Investigation of Potential Antioxidant, Thrombolytic and Neuropharmacological Activities of Homalomena aromatica Leaves Using Experimental and In Silico Approaches

Molecules. 2021 Feb 12;26(4):975. doi: 10.3390/molecules26040975.

Abstract

The leaves of Homalomena aromatica are traditionally used in Bangladesh for the treatment of different chronic ailments. The purpose of this study was to explore in vitro antioxidant, thrombolytic activities, and in vivo neuropharmacological effects of methanolic extract of Homalomena aromatica (MEHA) leaves. Antioxidant activity of MEHA was assessed by a DPPH free radical scavenging assay and total phenolics content, total flavonoids content were also measured. The thrombolytic activity was determined by percentage of clot lysis and neuropharmacological activities by hole board, tail suspension, forced swimming and elevated plus maze tests. The results showed that the IC50 value of the extract against DPPH was 199.51 μg/mL. Quantitative analysis displayed higher contents of phenolics and flavonoids (147.71 mg gallic acid equivalent/g & 66.65 mg quercetin equivalent/g dried extract, respectively). The extract also showed a significant clot lysis (33.31%) activity. In case of anxiolytic activity, the elevate plus maze (EPM) test demonstrated an increase in time spent in open arms, and in case of hole board test, the number of head dipping was also significantly increased (p < 0.05). All the test compared with control (1% Tween in water) and standard (diazepam 1 mg/kg), significant dose (200 & 400 mg/kg) dependent anxiolytic activity was found. In antidepressant activity, there was a significant decrease in period of immobility in both test models (tail suspension and forced swimming) (p < 0.05). Moreover, 13 compounds were identified as bioactive, showed good binding affinities to xanthine oxidoreductase, tissue plasminogen activator receptor, potassium channel receptor, human serotonin receptor targets in molecular docking experiments. Furthermore, ADME/T analysis revealed their drug-likeness, likely pharmacological actions and non-toxic upon consumption. Taken together, our finding support the traditional medicinal use of this plant, which may provide a potential source for future drug discovery.

Keywords: ADME profiling; H. aromatica; antidepressant; antioxidant; anxiolytic; essential oil; molecular docking; thrombolytic.

MeSH terms

  • Animals
  • Antidepressive Agents / chemistry
  • Antidepressive Agents / pharmacology
  • Antioxidants / chemistry*
  • Antioxidants / pharmacology
  • Araceae / chemistry*
  • Biphenyl Compounds / chemistry
  • Computer Simulation
  • Fibrin Clot Lysis Time
  • Fibrinolytic Agents / chemistry*
  • Fibrinolytic Agents / pharmacology
  • Flavonoids / chemistry
  • Free Radical Scavengers / chemistry
  • Free Radical Scavengers / pharmacology
  • Humans
  • Mice
  • Molecular Docking Simulation
  • Neuropharmacology
  • Phenols / chemistry
  • Picrates / chemistry
  • Plant Extracts / chemistry*
  • Plant Extracts / pharmacology
  • Plant Leaves / chemistry
  • Receptors, Serotonin / chemistry
  • Serotonin Antagonists / chemistry
  • Serotonin Antagonists / pharmacology
  • Swimming

Substances

  • Antidepressive Agents
  • Antioxidants
  • Biphenyl Compounds
  • Fibrinolytic Agents
  • Flavonoids
  • Free Radical Scavengers
  • Phenols
  • Picrates
  • Plant Extracts
  • Receptors, Serotonin
  • Serotonin Antagonists
  • 1,1-diphenyl-2-picrylhydrazyl