London: It has been discovered by an international team of researchers that a novel compound can stop the growth of parasites Plasmodium falciparum known as malaria – the mosquito-dead disease that kills nearly 500,000 people every year in the world.
The study, published in the journal Science, noted that the compound called TCMDC-135051 can be developed by the multinational pharmaceutical company GlaxoSmithKline to eliminate the parasite carried with mosquito in all stages of its life cycle.
The researchers, including those from the Sao Paulo Brazilian Research Foundation (FAPESP), noted that the drug acted specifically on protein in the parasite called the chiclin-dependent protein kinase – PfCLK3 – not interfered with. on human proteins.
The researchers noted that PfCLK3 controlled the activity and production of other proteins that require the parasite to stay alive, and by blocking these, P. falciparum was killed.
According to the study, a ban on PfCLK3 not only affected the progressive stage of development of the parasite – when it increased in human cells, and symptoms occurred – but also in the sexual phase, when it can be transmitted back to mosquitoes, repeating the cycle by infecting others.
To identify compounds that focused specifically on PfCLK3 protein, the researchers carried out a large-scale automated chemical analysis – through a process called high-through screening.
In the process, they analyzed nearly 25,000 compounds and were selected by TCMDC-135051 as the main exclusivity associated with the parasite protein, which was very strong in this regard.
The study also noted that the compound was effective against other species of Plasmodium.
"We also tested it in mice infected by Plasmodium berghei. The results of this in vivo trial showed that the parasite was removed from the bloodstream after five days of infection," said Paulo Godoi, co-author of the study from the University of Campinas in Brazil.
Since the parasite and humans have proteins similar to the PfCLK3, which retains almost all processes in cells, the researchers carried out experiments to confirm that TCMDC-135051 was safe, and that they did not act on human forms. protein.
The researchers found that the human protein similar to PfCLK3 was the parasite than the protein called PRPF4B.
"We had PRPF4B interacting with the new molecule at different concentrations, and was able to prevent the human pressure even at the highest concentration," Godoi said.
The researchers noted that the compound is no longer a potential drug, and it must be submitted to more tests to prove that it can be used clinically.
"We need to improve the safety of the molecule even further. It will then be ready for trials in humans. This will take between three and five years," said Andrew Tobin, leading study at the University of Glasgow in the UK. UK.