Objective: The present study was carried out to investigate the antinociceptive activity of the aqueous extract of Muntingia calabura (MCAE) leaves and to determine the effect of temperature and the involvement of the opioid receptor on the said activity using the abdominal constriction test (ACT) and hot-plate test (HPT) in mice.
Materials And Methods: The extract was prepared by soaking the dried powdered leaves of M. calabura in distilled water (dH(2)O) overnight, and the supernatant obtained was considered as a stock solution with 100% concentration. The stock solution was diluted to 1, 5, 10, 50 and 100% and used to determine the antinociceptive activity of MCAE. A further experiment was done with 50% concentration to determine the effect of temperature and naloxone involvement of the opioid receptor system in MCAE antinociceptive activity.
Results: At the various concentrations MCAE showed significant antinociceptive activity in both tests. However, the concentration-dependent activity was observed only in the ACT but not in the HPT. The 50% concentration of MCAEs were also stable against the effect of various temperatures as indicated by the presence of activity in both tests. The temperatures (40, 60 and 100 degrees C) also showed an enhanced extract activity only in the HPT. Pre-treatment with naloxone (2 and 10 mg/kg) blocked the extract activity in both tests, indicating the involvement of the opioid receptor system in MCAE antinociceptive activity.
Conclusion: Our data indicate that M. calabura leaves possess antinociceptive activity against chemically and thermally induced noxious stimuli. The bioactive compound(s) responsible for its antinociceptive activity is/are heat-stable and work partly via the opioid receptor system.
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http://dx.doi.org/10.1159/000098366 | DOI Listing |
IBRO Neurosci Rep
June 2025
Department of Basic Sciences, Faculty of Veterinary Medicine, Shahrekord University, Shahrekord, Iran.
Since ancient times many countries have employed medicinal plants as part of traditional medicine. Anethole is a substance found in various plants and has two isomers, cis-anethole (CA) and trans-anethole (TA). Currently, the food industry extensively use anethole as an aromatic and flavoring component.
View Article and Find Full Text PDFPain Rep
February 2025
Department of Ophthalmology, Harvard Medical School, Schepens Eye Research Institute of Massachusetts Eye and Ear, Boston, MA, USA.
Introduction: Ocular pain is a common complaint to eye care providers, associated with a variety of ocular conditions, among which dry eye disease (DED) is affecting millions of people worldwide. Despite being highly prevalent, ocular pain is not managed adequately in the clinic.
Objectives: The aim of this study was to investigate the analgesic potential of neurokinin-1 receptor (NK1R) antagonism in DED.
Eur J Neurosci
January 2025
Laboratory of Cortico-Visceral Physiology, Pavlov Institute of Physiology of the Russian Academy of Sciences, Saint Petersburg, Russia.
The serotonergic raphe magnus (RMg) and dorsal raphe (DR) nuclei are crucial pain-regulating structures, which nociceptive activity is shown to be altered in gut pathology, but the underlying neuroplastic changes remain unclear. Considering the importance of 5-HT1A receptors in modulating both pain and raphe neuronal activity, in this study, we aimed to determine whether 5-HT1A-dependent visceral and somatic nociceptive processing within the RMg and DR is modified in postcolitis conditions. In anaesthetised male Wistar rats, healthy control and recovered from TNBS-induced colitis, the microelectrode recordings of RMg and DR neuron responses to noxious colorectal distension (CRD) or tail squeezing (TS) were performed prior and after intravenous administration of 5-HT1A agonist, buspirone.
View Article and Find Full Text PDFJ Ethnopharmacol
January 2025
College of Pharmacy, Shenzhen Technology University, Shenzhen, 518118, Guangdong, China; Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, 90112, Songkhla, Thailand; Drug Delivery System Excellence Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, 90112, Songkhla, Thailand. Electronic address:
Ethnopharmacological Relevance: Fagonia bruguieri var. laxa Boiss., also known as Dhamansa or Dhamaran, is a well-known xerophyte traditionally used for managing pain, inflammation, fever, and related disease conditions.
View Article and Find Full Text PDFACS Pharmacol Transl Sci
January 2025
Department of Medicinal Chemistry and Institute for Translational Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Opioid agonist ligands bind opioid receptors and stimulate downstream signaling cascades for various biological processes including pain and reward. Historically, before cloning the receptors, muscle contraction assays using isolated organ tissues were used followed by radiolabel ligand binding assays on native tissues. Upon cloning of the opioid G protein-coupled receptors (GPCRs), cell assays using transfected opioid receptor DNA plasmids became the standard practice including S-GTPγS functional and cAMP based assays.
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