Compunds That Can Lead To A New Generation Of Antimalarial Drugs Discovered By Scientists
In aÂ study published yesterday in Science Express, theÂ online magazine of Science journal, a new antimalarial drug class was proven more effective in treating malaria than any other compoundÂ available until now.
Most compoundsÂ that are used for treating malaria are active in the blood stage of the diseases and drugs that also target the liver stage of theÂ diseaseÂ 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 mainlyÂ focused on the blood stage of the disease, due to more affordableÂ routine screening methods. The new drug class addresses and targets a newÂ 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, despiteÂ immense efforts to control it. Around 225 million people were living with malaria andÂ 800.000Â people lost their livesÂ in 2010 alone.
Parasites are transmitted by mosquitoesÂ bites.Â The parasitesÂ are present in theÂ mosquito saliva andÂ enter the human blood stream. They can alsoÂ 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) thenÂ after around 8 days the parasite leaves the liver and attacksÂ red blood cells, inÂ whichÂ itÂ multipliesÂ causing them toÂ rupture.
When redÂ bloodÂ cells are ruptured, harmfulÂ toxins are released into the blood leading to fever, chills, other flu-like symptoms, fulminant hepatitisÂ 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,Â which will be ableÂ to spread the disease.
In order for scientists to discover new compoundsÂ 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 fewÂ compounds seemed toÂ 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 theÂ most effective drug class called imidazolopiperazineÂ that was active both in blood and liver stages.Â The good news is thatÂ imidazolopiperazineÂ drug class is not related to any antimalarialÂ class available until now, and parasiteÂ resistance is veryÂ unlikely. When theÂ new compoundÂ was administeredÂ to mice it managed to protect the liverÂ and was superior to current available drugsÂ regarding theÂ blood stage of the disease.