The antinociceptive property of extracts is known but the analgesic activity of its bioactive constituent asiaticoside has not been reported. We evaluated the antinociceptive activity of orally (p. o.) administered asiaticoside (1, 3, 5, and 10 mg/kg) in mice using the 0.6% acetic acid-induced writhing test, the 2.5% formalin-induced paw licking test, and the hot plate test. The capsaicin- and glutamate-induced paw licking tests were employed to evaluate the involvement of the vanilloid and glutamatergic systems, respectively. Asiaticoside (3, 5, and 10 mg/kg, p. o.) reduced the rate of writhing (p < 0.0001) by 25.3, 47.8, and 53.9%, respectively, and increased the latency period (p < 0.05) on the hot plate at 60 min post-treatment until the end of the experiment. Moreover, asiaticoside (3, 5, and 10 mg/kg, p. o.) shortened the time spent in licking/biting the injected paw (p < 0.0001) in the early phase of the formalin test by 45.7, 51.4, and 52.7%, respectively, and in the late phase (p < 0.01) by 23.6, 40.5, and 50.6%, respectively. Antinociception induced by asiaticoside (10 mg/kg) was not antagonized by naloxone in both the 2.5% formalin-induced nociception and the hot plate test, indicating a nonparticipation of the opioidergic system. Asiaticoside (1, 3, 5, and 10 mg/kg, p. o.) reduced the duration of biting/licking the capsaicin-injected paw (p < 0.0001) by 40.5, 48.2, 59.5, and 63.5%, respectively. Moreover, asiaticoside (5 and 10 mg/kg) shortened the time spent in biting/licking the glutamate-injected paw (p < 0.01) by 29.9 and 48.6%, respectively. Therefore, asiaticoside (5 and 10 mg/kg, p. o.) induces antinociception possibly through the vanilloid and glutamatergic systems.
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http://dx.doi.org/10.1055/a-1144-3663 | DOI Listing |
Ann Agric Environ Med
December 2024
Department of Experimental Pharmacology, Institute of Rural Health, Lublin, Poland.
Introduction And Objective: The aim of the study was to investigate the effect of bee venom on the activity of two analgesics: ketoprofen (a non-steroidal anti-inflammatory drug) and tramadol (an opioid drug) in the acute thermal pain model (hot-plate test) in mice.
Material And Methods: Linear regression analysis was used to evaluate the dose-response relationship between logarithms of drug doses and their resultant maximum possible anti-nociceptive effects in the mouse hot-plate test. Doses that increased the anti-nociceptive effect by 20% (ED values) for bee venom, ketoprofen and tramadol, and their combination were calculated from linear equations.
ChemMedChem
December 2024
Uniwersytet Jagielloński Collegium Medicum, Department of Medicinal Chemistry, POLAND.
This study aimed to design new hybrid compounds with imidazolidin-2,4-dione and morpholine rings as broad spectrum anticonvulsants. To achieve this goal, all compounds were evaluated in animal seizure models, namely the maximal electroshock (MES), the subcutaneous pentylenetetrazole (scPTZ), and selected in the 6 Hz (32 mA) tests. The most promising compound, 5-isopropyl-3-(morpholinomethyl)-5-phenylimidazolidine-2,4-dione (19), demonstrated broader anticonvulsant activity than phenytoin or levetiracetam, with ED50 of 26.
View Article and Find Full Text PDFArch Razi Inst
June 2024
Department of Pharmacy Practice, Faculty of Pharmacy, University of Sindh, Jamshoro, Pakistan.
Today, the current chemical agents used for the management of pain cause numerous complications. They are associated with the occurrence of disorders in the digestive system, damage to the kidney, or addiction, which has prompted individuals to seek novel drugs that, apart from removing the side effects, are cost-effective and available. The present survey aimed to assess the antinociceptive and anti-inflammatory activity of Korovin methanolic extract (FEME) in male Swiss mice.
View Article and Find Full Text PDFReprod Sci
December 2024
Department of Gynecology and Obstetrics, Division of Reproductive Sciences & Women's Health Re-search, Johns Hopkins Medicine, Baltimore, MD, 21205, USA.
Pomegranate (Punica granatum) is a widely cultivated fruit historically recognized for its health benefits and is regarded as a nutritional powerhouse. Pomegranate has a unique composition of bioactive compounds including hydrolysable tannins, anthocyanins, and other polyphenolic components. Of those, punicalagin and its subsequent metabolites are the most extensively studied, demonstrating antioxidant, anti-inflammatory, anti-cancer, and anti-nociceptive activity.
View Article and Find Full Text PDFEur J Med Chem
December 2024
A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, bld. 1, Moscow, 119334, Russia. Electronic address:
Thevinols and their 3-O-demethylated relatives, orvinols, are derivatives of the Diels-Alder adduct of natural alkaloid thebaine with methyl vinyl ketone. Taken together, thevinols and orvinols constitute an important family of opioid receptor (OR) ligands playing an important role in both the OR mediated antinociception and OR antagonism. Herein, we disclose for the first time the antagonist activity of the N-allyl substituted orvinol derivative fluorinated within the pharmacophore associated with C(20) and its surrounding.
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