Comparison of the anti-inflammatory and analgesic effects of Gentiana macrophylla Pall. and Gentiana straminea Maxim., and identification of their active constituents

The anti-inflammatory and antinociceptive properties of four major compounds from the flowers of Verbascum pterocalycinum var. mutense were investigated. Saponin glycosides called ilwensisaponin A and C and iridoid glycosides known as ajugol and picroside IV were isolated from the methanolic extract. A dose-related anti-inflammatory and antinociceptive response were obtained in this study at doses of 100 and 200 mg/kg. The results of the evaluation of the anti-inflammatory activity induced by carrageenan and PGE1 showed that this species possesses active constituents that could diminish the cyclooxygenase activitiy. No effects were observed in the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema model. Our results support the anti-inflammatory and analgesic effects of Verbascum pterocalycinum var. mutense. Ilwensisaponins A and C could explain in part the anti-inflammatory and analgesic activities of this species. Although antinociceptive and anti-inflammatory activities of ajugol and picroside IV were found insignificant in the statistical analysis, ilwensisaponin A and C showed notable activity without inducing any apparent acute toxicity as well as gastric damage.

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Anti-inflammatory and Analgesic Effects of Ketoprofen in Palm Oil Esters Nanoemulsion

Journal of Oleo Science ◽

10.5650/jos.59.667 ◽

2010 ◽

Vol 59 (12) ◽

pp. 667-671 ◽

Cited By ~ 8

Author(s):

Sakeena M. H. F. ◽

Yam M. F. ◽

Elrashid S. M. ◽

Munavvar A. S. ◽

Azmin M. N.

Keyword(s):

Palm Oil ◽

Analgesic Effects ◽

Anti Inflammatory

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New ibuprofen derivatives with thiazolidine-4-one scaffold with improved pharmaco-toxicological profile

BMC Pharmacology and Toxicology ◽

10.1186/s40360-021-00475-0 ◽

2021 ◽

Vol 22 (1) ◽

Author(s):

Ioana-Mirela Vasincu ◽

Maria Apotrosoaei ◽

Sandra Constantin ◽

Maria Butnaru ◽

Liliana Vereștiuc ◽

...

Keyword(s):

Analgesic Effect ◽

Visceral Pain ◽

Biological Effects ◽

Maximum Effect ◽

Tail Flick ◽

Paw Edema ◽

Cell Viability Assay ◽

Thermal Nociception ◽

Analgesic Effects ◽

Anti Inflammatory

Abstract Background Aryl-propionic acid derivatives with ibuprofen as representative drug are very important for therapy, being recommended especially for anti-inflammatory and analgesic effects. On other hand 1,3-thiazolidine-4-one scaffold is an important heterocycle, which is associated with different biological effects such as anti-inflammatory and analgesic, antioxidant, antiviral, antiproliferative, antimicrobial etc. The present study aimed to evaluated the toxicity degree and the anti-inflammatory and analgesic effects of new 1,3-thiazolidine-4-one derivatives of ibuprofen. Methods For evaluation the toxicity degree, cell viability assay using MTT method and acute toxicity assay on rats were applied. The carrageenan-induced paw-edema in rat was used for evaluation of the anti-inflammatory effect while for analgesic effect the tail-flick test, as thermal nociception in rats and the writhing assay, as visceral pain in mice, were used. Results The toxicological screening, in terms of cytotoxicity and toxicity degree on mice, revealed that the ibuprofen derivatives (4a-n) are non-cytotoxic at 2 μg/ml. In addition, ibuprofen derivatives reduced carrageenan-induced paw edema in rats, for most of them the maximum effect was recorded at 4 h after administration which means they have medium action latency, similar to that of ibuprofen. Moreover, for compound 4d the effect was higher than that of ibuprofen, even after 24 h of administration. The analgesic effect evaluation highlighted that 4 h showed increased pain inhibition in reference to ibuprofen in thermal (tail-flick assay) and visceral (writhing assay) nociception models. Conclusions The study revealed for ibuprofen derivatives, noted as 4 m, 4 k, 4e, 4d, a good anti-inflammatory and analgesic effect and also a safer profile compared with ibuprofen. These findings could suggest the promising potential use of them in the treatment of inflammatory pain conditions.

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IL4-10 Fusion Protein Shows DMOAD Activity in a Rat Osteoarthritis Model

Cartilage ◽

10.1177/19476035211026736 ◽

2021 ◽

pp. 194760352110267

Author(s):

E.M. van Helvoort ◽

H.M. de Visser ◽

F.P.J.G. Lafeber ◽

K. Coeleveld ◽

S. Versteeg ◽

...

Keyword(s):

Fusion Protein ◽

Single Molecule ◽

Mechanical Allodynia ◽

Cartilage Damage ◽

Cartilage Degeneration ◽

Synovial Inflammation ◽

Interleukin 4 ◽

Analgesic Effects ◽

Metabolic Dysregulation ◽

Anti Inflammatory

Objective Ideally, disease-modifying osteoarthritis (OA) drugs (DMOAD) should combine chondroprotective, anti-inflammatory, and analgesic effects in a single molecule. A fusion protein of interleukin-4 (IL-4) and IL-10 (IL4-10 FP) possesses these combined effects. In this study, the DMOAD activity of rat IL4-10 FP (rIL4-10 FP) was tested in a rat model of surgically induced OA under metabolic dysregulation. Design rIL4-10 FP was produced with HEK293F cells. Bioactivity of purified rIL4-10 FP was determined in a whole blood assay. Male Wistar rats ( n = 20) were fed a high-fat diet (HFD) to induce metabolic dysregulation. After 12 weeks, OA was induced according to the Groove model. Two weeks after OA induction, rats were randomly divided into 2 groups and treated with 10 weekly, intra-articular injections of either rIL4-10 FP ( n = 10) or phosphate buffered saline (PBS; n = 10). Possible antibody formation was evaluated using ELISA, cartilage degeneration and synovial inflammation were evaluated by histology and mechanical allodynia was evaluated using the von Frey test. Results Intra-articular injections with rIL4-10 FP significantly reduced cartilage degeneration ( P = 0.042) and decreased mechanical allodynia ( P < 0.001) compared with PBS. Only mild synovial inflammation was found (nonsignificant), limiting detection of putative anti-inflammatory effects. Multiple injections of rIL4-10 FP did not induce antibodies against rIL4-10 FP. Conclusion rIL4-10 FP showed chondroprotective and analgesic activity in a rat OA model with moderate cartilage damage, mild synovial inflammation, and pain. Future studies will need to address whether less frequent intra-articular injections, for example, with formulations with increased residence time, would also lead to DMOAD activity.

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Flunixin Meglumine Reduces Milk Isoprostane Concentrations in Holstein Dairy Cattle Suffering from Acute Coliform Mastitis

Antioxidants ◽

10.3390/antiox10060834 ◽

2021 ◽

Vol 10 (6) ◽

pp. 834

Author(s):

Carsten C. F. Walker ◽

Jill L. Brester ◽

Lorraine M. Sordillo

Keyword(s):

Medical Intervention ◽

Systemic Involvement ◽

Analgesic Effects ◽

Markers Of Inflammation ◽

Inflammatory Mediator Production ◽

Flunixin Meglumine ◽

Coliform Mastitis ◽

Cox 2 ◽

Anti Inflammatory ◽

Oxidant Status

Dysfunctional inflammation contributes significantly to the pathogenesis of coliform mastitis and the classical pro-inflammatory enzyme cyclooxygenase-2 (COX-2) is the target of medical intervention using the non-steroidal anti-inflammatory drug (NSAID) flunixin meglumine (FM). Inhibition of COX-2 by FM can decrease concentrations of pro-inflammatory fatty acid-based mediators called eicosanoids, providing antipyretic and analgesic effects in dairy cows suffering from coliform mastitis. However, approximately 50% of naturally occurring coliform mastitis with systemic involvement results in death of the animal, even with NSAID treatment. Inadequate antioxidant potential (AOP) to neutralize reactive oxygen species (ROS) produced during excessive inflammation allows for oxidative stress (OS), contributing to tissue damage during coliform mastitis. Biomarkers of lipid peroxidation by ROS, called isoprostanes (IsoP), were used in humans and cattle to quantify the extent of OS. Blood IsoP were shown to be elevated and correlate with oxidant status during acute coliform mastitis. However, the effect of FM treatment on oxidant status and markers of OS has not been established. Blood IsoP concentrations were used to quantify systemic OS, whereas milk was used to assess local OS in the mammary gland. Results indicate that FM treatment had no effect on blood markers of inflammation but reduced the oxidant status index (OSi) by increasing blood AOP from pre- to post-FM treatment. Milk AOP significantly increased from pre- to post-FM treatment, whereas ROS decreased, resulting in a decreased OSi from pre- to post-FM treatment. The only blood IsoP concentration that was significantly different was 5-iso-iPF2α-VI, with a decreased concentration from pre- to post-FM treatment. Conversely, milk 5-iso-iPF2α-VI, 8,12-iso-iPF2α-VI, and total IsoP concentrations were decreased following FM treatment. These results indicated that administration of FM did improve systemic and local oxidant status and reduced local markers of OS. However, differential effects were observed between those animals that survived the infection and those that died, indicating that pre-existing inflammation and oxidant status greatly affect efficacy of FM and may be the key to reducing severity and mortality associated with acute coliform infections. Supplementation to improve AOP and anti-inflammatory mediator production may significantly improve efficacy of FM treatment.

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Assessment of the antioxidant, thrombolytic, analgesic, anti-inflammatory, antidepressant and anxiolytic activities of leaf extracts and fractions of Tetracera sarmentosa (L.) Vahl

Journal of Basic and Clinical Physiology and Pharmacology ◽

10.1515/jbcpp-2016-0173 ◽

2018 ◽

Vol 29 (1) ◽

pp. 81-93 ◽

Cited By ~ 7

Author(s):

Mir Muhammad Nasir Uddin ◽

Mohammad Shah Hafez Kabir ◽

Mahmud Hasan ◽

Zobaer Al Mahmud ◽

N. M. Mahmudul Alam Bhuiya ◽

...

Keyword(s):

Flowering Plant ◽

Clot Lysis ◽

Leaf Extracts ◽

Immersion Method ◽

Pure Ethanol ◽

Thrombolytic Activity ◽

Writhing Test ◽

Analgesic Effects ◽

Tail Immersion ◽

Anti Inflammatory

AbstractBackground:The plant under investigation (Tetracera sarmentosa) is a dicotyledonous flowering plant and belongs to the family Dilleniaceae. The goal of our investigation was to determine whether the leaf extracts of this plant held any significant medicinal properties.Methods:Leaves ofT. sarmentosawere extracted with pure ethanol (EETS) and methanol (METS), and then methanol extract fractioned withn-hexane (NHFMETS) and chloroform (CHFMETS). The extracts and fractions were tested for antioxidant activity, which was measured by using qualitative and quantitative procedures. Thrombolytic activity was evaluated by the clot lysis test. Analgesic activity was evaluated employing the acidic acid-induced writhing test, the formalin-induced paw licking test and tail immersion on Swiss albino mice. The anti-inflammatory activity test was studied using the paw edema test. Forced swimming, tail suspension, elevated plus maze and hole board model tests were used to evaluate neuropharmacological activity.Results:All the extracts and fractions possessed antioxidant effects. All the extracts, fractions and streptokinase exhibited significant (p<0.0001) clot lysis. The extracts and fractions produced significant analgesic effects as evaluated by the acetic acid writhing test, the formalin-induced paw licking test and the tail immersion method. Similarly, carrageenan-induced inflammation was significantly antagonized by the treatments. The extracts and fractions also significantly showed neuropharmacological (antidepressant and anxiolytic) effects.Conclusions:The overall results suggested that this plant deserves further investigation to isolate the active compounds which are responsible for these activities and to establish the mechanism of action.

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Anti-inflammatory and analgesic effects of 6α,7β–dihydroxy-vouacapan-17β-oic acid isolated from Pterodon emarginatus Vog. fruits

Inflammopharmacology ◽

10.1007/s10787-011-0081-9 ◽

2011 ◽

Vol 19 (3) ◽

pp. 139-143 ◽

Cited By ~ 21

Author(s):

Camila Benatti Galceran ◽

Jayme Antonio Aboin Sertie ◽

Clarissa Silva Lima ◽

José Carlos Tavares Carvalho

Keyword(s):

Analgesic Effects ◽

Anti Inflammatory

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Experience of application of topichesky naturopathic means for patients with ent pathology

Medical Council ◽

10.21518/2079-701x-2019-8-33-37 ◽

2019 ◽

pp. 33-37

Author(s):

G. N. Nikiforova ◽

V. M. Svistushkin ◽

L. S. Karapetian

Keyword(s):

Clinical Practice ◽

Surgical Interventions ◽

Arnica Montana ◽

Analgesic Effects ◽

Reactive Changes ◽

Inflammatory Processes ◽

Post Traumatic ◽

Reparative Effect ◽

Anti Inflammatory ◽

Reactive Processes

Post-traumatic reactive changes in the area of ENT-organs can cause cosmetic defects, contribute to the development of infectious and inflammatory processes. The formation of limited edema and bruising is natural after certain even adequately performed surgical interventions. In clinical practice, the question arises of the effective and safe use of local drugs that have anti-inflammatory, anti-edema and analgesic effects to accelerate the course of post-traumatic reactive processes. Naturopathic agents have high safety, sufficiently pronounced anti-inflammatory, analgesic and reparative effect. The drug based on arnica mountain (Arnica montana) is a unique topical drug that only contains fresh Arnica plants in a concentration of 7% TM. Efficiency and high safety of this drug allows us to recommend it for the treatment of bruises and hematomas of the skin in the area of ENT-organs, including after surgical interventions.

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Preliminary assessment of the anti-inflammatory and analgesic effects of methanol leaf extract of Cussonia barteri (Araliaceae) in rodents

Herba Polonica ◽

10.2478/hepo-2019-0015 ◽

2019 ◽

Vol 65 (3) ◽

pp. 22-31

Author(s):

Ighodaro Igbe ◽

Osaze Edosuyi ◽

Agbonlahor Okhuarobo ◽

Adarki Pongri ◽

Nkechi Maduako ◽

...

Keyword(s):

Acetic Acid ◽

Analgesic Effect ◽

Leaf Extract ◽

Methanol Extract ◽

Tail Flick ◽

Hot Plate ◽

Analgesic Effects ◽

Paw Oedema ◽

Anti Inflammatory ◽

Ear Oedema

Summary Introduction: Potato (Solanum tuberosum L.) is an important vegetable crop in Syria. Potato tuber moth Cussonia barteri is a small tree that grows in the sub-Saharan part of Africa. Various parts of the plant are used for the treatment of a variety of ailments in ethno-medicine. Objective: To evaluate the anti-inflammatory and analgesic effect of the methanol leaf extract of Cussonia barteri. Material and methods: The leaves were air-dried, powdered and repeatedly extracted with methanol using a Soxhlet apparatus. The resulting methanol extract (100, 200 and 400 mg/kg) was evaluated for anti-inflammatory activity using carrageenan-induced paw oedema, xylene-induced ear oedema and formalin-induced arthritis tests. Analgesic effect was evaluated using acetic acid-induced mouse writhing, hot plate and tail flick tests. Results: All doses of the extract significantly (p<0.05) reduced carrageenan-induced paw oedema, however the 400 mg/kg dose gave a sustained effect. The extract significantly inhibited xylene induced ear oedema at all doses. There were no significant (p>0.05) reductions in paw swellings due to formalin. In the acetic acid induced writhing test, the extract significantly (p<0.05) decreased writhing at 400 mg/kg only. Reaction times were not significantly different from the control in the hot plate and tail flick tests. Conclusion: This study has shown that the methanol extract possesses acute anti-inflammatory and peripherally mediated analgesic effects.

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Lactoferrin and Its Potential Impact for the Relief of Pain: A Preclinical Approach

Pharmaceuticals ◽

10.3390/ph14090868 ◽

2021 ◽

Vol 14 (9) ◽

pp. 868

Author(s):

Beatriz Godínez-Chaparro ◽

Fabiola Guzmán-Mejía ◽

Maria Elisa Drago-Serrano

Keyword(s):

Pain Treatment ◽

Low Density Lipoprotein ◽

Density Lipoprotein ◽

Kidney Injury ◽

Analgesic Efficacy ◽

Intestinal Bleeding ◽

Ulcer Formation ◽

Analgesic Effects ◽

Density Lipoprotein Receptor ◽

Anti Inflammatory

Pain is one of the most disabling symptoms of several clinical conditions. Neurobiologically, it is classified as nociceptive, inflammatory, neuropathic and dysfunctional. Opioids and nonsteroidal anti-inflammatory drugs (NSAIDs) are conventionally prescribed for the treatment of pain. Long-term administration of opioids results in the loss of analgesic efficacy, leading to increased dosage, tolerance, and addiction as the main drawbacks of their use, while the adverse effects of NSAIDs include gastric ulcer formation, intestinal bleeding, acute kidney injury, and hepatotoxicity. Lactoferrin is an iron-binding, anti-inflammatory glycoprotein that displays analgesic activities associated, in part, by interacting with the low-density lipoprotein receptor-related protein (LRP), which may result in the regulation of the DAMP–TRAF6–NFκB, NO–cGMP–ATP K+-sensitive channel and opioid receptor signaling pathways. This review summarizes and discusses for the first time the analgesic effects of lactoferrin and its presumable mechanisms based on pre-clinical trials. Given its anti-nociceptive and anti-inflammatory properties, lactoferrin may be used as an adjunct to enhance the efficacy and to decrease the tolerogenic effects of canonical therapeutic drugs prescribed for pain treatment.

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