Investigation of anti-inflammatory potential of 5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione compound

Almeida, Dionys de Souza; Silva, Daiany P.B.; Moreira, Lorrane Kelle da Silva; Menegatti, Ricardo; Lião, Luciano M.; Sanz, Germán; Vaz, Boniek G.; Ghedini, Paulo César; Costa, Élson Alves; Florentino, Iziara Ferreira

doi:10.1016/j.ejphar.2020.173388

Cited by 4 publications

(2 citation statements)

References 45 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As shown in Figures 2A,B , CR attenuated CFA-induced mechanical allodynia and thermal hyperalgesia, whereas only CR had no influence on mechanical allodynia and thermal hyperalgesia in control mice. Paw edema was measured to evaluate the anti-inflammatory activity of CR ( Almeida et al, 2020 ). As shown in Figure 2C , CFA induced significant left paw edema.…”

Section: Resultsmentioning

confidence: 99%

Caloric Restriction Alleviates CFA-Induced Inflammatory Pain via Elevating β-Hydroxybutyric Acid Expression and Restoring Autophagic Flux in the Spinal Cord

et al. 2022

View full text Add to dashboard Cite

Inflammatory pain is the most common type of pain encountered in clinical practice; however, the currently available treatments are limited by insufficient efficacy and side effects. Therefore, new methods to relieve inflammatory pain targeting new mechanisms are urgently needed. Preclinical investigations have shown that CR (calorie restriction) exerts analgesic effects in neuropathic and cancer pain; however, the effect of CR on chronic inflammatory pain remains unknown. During calorie restriction, autophagy, a lysosome-dependent degradation process, can be activated to support cell survival. In the present study, we investigated the analgesic effects of CR on complete Freund’s adjuvant (CFA)-induced inflammatory pain. The accumulation of LC3-II and p62 showed impaired autophagic flux in the ipsilateral spinal cord of mice with CFA-induced inflammatory pain. CR alleviated mechanical allodynia and thermal hyperalgesia and reduced paw edema and pro-inflammatory factors following CFA administration. CR exerted an analgesic effect by restoring autophagic flux in the spinal cord. Regarding the mechanisms underlying the analgesic effects of CR, β-hydroxybutyric acid (BHB) was studied. CR increased BHB levels in the ipsilateral spinal cord. Furthermore, exogenous BHB administration exerted an analgesic effect by restoring autophagic flux in the spinal cords of CFA-induced inflammatory pain mice. Taken together, these results illustrated that CR relieved inflammatory pain by restoring autophagic flux in the spinal cord, while BHB controlled the benefits of CR, suggesting that CR or BHB might be a promising treatment for inflammatory pain.

show abstract

Section: Resultsmentioning

confidence: 99%

Caloric Restriction Alleviates CFA-Induced Inflammatory Pain via Elevating β-Hydroxybutyric Acid Expression and Restoring Autophagic Flux in the Spinal Cord

et al. 2022

View full text Add to dashboard Cite

show abstract

“…The right hind-paw was used as a negative control. The plethysmograph method was used on both hind paws of each group of rats to measure the anti-inflammatory activity and compare it to the control and treatment groups [ 43 , 44 ]. This was performed to maintain a constant paw volume.…”

Section: Methodsmentioning

confidence: 99%

Central Composite Design (CCD) for the Optimisation of Ethosomal Gel Formulation of Punica granatum Extract: In Vitro and In Vivo Evaluations

Alam

Shakeel

Foudah

et al. 2022

Gels

View full text Add to dashboard Cite

This research manuscript’s objective was to develop the Punica granatum extract ethosome gel. The use of nanotechnology can improve transdermal drug delivery permeation of its major bioactive compound β-sitosterol. The optimised and developed formulations were further studied in vitro and in vivo. The assessment of the anti-inflammatory activity of the gel was performed in Albino rats. Methanolic extract was prepared and developed into an ethosome suspension and an ethosome gel. To optimise the formulation’s response in terms of particle size (nm) and entrapment efficiency (%), the central composite design (CCD) was used in 22 levels. The effects of factors such as lecithin (%) and ethanol (mL) in nine formulations were observed. Characterisation of ethosome gel was performed and the results showed the particle size (516.4 nm) and mean zeta potential (−45.4 mV). Evaluations of the gel formulation were performed. The results were good in terms of pH (7.1), viscosity (32,158 cps), spreadability (31.55 g cm/s), and no grittiness. In an in vitro study, the percentages of β-sitosterol release of ethosome gel (91.83%), suspension (82.74%), and extracts (68.15%) at 279 nm were recorded. The effects of the formulated gel on formalin-induced oedema in Albino rats showed good results in terms of anti-inflammatory activity. The comparative anti-inflammatory activity of Punica granatum extract and gel showed that the gel action was good for their topical application.

show abstract

Pharmacological evaluation of antinociceptive and anti-inflammatory activities of LQFM202: a new piperazine derivative

et al. 2022

View full text Add to dashboard Cite

Investigation of anti-inflammatory potential of 5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione compound

Cited by 4 publications

References 45 publications

Caloric Restriction Alleviates CFA-Induced Inflammatory Pain via Elevating β-Hydroxybutyric Acid Expression and Restoring Autophagic Flux in the Spinal Cord

Caloric Restriction Alleviates CFA-Induced Inflammatory Pain via Elevating β-Hydroxybutyric Acid Expression and Restoring Autophagic Flux in the Spinal Cord

Central Composite Design (CCD) for the Optimisation of Ethosomal Gel Formulation of Punica granatum Extract: In Vitro and In Vivo Evaluations

Pharmacological evaluation of antinociceptive and anti-inflammatory activities of LQFM202: a new piperazine derivative

Contact Info

Product

Resources

About