacity. These modulatory effects make the xanthonic scaffold a promising source of new derivatives with therapeutic potential. However, the mechanisms beyond the xanthones-mediated P-gp modulation and the chemical characteristics that make them more potent P-gp inhibitors or inducers/activators are still understudied. Furthermore, a new window of opportunity exists in the neuropathologies field, where xanthonic derivatives with potential to modulate P-gp should be further explored to optimize the prevention/treatment of brain pathologies.
- Subjects :
- Xanthones
Biological Availability
Endogeny
Pharmacology
Toxicology
030226 pharmacology & pharmacy
03 medical and health sciences
0302 clinical medicine
Pharmacokinetics
Animals
Humans
Drug Interactions
Inducer
ATP Binding Cassette Transporter, Subfamily B, Member 1
P-glycoprotein
Brain Diseases
biology
Chemistry
food and beverages
General Medicine
Bioavailability
Pharmaceutical Preparations
030220 oncology & carcinogenesis
biology.protein
Efflux
Subjects
Details
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....8ef283108484da593695aa411167ad5d
- Full Text :
- https://doi.org/10.6084/m9.figshare.14455854.v1