World Journal of
Pharmaceutical and Life Sciences

LC–MS–GUIDED ANALYTICAL AND MECHANISTIC EXPLORATION OF ARTEMISONE 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 compares the in vitro antiplasmodial efficacy and erythrocyte cytotoxicity of Artemisone and Artemisinin in Plasmodium falciparum–infected human red blood cells (RBCs). A five-assay evaluation was conducted to quantify parasite viability and host-cell safety. Parasite inhibition was determined using SYBR Green I fluorescence and parasite lactate dehydrogenase (pLDH) activity assays, while RBC integrity was assessed via hemolysis, host LDH release, and Annexin V binding assays. Artemisinin exhibited potent antimalarial activity, reducing parasite viability and metabolic activity to 18–22%, whereas Artemisone retained 79–81% viability, indicating weak antiparasitic potency. Both compounds showed minimal RBC toxicity, with Artemisone causing slightly higher eryptosis (12%) and LDH release (9%) than Artemisinin (5% and 4%, respectively). These findings suggest that Artemisinin demonstrates superior antiplasmodial efficacy and better selectivity, while Artemisone exhibits reduced potency but maintains acceptable host-cell tolerance. The data emphasize the structural influence of side-chain modifications on activity and highlight the need for optimization of Artemisone analogs to improve parasiticidal strength without compromising erythrocyte compatibility.

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