Abstract
Researchers at the University of Central Florida have identified new compounds that may treat malaria infections more effectively than current anti-malarial drugs. The malaria parasite, Plasmodium falciparum, has developed resistance to most anti-malarial treatments, including chloroquine and artemisinin. Since the UCF anti-malarial compounds have structures different from current antimalarials, the new compounds may have new cellular targets and have the ability to inhibit the growth of drug-resistant Plasmodium parasites, such as P. falciparum.
Technology 32882
UCF and Florida Atlantic University (FAU) researchers have isolated novel anti-malarial compounds from a library of enriched marine natural products, including cembranoid-type diterpenes, microsclerodermins, dercitamides and bis-indoles. Representative compound, Nortopsentin A, exhibits antiplasmodial activity against P. falciparum chloroquine-resistant Dd2 cells (IC50 0.6 micromole).
Technology 33963
UCF researchers have identified new anti-malarial compounds by 1) screening a library of optimized Aurora kinase inhibitors, and 2) repurposing human Aurora kinase proteins. Aurora kinase is a cell cycle regulatory protein involved in cell growth and development. The identified compounds inhibit the growth of chloroquine-resistant P. falciparum. These potent inhibitors (EC50 < 1 micromole) were identified in cell-based screening using SYBR Green I fluorescence-based assay.
Partnering Opportunity
The research teams are looking for partners to further develop the technologies for commercialization.
Stage of Development
Preclinical.
Benefit
Ability to act upon novel cellular targetsMay alleviate the problem of drug resistanceMay be used to treat or prevent one or more symptoms of malaria
Market Application
Anti-malarial drugs and malaria therapy
Publications
The Bis(Indolyl)Imidazole Alkaloid Nortopsentin A Exhibits Antiplasmodial Activity, American Society for Microbiology, Antimicrobial Agents and Chemotherapy, p. 2362–2364 May 2013 Volume 57 Number 5, doi:10.1128/AAC.02091-12.
Brochure
