The extract of Tri-Phol-That had strong antipyretic and analgesic effects via multi-target inhibition of COX-1, COX-2, and mPGES-1, possibly due to the combined effects of rutin, quercetin, and kaempferol.
Abstract
Despite the common use of herbal medicines rich in flavonoids to treat fever and pain, the pharmacological mechanisms involved in these effects are poorly understood. Therefore, this study assessed the antipyretic and analgesic effects of Tri-Phol-That extract, characterized its major flavonoids, and investigated its possible molecular interactions with key inflammatory mediators. The antipyretic activity was evaluated against a turpentine-induced pyrexia model in mice. Analgesic activity was evaluated using the acetic acid-induced writhing, tail immersion, and hot plate tests. The concentration of rutin, quercetin, and kaempferol was determined by high-performance liquid chromatography. Molecular docking was performed using GNINA against COX-2 (mouse: 1CX2, human: 5KIR), COX-1 (ovine: 3N8X), and mPGES-1 (human: 4YL1). Interaction profile studies were also performed in the Discovery Studio 2021. The hydroethanolic extract lowered rectal temperature in a dose-dependent manner, with maximum inhibition occurring at 100–200 mg/kg, although the effect was less potent than that of tolfenamic acid. The acetic acid-induced writhing test also showed strong dose-dependent peripheral antinociceptive activity with 84.64% inhibition at 200 mg/kg of extract, comparable to tolfenamic acid. The central analgesic effects of extracts were observed in hot plate tests. Weak central analgesic effects were also observed in tail immersion tests. HPLC analysis indicated rutin (4.01 μg/g), kaempferol (2.13 μg/g), and quercetin (0.96 μg/g) were the most abundant flavonoid compounds. Based on docking results, quercetin had the strongest binding affinity toward COX-2 (−8.44 kcal/mol). Rutin also exhibited the strongest binding affinity toward COX-1 (−7.55 kcal/mol) among the flavonoids tested. On the other hand, kaempferol exhibited the strongest binding affinity toward mPGES-1 (−9.97 kcal/mol). Results also showed that rutin, quercetin, and kaempferol interacted with catalytic residues of ARG120, TYR355, TYR385, SER530, and SER127. Thus, it can be concluded that the extract of Tri-Phol-That had strong antipyretic and analgesic effects via multi-target inhibition of COX-1, COX-2, and mPGES-1, possibly due to the combined effects of rutin, quercetin, and kaempferol. These results support the traditional medicinal use of this extract and provide justification for further investigation as a phytotherapeutic agent.
Inflammation and pain are major clinical burdens, and currently used conventional therapies often cause severe long-term adverse effects, prompting the search for safer natural alternatives. This study aimed to evaluate the phytochemical composition and the in vitro anti-inflammatory and in vivo analgesic potential of the methanolic seed extract of wild Musa acuminata (MAEx). Preliminary phytochemical screening was conducted using standard qualitative protocols. The anti-inflammatory effect was assessed via the human red blood cell (HRBC) membrane stabilization assay, while central and peripheral antinociceptive actions were investigated using the hot plate and acetic acid-induced writhing tests in Swiss albino mice, respectively. Phytochemical profiling revealed the presence of flavonoids, alkaloids, tannins, phenols, saponins, glycosides, and steroids. In vitro, MAEx exhibited dose-dependent protection against haemolysis, achieving 72.43% inhibition at 1000 µg/mL. In vivo, the extract significantly reduced peripheral pain, producing 64.17% and 65.83% inhibition of writhing at doses of 200 and 400 mg/kg, respectively, compared with 77.5% inhibition by the standard, diclofenac sodium. Furthermore, evaluation of central analgesic activity showed a progressive, time-dependent increase in thermal latency, with the 400 mg/kg dose reaching a maximum reaction time of 18.75 s at 90 min. In conclusion, the methanolic seed extract of Musa acuminata possesses potent anti-inflammatory and analgesic activities, which may be mediated by the synergistic effects of its abundant bioactive secondary metabolites. These findings provide scientific support for its traditional therapeutic applications and provide a basis for the isolation of its active components.
Md. Abdul Motaleb Bhuiya, Rounok Jahan Israt, Md. Sohel Rana et al.· European Journal of Medicina...· 0 citations
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
Solanum elaeagnifolium has been utilized for its analgesic, anti-inflammatory, and antioxidant properties to treat a range of conditions, including pain and inflammation. It possesses antibacterial, insecticidal, and molluscicidal properties as well. To investigate the pharmacological potential of the S. elaeagnifolium extract, in vitro, in vivo, and in silico studies were used. Albumin denaturation, heat-induced anti-haemolytic action, and lipooxygenase inhibition were the three techniques used to test anti-inflammatory effectiveness. The phenolic chemicals utilized were identified through the use of high-performance liquid chromatography (HPLC). The effectiveness of the extract in lowering problems connected to diabetes was further evaluated by evaluating fructosamines, carbonyl groups, and β-amyloid formations in albumin glycation. Regarding in vivo studies, the Writhing test and the tail flick test were the two techniques used to evaluate analgesic activity. For docking analysis, we used the following identifiers: cyclooxygenase (PDB ID: 6COX), lipooxygenase (PDB ID: 3V99) and VC1 domain of the receptor for advanced glycation products (PDB ID: 7LMW). The most prevalent phenolic chemicals, according to HPLC analysis, were 3,4-dihydroxybenzoic acid (4.78%), caffeic acid (1.28%), gallic acid (8.18%), ursolic acid (2.6%), syringic acid (1.78%), quercetin (24.09%), catechin (6.67%), and p-coumaric acid (20.49%). Significant suppression of albumin glycation and fructosamine production was demonstrated by the extract, indicating that it may help lessen difficulties associated with diabetes. Furthermore, the extract demonstrated a strong anti-inflammatory impact, with an IC50 of 146 ± 1.17 μg/mL for lipooxygenase inhibition, 87.64 ± 5.35 μg/mL for anti-haemolytic action, and 86.94 ± 1.63 μg/mL for albumin denaturation inhibition. A similar analgesic effect to those of analgesic medications was also demonstrated by SEFE extract. Reinforcing the relevance of the observed effects, the in silico study of the tested activities validated these findings. These findings indicate significant pharmacological promise in the management of diabetes consequences, including inflammation and protein glycation, as well as an analgesic.
Mohammed Bouslamti, Rhizlan Abdnim, Rafik El-mernissi et al.· Current Issues in Molecular...· 0 citations
Ageratum conyzoides is an extensively distributed medicinal plant which has been used in various folk medical practices worldwide for pain relief and treatment of inflammatory conditions, fever, and metabolic syndromes. The aim of this study was to scientifically validate the in vivo pharmacological effects of methanolic extract of the leaves of Ageratum conyzoides, mainly its analgesic, anti-inflammatory, and antidiabetic properties. The analgesic activity was tested on mice using acetic acid induced writhing method. The methanolic extract showed 44.45% inhibition of writhing behavior in mice at a dose of 500 mg/kg body weight, while diclofenac sodium caused 82.22% inhibition of writhing. In the anti-inflammatory evaluation using carrageenan induced paw edema method, the extract showed 54.02% inhibition, whereas diclofenac sodium caused 80.39% inhibition. Antidiabetic effect was determined from the measurement of plasma glucose concentrations in diabetic mice at different periods of time. Blood glucose concentration was decreased by 46.03% due to the action of methanolic extract, and metformin decreased the plasma glucose concentration by 81.23%. From the above experiments, it was concluded that the methanolic extract of leaves of Ageratum conyzoides has potent analgesic and anti-inflammatory properties as well as moderate hypoglycemic activity. It might be due to the bioactivity of some phytochemicals. Further studies should be carried out on this plant for better characterization of its phytochemical components and mechanism of action.
Fahamida Binta Anower, Lamia Akther Enni, Alamgir Hossain et al.· Asian Journal of Basic Scien...· 0 citations
Background: Xanthium strumarium L. is a medicinal herb extensively used in traditional medicine as a remedy for different diseases. In order to
evaluate the anti-diabetic, anti-inflammatory, and antioxidant effects of the ethanolic leaf extract of Xanthium strumarium, this study was conducted.
Methods: For the assessment of the anti-inflammatory effect, carrageenan-induced paw edema in mice model was used. The anti-diabetic effect was
tested in an oral glucose tolerance test (OGTT) model. Anti-oxidant effect was analyzed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical
scavenging assay. Ethanolic extract of Xanthium strumarium was used in a dose of 500 mg/kg body weight and was compared with standard drugs
such as diclofenac sodium (10 mg/kg) and metformin (100 mg/kg).
Results: In the study on anti-inflammatory activity, the ethanolic extract of Xanthium strumarium resulted in significant reduction in paw edema in
comparison with diclofenac sodium (68.85 % and 82.24 % respectively). In the OGTT model, the extract significantly decreased plasma glucose
levels during the experiment with 58.14 % inhibition compared to 84.41 % of metformin. In the DPPH assay, the extract possessed concentration
dependent anti-oxidative activity with percentage inhibition rising from 4.38 % at 1 mg/ml to 56.75 % at 100 mg/ml and ascorbic acid with 8.76 % to
85.72 % inhibition over the same concentration range.
Conclusion: As a result of this study, it could be concluded that ethanolic leaf extract of Xanthium strumarium possesses significant anti-diabetic,
anti-inflammatory and anti-oxidant activity. Pharmacological effects found in the study confirm the use of this plant in traditional medicine and make
it promising in terms of finding a natural bioactive compound for the treatment of diabetes, inflammation, and oxidation associated diseases.
Md. Mahbubol Alam, Md. Jewel Islam, Shourav Nandi et al.· Asian Journal of Basic Scien...· 0 citations
Despite the widespread use of conventional analgesic and anti-inflammatory drugs, their clinical utility is often limited by adverse effects, necessitating the search for safer alternatives from medicinal plants. This study investigated the analgesic and anti-inflammatory activities of the 80% methanolic root extract of Grewia schweinfurthii Burret and an isolated bioactive compound using established rodent models. Air-dried roots were extracted by maceration with 80% methanol, and acute oral toxicity was evaluated following OECD guidelines. Analgesic activity was assessed using the acetic acid–induced writhing and hot plate models in mice, while anti-inflammatory activity was evaluated using carrageenan-induced paw edema in rats. A bioactive compound, 4 (2ʺ-(4′-isopropylphenyl) propan-2ʺ-yl)-2,3-dihydrofuran, was isolated via column chromatography and tested for anti-inflammatory activity. In the writhing test, the extract produced significant (p < 0.001) dose-dependent inhibition of abdominal constrictions, with 13.90%, 56.81%, and 75.48% inhibition at 100, 200, and 400 mg/kg, respectively, compared to 80.77% inhibition by aspirin (150 mg/kg). In the hot plate model, the 400 mg/kg dose significantly prolonged latency time from a baseline of 5.67 ± 0.33 s to 9.17 ± 1.01 s at 120 min (p < 0.05), indicating central analgesic activity. In the carrageenan-induced paw edema model, the extract demonstrated marked anti-inflammatory effects, with 93% inhibition at 400 mg/kg at the 5th hour, comparable to indomethacin (95% inhibition). The isolated compound exhibited significant dose-dependent anti-inflammatory activity, achieving 75% inhibition at 40 mg/kg at 5 hours (p < 0.001). Overall, the findings demonstrate that G. schweinfurthii root extract and its isolated compound possess significant peripheral and central analgesic as well as potent anti-inflammatory activities, supporting the plant’s traditional use; however, further mechanistic, toxicological, and pharmacokinetic studies are required before clinical relevance can be established.
Abdi Leta Gemechu, Mirutse Giday, Solomon Tadesse et al.· PLoS ONE· 1 citation