Abstract
LC–MS–ASSISTED CHARACTERIZATION AND PHARMACODYNAMIC INVESTIGATION OF ARTEMETHER IN PLASMODIUM FALCIPARUM CELL LINE CULTURES
Dr. Syed Ahmed Hussain*, Ghousia Begum, Nada Ahmed Al Amoodi, Fariya Sultana, Bilquis Begum, Somabatthini Shruthi, Ayesha Ayub Khan, Muskan Khatoon
ABSTRACT
This study compares the in vitro antimalarial activity and host-cell cytotoxicity of Artemether and Artemisinin in Plasmodium falciparum cultures maintained in human red blood cells (RBCs). A five-assay evaluation was performed to assess both parasite inhibition and erythrocyte safety. Parasite viability, measured via SYBR Green I fluorescence and parasite lactate dehydrogenase (pLDH) assays, revealed that Artemether retained 70–74% viability, while Artemisinin reduced viability to 18–22%, confirming its superior antiparasitic potency. Host-cell safety assays, including hemolysis, LDH release, and Annexin V binding, demonstrated minimal RBC damage for both agents (<10%), indicating excellent biocompatibility. These findings suggest that Artemisinin exhibits stronger antiplasmodial efficacy with similar host-cell safety, likely due to more efficient endoperoxide activation within the parasite’s heme environment. In contrast, Artemether displayed moderate activity, consistent with its slower conversion kinetics. Overall, Artemisinin outperformed Artemether in potency while maintaining a comparable safety margin, reinforcing its central role in artemisinin-based combination therapies (ACTs).
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