Compunds That Can Lead To A New Generation Of Antimalarial Drugs Discovered By Scientists
In a study published yesterday in Science Express, the online magazine of Science journal, a new antimalarial drug class was proven more effective in treating malaria than any other compound available until now.
Most compounds that are used for treating malaria are active in the blood stage of the diseases and drugs that also target the liver stage of the disease present nasty side effects. The new antimalarial drug class, discovered by scientists proved to be very effective both in the blood and liver stage.
Up until now the research effort mainly focused on the blood stage of the disease, due to more affordable routine screening methods. The new drug class addresses and targets a new gene, fighting malaria in the liver stage. The study was conducted on mice and showed promising results.
Malaria remains one of the leading causes of death in many parts of the world, despite immense efforts to control it. Around 225 million people were living with malaria and 800.000 people lost their lives in 2010 alone.
Parasites are transmitted by mosquitoes bites. The parasites are present in the mosquito saliva and enter the human blood stream. They can also be transmitted during a blood transfusion or from mother to fetus during pregnancy. The most affected geographical areas are Africa, Asia and The Americas. The parasites invade the liver first (the first 30 minutes after the bite) then after around 8 days the parasite leaves the liver and attacks red blood cells, in which it multiplies causing them to rupture.
When red blood cells are ruptured, harmful toxins are released into the blood leading to fever, chills, other flu-like symptoms, fulminant hepatitis and acute kidney failure in some severe cases. If the sick person is bitten at this point, the parasite will invade the mosquito’s digestive system, which will be able to spread the disease.
In order for scientists to discover new compounds that can act on different stages of the parasite’s life cycle, they screened thousand of potential substances that were already known for acting against the parasite in the blood stage. Only a few compounds seemed to act on the liver stage also, demonstrating the fact that about 75 percent of the drugs used to treat malaria, were not effective in eliminating the disease.
The scientists then isolated the most effective drug class called imidazolopiperazine that was active both in blood and liver stages. The good news is that imidazolopiperazine drug class is not related to any antimalarial class available until now, and parasite resistance is very unlikely. When the new compound was administered to mice it managed to protect the liver and was superior to current available drugs regarding the blood stage of the disease.