Novel Compounds to Treat Malaria May Also Alleviate Parasite Drug Resistance

Technology #32882

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Categories
Researchers
Debopam Chakrabarti, Ph.D.
External Link (med.ucf.edu)
Ratna Chakrabarti, Ph.D.
External Link (med.ucf.edu)
Amy Wright, Ph.D.
External Link (www.fau.edu)
Managed By
Brion Berman
Assistant Director 407.882.0342
Patent Protection
US Patent 9,181,251 B2

ID: 33963

US Patent Pending
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

New Marine-Based Compounds and Aurora Kinase Inhibitors May Effectively Combat Malaria

UCF researchers 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 anti-malarials, the new compounds can potentially be used to treat new cellular targets and inhibit the growth of drug-resistant Plasmodium parasites, such as P. falciparum.

Technical Details

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 0.6μM).

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 µM) 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

Benefits

  • Ability to act upon novel cellular targets
  • May alleviate the problem of drug resistance
  • May be used to treat or prevent one or more symptoms of malaria

Applications

Anti-malarial drugs and malaria therapy