BACCHARIN

Enzyme inhibitor

This anti-leukemia agent (FW = 562.61 g/mol; CAS 61251-97-6), also named (2'S,3'R,4'S, 7'R,9R,10S)-7'-deoxo-2'-deoxy-2',3':9,10-bisoxy-9,10- dihydro-4'-hydroxy-7'-[(R)-1-hydroxyethyl]verrucarin A, from the toxic South American plant known as green propolis (Baccharis megapotamica), is a likely mycotoxin that was later modified by Baccharis megapotamica. Baccharin is also a potent competitive inhibitor (Ki = 56 nM) of human aldo-keto reductase (AKR) 1C3, also known as 17β-hydroxysteroid dehydrogenase (Type 5) and prostaglandin F synthase. AKR is regarded as a druggable target in the treatment of prostate and breast cancers. Baccharin shows no significant inhibition toward the AKR1C1, AKR1C2, and AKR1C4 isoforms. Moreover, non-prenyl analogues of baccharin as selective and potent inhibitors for AKR1C3.