Chemical characterization, pharmacological effects, and toxicity of an ethanol extract of Celtis pallida Torr. (Cannabaceae) aerial parts

J Ethnopharmacol. 2018 Jun 12:219:126-132. doi: 10.1016/j.jep.2018.03.014. Epub 2018 Mar 12.

Abstract

Ethnopharmacological relevance: Celtis pallida Torr (Cannabaceae) is employed as a folk medicine for the treatment of inflammation, pain, skin infections, and diarrhea, among other diseases.

Aim of the study: The purpose of this work was to assess the chemical composition, the in vitro and in vivo toxicity, the antimicrobial, anti-inflammatory, antidiarrheal, antinociceptive, locomotor, and sedative effects of an ethanolic extract obtained from Celtis pallida aerial parts (CPE).

Materials and methods: The composition of CPE was carried out by GC-MS. The in vitro and in vivo toxic activity of CPE was estimated with the comet assay (10-1000 µg/ml) for 5 h in peripheral blood mononuclear cells, and the acute toxicity test (500-5000 mg/kg p.o.), for 14 days, respectively. The antimicrobial effect of CPE was evaluated using the minimum inhibitory concentration (MIC) assay, whereas the antidiarrheal activity (10-200 mg/kg p.o.) was calculated using the castor oil test. The antinociceptive effects of CPE (50-200 mg/kg p.o.) were estimated with the acetic acid and formalin tests, as well as the hot plate test. The sedative and locomotor activities of CPE (50-200 mg/kg p.o.) were assessed with the pentobarbital-induced sleeping time test and the rotarod test, respectively.

Results: The main compound found in CPE was the triterpene ursolic acid (22% of the extract). CPE at concentrations of 100 µg/ml or higher induced genotoxicity in vitro and showed low in vivo toxicity (LD50 > 5000 mg/kg p.o.). Additionally, CPE lacked (MIC > 400 µg/ml) antimicrobial activity but exerts antinociceptive (ED50 = 12.5 ± 1.5 mg/kg) and antidiarrheal effects (ED50 = 2.8 mg/kg), without inducing sedative effects or altering the locomotor activity. The antinociceptive activity of CPE suggests the participation of adrenoceptors, as well as the nitric oxide/cyclic guanosine monophosphate (cGMP) pathway.

Conclusion: C. pallida exerts its antinociceptive effects probably mediated by the nitric oxide/cyclic guanosine monophosphate (cGMP) pathway.

Keywords: Antimicrobial; Carbamoyl choline (PubChem CID:5831); Celtis pallida; Clonazepam (PubChem CID:2802); Diarrhea; Dimethyl sulfoxide (PubChem CID:679); Glibenclamide (PubChem CID:3488); Inflammation; Naloxone (PubChem CID:5464092); Naproxen sodium (PubChem CID: 23681059); Pain; Tramadol hydrochloride (PubChem CID:63013); pentobarbital (PubChem CID: 4737).

MeSH terms

  • Analgesics / isolation & purification
  • Analgesics / pharmacology*
  • Analgesics / toxicity
  • Animals
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / toxicity
  • Antidiarrheals / isolation & purification
  • Antidiarrheals / pharmacology
  • Antidiarrheals / toxicity
  • Cannabaceae*
  • Dose-Response Relationship, Drug
  • Ethanol / pharmacology
  • Mice
  • Mice, Inbred BALB C
  • Mutagenicity Tests / methods
  • Pain Measurement / drug effects*
  • Pain Measurement / methods
  • Plant Components, Aerial*
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Plant Extracts / toxicity
  • Ulmaceae

Substances

  • Analgesics
  • Anti-Inflammatory Agents
  • Antidiarrheals
  • Plant Extracts
  • Ethanol