Adelmidrol, in combination with hyaluronic acid, displays increased anti-inflammatory and analgesic effects against monosodium iodoacetate-induced osteoarthritis in rats

Arthritis is a widespread inflammatory disease associated with progressive articular surface degradation, ongoing pain, and hyperalgesia causing the development of functional limitations and disability. TRPV1 channel is one of the high-potential targets for the treatment of inflammatory diseases. Polypeptide APHC3 from sea anemone Heteractis crispa is a mode-selective TRPV1 antagonist that causes mild hypothermia and shows significant anti-inflammatory and analgesic activity in different models of pain. We evaluated the anti-inflammatory properties of APHC3 in models of monosodium iodoacetate (MIA)-induced osteoarthritis and complete Freund’s adjuvant (CFA)-induced rheumatoid monoarthritis in comparison with commonly used non-steroidal anti-inflammatory drugs (NSAIDs) such as diclofenac, ibuprofen, and meloxicam. Subcutaneous administration of APHC3 (0.1 mg/kg) significantly reversed joint swelling, disability, grip strength impairment, and thermal and mechanical hypersensitivity. The effect of APHC3 was equal to or better than that of reference NSAIDs. Protracted treatment with APHC3 decreased IL-1b concentration in synovial fluid, reduced inflammatory changes in joints, and prevented the progression of cartilage degradation. Therefore, polypeptide APHC3 has the potential to be an analgesic and anti-inflammatory substance for the alleviation of arthritis symptoms.

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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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Analgesic and Anti-Inflammatory Effects of Aucklandia lappa Root Extracts on Acetic Acid-Induced Writhing in Mice and Monosodium Iodoacetate-Induced Osteoarthritis in Rats

Plants ◽

10.3390/plants10010042 ◽

2020 ◽

Vol 10 (1) ◽

pp. 42

Author(s):

Hee-Geun Jo ◽

Geon-Yeong Lee ◽

Chae Yun Baek ◽

Ho Sueb Song ◽

Donghun Lee

Keyword(s):

Acetic Acid ◽

Weight Bearing ◽

Bone Diseases ◽

Joint Disease ◽

Root Extracts ◽

Raw264.7 Macrophages ◽

Age Related ◽

Monosodium Iodoacetate ◽

Anti Inflammatory

Osteoarthritis (OA) is an age-related joint disease and one of the most common degenerative bone diseases among elderly people. The currently used therapeutic strategies relying on nonsteroidal anti-inflammatory drugs (NSAIDs) and steroids for OA are often associated with gastrointestinal, cardiovascular, and kidney disorders, despite being proven effective. Aucklandia lappa is a well-known traditional medicine. The root of A. lappa root has several bioactive compounds and has been in use as a natural remedy for bone diseases and other health conditions. We evaluated the A. lappa root extracts on OA progression as a natural therapeutic agent. A. lappa substantially reduced writhing numbers in mice induced with acetic acid. Monosodium iodoacetate (MIA) was injected into the rats through their knee joints of rats to induce experimental OA, which shows similar pathological characteristics to OA in human. A. lappa substantially reduced the MIA-induced weight-bearing of hind limb and reversed the cartilage erosion in MIA rats. IL-1β, a representative inflammatory mediator in OA, was also markedly decreased by A. lappa in the serum of MIA rats. In vitro, A. lappa lowered the secretion of NO and suppressed the IL-1β, COX-2, IL-6, and iNOS production in RAW264.7 macrophages activated with LPS. Based on its analgesic and anti-inflammatory effects, A. lappa could be a potential remedial agent against OA.

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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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Hyaluronic Acid-Modified and TPCA-1-Loaded Gold Nanocages Alleviate Inflammation

Pharmaceutics ◽

10.3390/pharmaceutics11030143 ◽

2019 ◽

Vol 11 (3) ◽

pp. 143 ◽

Cited By ~ 4

Author(s):

Jingnan Zhao

Keyword(s):

Hyaluronic Acid ◽

Inflammatory Cells ◽

Oxygen Species ◽

Necrosis Factor Alpha ◽

Tnf Α ◽

Nanogold Particles ◽

Gold Nanocages ◽

Factor Alpha ◽

Anti Inflammatory ◽

Necrosis Factor

Gold nanocages (AuNCs) are biocompatible and porous nanogold particles that have been widely used in biomedical fields. In this study, hyaluronic acid (HA) and peptide- modified gold nanocages (HA-AuNCs/T/P) loaded with 2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide (TPCA-1) were prepared to investigate their potential for combating inflammation. TPCA-1 was released from AuNCs, intracellularly when HA was hydrolyzed by hyaluronidase. HA-AuNCs/T/P show a much higher intracellular uptake than AuNCs/T/P, and exhibit a much higher efficacy on the suppression of tumor necrosis factor alpha (TNF-α) and interleukin 6 (IL-6) than free TPCA-1, suggesting great improvement to the anti-inflammatory efficacy of TPCA-1 through the application of AuNCs. HA-AuNCs/T/P can also reduce the production of reactive oxygen species in inflammatory cells. This study suggests that HA-AuNCs/T/P may be potential agents for anti-inflammatory treatment, and are worthy of further investigation.

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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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