Dokumentdetails
ID
oai:HAL:hal-02924754v1
Thema
betulinic acid α-cyclodextrin influenza virus entry inhibitor [SDV.BBM]Life Sciences [q-bio]/Bio...Autor
Chen, Yingying Wang, Xinchen Zhu, Yinbiao Si, Longlong Zhang, Bo Zhang, Yongmin Zhang, Lihe Zhou, Demin Xiao, SulongLangue
enEditor
HAL CCSD;American Chemical Society
Kategorie
Wissenschaften: Lebenswissenschaften
Jahr
2020
Auflistungsdatum
15.12.2023
Schlüsselwörter
entry conjugate influenza virusZusammenfassung
International audience; Naturally occurring pentacyclic triterpenes, such as betulinic acid (BA) and its derivatives, exhibit various pharmaceutical activities and have been the subject of great interest, in particular for their antiviral properties.
Here, we found a new anti-influenza virus conjugate, hexakis 6-deoxy-6-[4-N-(3β-hydroxy-lup-20(29)-en-28-oate)aminomethyl-1H-1,2,3-triazol-1-yl]-2,3-di-O-acetyl-α-cyclodextrin (CYY1-11, 1), in a mini library of pentacyclic triterpene–cyclodextrin conjugates by performing a cell-based screening assay and then exploring the underlying mechanisms.
Our results showed that conjugate 1 possessed a high-level activity against the influenza virus A/WSN/33 with an IC50 value of 5.20 μM (SI > 38.4).
The study of the mechanism of action indicated that conjugate 1 inhibited viral replication by directly targeting the influenza hemagglutinin protein (KD = 1.50 μM), thus efficiently preventing the attachment of the virion to its receptors on host cells and subsequent infection.
This study suggests that multivalent BA derivatives have possible use as a new class of influenza virus entry inhibitors.
Chen, Yingying,Wang, Xinchen,Zhu, Yinbiao,Si, Longlong,Zhang, Bo,Zhang, Yongmin,Zhang, Lihe,Zhou, Demin,Xiao, Sulong, 2020, Synthesis of a Hexavalent Betulinic Acid Derivative as a Hemagglutinin- Targeted Influenza Virus Entry Inhibitor, HAL CCSD;American Chemical Society
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