Based on the previously reported neuroprotective, neurochemical, and behavioral effects of syringic acid, the present study was designed to investigate its antinociceptive and anti-inflammatory potential and to elucidate its possible mechanisms of action using in vitro and in silico methods. The antinociceptive effects of syringic acid were evaluated using the tail-clip, tail-immersion, hot-plate, formalin, and acetic acid-induced writhing tests in Balb/c mice, whereas its anti-inflammatory activity was assessed using the carrageenan-induced paw edema model in Sprague-Dawley rats. Motor performance was examined using the activity meter and Rota-rod tests. The potential ulcerogenic effect was also evaluated. Syringic acid (50 and 100 mg/kg, p.o.) did not significantly alter motor performance. It also did not alter nociceptive response parameters in the tail-clip, tail-immersion, or hot-plate tests. However, it significantly decreased writhing behavior in the writhing test and reduced paw-licking time during the second phase of the formalin test. Moreover, syringic acid attenuated carrageenan-induced paw edema. These findings indicate that syringic acid exerts peripheral antinociceptive and anti-inflammatory activities. In addition, acute administration of syringic acid did not induce gastric ulceration in mice. Enzyme inhibition studies showed that syringic acid inhibited cyclooxygenase-2 and 5-lipoxygenase at μM concentrations. In silico studies further revealed stable interactions between syringic acid and both enzymes.
Şeyda Yön, Cevşen Yazıcı Şenocak, Gizem Türkoğlu Sağlık et al.· ACS Omega· 0 citations
Objective: The present investigation was undertaken to synthesize and systematically evaluate a series of thiophene mannich base derivatives for their analgesic and anti‑inflammatory potential using validated experimental models. The study aimed to assess both central and peripheral mechanisms of analgesia, as well as acute and chronic inflammatory responses.Material and Method: Algesia was induced using both thermal and chemical methods to evaluate central and peripheral analgesic effects, respectively. Inflammation was induced through peripheral models, namely carrageenan-induced paw edema, granuloma pouch, and formalin-induced paw edema. The test compounds were administered at a dosage of 55 mg/kg. Pentazocine (10 mg/kg, s.c.) served as the reference drug for the central analgesic model, whereas diclofenac (10 mg/kg) was used as the standard drug for peripheral analgesic and inflammatory models. Evaluation of analgesic and anti-inflammatory activity demonstrated that test compound 1, significantly prolonged response latency in the hot plate method, reduced the number of abdominal writhes induced by 1% acetic acid, decreased carrageenan- and formalin-induced paw edema, and reduced the volume of exudates in the air pouch model. Inflammatory markers such as Myloperoxidase enzyme, IL-6 and WBC counts were assessed.Result and Discussion: The test compound 1, has shown significant analgesic and anti-inflammatory activity.
Girish A. Hampannavar, N. Jeedi· Ankara Universitesi Eczacili...· 0 citations
The present study aimed to comparatively evaluate the antinociceptive and anti-inflammatory effects of oleic acid (OA) and linoleic acid (LA), administered individually and in combination, and to investigate their impact on serum pro-inflammatory cytokines in an experimental animal model. A total of 96 rats were orally treated with OA (45–90 mg/kg), LA (45–90 mg/kg), OA + LA (45+45 mg/kg and 90+90 mg/kg), standard analgesics (indomethacin and acetylsalicylic acid, ASA), or vehicle control. The antinociceptive properties were examined through Tail Flick, Hot Plate, and writhing test induced by acetic acid injection, whereas the anti-inflammatory properties were examined through carrageenan-induced paw edema. The concentrations of TNF-α and IL-1β in serum were determined by ELISA. OA demonstrated statistically significant antinociceptive effects in both central and peripheral pain models, exhibiting efficacy comparable to ASA. In contrast, LA alone did not produce significant analgesic effects. Notably, co-administration of OA and LA attenuated the analgesic efficacy observed with OA alone. In the carrageenan-induced inflammation model, both OA and OA + LA significantly reduced paw edema, with effects comparable to indomethacin, whereas LA alone showed limited anti-inflammatory activity. Biochemically, both OA and LA significantly elevated serum TNF-α levels, while no significant differences were observed among groups in IL-1β levels. These findings suggest that OA possesses pronounced antinociceptive and anti-inflammatory properties. However, the reduced efficacy observed with combined administration and the elevation of cytokines indicate that OA and LA might work via different pathways, thus warranting further investigation into their dose-dependent interactions.
A. Öner, Esin Akarsu Orunç· The Veterinary Journal· 0 citations
Neuropathic pain is a disorder that represents a significant clinical challenge, while is refractory to therapeutic interventions. Given that the histamine H3 receptor (H3R) is a promising target for new analgesics, we aimed to determine the effects of a novel H3R antagonist (pKi=8.2), LINS01022 (1-(2,3-dihydrobenzofuran-2-yl)methylpiperazine), in neuropathic pain model (chronic constriction injury). Recognizing the significant impact of sex on chronic pain, all experiments were conducted in male and female mice. We investigated the effects of a single intraperitoneal (i.p.) LINS01022 injections (10, 20, 30 mg/kg) on mechanical (von Frey) and thermal (cold plate, tail flick) stimuli to determine dose-, time-, and sex-dependent analgesic profile. To characterize LINS01022 (20 mg/kg) influence on the metabolism parameters, we conducted behavioral profiling studies using an innovative, high-resolution Promethion Metabolic Cages system. Mechanical and thermal thresholds were also assessed after repeated LINS01022 (20 mg/kg/day) treatment, and the possible participation of spinal glutamine, glutamate and γ-aminobutyric acetic acid, and supraspinal glia activation was determined. Additionally, we investigated the LINS01022 influence on locomotor activity (open-field). LINS01022 reduced hypersensitivity in a dose- and time-dependent manner, with greater efficacy in males, and this analgesic effect was not corelated with changes in neurotransmitters level or glia activation. Importantly, the H3R antagonist did not impair locomotor activity and metabolic parameters. This research provides the first evaluation of LINS01022's analgesic efficacy and its favourable safety profile in neuropathic pain. These results suggest that a novel H3R antagonist is a promising drug candidate and a valuable pharmacological tool for further investigation.
Magdalena Maciuszek, M. Białoń, Mateusz Królewski et al.· European Journal of Pharmaco...· 0 citations
The studied compounds of the indenopyrrole series and their indenopyridazine derivatives are virtually non-toxic compounds, exhibit an anti-inflammatory effect and reduce the severity of pain associated with inflammation.
O. N. Gein, N. V. Nosova, E. Chizhova et al.· Acta Biomedica Scientia· 0 citations
Azilsartan, an angiotensin receptor blocker, has been widely used in the treatment of hypertension. Its unique structure is hypothesised to confer multiple pleiotropic effects, including anti-inflammatory and anti-apoptotic properties, with potential antioxidant effects being exploratory. The present study was conducted to evaluate the anti-inflammatory, antinociceptive, and antioxidative properties of azilsartan in thermally and chemically induced nociceptive rodent models. Wistar albino rats (200–250 g) and Swiss albino mice (25–30 g) of either sex were procured from the Central Animal Facility, AIIMS Bhopal. Two doses of azilsartan (1 mg/kg and 4 mg/kg) were investigated after approval from the institutional animal ethics committee. Anti-inflammatory and anti-nociceptive properties were evaluated using chemically induced inflammatory models, including carrageenan, Freund’s complete adjuvant (FCA)-induced arthritis, thermally induced nociceptive models and Aspirin-induced gastric ulcer. Azilsartan produced significant anti-inflammatory effects in chemically induced models. In the carrageenan-induced paw edema model, at 6 h, paw volume was reduced to 1.59 ± 0.02 ml with azilsartan 4 mg/kg vs. 1.86 ± 0.01 ml in controls (32% inhibition, p < 0.01). In the FCA-induced arthritis model, by day 14, joint size was reduced by 27% with azilsartan 4 mg/kg (p < 0.05 vs. control). Histopathological and immunohistochemical analyses demonstrated reduced inflammatory infiltration and decreased TNF-α expression in azilsartan-treated groups. Azilsartan also showed dose-dependent protection against aspirin-induced gastric ulceration, with 36% and 45% inhibition at doses of 1 and 4 mg/kg, respectively (p < 0.001). Mean MDA levels were 350 pg/mL in controls vs. 115 pg/mL with azilsartan 4 mg/kg (p = 0.12). No significant analgesic effect was observed in thermally induced nociceptive models (hot plate and tail flick tests). Azilsartan exhibits significant anti-inflammatory and inflammation-associated pain–modulating effects in preclinical models, but does not demonstrate significant analgesic activity in acute thermal nociception. Not applicable.
S. Atal, Santenna Chenchula, P. Ponmani et al.· Beni-Suef University Journal...· 0 citations
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