Abstract
LC–MS–SUPPORTED ANALYTICAL ELUCIDATION AND EFFICACY PROFILING OF ARTEETHER IN PLASMODIUM FALCIPARUM CELL LINE CULTURES
Ghousia Begum*, Dr. Syed Ahmed Hussain, Nada Ahmed Al Amoodi, Fariya Sultana, Bilquis Begum, Somabatthini Shruthi, Ayesha Ayub Khan, Muskan Khatoon
ABSTRACT
This study evaluates the in vitro antiplasmodial efficacy and host-cell cytotoxicity of Arteether compared to Artemisinin in Plasmodium falciparum cultures maintained within human red blood cells (RBCs). A five-assay panel was employed to assess both parasite viability and erythrocyte safety. Parasite inhibition was measured using SYBR Green I fluorescence and parasite lactate dehydrogenase (pLDH) activity, while cytotoxicity was quantified via hemolysis, host LDH release, and Annexin V binding. Arteether demonstrated potent parasite inhibition (25–28% viability remaining) similar to Artemisinin (18–22%), confirming effective parasiticidal activity. However, Arteether induced markedly higher RBC damage, including hemolysis (21%), LDH release (27%), and eryptosis (31%), compared to Artemisinin’s minimal cytotoxicity (3–5%). These results reveal that Arteether, while retaining strong antiparasitic potency, exerts substantial erythrocyte toxicity, likely due to its lipophilic nature and enhanced membrane interaction. In contrast, Artemisinin remains highly selective for the parasite with negligible host-cell stress, reaffirming its superior therapeutic index for antimalarial applications.
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