In-vitro evaluation of antileishmanial activity and toxicity of artemether with focus on its apoptotic effect

Artemisinin and its derivatives are very important new class of antimalarial drugs. One of the most important artemisinin derivatives is artemether. The antiparasitic activity of artemether as a derivative of artemisinin is related to endoperoxide bridge in its structure. The aim of this study was the evaluation of antileishmanial effect of artemether, with more focus on its apoptotic effect. In this study we used artemether in concentration of 5, 10, 25, 50 and 100 microg/mL for promastigote assay, promastigote proliferation measurements by MTT assay, detection of apoptotic cells by Flow cytometry analysis and DNA ladder assay. The application of artemether, promastigote IC[50] was measured as 25 microg/mL. The percentage of apoptotic promastigotes by using 25 microg/mL of artemether was 42.28. The results of present study showed that artemether has inhibition effect on intracellular and extracellular growth of Leishmania major. Promastigotes of Leishmania major undergo apoptosis after exposure to artemether

effect of artemether-induced apoptosis in promastigotes of leishmania major [MRHO/IR/75/ER] under in-vitro conditions

Leishmaniasis is one of the significant causes of morbidity and mortality in several countries. It is an important problem in endemic areas such as Iran. The goal in treatment of leishmaniasis is to reduce the disease period and leave no evidence of any remaining scars or lesions. A derivative of artemisinin is artemether. Scientists believe that the strong action of artemether against parasites is due to the presence of an endoperoxide bridge. Due to problems in the treatment of Leishmania major, in this research we have studied the effect of artemether on Leishmania major under in vitro conditions. Parasites were cultured in NNN and RPMI, after which artemether at concentrations of 5, 10, 25, 50 and 100 microg/ml were used for the promastigote assay. Apoptosis was detected by flow cytometry and DNA ladder assay. The inhibitory concentration [IC50] of artemether was determined to be 25 microg/ml. The percentage of apoptotic promastigotes at 25 imcrog/ml of artemether was 42.28. The results of DNA fragmentation show that exposure of Leishmania major promastigote cells to 25 microg/ml of artemether lead to DNA fragmentation. We have proven the effect of artemether on apoptosis of Leishmania major by flow cytometry and the DNA ladder assay