Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.
Identifieur interne : 001601 ( Main/Exploration ); précédent : 001600; suivant : 001602Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.
Auteurs : Dae Wook Kim ; Kyung Hye Seo ; Marcus J. Curtis-Long ; Kyeong Yeol Oh ; Jong-Won Oh ; Jung Keun Cho ; Kon Ho Lee ; Ki Hun ParkSource :
- Journal of enzyme inhibition and medicinal chemistry [ 1475-6374 ] ; 2014.
Descripteurs français
- KwdFr :
- MESH :
- embryologie : Psoralea.
- pharmacologie : Phénols.
- Graines, Virus du SRAS.
English descriptors
- KwdEn :
- MESH :
- chemical , pharmacology : Phenols.
- chemistry : Seeds.
- drug effects : SARS Virus.
- embryology : Psoralea.
Abstract
Severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) is a key enzyme that plays an important role in SARS virus replication. The ethanol extract of the seeds of Psoralea corylifolia showed high activity against the SARS-CoV PLpro with an IC50 of value of 15 µg/ml. Due to its potency, subsequent bioactivity-guided fractionation of the ethanol extract led to six aromatic compounds (1-6), which were identified as bavachinin (1), neobavaisoflavone (2), isobavachalcone (3), 4'-O-methylbavachalcone (4), psoralidin (5) and corylifol A (6). All isolated flavonoids (1-6) inhibited PLpro in a dose-dependent manner with IC50 ranging between 4.2 and 38.4 µM. Lineweaver-Burk and Dixon plots and their secondary replots indicated that inhibitors (1-6) were mixed inhibitors of PLpro. The analysis of KI and KIS values proved that the two most promising compounds (3 and 5) had reversible mixed type I mechanisms.
DOI: 10.3109/14756366.2012.753591
PubMed: 23323951
Affiliations:
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Le document en format XML
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<front><div type="abstract" xml:lang="en">Severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) is a key enzyme that plays an important role in SARS virus replication. The ethanol extract of the seeds of Psoralea corylifolia showed high activity against the SARS-CoV PLpro with an IC50 of value of 15 µg/ml. Due to its potency, subsequent bioactivity-guided fractionation of the ethanol extract led to six aromatic compounds (1-6), which were identified as bavachinin (1), neobavaisoflavone (2), isobavachalcone (3), 4'-O-methylbavachalcone (4), psoralidin (5) and corylifol A (6). All isolated flavonoids (1-6) inhibited PLpro in a dose-dependent manner with IC50 ranging between 4.2 and 38.4 µM. Lineweaver-Burk and Dixon plots and their secondary replots indicated that inhibitors (1-6) were mixed inhibitors of PLpro. The analysis of KI and KIS values proved that the two most promising compounds (3 and 5) had reversible mixed type I mechanisms.</div>
</front>
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<name sortKey="Kim, Dae Wook" sort="Kim, Dae Wook" uniqKey="Kim D" first="Dae Wook" last="Kim">Dae Wook Kim</name>
<name sortKey="Lee, Kon Ho" sort="Lee, Kon Ho" uniqKey="Lee K" first="Kon Ho" last="Lee">Kon Ho Lee</name>
<name sortKey="Oh, Jong Won" sort="Oh, Jong Won" uniqKey="Oh J" first="Jong-Won" last="Oh">Jong-Won Oh</name>
<name sortKey="Oh, Kyeong Yeol" sort="Oh, Kyeong Yeol" uniqKey="Oh K" first="Kyeong Yeol" last="Oh">Kyeong Yeol Oh</name>
<name sortKey="Park, Ki Hun" sort="Park, Ki Hun" uniqKey="Park K" first="Ki Hun" last="Park">Ki Hun Park</name>
<name sortKey="Seo, Kyung Hye" sort="Seo, Kyung Hye" uniqKey="Seo K" first="Kyung Hye" last="Seo">Kyung Hye Seo</name>
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