Biological Activity
AS-2077715 is a fungal metabolite and an inhibitor of fungal mitochondrial complex III (cytochrome bc1; IC50 = 80 ng/ml for T. mentagrophytes complex III).1 It is selective for fungal over mammalian complex III (IC50s = 480 and 860 ng/ml for murine EL-4 cell and human Jurkat cell complex III, respectively). AS-2077715 inhibits ATP production in (IC50 = 0.33 μg/ml) and is fungicidal against T. mentagrophytes when used at concentrations of 1 and 10 μg/ml. In vivo, AS-2077715 (10 and 20 mg/kg) reduces the number of foot pad skin colony forming units (CFUs) in a guinea pig model of T. mentagrophytes infection.2
References
1.Ohsumi, K., Watanabe, M., and Fujie, A.AS2077715 Is a selective inhibitor of fungal mitochondrial cytochrome Bc? complexJ. Antibiot. (Tokyo)67(10)713-716(2014)
2.Ohsumi, K., Murai, H., Nakamura, I., et al.Therapeutic efficacy of AS2077715 against experimental tinea pedis in guinea pigs in comparison with terbinafineJ. Antibiot. (Tokyo)67(10)717-719(2014)
