Aug 2026· Acta Biomedica Scientia· 0 citations· 6 references
TL;DR
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.
Abstract
Background
. Currently, the main groups of anti-inflammatory drugs used in medical practice are steroidal (glucocorticoids) and non-steroidal agents. However, despite their widespread use, these groups of anti-inflammatory drugs have a fairly wide range of negative side effects, which makes the search for low-toxic substances with anti-inflammatory effects currently relevant.
The aim
. To study anti-inflammatory, antinociceptive activity and acute toxicity of individual representatives of indenopyrroles and indenopyridazines.
Methods
. The acute toxicity of the studied compounds was studied using the method of Prozorovsky VB. Anti-inflammatory activity was assessed in a carrageenan-induced rat paw edema model. The production of active oxygen radicals by leukocytes was evaluated using luminol-dependent chemiluminescence. The antinociceptive activity of the compounds was assessed using the “writhing” and “hot plate” tests in mice.
Results.
The obtained results allowed the studied compounds to be classified as “practically nontoxic” (LD50 > 1000 mg/kg). Compounds 1в of the indenopyrrole series and indenopyridazines 2а-в were found to exhibit anti-inflammatory activity, reducing the severity of exudative inflammation. Compound 2a exhibited the greatest antiexudative activity, reducing edema by more than 60 % (p < 0.01). Compounds 2a-в and compound 1в reduced the production of reactive oxygen species by more than 40 % (p < 0.05) compared to the control. In the “hot plate” test, the studied compounds 1a, 1в, 2a-в exhibited an antinociceptive effect comparable to nimesulide; in the “acetic acid-induced writhing” test, the effect of compounds 1a, 2б, 2в was comparable to nimesulide, and the effect of compound 2a exceeded the comparison drug by 32.96 % (p < 0.05).
Conclusion
. 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.
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.
Hanane El Fatimi, H. Khalki, Martin Ndayambaje et al.· Naunyn-Schmiedeberg's Archiv...· 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
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
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
Inflammatory pain mediated by pro‐inflammatory factors remains a major clinical challenge, highlighting the need for safer alternatives to conventional anti‐inflammatory drugs. Here, the antinociceptive effects of methanolic extracts from the aerial parts of Alchemilla daghestanica (AD) and Alchemilla minusculiflora (AM) were evaluated in mice using the formalin test, and anti‐inflammatory activity was assessed by measuring formalin‐induced paw edema. Phytochemical characterization was performed by LC–MS/MS, and potential activities of major constituents were predicted using PASS Online. LC–MS/MS identified miquelianin as the predominant compound in both extracts. AD (100–200 mg/kg) and AM (200 mg/kg) significantly inhibited the inflammatory phase of the formalin test (p < 0.001 and p < 0.01, respectively) without affecting the neurogenic phase, and AM extract reduced paw edema (p < 0.05). PASS predicted high probabilities (Pa > 0.7) for anti‐inflammatory activity of miquelianin, isoquercitrin, and tannic acid. These findings suggest that these extracts may represent valuable candidates for further investigation in inflammatory pain management.
Elif Nur Barut, Belkıs Sadoğlu, Ayşenur Özduman et al.· Chemistry and Biodiversity· 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