RUGULOSIN

(+)-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 (+ form) is an intense yellow pigment produced by Penicillium and Aspergillus.

(+)-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.

ChEBI: Rugulosin is a cyclic ketone and an organic polycyclic compound.

[1] Y UENO. Chronic toxicity and hepatocarcinogenicity of (+) rugulosin, an anthraquinoid mycotoxin from penicillium species: preliminary surveys in mice.[J]. Journal of Toxicological Sciences, 1980, 5 4: 295-302. DOI: 10.2131/jts.5.295
[2] SHEO B SINGH. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites.[J]. Journal of Industrial Microbiology & Biotechnology, 2003, 30 12: 721-731. DOI: 10.1007/s10295-003-0101-x
[3] F TASHIRO  Y U  K Hiral. Inhibitory effects of carcinogenic mycotoxins on deoxyribonucleic acid-dependent ribonucleic acid polymerase and ribonuclease H.[J]. Applied and Environmental Microbiology, 1979, 38 2: 191-196. DOI: 10.1128/aem.38.2.191-196.1979
[4] PATRICIA WATTS . Cytotoxicity against insect cells of entomopathogenic fungi of the genera Hypocrella (anamorph Aschersonia): possible agents for biological control[J]. Mycological research, 2003, 107 5: Pages 581-586. DOI: 10.1017/s0953756203007846