(+)-Rugulosin is a pigment and mycotoxin produced by certain fungi. It inhibits HIV-1 integrase activity with IC50 values of 19 and 25 μM in coupled and strand transfer assays, respectively. It also inhibits ribonuclease H in rat liver by 83% at a concentration of 157 μM and ribonucleases H1, H2, and H3 in T. pyriformis by 100, 99, and 100%, respectively, at a concentration of 313 μM. (+)-Rugulosin leads to hepatic injury and liver cell hyperplasia in mice when administered in the diet. It is cytotoxic to insect cells but not mammalian C6/36, L929, and HepG2 cells (ID50s = 1.2, >200, 23.7, and >200 μg/ml, respectively).
(+)-Rugulosin is an intense yellow pigment produced by some species of Penicillium, Aspergillus and the fungal symbiotants of some lichens. (+)-Rugulosin shows antibacterial and insecticidal activity and has found application as a bioinsecticide, notably as the active secondary metabolite in endophytic fungi of seedlings.
