Assessment of in vitro and in vivo antimalarial efficacy and GC-fingerprints of selected medicinal plant extracts

Exp Parasitol. 2020 Dec:219:108011. doi: 10.1016/j.exppara.2020.108011. Epub 2020 Sep 30.

Abstract

A hallmark of mortality and morbidity, malaria is affecting nearly half of the world's population. Emergence of drug-resistant strains of malarial parasite prompts identification and evaluation of medicinal plants and their constituents that may hold the key to a new and effective anti-malarial drug. In this context, nineteen methanolic extracts from seventeen medicinal plants were evaluated for anti-plasmodial potential against Plasmodium falciparum strain 3D7 (Chloroquine (CQ) sensitive) and INDO (CQ resistant) using fluorescence based SYBR-Green assay and for cytotoxic effects against mammalian cell lines. Leaf extract of two plants showed promising in vitro anti-malarial activity (Pf3D7 IC50 ≤ 10 μg/ml); one plant extract showed good activity (Pf3D7 IC50 = 10.1-20 μg/ml); seven were moderately active (IC50 = 20.1-50 μg/ml), four plant extracts showed poor activity (PfD7 IC50 = 50.1-100 μg/ml) and five extracts showed no activity up to IC50 = 100 μg/ml. Further, six extracts were found equipotent to PfINDO (resistance index ranging 0.4-2) and relatively nontoxic to mammalian cell lines HEK293 (cytotoxicity index ranging 1.4-12.5). Based on good resistance and selectivity indices, three extracts were evaluated for in vivo activity in Plasmodium berghei ANKA infected mice at a dose of 500 mg/kg and they showed significant suppression of P. berghei parasitemia. Further, these active plant extracts were fractionated using silica-gel chromatography and their fractions were evaluated for anti-plasmodial action. Obtained fractions showed enrichment in antimalarial activity. Active fractions were analyzed by gas chromatography and mass-spectrometery. Results suggests that the three active plant extracts could serve as potent source of anti-malarial agent and therefore require further analysis.

Keywords: Cytotoxicity; Drug resistance; Gas chromatography; Medicinal plants; Plasmodium berghei; Silica gel chromatography.

MeSH terms

  • Acacia / chemistry
  • Animals
  • Antimalarials / classification
  • Antimalarials / pharmacology*
  • Antimalarials / toxicity
  • Chromatography, High Pressure Liquid
  • Dose-Response Relationship, Drug
  • Ethnopharmacology
  • Female
  • Gas Chromatography-Mass Spectrometry
  • HEK293 Cells
  • Humans
  • India
  • Inhibitory Concentration 50
  • Medicine, East Asian Traditional
  • Mice
  • Mice, Inbred BALB C
  • Plant Extracts / pharmacology*
  • Plant Extracts / toxicity
  • Plant Leaves / chemistry
  • Plants, Medicinal / chemistry*
  • Plants, Medicinal / classification
  • Plasmodium berghei / drug effects*
  • Plasmodium falciparum / drug effects*
  • Rubus / chemistry
  • Syzygium / chemistry

Substances

  • Antimalarials
  • Plant Extracts