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Synthesis and Biochemical Evaluation of Baicalein Prodrugs
- Source :
- Pharmaceutics, Vol 13, Iss 9, p 1516 (2021)
- Publication Year :
- 2021
- Publisher :
- MDPI AG, 2021.
-
Abstract
- Baicalein (5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one), a flavonoid analog from Scutellaria baicalensis, possesses several pharmacological activities including antioxidant, antiproliferative, and anti-inflammatory activities. We previously reported that baicalein inhibits the thymic stromal lymphopoietin (TSLP)/TSLP receptor (TSLPR) signaling pathways and can be used as an active ingredient in the treatment of asthma and atopic dermatitis. However, baicalein is rapidly metabolized to baicalin and baicalein-6-O-glucuronide in vivo, which limits its preclinical and clinical use. In this study, we designed, synthesized, and evaluated baicalein prodrugs that protect the OH group at the 7-position of the A ring in baicalein with the amino acid carbamate functional group. Comprehensive in vitro and in vivo studies identified compound 2 as a baicalein prodrug candidate that improved the plasma exposure of baicalein in mouse animal studies. Our results demonstrated that this prodrug approach could be further adopted to discover oral baicalein prodrugs.
- Subjects :
- baicalein
prodrug
carbamate
pharmacokinetics
Pharmacy and materia medica
RS1-441
Subjects
Details
- Language :
- English
- ISSN :
- 19994923
- Volume :
- 13
- Issue :
- 9
- Database :
- Directory of Open Access Journals
- Journal :
- Pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.226a823bea14203acaebd6c0ae238ee
- Document Type :
- article
- Full Text :
- https://doi.org/10.3390/pharmaceutics13091516