Anti-plasmodial and chloroquine resistance suppressive effects of embelin

Abstract

Background:Emergence of chloroquine (CQ) resistance among different strains of Plasmodium falciparum is the worst catastrophe that has ever perplexed the dedicated efforts to eradicate malaria. This urged the scientists to search for new alternatives or sensitizers to augment its antiplasmodium effect.Materials and Method:In this experiment, the potential of embelin, isolated from Embelia ribes, to inhibit the growth and sensitize CQ action was screened using SYBRE-green-I based drug sensitivity and isobologram assays, respectively. Its effect on red blood cells stability was screened to assess its safety. To explore its molecular mechanism, its effect on plasmodial Hemozoin and the in vitro β-hematin formation was screened as well. Furthermore, its anti-oxidant activity was measured using the conventional in vitro tests and its molecular characters were obtained using Molispiration program.Results:The results showed that its anti-plasmodial effect was weaker than CQ but synergism was obtained when they were combined at ratios lower than 5:5 CQ/embelin. Furthermore, β-hematin formation was inhibited by embelin without showing any synergism after mixing with CQ.Conclusion:Overall, embelin is not ideal to be suggested as a conventional antiplasmodium but it has a potential to ameliorate CQ resistance. Furthermore, its action is not related to its impact on hemozoin formation. Further, investigations are recommended to illustrate its detailed mechanism of action.Abbreviation used: CQ-DV-PBS-HEPES: Chloroquine-Digestive vacuole-Phosphate-buffer-saline-4-(2-hydroxyethyl-1-piperazin-ethan-sulphoni-acid), EDTA: Ethylen-diamin-tetra-acetic-acid, g.m.wt: Gram molecular weight, cMCM: Complete-malaria-culture-medium, Hct: Hematocrite, PRBCs: Parasitized-redblood-cells, nRBCs: Normal-red-blood-cells, RT: Room temperature, IC: Inhibitory concentration, FIC: Fractional inhibitory concentration, iCM: Incomplete-culturemedium, BSA: Bovin serum albumin, MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, DPPH: 2,2-diphenyl-1- picrylhydrazy, BHT: Butylatedhydroxyl-toleuen, PSA: Polar surface area, ClogP: Log partition coefficient (octanol/water), GPCR: G-protein-coupled-receptors, DMSO: Dimethylsulphoxide, NaOH: Sodium hydroxide

Antibacterial and Anti-Quorum Sensing Properties of Silver Nanoparticles Phytosynthesized Using Embelia ruminata

“…This result may be due to the solubility of phytocompounds in the extracting solvent. Embelin, the principal compound of the genus Embelia , has a lipophilic affinity [ 71 , 72 ]. It is possible that embelin and other lipophilic compounds were not soluble in the aqueous extraction process for Ag nanosynthesis [ 73 ].…”

Active Compounds and Antimalaria Properties of some Medicinal Plants in Indonesia – A Review

“…Currently, plasmodium parasites are showing resistance to chloroquine and some antimalarial compounds. 3 Therefore, new antimalarial drugs that could effectively combat the presence of plasmodium are direly needed. Compounds derived from medicinal plants have been used to treat diseases since ancient time and currently it is used as a substance of modern medicine.…”

Design, synthesis, antifungal activity, and 3D-QSAR of coumarin derivatives

“…They exhibit a broad spectrum of biological activities, including anticancer, antioxidant, antiplasmodial, antimalarial, antivirus, antibacterial, and antifungal. [1][2][3][4][5][6][7] The varied pharmacological activities and relatively simple structures of these compounds have spurred great interest in their possible therapeutic uses. In addition to coumarin's use as the lead compound for the preparation of potent pharmacological molecules, it has also received considerable research attention for its interesting insecticidal, nematicidal, allelopathic, and antimicrobial activities in agriculture.…”