Brazilian study could lead to new drug production for malaria

Research has shown that the molecule, derived from the clbad of marinoquinolines, has shown selectivity and low toxicity, acting on the parasite [o protozoário causador da malária] and not on any other cells of the host. It was developed at the Center for Research and Innovation in Biodiversity and Drugs (CIBFar) – a Center for Research, Innovation and Dissemination (Cepid) funded by FAPESP. The study also received financial support from the National Council for Scientific and Technological Development (CNPq) and the Serrapilheira Institute

"A few years ago, Professor Roque is already working with a clbad of molecules , natural marine products, marinoquinolines bacteria, and a work has been published for some time on the anti-infectious activity of these molecules, "explained Guido

However, natural products had a moderate or low action against pathogens. But for this study, the power of the molecules has been increased. The initial goal was to increase the potency of the molecules because they were weak.

"We needed a molecule that could kill the parasite and be a candidate, and we finally got a molecule that was powerful enough, a low concentration, that is, say a small amount that would kill the parasite, "said Guido. "And more importantly, we have been able to make the molecule selective, kill the parasite without killing the cells or be toxic to human cells."

During the study, the researchers began to observe that in addition, this molecule also had another advantage: it acted on more than one form of parasite. "We could see that this molecule not only killed that form [de parasita] that was in the blood, but also killed the form that was in the liver," said the professor.

The molecule has also been successful in killing drug-resistant strains. Currently, the most widely used drug in the treatment of malaria is artemisinin, which, although effective, already exists over the years. "Although we have a cure for this disease, and it is effective, we have already begun to see the emergence of strains resistant to this drug," says Guido

It's while the researchers have discovered another benefit of the molecule. "We can see that malaria, being a parasite that has existed for a long time, can generate resistance to the drugs currently used, so we need new treatments, so we tested against resistant strains of the parasite, those that are no longer sensitive. to the drug and we were able to show that this molecule was also able to kill these resistant parasites. "

So, Guido said, there is a powerful molecule to kill the parasite, which killed the resistant and was quite selective

Tests ]

Up to now, studies have been carried out in the laboratory and also tested on mice affected by malaria. Studies have focused on malaria caused by the protozoan Plasmodium falciparum . "The untreated group [de camundongos doentes] died about 15 or 20 days old, and the treated mice survived for 30 days of experimentation, showing that the molecule was well tolerated by the body and did not become toxic. And the treated group, in addition to surviving during this time of study, had a reduced parasite load in the blood, "he said, speaking of the results of animal testing.

Several steps are still needed – and years of study and testing – so that the drug is tested in humans and produced. Until now, studies have been conducted on the most lethal form of malaria, and it remains necessary to evaluate other forms of protozoa, such as Plasmodium vivax more widespread in Brazil. "We have not published these results yet, but we have seen that this molecule can also kill vivax ."

According to Guido, another necessary step is to develop the pharmacokinetic part of the project – drug, that is, to improve the characteristics of this molecule so that it can be administered orally. "It must enter our body, be absorbed by the intestine and be distributed – because the parasite is in the bloodstream, metabolized, eliminated, excreted – we improve these characteristics of the molecules."

"Si you could do that, you would have a preclinical candidate, and then we would go to clinical trials, "he added. He recalled, however, that all these processes and steps can still make it 10 to 15 years for the drug to be produced.

Malaria

Malaria is a feverish infectious disease caused by protozoa transmitted by the female infected mosquito Anopheles . According to the Ministry of Health, everyone can contract malaria, but healing is possible if the disease is treated in a timely and appropriate manner. However, malaria can progress to a severe form and death.

The symptoms usually badociated with malaria are high fever, chills, tremors, sweating and headaches, which can occur cyclically. Many people experience nausea, vomiting, fatigue and a lack of appetite.

The disease currently kills an estimated 445,000 people each year, according to the World Health Organization (WHO). "By dividing this number by the number of minutes in the year, we perceive the reason for [quase] one death [por malária] every minute," said Guido. Malaria is the deadliest parasite in the world. "If we do nothing today, he will kill many more in a few years," he added.

Most deaths occur in Africa, most of them children. According to the professor, among those who die, 75% are children. "This study has a huge social impact," he said.

Edition: Nádia Franco