Synthesis and Biochemical Evaluation of Baicalein Prodrugs
- Authors
- Son, Sang-Hyun; Kang, Jinhong; Ahn, Myunghwan; Nam, Soyeon; Jung, Yong Woo; Lee, Ki Yong; Jeon, Young Ho; Byun, Youngjoo; Lee, Kiho
- Issue Date
- Sep-2021
- Publisher
- MDPI
- Keywords
- baicalein; carbamate; pharmacokinetics; prodrug
- Citation
- PHARMACEUTICS, v.13, no.9
- Indexed
- SCIE
SCOPUS
- Journal Title
- PHARMACEUTICS
- Volume
- 13
- Number
- 9
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/136735
- DOI
- 10.3390/pharmaceutics13091516
- ISSN
- 1999-4923
- 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.
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