Jul 2026· Naunyn-Schmiedeberg's Archives of Pharmacology· 0 citations· 45 references
Medicine
TL;DR
MAL exhibits potent anti-inflammatory and analgesic properties, particularly at 25 mg/kg, reducing neutrophil-mediated inflammation, and represents a promising candidate for further pharmacological development.
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
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
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.
Shubham Atal, Santenna Chenchula, P. Ponmani et al.· Beni-Suef University Journal...· 0 citations
It was evaluated in this study that aripiprazole showed inhibition of protein degradation and stability of human red blood cell membrane in concentration gradient manner, demonstrating maximum activity at concentration of 6400 µg/ml.
Aroosa Akber, Alamgeer, H. Irfan et al.· InflammoPharmacology· 0 citations
In this study, the pharmacological and mechanistic potential of a selected synthetic triazole derivative, 4-(4-Fluorophenyl)-3-(p-tolyl)-1H-1,2,4-triazole-5(4H)-thione (TriQ), was evaluated in an acetic acid-induced ulcerative colitis (UC) mice model using an integrated approach involving molecular docking, molecular dynamics (MD) simulations, biochemical assays, gene expression analysis, and histopathological evaluation. TriQ was selected based on the pharmacological relevance of triazole scaffolds, particularly those containing fluorophenyl and aryl substitutions, which are associated with enhanced anti-inflammatory and antioxidant properties and improved target-binding interactions. In silico analysis revealed strong binding affinities of TriQ toward key inflammatory mediators, including Nuclear Factor kappa B (NF-κB), Interleukin-6 (IL-6), and Tumor Necrosis Factor-alpha (TNF-α), stabilized through hydrogen bonding and hydrophobic interactions. MD simulations confirmed the structural stability and consistent conformational behavior of the TriQ-protein complexes over a 100 ns trajectory. In vivo administration of TriQ (5, 10, and 20 mg/kg) significantly alleviated acetic acid-induced colitis, with the highest efficacy observed at 20 mg/kg. Treatment markedly improved disease activity index and restored altered hematological and biochemical parameters, along with normalization of hepatic and renal function markers. TriQ also enhanced endogenous antioxidant defenses, including catalase (CAT), glutathione S-transferase (GST), and reduced glutathione (GSH), while suppressing oxidative stress and inflammatory mediators such as myeloperoxidase (MPO) and nitric oxide (NO). At the molecular level, TriQ significantly downregulated pro-inflammatory cytokines (IL-1β, IL-6, IL-8, and TNF-α) and upregulated heme oxygenase-1 (HO-1) expression, as confirmed by ELISA and qRT-PCR analyses. Histopathological findings demonstrated marked preservation of colonic architecture, and reduced epithelial injury. Collectively, these findings demonstrate that TriQ exerts potent anti-inflammatory and antioxidant effects primarily through modulation of the NF-κB/HO-1 signaling axis, highlighting its potential as a promising lead candidate for the development of novel anti-ulcerative colitis therapeutics.
Abdul Qadir, S. Khan, Humaira Nadeem et al.· Biochemical and Biophysical...· 0 citations
INTRODUCTION/OBJECTIVE
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) exert their pharmacological effects by inhibiting Cyclooxygenase (COX) enzymes and are widely used in the treatment of inflammation. The new potential anti-inflammatory agents of indolebased oxadiazole derivatives were developed.
METHODS
A structure-activity relationship study of 62 indomethacin derivatives was designed, synthesized, and tested for COX-2 inhibition and anti-inflammatory activity in vitro. The structures were confirmed by 1H-NMR, 13C-NMR, and ESI-MS. Drug-likeness and pharmacokinetic properties were predicted by PreADME. Molecular docking was conducted to explore the binding interactions of these compounds with COX-2.
RESULTS
Compounds 4a and 4f exhibited superior COX-2 inhibitory activity compared to indomethacin and celecoxib at a concentration of 500 nM. Compounds 4a and 4f (0.0001-1 μM) showed no cytotoxicity while inhibiting COX-2 in the Raw264.7 cell line. Molecular docking results indicated that compounds 4a and 4f have affinity and interaction with COX-2.
CONCLUSION
Compounds 4a and 4f show selective COX-2 inhibition as potent antiinflammatory agents for the treatment of inflammatory diseases. Molecular docking studies have shown high affinity for COX-2, and the pharmacokinetic properties suggest that 4f can be categorized as a drug-like compound. Compounds 4a and 4f can be considered for further investigation.
Siyuan Ma, Jiayi Cai, Zixuan Yang et al.· Medicinal chemistry· 0 citations