Evaluation of the antinociceptive activities of enaminone compounds on the formalin and hot plate tests in mice

Masocha, Willias; Kombian, Samuel B.; Edafiogho, Ivan O.

doi:10.1038/srep21582

Cited by 37 publications

(14 citation statements)

References 39 publications

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“…The forty female mice (referring to the pharmacological experimental method [16], hot plates would burn the genitals of male mice) with a pain threshold between 5 s and 30 s were selected and divided randomly into four groups and were intragastrically administered as mentioned above. After 6 days of continuous intragastric administration, the values of the pain threshold after 0.5-h, 1.5-h and 2-h administration of each group were determined by the hot-plate method [17,18].…”

Section: Hot-plate Study In Micementioning

confidence: 99%

Comparison of the acute toxicity, analgesic and anti-inflammatory activities and chemical composition changes in Rhizoma anemones Raddeanae caused by vinegar processing

Wang

Zhou

Xie

et al. 2020

BMC Complement Med Ther

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Background: As the dry rhizome of Anemone raddeana Regel, Rhizoma Anemones Raddeanae (RAR), which belongs to Ranunculaceae, is usually used to treat wind and cold symptoms, hand-foot disease and spasms, joint pain and ulcer pain in China. It is well known that the efficacy of RAR can be distinctly enhanced by processing with vinegar due to the reduced toxicity and side effects. However, the entry of vinegar into liver channels can cause a series of problems. In this paper, the differences in the acute toxicity, anti-inflammatory and analgesic effects between RAR and vinegar-processed RAR were compared in detail. The changes in the chemical compositions between RAR and vinegar-processed RAR were investigated, and the mechanism of vinegar processing was also explored. Methods: Acute toxicity experiments were used to examine the toxicity of vinegar-processed RAR. A series of studies, such as the writhing reaction, ear swelling experiment, complete Freund's adjuvant-induced rat foot swelling experiment and cotton granuloma, in experimental mice was conducted to observe the anti-inflammatory effect of vinegar-processed RAR. The inflammatory cytokines of model rats were determined by enzyme-linked immunosorbent assay (ELISA). Liquid Chromatography-Quadrupole-Time of Flight mass spectrometer Detector (LC-Q-TOF) was used to analyse the chemical compositions of the RARs before and after vinegar processing. Results: Neither obvious changes in mice nor death phenomena were observed as the amount of vinegar-processed RAR in crude drug was set at 2.1 g/kg. Vinegar-processed RAR could significantly prolong the latency, reduce the writhing reaction time to reduce the severity of ear swelling and foot swelling, and remarkably inhibit the secretion of Interleukin-1β(IL-1β), Interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) proinflammatory cytokines. The content of twelve saponins (e.g., Eleutheroside K) in RAR was decreased after vinegar processing, but six other types (e.g., RDA) were increased. Conclusions: These results revealed that vinegar processing could not only improve the analgesic and antiinflammatory effects of RAR but also reduce its own toxicity. Trial registration: Not applicable.

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Section: Hot-plate Study In Micementioning

confidence: 99%

Comparison of the acute toxicity, analgesic and anti-inflammatory activities and chemical composition changes in Rhizoma anemones Raddeanae caused by vinegar processing

Wang

Zhou

Xie

et al. 2020

BMC Complement Med Ther

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“…The hot plate test method is based on that previously reported by Masocha 46 . 10 ICR mice (female, 6–8 weeks, 18–24 g) in each group.…”

Section: Methodsmentioning

confidence: 99%

Discovery of 4-arylthiophene-3-carboxylic acid as inhibitor of ANO1 and its effect as analgesic agent

Wang

Gao

Zhao

et al. 2021

Acta Pharmaceutica Sinica B

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Anoctamin 1 (ANO1) is a kind of calcium-activated chloride channel involved in nerve depolarization. ANO1 inhibitors display significant analgesic activity by the local peripheral and intrathecal administration. In this study, several thiophenecarboxylic acid and benzoic acid derivatives were identified as novel ANO1 inhibitors through the shape-based virtual screening, among which the 4-arylthiophene-3-carboxylic acid analogues with the best ANO1 inhibitory activity were designed, synthesized and compound 42 (IC 50 = 0.79 μmol/L) was finally obtained. Compound 42 selectively inhibited ANO1 without affecting ANO2 and intracellular Ca 2+ concentration. Subsequently, the analgesic effect was investigated by intragastric administration in pain models. Compound 42 significantly attenuated allodynia which was induced by formalin and chronic constriction injury. Through homology modeling and molecular dynamics, the binding site was predicted to be located near the calcium-binding region between α 6 and α 8. Our study validates ANO1 inhibitors having a significant analgesic effect by intragastric administration and also provides selective molecular tools for ANO1-related research.

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“…In a parallel experiment, naltrexone (1 mg/kg) was administrated s.c. 5 min prior to morphine injection. Hot-plate test results were analyzed using two-way repeated measures ANOVA, followed by Bonferroni post-tests in GraphPad Prism 5 software (GraphPad Software Inc., La Jolla, CA) (46).…”

Section: Methodsmentioning

confidence: 99%

Binge-Like Exposure to Ethanol Enhances Morphine's Anti-nociception in B6 Mice

Chang

Huang

Han³

et al. 2019

Front. Psychiatry

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Elevation of the blood ethanol concentration (BEC) to > 80 mg/dL (17.4 mM) after binge drinking enhances inflammation in brain and neuroimmune signaling pathways. Morphine abuse is frequently linked to excessive drinking. Morphine exerts its actions mainly via the seven transmembrane G-protein-coupled mu opioid receptors (MORs). Opioid use disorders (OUDs) include combination of opioids with alcohol, leading to opioid overdose-related deaths. We hypothesized that binge drinking potentiates onset and progression of OUD. Using C57BL/6J (B6) mice, we first characterized time-dependent inflammatory gene expression change as molecular markers using qRT-PCR within 24 h after binge-like exposure to high-dose, high-concentration ethanol (EtOH). The mice were given one injection of EtOH (5 g/kg, 42% v/v, i.g.) and sacrificed at 2.5 h, 5 h, 7.5 h, or 24 h later. Inflammatory cytokines interleukin (IL)-1β, IL-6, and IL-18 were elevated in both the striatum (STr) and the nucleus accumbens (NAc) of the mice. We then investigated the expression profile of MOR in the STr at 2 min, 5 h, or 24 h after the first EtOH injection and at 24 h and 48 h after the third injection. This binge-like exposure to EtOH upregulated MOR expression in the STr and NAc, an effect that could enhance morphine's anti-nociception. Therefore, we examined the impact of binge-like exposure to EtOH on morphine's anti-nociception at the behavioral level. The mice were treated with or without 3-d binge-like exposure to EtOH, and the anti-nociceptive changes were evaluated using the hot-plate test 24 h after the final (3rd) EtOH injection with or without a cumulative subcutaneous dose (0, 0.1, 0.3, 1.0, and 3.0 mg/kg) of morphine at intervals of 30 min. The response curve of the mice given EtOH was shifted to the left, showing enhanced latency to response to morphine up to 3 mg/kg. Furthermore, co-treatment with the MOR antagonist naltrexone blocked morphine's anti-nociception in animals given either EtOH or saline. This confirms that MOR is involved in binge-like exposure to EtOH-induced changes in morphine's anti-nociception. Our results suggest that EtOH enhanced latency to analgesic response to morphine, and such effect might initiate the onset and progression of OUDs.

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Evaluation of the antinociceptive activities of enaminone compounds on the formalin and hot plate tests in mice

Cited by 37 publications

References 39 publications

Comparison of the acute toxicity, analgesic and anti-inflammatory activities and chemical composition changes in Rhizoma anemones Raddeanae caused by vinegar processing

Comparison of the acute toxicity, analgesic and anti-inflammatory activities and chemical composition changes in Rhizoma anemones Raddeanae caused by vinegar processing

Discovery of 4-arylthiophene-3-carboxylic acid as inhibitor of ANO1 and its effect as analgesic agent

Binge-Like Exposure to Ethanol Enhances Morphine's Anti-nociception in B6 Mice

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