Chemical characterization, pharmacological effects, and toxicity of an ethanol extract of Celtis pallida Torr. (Cannabaceae) aerial parts
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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%25 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. © 2018 Elsevier B.V.
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Antimicrobial; Celtis pallida; Diarrhea; Inflammation; Pain acetic acid; adrenergic receptor; antinociceptive agent; behenic acid; behenyl alcohol; Celtis pallida Torr extract; glycerol stearate; guanosine phosphate; heptadecanoic acid; lignoceric acid; linoleic acid; linolenic acid; lupeol; malic acid; nitric oxide; palmitic acid; pentobarbital; plant extract; sedative agent; sitosterol; squalene; stearic acid; triterpene; unclassified drug; ursolic acid; alcohol; analgesic agent; antidiarrheal agent; antiinflammatory agent; plant extract; aerial plant part; animal experiment; animal model; animal tissue; antidiarrheal activity; antiinflammatory activity; antimicrobial activity; Article; Cannabaceae; Celtis pallida Torr; chemical analysis; chemical composition; controlled study; drug activity; formalin test; genotoxicity; in vitro study; in vivo study; LD50; locomotion; minimum inhibitory concentration; motor coordination; mouse; nonhuman; peripheral blood mononuclear cell; rotarod test; sleep time; animal; Bagg albino mouse; dose response; drug effect; isolation and purification; mutagen testing; pain measurement; procedures; Ulmaceae; Analgesics; Animals; Anti-Inflammatory Agents; Antidiarrheals; Cannabaceae; Dose-Response Relationship, Drug; Ethanol; Mice; Mice, Inbred BALB C; Mutagenicity Tests; Pain Measurement; Plant Components, Aerial; Plant Extracts; Ulmaceae
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