Nanoparticles prolong N-palmitoylethanolamide anti-inflammatory and analgesic effects in vivo

2016 ◽  
Vol 141 ◽  
pp. 311-317 ◽  
Author(s):  
Diana Tronino ◽  
Alessia Offerta ◽  
Carmine Ostacolo ◽  
Roberto Russo ◽  
Carmen De Caro ◽  
...  
Keyword(s):  
Analgesic Effects ◽  
Anti Inflammatory

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.

In Vivo Anti-Inflammatory and Analgesic Effects of Aqueous Extract of Cistus ladanifer L. From Morocco

2016 ◽  
Vol 23 (6) ◽  
pp. e1554-e1559 ◽  
Author(s):  
Amal El Hamsas El Youbi ◽  
Latifa El Mansouri ◽  
Smahane Boukhira ◽  
Abdeljlil Daoudi ◽  
Dalila Bousta
Keyword(s):  
Aqueous Extract ◽  
Cistus Ladanifer ◽  
Analgesic Effects ◽  
Anti Inflammatory

scholarly journals Analgesic and Anti-Inflammatory Activities of Resveratrol through Classic Models in Mice and Rats

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Guangxi Wang ◽  
Zhiqiang Hu ◽  
Xu Song ◽  
Qiankun Cui ◽  
Qiuting Fu ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Biological Activities ◽  
Drug Candidate ◽  
Hot Plate ◽  
Sod Activity ◽  
Analgesic Effects ◽  
Mouse Ear ◽  
Anti Inflammatory ◽  
Ear Oedema

Background. Inflammation and pain are closely related to humans’ and animals’ health.Resveratrol(RSV) is a natural compound with various biological activities. The current study is aimed to evaluate the analgesic and anti-inflammatory activities of RSV in vivo. Materials and Methods. The analgesic effects were assessed by the acetic acid-induced writhing and hot plate tests. The anti-inflammatory effects were determined using the xylene-induced mouse ear oedema, the acetic acid-induced rat pleurisy, and carrageenan-induced rat synovitis tests, respectively.Results. The analgesic results showed that RSV could significantly inhibit the number of writhes and improve the time and pain threshold of mice standing on hot plate. The anti-inflammatory results showed that RSV could inhibit the ear oedema of mice. In acetic acid-induced pleurisy test, RSV could significantly inhibit the WBC and pleurisy exudates, could decrease the production of NO, and elevate the activity of SOD in serum. In carrageenan-induced synovitis test, RSV could reduce the content of MDA and elevate the T-SOD activity in serum; RSV could inhibit the expressions of TP, PGE2, NO, and MDA.Conclusion. Shortly, these results indicated that RSV had potent analgesic and anti-inflammatory activities and could be a potential new drug candidate for the treatment of inflammation and pain.

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.

Inhibition of LPS-Induced iNOS, COX-2 and Inflammatory Mediator Expression by Paeonol through the MAPKs Inactivation in RAW 264.7 Cells

2009 ◽  
Vol 37 (01) ◽  
pp. 181-194 ◽  
Author(s):  
Hee-Sung Chae ◽  
Ok-Hwa Kang ◽  
Young-Seob Lee ◽  
Jang-Gi Choi ◽  
You-Chang Oh ◽  
...  
Keyword(s):  
Inflammatory Mediator ◽  
Raw 264.7 Cells ◽  
Erk Activation ◽  
Analgesic Effects ◽  
A Cell ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Biting Time

We evaluated the in vivo anti-inflammatory and analgesic activities of orally administered paeonol in mice, and also investigated the anti-inflammatory activity of paeonol in a cell line. Paeonol significantly reduced the edema induced by arachidonic acid in rats. The analgesic effects were assayed using 2 different models, i.e., by acetic acid-induced writhing response and by formalin induced licking and biting time. Moreover, we examined the effects of paeonol on the release of inflammatory mediators such as NO , PGE2 and IL-6. Our results demonstrated that paeonol inhibited LPS induced expression of NO , PGE2 and IL-6. Paeonol prevented LPS induced iNOS, COX-2 and ERK activation. Therefore, paeonol appears to have potential as a treatment for inflammatory disease and analgesic.

scholarly journals (-)-Englerin-A Has Analgesic and Anti-Inflammatory Effects Independent of TRPC4 and 5

2021 ◽  
Vol 22 (12) ◽  
pp. 6380
Author(s):  
João de Sousa Valente ◽  
Khadija M Alawi ◽  
Sabah Bharde ◽  
Ali A. Zarban ◽  
Xenia Kodji ◽  
...  
Keyword(s):  
Thermal Hyperalgesia ◽  
Dependent Manner ◽  
Drg Neurons ◽  
East African ◽  
Cellular Mechanisms ◽  
Analgesic Effects ◽  
Englerin A ◽  
Anti Inflammatory ◽  
Dose Dependent

Recently, we found that the deletion of TRPC5 leads to increased inflammation and pain-related behaviour in two animal models of arthritis. (-)-Englerin A (EA), an extract from the East African plant Phyllanthus engleri has been identified as a TRPC4/5 agonist. Here, we studied whether or not EA has any anti-inflammatory and analgesic properties via TRPC4/5 in the carrageenan model of inflammation. We found that EA treatment in CD1 mice inhibited thermal hyperalgesia and mechanical allodynia in a dose-dependent manner. Furthermore, EA significantly reduced the volume of carrageenan-induced paw oedema and the mass of the treated paws. Additionally, in dorsal root ganglion (DRG) neurons cultured from WT 129S1/SvIm mice, EA induced a dose-dependent cobalt uptake that was surprisingly preserved in cultured DRG neurons from 129S1/SvIm TRPC5 KO mice. Likewise, EA-induced anti-inflammatory and analgesic effects were preserved in the carrageenan model in animals lacking TRPC5 expression or in mice treated with TRPC4/5 antagonist ML204.This study demonstrates that while EA activates a sub-population of DRG neurons, it induces a novel TRPC4/5-independent analgesic and anti-inflammatory effect in vivo. Future studies are needed to elucidate the molecular and cellular mechanisms underlying EA’s anti-inflammatory and analgesic effects.

Investigation of in vivo anti-inflammatory and analgesic effects of rose hip powder (Rosa canina L.)

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
L Saaby ◽  
AK Jäger ◽  
A Heegaard ◽  
SB Christensen
Keyword(s):  
Rosa Canina ◽  
Analgesic Effects ◽  
Rose Hip ◽  
Anti Inflammatory

Formulation Development, Characterization, and Evaluation of a Novel Dexibuprofen-Capsaicin Skin Emulgel with Improved In Vivo Anti-inflammatory and Analgesic Effects

2020 ◽  
Vol 21 (6) ◽  
Author(s):  
Imran Khan Burki ◽  
Muhammad Khalid Khan ◽  
Barkat Ali Khan ◽  
Bushra Uzair ◽  
Valdir A. Braga ◽  
...  
Keyword(s):  
Formulation Development ◽  
Analgesic Effects ◽  
Anti Inflammatory

scholarly journals Anti-Hyperalgesic Properties of Menthol and Pulegone

2021 ◽  
Vol 12 ◽  
Author(s):  
Louis Hilfiger ◽  
Zélie Triaux ◽  
Christophe Marcic ◽  
Eléa Héberlé ◽  
Fathi Emhemmed ◽  
...  
Keyword(s):  
Inflammatory Pain ◽  
Inflammatory Diseases ◽  
Gas Chromatography Mass Spectrometry ◽  
Mentha Piperita ◽  
Necrosis Factor Alpha ◽  
Analgesic Effects ◽  
Anti Inflammatory ◽  
Inflammatory Molecules

Context: Menthol, the main monoterpene found in Mentha piperita L. (M. piperita) is known to modulate nociceptive threshold and is present in different curative preparations that reduce sensory hypersensitivities in pain conditions. While for pulegone, a menthol-like monoterpene, only a limited number of studies focus on its putative analgesic effects, pulegone is the most abundant monoterpene present in Calamintha nepeta (L.) Savi (C. nepeta), a plant of the Lamiaceae family used in traditional medicine to alleviate rheumatic disorders, which counts amongst chronic inflammatory diseases.Objectives: Here, we analyzed the monoterpenes composition of C. nepeta and M. piperita. We then compared the putative anti-hyperalgesic effects of the main monoterpenes found, menthol and pulegone, in acute inflammatory pain conditions.Methods:C. nepeta and M. piperita extracts were obtained through pressurized liquid extraction and analyzed by gas chromatography-mass spectrometry. The in vitro anti-inflammatory activity of menthol or pulegone was evaluated by measuring the secretion of the tumour necrosis factor alpha (TNF α) from LPS-stimulated THP-1 cells. The in vivo anti-hyperalgesic effects of menthol and pulegone were tested on a rat inflammatory pain model.Results: Pulegone and menthol are the most abundant monoterpene found in C. nepeta (49.41%) and M. piperita (42.85%) extracts, respectively. In vitro, both pulegone and menthol act as strong anti-inflammatory molecules, with EC50 values of 1.2 ± 0.2 and 1.5 ± 0.1 mM, respectively, and exert cytotoxicity with EC50 values of 6.6 ± 0.3 and 3.5 ± 0.2 mM, respectively. In vivo, 100 mg/kg pulegone exerts a transient anti-hyperalgesic effect on both mechanical (pulegone: 274.25 ± 68.89 g, n = 8; vehicle: 160.88 ± 35.17 g, n = 8, p < 0.0001), thermal heat (pulegone: 4.09 ± 0.62 s, n = 8; vehicle: 2.25 ± 0.34 s, n = 8, p < 0.0001), and cold (pulegone: 2.25 ± 1.28 score, n = 8; vehicle: 4.75 ± 1.04 score, n = 8, p = 0.0003). In a similar way, 100 mg/kg menthol exerts a transient anti-hyperalgesic effect on both mechanical (mechanical: menthol: 281.63 ± 45.52 g, n = 8; vehicle: 166.25 ± 35.4 g, n = 8, p < 0.0001) and thermal heat (menthol: 3.65 ± 0.88 s, n = 8; vehicle: 2.19 ± 0.26 s, n = 8, <0.0001).Conclusion: Here, we show that both pulegone and menthol are anti-inflammatory and anti-hyperalgesic monoterpenes. These results might open the path towards new compound mixes to alleviate the pain sensation.

Sign in / Sign up

Export Citation Format

Share Document