scholarly journals Anti-Inflammatory and Analgesic Effects of TRPV1 Polypeptide Modulator APHC3 in Models of Osteo- and Rheumatoid Arthritis

Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 39
Author(s):  
Yulia A. Logashina ◽  
Yulia A. Palikova ◽  
Viktor A. Palikov ◽  
Vitaly A. Kazakov ◽  
Sviatlana V. Smolskaya ◽  
...  
Keyword(s):  
Mild Hypothermia ◽  
Inflammatory Diseases ◽  
Articular Surface ◽  
Functional Limitations ◽  
Subcutaneous Administration ◽  
Cartilage Degradation ◽  
Analgesic Effects ◽  
Monosodium Iodoacetate ◽  
Anti Inflammatory ◽  
Trpv1 Antagonist

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.

scholarly journals Evaluation of analgesic and anti-inflammatory activities of Warionia saharae essential oil

2021 ◽  
pp. 1-10
Author(s):  
Mimouna Yakoubi ◽  
Nasser Belboukhari ◽  
Khaled Sekkoum ◽  
Mohammed Bouchekara ◽  
Hassan Y. Aboul-Enein
Keyword(s):  
Essential Oil ◽  
Traditional Medicine ◽  
Analgesic Activity ◽  
Inflammatory Diseases ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Standard Drug ◽  
Analgesic Effects ◽  
Test Models ◽  
Anti Inflammatory

Warionia saharae Benth & Coss (W.s) (Asteraceae) is a monospecific genus endemic to Algeria and Morocco. Its leaves are used in their traditional medicine, such as gastrointestinal and inflammatory diseases; for instance, rheumatoid arthritis treatment. In this work, our team investigated the anti-inflammatory and analgesic effects of essential oil extracted from the dried upper parts of Warionia saharae based on different standard experimental test models. The analgesic activity was assessed by central and peripheral models, such as “hot plate” and “writhing” tests on Swiss albino mice. The hot plate test used latency measurements to assess acute cutaneous pain sensitivity, as a result; the latency of the hind-paw pain response was by licking and either shaking or jumping, those occurrences were recorded. Writhing test as a chemical method used to induce pain of peripheral origin in mice by injecting acetic acid intraperitoneally (IP). This results in characteristic stretching behavior of the animals (cramps and contortions). The evaluation of the analgesic activity, shows that the essential oil of this plant induces a decrease in the number of abdominal cramps in the contortion test and a maximum inhibition of pain. As for the anti-inflammatory effect, it was studied by the “paw edema” test, a phlogogenic agent (formaldehyde) was used to stimulate inflammation in the paws of mice. Anti-inflammatory properties can be observed by inhibiting this edema compared to the standard drug Diclofenac. In conclusion, Warionia saharae essential oil (75 mg/kg) showed a strong anti-inflammatory and analgesic activities which supports the conventional use of this plant in traditional medicine.

scholarly journals Betulinic Acid-Azaprostanoid Hybrids: Synthesis and Pharmacological Evaluation as Anti-inflammatory Agents

2020 ◽  
Vol 19 (3) ◽  
pp. 254-267
Author(s):  
Tatyana S. Khlebnicova ◽  
Yuri A. Piven ◽  
Fedor A. Lakhvich ◽  
Iryna V. Sorokina ◽  
Tatiana S. Frolova ◽  
...  
Keyword(s):  
Cell Lines ◽  
Betulinic Acid ◽  
Inflammatory Diseases ◽  
Toxic Agent ◽  
Analgesic Effects ◽  
Low Toxic ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Background: Prevention and treatment of chronic inflammatory diseases require effective and low-toxic medicines. Molecular hybridization is an effective strategy to enhance the biological activity of new compounds. Triterpenoid scaffolds are in the focus of attention owing to their anti-inflammatory, antiviral, antiproliferative, and immunomodulatory activities. Heteroprostanoids have different pleiotropic effects in acute and chronic inflammatory processes. Objective: The study aimed to develop structurally new and low toxic anti-inflammatory agents via hybridization of betulinic acid with azaprostanoic acids. Methods: A series of betulinic acid-azaprostanoid hybrids was synthesized. The synthetic pathway included the transformation of betulin via Jones' oxidation into betulonic acid, reductive amination of the latter and coupling obtained by 3β-amino-3-deoxybetulinic acid with the 7- or 13-azaprostanoic acids and their homo analogues. The hybrids 1-9 were investigated in vivo on histamine-, formalin- and concanavalin A-induced mouse paw edema models and two models of pain - the acetic acid-induced abdominal writhing and the hotplate test. The hybrids were in vitro evaluated for cytotoxic activity on cancer (MCF7, U- 87 MG) and non-cancer humane cell lines. Results: In the immunogenic inflammation model, the substances showed a pronounced anti-inflammatory effect, which was comparable to that of indomethacin. In the models of the exudative inflammation, none of the compounds displayed a statistically significant effect. The hybrids produced weak or moderate analgesic effects. All the agents revealed low cytotoxicity on human immortalized fibroblasts and cancer cell lines compared with 3β- amino-3-deoxybetulinic acid and doxorubicin. Conclusion: The results indicate that the principal anti-inflammatory effect of hybrids is substantially provided with the triterpenoid scaffold and in some cases with the azaprostanoid scaffold, but the latter makes a significant contribution to reducing the toxicity of hybrids. Hybrid 1 is of interest as a potent low toxic agent against immune-mediated inflammation.

scholarly journals Mechanisms Underlying the Antinociceptive, Antiedematogenic, and Anti-Inflammatory Activity of the Main Flavonoid fromKalanchoe pinnata

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Raquel Teixeira Ferreira ◽  
Marcela Araújo Soares Coutinho ◽  
David do Carmo Malvar ◽  
Elson Alves Costa ◽  
Iziara Ferreira Florentino ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Inflammatory Diseases ◽  
Subcutaneous Administration ◽  
Mechanisms Of Action ◽  
Selectivity Index ◽  
Kalanchoe Pinnata ◽  
Flavonoid Quercetin ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Kalanchoe pinnata(KP) is popularly used for treating inflammatory diseases. This study investigated the antinociceptive, antiedematogenic, and anti-inflammatory potential of the subcutaneous administration of KP flower aqueous extract (KPFE), its ethyl acetate (EtOAcF) and butanol (BuOHF) fractions, and the main KP flavonoid [quercetin 3-O-α-L-arabinopyranosyl (1→2)α-L-rhamnopyranoside] (KPFV) in mice, as well as its possible mechanisms of action. KPFE (30–300 mg/kg) and KPFV (1–10 mg/kg) inhibited the acetic acid-induced writhing (ID50= 164.8 and 9.4 mg/kg, resp.). KPFE (300 mg/kg), EtOAcF (12 mg/kg), BuOHF (15 mg/kg), or KPFV (0.3–3.0 mg/kg) reduced leukocyte migration on carrageenan-induced pleurisy (ID50= 2.0 mg/kg for KPFV). KPFE (3–30 mg/kg) and KPFV (0.3–3.0 mg/kg) reduced the croton oil-induced ear edema (ID50= 4.3 and 0.76 mg/kg, resp.). KPFE and KPFV reduced the TNF-αconcentration in the pleural exudates on carrageenan-induced pleurisy test. Moreover, KPFV inhibited COX-1 (IC50= 22.1 μg/mL) and COX-2 (IC50> 50 μg/mL). The selectivity index (COX-1IC50/COX-2IC50) was <0.44. These results indicate that KPFE and KPFV produced antinociceptive, antiedematogenic, and anti-inflammatory activities through COX inhibition and TNF-αreduction, revealing that the main flavonoid in KP flowers and leaves plays an important role in the ethnomedicinal use of the plant.

scholarly journals Analgesic and Anti-Inflammatory Activities of Methanol Extract ofFicus pumilaL. in Mice

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Chi-Ren Liao ◽  
Chun-Pin Kao ◽  
Wen-Huang Peng ◽  
Yuan-Shiun Chang ◽  
Shang-Chih Lai ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Methanol Extract ◽  
Inflammatory Diseases ◽  
Paw Edema ◽  
Tissue Destruction ◽  
Hplc Fingerprint ◽  
Analgesic Effects ◽  
Inflammatory Mechanism ◽  
Tnf Α ◽  
Anti Inflammatory

This study investigated possible analgesic and anti-inflammatory mechanisms of the methanol extract ofFicus pumila(FPMeOH). Analgesic effects were evaluated in two models including acetic acid-induced writhing response and formalin-induced paw licking. The results showedFPMeOHdecreased writhing response in the acetic acid assay and licking time in the formalin test. The anti-inflammatory effect was evaluated by λ-carrageenan-induced mouse paw edema and histopathological analyses.FPMeOHsignificantly decreased the volume of paw edema induced by λ-carrageenan. Histopathologically,FPMeOHabated the level of tissue destruction and swelling of the edema paws. This study indicated anti-inflammatory mechanism ofFPMeOHmay be due to declined levels of NO and MDA in the edema paw through increasing the activities of SOD, GPx, and GRd in the liver. Additionally,FPMeOHalso decreased the level of inflammatory mediators such as IL-1β, TNF-α, and COX-2. HPLC fingerprint was established and the contents of three active ingredients, rutin, luteolin, and apigenin, were quantitatively determined. This study provided evidence for the classical treatment ofFicus pumilain inflammatory diseases.

scholarly journals Investigation of the Anti-Inflammatory and Analgesic Activities of Ethanol Extract of Stem Bark of SonapathaOroxylum indicum In Vivo

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
K. Lalrinzuali ◽  
M. Vabeiryureilai ◽  
Ganesh Chandra Jagetia
Keyword(s):  
Inflammatory Diseases ◽  
Ethanol Extract ◽  
Stem Bark ◽  
The Body ◽  
Protective Measure ◽  
Analgesic Effects ◽  
Oroxylum Indicum ◽  
Anti Inflammatory ◽  
Analgesic Activities

Inflammation is all a pervasive phenomenon, which is elicited by the body in response to obnoxious stimuli as a protective measure. However, sustained inflammation leads to several diseases including cancer. Therefore it is necessary to neutralize inflammation. Sonapatha (Oroxylum indicum), a medicinal plant, is traditionally used as a medicine in Ayurveda and other folk systems of medicine. It is commonly used to treat inflammatory diseases including rheumatoid arthritis and asthma. Despite this fact its anti-inflammatory and analgesic effects are not evaluated scientifically. Therefore, the anti-inflammatory and analgesic activities of Sonapatha (Oroxylum indicum) were studied in Swiss albino mice by different methods. The hot plate, acetic acid, and tail immersion tests were used to evaluate the analgesic activity whereas xylene-induced ear edema and formalin induced paw edema tests were used to study the anti-inflammatory activity of Sonapatha. The administration of mice with 250 and 300 mg/kg b.wt. ofO. indicumreduced pain and inflammation indicating that Sonapatha possesses analgesic and anti-inflammatory activities. The maximum analgesic and anti-inflammatory activities were observed in mice receiving 300 mg/kg b.wt. ofO. indicumethanol extract.Our study indicates thatO. indicumpossesses both anti-inflammatory and analgesic activities and it may be useful as an anti-inflammatory agent in the inflammation related disorders.

Evaluation of anti-inflammatory and analgesic activities and the phytochemical study of Astragalus arbusculinus gum in animal models

2015 ◽  
Vol 26 (4) ◽  
Author(s):  
Asie Shojaii ◽  
Manijeh Motevalian ◽  
Nazanin Rahnama
Keyword(s):  
Aqueous Extract ◽  
Wistar Rats ◽  
Inflammatory Diseases ◽  
Phytochemical Study ◽  
Analgesic Effects ◽  
Male Wistar Rats ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
First Time ◽  
Different Doses

AbstractThe importance of inflammatory diseases and side effects of conventional drugs necessitate the finding of new anti-inflammatory agents from natural sources. In this study, for the first time, the anti-inflammatory and analgesic effects of the aqueous extract ofThirty-five male Wistar rats were divided into five groups and pretreated with different doses ofThe extract ofThe aqueous extract of

scholarly journals Analgesic and Anti-Inflammatory Activities of the Ethanolic Extract ofArtemisia morrisonensisHayata in Mice

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Shen-Chieh Chou ◽  
Yung-Jia Chiu ◽  
Chao-Jung Chen ◽  
Ying-Chih Lin ◽  
Chung-Hao Wu ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Inflammatory Diseases ◽  
Ethanolic Extract ◽  
Paw Edema ◽  
Necrosis Factor Alpha ◽  
Isolation And Purification ◽  
Analgesic Effects ◽  
Inflammatory Mechanism ◽  
Anti Inflammatory ◽  
Ethnobotanical Uses

The aim of this study was to investigate the possible analgesic and anti-inflammatory mechanisms of the ethanolic extract ofA. morrisonensisHayata (AMEtOH). Two models were employed for evaluation of the analgesic effects: acetic acid-induced writhing response and formalin-induced paw licking. The results demonstrated thatAMEtOHdecreased writhing response for both the acetic acid assay and the licking time in the formalin test. The anti-inflammatory effect was evaluated by paw edema of mice induced byλ-carrageenan.AMEtOHsignificantly decreased induced paw edema three to four hours afterλ-carrageenan injection. Additionally, the results indicated that the anti-inflammatory mechanism ofAMEtOHmay be due to the declined levels of nitric oxide (NO) and malondialdehyde (MDA) in the edematous paw. Furthermore,AMEtOHdecreased the tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) levels, leading to the reduction of prostaglandins and subsequently alleviated edema. Isolation and purification of theAMEtOHextract determinedp-hydroxyacetophenone to be a major component at 130 mg/g of extract. No mortality was observed in the acute toxicity test given at the dose of 10 g/kg. This study demonstrated the possible mechanisms for the analgesic and anti-inflammatory effects ofAMEtOHfor mice and provided evidence for the ethnobotanical uses ofA. morrisonensisin treating inflammatory diseases.

scholarly journals Trans-Cinnamaldehyde Inhibits IL-1β-Stimulated Inflammation in Chondrocytes by Suppressing NF-κB and p38-JNK Pathways and Exerts Chondrocyte Protective Effects in a Rat Model of Osteoarthritis

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Tianwei Xia ◽  
Runzi Gao ◽  
Guowei Zhou ◽  
Jinzhu Liu ◽  
Jinsheng Li ◽  
...  
Keyword(s):  
Cell Viability ◽  
Cartilage Degradation ◽  
Cartilage Destruction ◽  
Dependent Manner ◽  
Protective Effects ◽  
Monosodium Iodoacetate ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Objective. Trans-cinnamaldehyde (TCA), a compound from Cinnamomum cassia Presl, has been reported to have anti-inflammatory effect. However, its effect on cartilage degradation in osteoarthritis is unclear. This study is designed to examine the effects of TCA on cartilage in vitro and in vivo. Material and Methods. SW1353 cells and human primary chondrocytes were treated with varying concentrations of TCA (2-20 μg/ml) for 2 h followed by IL-1β stimulation. Cell viability was examined by the MTT assay. Expression of MMP-1, MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5 was examined by Western blot and RT-qPCR. Monosodium iodoacetate (MIA)-induced OA was established in rats to assess the chondrocyte protective effects of intraperitoneal injection of TCA (50 mg/kg). Results. TCA at a concentration of 10 μg/ml had no significant effect on cell viability. MMP-1, MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5 were decreased by TCA 2-10 μg/ml in a dose-dependent manner (all P<0.05). Pretreatment with TCA decreased the degradation of IκBα and increased the expression of p-IκBα, indicating that NF-κB inactivation was induced by TCA in IL-1β-stimulated SW1353 cells. Pretreatment with TCA decreased the levels of p-p38 and p-JNK, while the levels of p-ERK were not significantly affected. TCA 10 μg/ml significantly decreased expression levels of MMP-1, MMP-3, MMP-13, ADAMTS-4, and ADAMTS-5. In vivo results showed that TCA alleviated cartilage destruction and the OARSI scores. Conclusion. TCA possesses anti-inflammatory effect in vitro and exerts chondrocyte protective effects in vivo, in which NF-κB and p38-JNK were involved.

scholarly journals Osteoarthritis treatment with a novel nutraceutical acetylated ligstroside aglycone, a chemically modified extra-virgin olive oil polyphenol

2020 ◽  
Vol 11 ◽  
pp. 204173142092270
Author(s):  
María C de Andrés ◽  
Mia S Meiss ◽  
Marina Sánchez-Hidalgo ◽  
Alejandro González-Benjumea ◽  
Jose G Fernández-Bolaños ◽  
...  
Keyword(s):  
Olive Oil ◽  
Inflammatory Diseases ◽  
Virgin Olive Oil ◽  
Extra Virgin Olive Oil ◽  
Cartilage Degradation ◽  
Cartilage Explants ◽  
Low Grade ◽  
Nitric Oxide Release ◽  
Anti Inflammatory ◽  
Inflammatory Profile

Recent studies have shown that dietary patterns confer protection from certain chronic diseases related to oxidative stress, the immune system and chronic low-grade inflammatory diseases. The aim of this study was to evaluate the anti-inflammatory potential and the capacity to attenuate cartilage degradation using extra-virgin olive oil–derived polyphenols for the treatment of osteoarthritis. Results show that both nutraceuticals ligstroside aglycone and acetylated ligstroside aglycone showed an anti-inflammatory profile. Acetylated ligstroside aglycone significantly reduced the expression of pro-inflammatory genes including NOS2 and MMP13 at both RNA and protein levels; decreased nitric oxide release; and, importantly, reduced proteoglycan loss in human osteoarthritis cartilage explants. Our study demonstrated that a new synthetic acetylated ligstroside aglycone derivative offers enhanced anti-inflammatory profile than the natural nutraceutical compound in osteoarthritis. These results substantiate the role of nutraceuticals in osteoarthritis with implications for therapeutic intervention and our understanding of osteoarthritis pathophysiology.

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