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Novel compound identified for histoplasmosis treatment
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A new compound with antifungal properties, compound 41F5, is currently under investigation as a potential treatment option for naturally drug-resistant histoplasmosis and cryptococcosis infections.
In a pilot study, 41F5 was 60 times more toxic to fungal cells than human cells, successfully inhibited Histoplasma growth in liquid culture and protected infected host cells from Histoplasma-induced microphage death, Chad Rappleye, PhD, a microbiologist in the Center for Microbial Interface Biology at Ohio State’s Wexner Medical Center, and colleagues reported in Antimicrobial Agents and Chemotherapy.
“There are people here in the United States and around the world suffering from varying degrees of histoplasmosis that need a safer and better treatment option,” Rappleye said in a press release.
An estimated 100,000 Histoplasma infections occur each year in the United States, most of which are self-limited. However, each year a few thousand people develop chronic or life-threatening histoplasmosis infections. The only available antifungal treatment options have toxic side effects and can cost upward of $50,000 per patient.
So, Rappleye and colleagues developed a fluorescent staining technique and screened 3,600 commercially available small molecule compounds to identify agents that inhibited fungal but not human cells.
Among the seven compounds they identified that inhibited Histoplasma growth, compound 41F5 had the greatest selectivity for yeast relative to host with 50% inhibitory concentrations of 0.87 mcM. The compound consists of an aminothiazole core with an alicyclic substituent at the 2-position and an aromatic substituent at the 5-position.
Rappleye and colleagues are currently working with Werner Tjarks, PhD, a medicinal chemist at Ohio State University, to see whether 41F5’s selectivity and toxicity profile can be enhanced for further testing.
Disclosure: The researchers reported no relevant financial disclosures.
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