In vivo methods for the evaluation of anti-inflammatory and antinoceptive potential

Junior, Almeida; de, Silvio

doi:10.5935/2595-0118.20190070

Cited by 12 publications

(6 citation statements)

References 29 publications

(31 reference statements)

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“…Different mechanisms of actions are involved leading to releasing of several mediators such as histamine, bradykinin, and serotonin by the cells during 1 h [43,44]. In the next 2-3 h, prostaglandins (PGE1, PGE2) responsible for acute inflammation are released [44,45].…”

Section: Discussionmentioning

confidence: 99%

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

et al. 2020

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The purpose of this study was to evaluate the in vivo biological potential of new azetidine-2-one derivatives of ferulic acid (6a–f). First, the in vivo acute toxicity of azetidine-2-one derivatives of ferulic acid on Swiss white mice was investigated and, based on the obtained results, it can be stated that the studied derivatives belong to compounds with moderate toxicity. The in vivo anti-inflammatory potential of these derivatives was determined in a model of acute inflammation induced by carrageenan in rats and in a chronic inflammation model induced in rats using the granuloma test. In the acute inflammation model, all the studied compounds had a maximum anti-inflammatory effect 24 h after administration, which suggests that these compounds may be classified, from a pharmacokinetic point of view, in the category of long-acting compounds. The most active compound in the series was found to be compound 6b. In the case of the chronic inflammation model, it was observed that the studied compounds (6a–f) reduced the formation of granulation tissue compared to the control group, having an intense effect of inhibiting the proliferative component. The most important inhibitory effect of inhibiting the proliferative component was recorded for compound 6b. Additionally, the investigation of liver function was performed by determining the serum levels of liver enzymes aspartate transaminase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and bilirubin (total and direct). The results showed that, in the series of azetidin-2-one derivatives, the liver enzymes concentration values were close to those recorded for the reference anti-inflammatories (diclofenac sodium and indomethacin) and slightly higher compared to the values for the healthy control group. At the end of the experiment, the animals were euthanized and fragments of liver, lung, and kidney tissue were taken from all groups in the study. These were processed for histopathological examination, and we noticed no major changes in the groups treated with the azetidine 2-one derivatives of ferulic acid compared to the healthy groups.

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Section: Discussionmentioning

confidence: 99%

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

et al. 2020

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“…The effects of treatment with drugs on inflammatory components in the present study were evaluated using a carrageenan and zymosan-induced air-pouch model. These tests induce acute and not immune inflammation, that is well-validated, and widely reproduced in numerous studies ( 43 , 44 ). Signs of inflammation (edema, hyperalgesia, erythema) become visible shortly after subcutaneous injection of such stimuli through the activation of pro-inflammatory agents ( 43 ).…”

Section: Discussionmentioning

confidence: 96%

“…Another important point related to the chemical characteristics of these substituents is the hydrophilic radicals that favor lower toxicity of the compounds ( 5 , 44-46 ). However, further in vivo studies are required to investigate the specific underlying mechanisms.…”

Section: Discussionmentioning

confidence: 99%

PA‑Int5: An isatin‑thiosemicarbazone derivative that exhibits anti‑nociceptive and anti‑inflammatory effects in Swiss mice

et al. 2021

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Pain and inflammation are symptoms of various diseases, and they can be modulated by different pathways, thus highlighting the importance of investigating the therapeutic effects of novel compounds. Previous studies have shown that isatin-thiosemicarbazone exhibits antitumor, antifungal antibacterial and other biological properties. Based on the wide range of biological effects of these compounds, the aim of the present study was to investigate the central nervous system (CNS) performance, and the anti-nociceptive and anti-inflammatory activity of (Z)-2-(5-nitro-2-oxoindolin-3-ilidene)-N-hydroazinecarbothioamide (PA-Int5) in treated mice. Three doses of PA-Int5 were tested orally (1.0, 2.5 and 5.0 mg/kg) in the nociceptive and inflammatory animal models. Additionally, the potential sedative effects of PA-Int5 (5 mg/kg, oral gavage) were investigated using an open ﬁeld and rotarod tests, to exclude any possible unspecific effects of the nociceptive assays. Anti-nociceptive activity was assessed using the acetic acid-induced abdominal contortion and formalin tests, whereas anti-inflammatory activity was assessed using a carrageenan-induced paw edema and zymosan-induced air-pouch models. PA-Int5 (5 mg/kg) induced anti-nociceptive activity in the abdominal contortion model. In the formalin test, PA-Int5 (at 2.5 and 5 mg/kg) reduced nociception in the second phase. At the higher dose tested, PA-Int5 did not affect spontaneous locomotion or motor coordination. The data revealed that at all doses tested, the compound significantly reduced paw edema following carrageenan administration. In the zymosan-induced air-pouch model, PA-Int5 potently inhibited leukocyte migration and protein levels at the site of inflammation. When combined, the results revealed, for the first time, that PA-Int5 exhibited anti-nociceptive and anti-inflammatory activities, and highlights its potential, as well that of other derivatives, as novel candidates for pain relief.

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“…Importante ressaltar que o processo de aprendizado, assim como curva de aprendizado, depende da região e acesso à tecnologia em que o médico cirurgião está Brazilian Journal of Health Review, Curitiba, v.4, n.3, p. 9818-9829 may./jun. 2021 inserido (Almeida Junior, 2019;Coelho et al, 2020;Moreira et al, 2020). Dessa forma, é extremamente justificável a divulgação deste relato de caso sobre o quadro de GIST.…”

Section: Discussionunclassified

Tumor estromal gastrointestinal positivo para CD117 e CD34 em relato de caso e revisão / Gastrointestinal stromal tumor positive for CD117 and CD34 in case report and review

Gomes¹,

Santos²,

Feitosa³

et al. 2021

Braz. J. Hea. Rev.

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Paciente, sexo masculino, 57 anos, entrada no sistema de emergência com desconforto em região hipogástrica se assemelhando a uma "pontada". Nega comorbidades, internações anteriores e etilismo. Exame físico apresenta pressão arterial (120x80 mmHg), FC (83 bpm), TC (37ºC), FR (16 irpm) e ACV: BNF 2T S/S, AR: MV +, S/RA. Exames laboratoriais com perfil hematológico dentro do esperado, índices de coagulação normais, enzimas hepáticas e exame de urina dentro da normalidade, conferindo alterações apenas no sódio, caracterizando uma hipernatremia leve. Realizado exames de imagem como raio-x (sem alterações), colonoscopia (sem alterações), tomografia com presença de massas hipodensa com 13,0 x 12,6 x 7,5 cm (CC x LL x AP). Em região hipogástrica e a ressonância magnética de abdome apresentou massa em região mesogástrica medindo 7,4 cm x 12,2 cm x 10,5 cm com volume estimado de 474,0 cm³. Procedimento de laparoscopia realizado com retirada de massa tumoral e envio para histopatologia e imunohistoquímica. Presença de neoplasia mesenquimal metastático corados por hematoxilina eosina e revelado positivo para AML, CD117, CD34 e DOG1 na imunohistoquímica.

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In vivo methods for the evaluation of anti-inflammatory and antinoceptive potential

Cited by 12 publications

References 29 publications

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

PA‑Int5: An isatin‑thiosemicarbazone derivative that exhibits anti‑nociceptive and anti‑inflammatory effects in Swiss mice

Tumor estromal gastrointestinal positivo para CD117 e CD34 em relato de caso e revisão / Gastrointestinal stromal tumor positive for CD117 and CD34 in case report and review

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