Synthesis and Biochemical Evaluation of Baicalein Prodrugs
DC Field | Value | Language |
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dc.contributor.author | Son, Sang-Hyun | - |
dc.contributor.author | Kang, Jinhong | - |
dc.contributor.author | Ahn, Myunghwan | - |
dc.contributor.author | Nam, Soyeon | - |
dc.contributor.author | Jung, Yong Woo | - |
dc.contributor.author | Lee, Ki Yong | - |
dc.contributor.author | Jeon, Young Ho | - |
dc.contributor.author | Byun, Youngjoo | - |
dc.contributor.author | Lee, Kiho | - |
dc.date.accessioned | 2022-02-24T11:40:37Z | - |
dc.date.available | 2022-02-24T11:40:37Z | - |
dc.date.created | 2022-02-07 | - |
dc.date.issued | 2021-09 | - |
dc.identifier.issn | 1999-4923 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/136735 | - |
dc.description.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. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | MDPI | - |
dc.subject | SCUTELLARIAE RADIX | - |
dc.subject | METABOLISM | - |
dc.subject | EXPRESSION | - |
dc.title | Synthesis and Biochemical Evaluation of Baicalein Prodrugs | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Jung, Yong Woo | - |
dc.contributor.affiliatedAuthor | Lee, Ki Yong | - |
dc.contributor.affiliatedAuthor | Jeon, Young Ho | - |
dc.contributor.affiliatedAuthor | Byun, Youngjoo | - |
dc.contributor.affiliatedAuthor | Lee, Kiho | - |
dc.identifier.doi | 10.3390/pharmaceutics13091516 | - |
dc.identifier.scopusid | 2-s2.0-85115355762 | - |
dc.identifier.wosid | 000700924500001 | - |
dc.identifier.bibliographicCitation | PHARMACEUTICS, v.13, no.9 | - |
dc.relation.isPartOf | PHARMACEUTICS | - |
dc.citation.title | PHARMACEUTICS | - |
dc.citation.volume | 13 | - |
dc.citation.number | 9 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | METABOLISM | - |
dc.subject.keywordPlus | SCUTELLARIAE RADIX | - |
dc.subject.keywordAuthor | baicalein | - |
dc.subject.keywordAuthor | carbamate | - |
dc.subject.keywordAuthor | pharmacokinetics | - |
dc.subject.keywordAuthor | prodrug | - |
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