(+)-Rugulosin is a type of dianthrone mycotoxin derived from fungi such as Penicillium species. (+)-Rugulosin shows markedly specific antibacterial activity and moderately antifungal activity[1].
In vitro, (+)-Rugulosin exhibited cytotoxicity ranging from sub-micromolar to low-micromolar levels against various tumor cells, with 24h IC50s in L929, HeLa KB3.1, A431, MCF-7, A549, PC-3, SKOV-3 were 1.84μM, 0.276μM, 0.683μM, 0.138μM, 1.106μM, 1.475μM, and 0.590μM, respectively[2].
In vivo, (+)-Rugulosin exhibited hepatotoxicity and chronic accumulation toxicity in mice. Subcutaneous injection at a dose of 100mg/kg/day for 3 days caused an increase in serum glutamic oxaloacetic transaminase (GOT) and damage to liver mitochondria and microsomes. Continuous oral administration (+)-Rugulosin at a dose of 50-100mg/kg/day for 32 days led to weight loss, liver function impairment and death. Long-term feed exposure to (+)-Rugulosin (1.5mg/5g diet/animal/day; 22 days) induced hepatic proliferative nodules and show weak liver carcinogenicity[3].
References:
[1]. Breen, J., et al. "Studies in the biochemistry of micro-organisms. 95. Rugulosin, a crystalline colouring matter of Penicillium rugulosum Thom." Biochemical Journal 60.4 (1955): 618.
[2]. Manzano, Joe Anthony H., et al. "Dimeric Anthraquinone Rugulosin A Induces Apoptosis in Lung Adenocarcinoma and Targets PI3K/AKT/MAPK Pathways In Silico." ACS Omega 11.12 (2026): 18744-18759.
[3]. UENO, Yoshio, et al. "Chronic toxicity and hepatocarcinogenicity of (+) rugulosin, an anthraquinoid mycotoxin from penicillium species: preliminary surveys in mice." The Journal of Toxicological Sciences 5.4 (1980): 295-302.