Heptelidic acid

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic^[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases^[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC₅₀of 90 μM^[3]. In Vitro: Heptelidic acid is a sesquiterpene antibiotic, found in the culture filtrate of three different strains of fungi isolated from soil samples. Heptelidic acid produces organisms, fermentation, isolation and characterization^[1].
Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells^[2].Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC₅₀ value of 40 μM after 8 h of Etoposide treatment^[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from the Trichoderma fungus, can directly bind to the active site of human GAPDH. The expression of T. koningii KAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressing T. koningii KAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC₅₀=5 μM^[3]. In Vivo: Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo^[3].