SrasV1, Main, Exploration, bibRecord, 001601

Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.

Identifieur interne : 001601 ( Main/Exploration ); précédent : 001600; suivant : 001602

Phenolic 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 Park

Source :

Journal of enzyme inhibition and medicinal chemistry [ 1475-6374 ] ; 2014.

RBID : pubmed:23323951

Descripteurs français

KwdFr :
- Graines (), Phénols (pharmacologie), Psoralea (embryologie), Virus du SRAS ().
MESH :
- embryologie : Psoralea.
- pharmacologie : Phénols.
- Graines, Virus du SRAS.

English descriptors

KwdEn :
- Phenols (pharmacology), Psoralea (embryology), SARS Virus (drug effects), Seeds (chemistry).
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:

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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Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.

Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri

Pour générer des pages wiki

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