Anti-plasmodial and chloroquine resistance suppressive effects of embelin

O. I. Zaid, R. Abd Majid, Hasidah Mohd. Sidek, M. N. Sabariah, K. Al-Zihiry, Sattar Rahi, R. Basir

Research output: Contribution to journalArticle

1 Citation (Scopus)

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.

Original languageEnglish
Pages (from-to)S48-S55
JournalPharmacognosy Magazine
Volume13
Issue number49
DOIs
Publication statusPublished - 1 Jan 2017

Fingerprint

Chloroquine
Hemin
Dimethyl Sulfoxide
Malaria
Embelia
Erythrocytes
Ribes
HEPES
Octanols
Butylated Hydroxytoluene
Sodium Hydroxide
embelin
Plasmodium falciparum
G-Protein-Coupled Receptors
Vacuoles
Oxidants
Serum Albumin
Edetic Acid
Acetic Acid
Culture Media

Keywords

  • Chloroquine
  • embelin
  • isobologram
  • Plasmodium falciparum
  • resistance
  • SYBR-green-I

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

Cite this

Zaid, O. I., Majid, R. A., Mohd. Sidek, H., Sabariah, M. N., Al-Zihiry, K., Rahi, S., & Basir, R. (2017). Anti-plasmodial and chloroquine resistance suppressive effects of embelin. Pharmacognosy Magazine, 13(49), S48-S55. https://doi.org/10.4103/0973-1296.203982

Anti-plasmodial and chloroquine resistance suppressive effects of embelin. / Zaid, O. I.; Majid, R. Abd; Mohd. Sidek, Hasidah; Sabariah, M. N.; Al-Zihiry, K.; Rahi, Sattar; Basir, R.

In: Pharmacognosy Magazine, Vol. 13, No. 49, 01.01.2017, p. S48-S55.

Research output: Contribution to journalArticle

Zaid, OI, Majid, RA, Mohd. Sidek, H, Sabariah, MN, Al-Zihiry, K, Rahi, S & Basir, R 2017, 'Anti-plasmodial and chloroquine resistance suppressive effects of embelin', Pharmacognosy Magazine, vol. 13, no. 49, pp. S48-S55. https://doi.org/10.4103/0973-1296.203982
Zaid, O. I. ; Majid, R. Abd ; Mohd. Sidek, Hasidah ; Sabariah, M. N. ; Al-Zihiry, K. ; Rahi, Sattar ; Basir, R. / Anti-plasmodial and chloroquine resistance suppressive effects of embelin. In: Pharmacognosy Magazine. 2017 ; Vol. 13, No. 49. pp. S48-S55.
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