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Artemisinin (ART) is an endoperoxide molecule derived from the medicinal plant <i>Artemisia annua</i> L. and is clinically used as an antimalarial drug. As a secondary metabolite, the benefit of ART production to the host plant and the possible associated mechanism are not understood. It has previously been reported that <i>Artemisia annua</i> L. extract or ART can inhibit both insect feeding behaviors and growth; however, it is not known whether these effects are independent of each other, i.e., if growth inhibition is a direct outcome of the drug’s antifeeding activity. Using the lab model organism <i>Drosophila melanogaster</i>, we demonstrated that ART repels the feeding of larvae. Nevertheless, feeding inhibition was insufficient to explain its toxicity on fly larval growth. We revealed that ART provoked a strong and instant depolarization when applied to isolated mitochondria from <i>Drosophila</i> while exerting little effect on mitochondria isolated from mice tissues. Thus, ART benefits its host plant through two distinct activities on the insect: a feeding-repelling action and a potent anti-mitochondrial action which may underlie its insect inhibitory activities.