AI Article Synopsis
- Baicalein is a flavonoid with multiple health benefits, including antioxidant, antiproliferative, and anti-inflammatory effects, and shows promise in treating asthma and atopic dermatitis.
- Rapid metabolism of baicalein to inactive forms limits its clinical use, necessitating the development of alternative formulations.
- The study successfully designed and tested new baicalein prodrugs that enhance its plasma levels in mice, suggesting a viable path for creating effective oral forms of baicalein.
Article Abstract
Baicalein (5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one), a flavonoid analog from , 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--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 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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8472512 | PMC |
| http://dx.doi.org/10.3390/pharmaceutics13091516 | DOI Listing |
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- Rapid metabolism of baicalein to inactive forms limits its clinical use, necessitating the development of alternative formulations.
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