Objective: Chloroquine is used as conventional drug therapy for the treatment of malaria. The existence of resistance for chloroquine shown among various species of Plasmodium leads to the search for more efficacious therapy to treat malaria. Probiotics (Lactobacillus casei) have been tried as add-on therapy with chloroquine. Probiotics are ingested microorganisms associated with a beneficial effect on humans and other species. The study was done to check the efficacy of probiotics as an add-on therapy along with conventional drug therapy (chloroquine) to treat malaria.Results: Probiotics in combination with chloroquine showed complete suppression in parasitemia count. Representation of parasitemia count was done using mean ± SD. P<0.05 is considered significant. The results showed a reduction in parasitemia with probiotics treatment, which was further confirmed through histological observation of two major organs liver and spleen. Interestingly, further suppression of parasitemia and hemosiderosis was observed when probiotics were given along with chloroquine.
Objective: Malaria is a major global health concern with the urgent need for new treatment alternatives due to the alarming increase of drug-resistant Plasmodium strains. Chalcones and its derivatives are important pharmacophores showing antimalarial activity. Substandard pharmacokinetic variables are often responsible for insufficient therapeutic effect. Determination of the pharmacokinetic variables at the preliminary step of drug development for any drug candidates is an essential component of in vivo antimalarial efficacy tests. Therefore, three chalcone derivatives, 1, 2, and 3, having antimalarial potency were studied further for potential therapeutic efficacy. Results: In vivo pharmacokinetic studies of these three derivatives were performed on New Zealand White rabbits. The three derivatives were administered intra-peritoneally or orally at effective dose concentration and blood samples at different time points were collected. The determination of drug concentration was done through reverse phase-high performance liquid chromatography. The peak plasma concentration of derivative 1, 2, and 3 were 1.96 ± 0.46 µg/mL, 69.89 ± 5.49 µg/mL, and 3.74 ± 1.64 µg/mL. The results indicate a very low bioavailability of these derivatives. The present study gives a benchmark to advance the investigation of more derivatives in order to revamp the pharmacokinetic variables while maintaining both potency and metabolic constancy.
Objective Chalcones (1, 3-diaryl-2-propen-1-ones) and its derivatives are widely explored from the past decade for its antimalarial activity. To elucidate their mechanism of action on the malaria parasite, the ultrastructural changes with the action of these derivatives in different organelles of the parasite were studied in vitro. Infected RBCs (CQ sensitive (MRC-2) and CQ resistant (RKL-9) Plasmodium strain) were treated with three chalcone derivatives 2, 6 and 7 and standard drugs, i.e., CQ and artemisinin at twice their respective IC50 values for 24 h and then harvested, washed, fixed, embedded and stained to visualize ultra-structure changes before and after intervention of treatment under in vitro condition through transmission electron microscope.Results The ultrastructural changes demonstrate the significant disturbance of all parasite membranes, including those of the nucleus, mitochondria and food vacuole, in association with a marked reduction of ribosomes in the trophozoites and cessation of developing schizonts which suggest multiple mechanisms of action by which chalcone derivatives act on the malaria parasite. The present study opens up perspectives for further exploration of these derivatives in vivo malaria model to discover more about its effect and mechanism of action.
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