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

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.

• Authors: 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
• Journal: Journal of enzyme inhibition and medicinal chemistry (J Enzyme Inhib Med Chem) Vol. 29 Issue 1 Pg. 59-63 (Feb 2014) ISSN: 1475-6374 [Electronic] England
• PMID: 23323951 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Phenols

Topics

• Phenols (pharmacology)
• Psoralea (embryology)
• Severe acute respiratory syndrome-related coronavirus (drug effects)
• Seeds (chemistry)