Antimycin A4

Antimycin A4 (CAS No.: 27220-59-3) is an antibiotic compound derived from Streptomyces sp. Its core therapeutic targets include ATP-citrate lyase and the electron transport chain between cytochromes b and c₁ in the mitochondrial respiratory chain, with an inhibition constant (Ki) of 64.8 μM against magnesium citrate, the substrate of ATP-citrate lyase. The harvested concentration after 4 days of in vitro fermentation culture is 3.5 μg/mL, and the effective inhibitory concentration in in vitro experiments is around its Ki value (64.8 μM). Its biological activities are mainly reflected in inhibiting the activity of ATP-citrate lyase, blocking the biosynthesis of fatty acids and cholesterol, and is expected to reduce serum triglyceride and low-density lipoprotein cholesterol levels. Meanwhile, it has antibacterial activity, inhibits eukaryotic energy metabolism, and can be used as a commercial fungicide. In addition, it is a commonly used tool compound for studying the mitochondrial respiratory chain and energy metabolism. Its chemical structure contains a carboxyphenol amide unit, a nine-membered cyclic bis-lactone, and specific alkyl side chains.

References:

[1] Barrow CJ, Oleynek JJ, Marinelli V, Sun HH, Kaplita P, Sedlock DM, Gillum AM, Chadwick CC, Cooper R. Antimycins, inhibitors of ATP-citrate lyase, from a Streptomyces sp. J Antibiot (Tokyo). 1997 Sep;50(9):729-33. doi: 10.7164/antibiotics.50.729. PMID: 9360616.