| Title | A New, Highly Effective And Selective Molecule To Fight Malaria | |
| Date | Tuesday August 14 2018, @10:49PM | |
| Author | Fnord666 | |
| Topic | ||
| from the dept. | ||
A novel laboratory-synthesized molecule, based on natural compounds known as marinoquinolines found in marine gliding bacteria, is a strong candidate for the development of a new antimalarial drug.
In tests, the molecule proved capable of killing even the strain that resists conventional antimalarials. The molecule displays low toxicity and high selectivity, acting only on the parasite and not on other cells of the host organism.
The molecule was developed in Brazil at the Center for Research and Innovation in Biodiversity and Drug Discovery (CIBFar). The researchers tested the molecule in strains cultured in vitro as well as in mice using Plasmodium berghei, since mice are immune to infection by Plasmodium falciparum, which causes the most aggressive type of malaria.
"In mice, the number of parasites in the bloodstream (parasitemia) had fallen 62 percent by the fifth day of the test. After 30 days, all the mice given doses of the molecule were still alive," said Rafael Guido, a professor at the University of São Paulo's São Carlos Physics Institute (IFSC-USP).
Guido co-authors an article published in the Journal of Medicinal Chemistry, in which the researchers describe the molecule's inhibitory action in the blood and liver stages of the parasite's asexual cycle, which is responsible for the signs and symptoms of the disease.
[...] According to Duarte Correia, the first 50 molecules developed from marinoquinolines were tested in the FAPESP-supported study. "This work hasn't ended with this publication. We're still developing other compounds," he said.
The researchers are also characterizing the potential of this class to treat malaria caused by P. vivax, the most prevalent form in Brazil and are developing the pharmacokinetic part of the project (how drugs move through the organism).
"If the pharmokinetic properties, especially solubility, absorption, distribution, metabolism and excretion, aren't adequate, the compound can build up in the organism and become toxic to the patient, making it inappropriate for treatment. After completing this step, we plan to perform preclinical and clinical trials," Guido said.
Anna Caroline Campos Aguiar et al, Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity, Journal of Medicinal Chemistry (2018). DOI: 10.1021/acs.jmedchem.8b00143 Read more at: https://phys.org/news/2018-08-highly-effective-molecule-malaria.html#jCp
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