AmAT19, an acetyltransferase from Astragalus membranaceus, catalyses specific 6α-OH acetylation for tetracyclic triterpenes and steroids.
Org Biomol Chem
; 19(33): 7186-7189, 2021 09 07.
Article
in English
| MEDLINE | ID: covidwho-1559295
ABSTRACT
Tetracyclic triterpenes and steroids are pharmacologically important molecules, and acetylation could improve their bioactivities. In this study, a highly regio- and stereo-specific acetyltransferase, AmAT19, was discovered from Astragalus membranaceus. AmAT19 could selectively catalyze the 6α-OH acetylation of four tetracyclic triterpenes and steroids. The strict selectivity is associated with different orientations of the 6α/ß-OH as indicated by molecular docking. Acetylated products 1a, 3a and 4a remarkably increased the inhibitory activity against the 3-chymotrypsin-like protease (3CLpro) of SARS-CoV-2, compared to 1, 3, and 4. AmAT19 could be a promising catalyst for specific 6α-OH acetylation to expand the molecular diversity of triterpenes and steroids.
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Acetyltransferases
/
Steroids
/
Triterpenes
/
Astragalus Plant
Language:
English
Journal:
Org Biomol Chem
Journal subject:
Biochemistry
/
Chemistry
Year:
2021
Document Type:
Article
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