scholarly journals Hydroethanolic Extract of Grape Peel from Vitis labrusca Winemaking Waste: Antinociceptive and Anti-Inflammatory Activities

2021 ◽  
Vol 60 (1) ◽  
Author(s):  
Cristiana F. G. Silva ◽  
Victor Fattori ◽  
Caroline R. Tonetti ◽  
Marcos A. S. Ribeiro ◽  
Ricardo L. N. Matos ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Biological Effects ◽  
Multiple Reaction Monitoring ◽  
Thermal Hyperalgesia ◽  
Neutrophil Recruitment ◽  
Grape Pomace ◽  
Paw Edema ◽  
Vitis Labrusca ◽  
Anti Inflammatory ◽  
Hydroethanolic Extract

Research background. Extracts from grape pomace, including the wine, showed many biological effects such as antioxidant and anti-inflammatory activities. Unfortunately winemakers discard the bagasse and the waste is less useful, however it contains bioactive compounds which result in antioxidant and anti-inflammatory properties. The work aimed to analyze the hydroethanolic extract of peels from agro-industrial waste from Vitis labrusca and to evaluate its antinociceptive and anti-inflammatory assays. This study is relevant for reusing a residue and adding value to the grape economic chain. Experimental approach. A representative sample of pomace was obtained and the peels were applied to produce the extract. The phenolic compounds were determined by multiple reaction monitoring mode of mass spectrometry methods and Folin-Ciocalteu, using gallic acid as standard. The biological analyzes were carried out using mice orally treated with crude extract at doses (30, 100, and 300 mg/kg). We evaluated mechanical hyperalgesia by the von Frey method, thermal heat hyperalgesia using a hot plate at 55 °C, paw edema using a pachymeter, and neutrophil recruitment by measurement of myeloperoxidase enzyme activity. The nephrotoxicity and hepatotoxicity were evaluated by biochemical analyses using blood samples that were collected after the Vitis labrusca administration. Results and conclusions. The peels correspond to 75 % of all wet winemaking residue and 59 % on a dry basis. We identified nine anthocyanins (3-O-glucoside: peonidin, delphinidin, petunidin, and malvidin; 3-p-coumaroyl-glucoside: cyanidin, peonidin, petunidin, and malvidin, and malvidin-3,5-diglucoside), five flavonoids (apigenin-7-glucoside, luteolin-7-glucoside, quercetin-3-galactoside, isorhamnetin-3-glucoside, and myricetin-3-rutinoside), and 26.62 mg GAE/g of phenolic compounds. In vivo assays, showed that Vitis labrusca extract at concentrations 100 and 300 mg/kg reduced carrageenan-induced mechanical and thermal hyperalgesia, 50 % of the paw edema, and neutrophil recruitment. In addition, there were no nephrotoxicity and hepatotoxicity. Our extract obtained from winemaking residue has analgesic and anti-inflammatory action, related at least in part to the presence of phenolic compounds, and it has no toxicity to renal and hepatic tissues. Novelty and scientific contribution. We demonstrated that this waste can be used for the production of antioxidant and anti-inflammatory products (pharmaceutical and cosmetics) without toxicity, contributing to the environmental economy.

scholarly journals New ibuprofen derivatives with thiazolidine-4-one scaffold with improved pharmaco-toxicological profile

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.

scholarly journals TRPV1 Blocker HCRG21 Suppresses TNF-α Production and Prevents the Development of Edema and Hypersensitivity in Carrageenan-Induced Acute Local Inflammation

Biomedicines ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 716
Author(s):  
Oksana Sintsova ◽  
Irina Gladkikh ◽  
Anna Klimovich ◽  
Yulia Palikova ◽  
Viktor Palikov ◽  
...  
Keyword(s):  
Transient Receptor Potential ◽  
Thermal Hyperalgesia ◽  
Control Group ◽  
Transient Receptor Potential Vanilloid ◽  
Paw Edema ◽  
Mice Model ◽  
Edema Formation ◽  
Sensitivity Experiment ◽  
Tnf Α ◽  
Anti Inflammatory

Currently the TRPV1 (transient receptor potential vanilloid type 1) channel is considered to be one of the main targets for pro-inflammatory mediators including TNF-α. Similarly, the inhibition of TRPV1 activity in the peripheral nervous system affects pro-inflammatory mediator production and enhances analgesia in total. In this study, the analgesic and anti-inflammatory effects of HCRG21, the first peptide blocker of TRPV1, were demonstrated in a mice model of carrageenan-induced paw edema. HCRG21 in doses of 0.1 and 1 mg/kg inhibited edema formation compared to the control, demonstrated complete edema disappearance in 24 h in a dose of 1 mg/kg, and effectively reduced the productionof TNF-α in both doses examined. ELISA analysis of blood taken 24 h after carrageenan administration showed a dramatic cytokine value decrease to 25 pg/mL by HCRG21 versus 100 pg/mL in the negative control group, which was less than the TNF-α level in the intact group (40 pg/mL). The HCRG21 demonstrated potent analgesic effects on the models of mechanical and thermal hyperalgesia in carrageenan-induced paw edema. The HCRG21 relief effect was comparable to that of indomethacin taken orally in a dose of 5 mg/kg, but was superior to this nonsteroidal anti-inflammatory drug (NSAID) in duration (which lasted 24 h) in the mechanical sensitivity experiment. The results confirm the existence of a close relationship between TRPV1 activity and TNF-α production once again, and prove the superior pharmacological potential of TRPV1 blockers and the HCRG21 peptide in particular.

ANTIULCER AND ANTI-INFLAMMATORY ACTIVITIES OF HYDROALCOHOLIC EXTRACTS OF STEM BARK AND LEAF OF ANOGEISSUS PENDULA EDGEW

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 41-46
Author(s):  
Deeksha Singh ◽  
◽  
Amit Nayak ◽  
Rakesh Yadav ◽  
Uttam Singh Baghel ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Stem Bark ◽  
Inflammatory Activity ◽  
Antiulcer Activity ◽  
Paw Edema ◽  
Ulcer Index ◽  
Pylorus Ligation ◽  
Anti Inflammatory ◽  
Anogeissus Pendula

Anogeissus pendula Edgew has been reported to be used in gastric disorder even though no attempt has been made to evaluate the same. The present study was designed to evaluate the hydroalcoholic extracts of stem bark and leaves for in vivo acute antiulcer and anti-inflammatory activities. Antiulcer activity was studied by pylorus ligation induced ulcers while anti-inflammatory activities was studied by carrageenan induced paw edema. The extract of stem bark at 200 and 400 mg/kg b. w., significantly (P<0.05) reduced ulcer index whereas extracts of both stem bark and leaves significantly (P<0.001) reduced paw diameter at the fifth hour. The hydroalcholic extract of stem bark of A. pendula possesses more significant antiulcer and anti-inflammatory activity than the hydroalcholic extract of leaves may be due to the presence of higher amount of phenolic compounds.

scholarly journals Anti-platelet and anti-inflammatory properties of an ethanol-water red grape pomace extract

2020 ◽  
Vol 79 (OCE2) ◽  
Author(s):  
Maria Choleva ◽  
Maria Tsota ◽  
Vassiliki Boulougouri ◽  
Anthi Panara ◽  
Nikolaos S. Thomaidis ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Phenolic Compounds ◽  
Healthy Volunteers ◽  
Grape Pomace ◽  
Light Transmittance ◽  
Cell Protein ◽  
Total Phenolic ◽  
Suitable Alternative ◽  
Anti Inflammatory ◽  
Red Grape

AbstractPrevious reports support that wine contains a mixture of micro-constituents in a proper quality and quantity that possess cardio-protective effect partly through Platelet-Activating Factor (PAF) inhibition. Grape pomace (GP) is a source of wine-like micro-constituents that may be a suitable alternative in food fortification. Limited data exist concerning their effects on thrombosis and inflammation. Therefore, the purpose of this study was to examine a grape pomace extract regarding its anti-platelet and anti-inflammatory properties. GP from four red grape varieties were extracted with 80% ethanol (GP:solvent 1:5w/v). The extract's total phenolic compounds were evaluated and the phenolic profile was performed by Ultrahigh-Performance-Liquid-Chromatography coupled to Mass-Spectrometry and the determination of fatty acids profile was performed by Gas-Chromatography. The extract's anti-platelet properties were tested in healthy volunteers’ platelet rich plasma by the light transmittance method, against three agonists: PAF, ADP and TRAP. The results expressed as IC50 values (μg of extract that cause 50% inhibition of aggregation) and EC50 values (agonist concentration that causes 50% of the maximum aggregation) in the extract's presence and absence. Concerning the extract's anti-inflammatory properties, peripheral blood mononuclear cells from healthy volunteers were pre-incubated with different extract concentrations, which were tested for their effect on cell viability, for 1 h and then stimulated with LPS for 4 h. Secretion of IL-1β and TNF-a was measured and normalized with the total cell protein. Phenolic compounds were calculated at 8.79 ± 1.17 mg gallic acid per g of GP. The most abundant ones were catechin, epicatechin and quercetin at 202.9 ± 6.9, 84.8 ± 1.5 and 83.7 ± 3.5μg per g of GP respectively. Out of the 18 fatty acids detected, the most abundant ones were palmitic, oleic, linoleic, and linolenic acid at 28.7 ± 0.1, 11.4 ± 0.01, 32.5 ± 0.07, 12.7 ± 0.005 g per 100 g of fat. The extract's IC50 was calculated at 162.1 ± 66.9, 181.2 ± 82.3 and 156.3 ± 97.5μg against PAF, ADP and TRAP, respectively. The EC50 values in the presence of 150μg extract were increased (lower platelet aggregation sensitivity) approximately at 100%, 45% and 13% against PAF, ADP and TRAP respectively, compared to EC50 values in the absence of extract. The presence of 500 and 1000μg/mL of extract reduced LPS-induced TNF-a secretion at approximately 38.2% (p = 0.04) and 6.0% (p < 0.000), respectively. Potent anti-platelet and anti-inflammatory properties are combined in a grape pomace extract. The use of its bioactive micro-constituents is likely to lead to the production of functional foods with cardioprotective properties.

scholarly journals Antioxidant and anti-inflammatory activities of winery wastes seeds of Vitis labrusca

2011 ◽  
Vol 41 (7) ◽  
pp. 1233-1238 ◽  
Author(s):  
Gustavo Scola ◽  
Virginia Demarchi Kappel ◽  
José Claudio Fonseca Moreira ◽  
Felipe Dal-Pizzol ◽  
Mirian Salvador
Keyword(s):  
Phenolic Compounds ◽  
Phenolic Content ◽  
Biological Activities ◽  
Total Phenolic ◽  
Vitis Labrusca ◽  
Grape Seeds ◽  
Wine Production ◽  
Beneficial Effects ◽  
Environmental Balance ◽  
Anti Inflammatory

There are many studies about the biological activities of Vitis vinifera grape seeds, which are rich in phenolic compounds, known by their several health beneficial effects. However, until now there is no data about biological activities of the seeds of V. labrusca, specie found in South and North America. Every year, the global wine production (around 260 million hL) generates about 19.5 million ton of wastes, which are usually discarded in the environment. The aim of this research was to evaluate the antioxidant and anti-inflammatory activities of aqueous extracts of seeds from wine wastes of Vitis labrusca (cv. 'Bordo' and 'Isabella'). Both extracts showed significant antioxidant and anti-inflammatory activities, which are positively correlated with total phenolic content, suggesting that these compounds might be the major contributors to the biological activity of these extracts. These results indicate that water extraction from winery wastes is an option to obtain phenolic compounds with antioxidant and anti-inflammatory activities helping to maintain environmental balance.

scholarly journals Bioprocessed Wheat Ingredients: Characterization, Bioaccessibility of Phenolic Compounds, and Bioactivity During in vitro Digestion

2021 ◽  
Vol 12 ◽  
Author(s):  
Irene Tomé-Sánchez ◽  
Ana Belén Martín-Diana ◽  
Elena Peñas ◽  
Juana Frias ◽  
Daniel Rico ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Dietary Fiber ◽  
Raw Materials ◽  
Biological Effects ◽  
In Vitro Digestion ◽  
Hydroxycinnamic Acids ◽  
Total Phenolic ◽  
Insoluble Dietary Fiber ◽  
Anti Inflammatory

To enlarge the applications of whole wheat grain (WWG) and wheat bran (WB) as functional ingredients in foodstuffs that can promote human health, researchers have explored bioprocessing approaches to improve the bioaccessibility of phenolic compounds from these food matrices and, subsequently, their biological effects. The objective of this study was to compare the composition in nutrients, anti-nutrients, and bioactive compounds of WWG and WB, and their respective bioprocessed products: sprouted wheat (GERM) and WB hydrolysate (stabilized by spray-drying [SPD] and microencapsulated [MEC]). In addition, to evaluate the functional properties of these ingredients, the bioaccessibility of phenolic compounds and their potential antioxidant and anti-inflammatory activities were monitored in different digestion steps. GERM had increased amounts of insoluble dietary fiber, higher diversity of oligosaccharides, and higher concentration of monosaccharides, free phosphorous, and phenolic compounds than WWG. SPD had improved content of soluble dietary fiber, oligosaccharides, monosaccharides, free phosphorous, and phenolic compounds (vs. WB), whereas MEC was mainly composed of protein and had nearly 2-fold lower content of SPD components. All the ingredients showed lower amounts of phytic acid as compared with raw materials. In all samples, hydroxycinnamic acids were the most representative polyphenols followed by minor amounts of hydroxybenzoic acids and flavonoids. Gastrointestinal digestion of GERM, SPD, and MEC revealed high stability of total phenolic compounds in both gastric and intestinal phases. Hydroxycinnamic acids were the most bioaccessible compounds during digestion among the three bioprocessed wheat ingredients studied, although their bioaccessibility varied across ingredients. In this sense, the bioaccessibility of ferulic acid (FA) derivatives increased in GERM with progression of the digestion, while it was reduced in SPD and MEC up to the end of the intestinal phase. Microencapsulation of SPD with pea protein led to generally to lower bioaccessible amounts of phenolic acids. Comparison analysis of biological effects highlighted SPD for its most potent antioxidant effects in the gastrointestinal tract (3 out 4 antioxidant parameters with highest values), while no clear differences were observed with regard to in vitro anti-inflammatory activity. Overall, these results support the potential application of GERM, SPD, and MEC as functional and nutraceutical ingredients.

scholarly journals INVESTIGATION OF ANTI-INFLAMMATORY AND ANTINOCICEPTIVE EFFECTS OF AQUEOUS EXTRACTS OF ARTEMISIA AFRA IN WISTAR RATS

2018 ◽  
Vol 11 (12) ◽  
pp. 190 ◽  
Author(s):  
Mavuto Gondwe ◽  
Anda Mpalala ◽  
Lusanda Zongo ◽  
David Kamadyaapa ◽  
Eugene Ndebia ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Biological Effects ◽  
Control Group ◽  
Paw Edema ◽  
Hot Plate ◽  
Traditional Practice ◽  
Hot Plate Test ◽  
Writhing Test ◽  
Antinociceptive Effects ◽  
Anti Inflammatory

Objective: The objective of the study was to evaluate the anti-inflammatory and antinociceptive effects of Artemisia afra.Methods: Animals were randomly divided into five groups of six animals each and administered with normal saline (2 ml/kg), indomethacin (10 mg/ kg), and A. afra at doses of 100, 200, and 400 mg/kg, respectively. For the anti-inflammatory activity, carrageenan-induced paw edema was used while the hot plate and acetic acid induced-writhing tests were used to assess the antinociceptive activity.Results: Pretreatment with A. afra at a dose of 100 mg/kg did not show any significant biological effects (p>0.05) for any of the three tests, when compared against saline-treated control group. At a dose of 200 mg/kg, A. afra demonstrated significant effects (p<0.01), during the 5th h reducing carrageenan-induced paw edema by 12%. The highest dose (400 mg/kg) of A. afra demonstrated more potent effects by decreasing the carrageenan-induced paw swelling (p<0.001–0.05) during the 3rd, 4th, and 5th h, by up to 38% when compared against saline-treated control group. Both the 200 and 400 mg/kg, A. afra doses achieved a significant increase (p<0.05) in reaction time in the hot plate test. In the acetic acid-induced writhing test, pretreatment with A. afra (400 mg/kg) significantly reduced pain by 39% (p<0.01) by comparison with the saline control.Conclusion: Experimental data demonstrated that aqueous extract of A. afra possesses anti-inflammatory and antinociceptive properties in experimental acute inflammation and pain. These findings support the usage of A. afra in managing inflammation and pain in traditional practice.

scholarly journals Anti-Inflammatulatory Activity of Hydro-Ethanolic Bark Extracts of Piliostigma reticulatum Hochst (Caesalpiniaceae) and Analysis by HPLC-DAD and HPLC-MS of its Methanol Fraction

2020 ◽  
Vol 10 (3) ◽  
pp. 97-106
Author(s):  
Serigne Ibra Mbacke Dieng ◽  
Céline Mathieu ◽  
Madièye Séne ◽  
Kady Badji-Diatta ◽  
Abdou Sarr ◽  
...  
Keyword(s):  
Wistar Rats ◽  
Condensed Tannin ◽  
Chemical Study ◽  
Inflammatory Activity ◽  
Bark Extract ◽  
Paw Edema ◽  
Methanol Fraction ◽  
Anti Inflammatory ◽  
Hydroethanolic Extract ◽  
Piliostigma Reticulatum

Use of plants as remedies dates back to the time of the oldest civilizations. Among these active ingredients, polyphenols play an important role. Piliostigma reticulatum, a plant whose barks are rich in condensed tannin is often used as an anti-inflammatory. The purpose of this work was to correlate the anti-inflammatory activity of extracts with their chemical composition through chromatography fractionation analyses (HPLC-DAD and HPLC-MS). The barks were extracted by moderate hydroethanol decoction followed by silica gel splitting with successively ethyl acetate, methanol and water. Anti-inflammatory activity was evaluated by the method of carrageenan induced hind paw edema in Wistar rats.  The chemical study was carried out by HPLC-DAD and HPLC-MS after isolation of the compounds by fractionation on Sephadex LH-20 gel. The bark hydroethanolic extract had shown ability to inhibit significantly the inflammation induced by carraghenan. Among the hydroethanolic bark extract fractions that methanol fraction had the best activity at 10 mg/kg with inhibition percentages similar to those of acetylsalicylic acid with 48.51% ± 2.26; 54.71% ± 5.13; 64.19% ± 6.70 vs. 54.69% ± 7.23; 57.83% ± 9; 65.13% ± 8.44 respectively. The HPLC-DAD analysis showed that the SF5 sub-fraction presented the best chromatogram with several peaks, three of which were high intensity. The latter would correspond to monomer, dimer and trimer of catechin according to the weights [M-H] + m / z: 291.07; 579.18; 867.27 obtained by HPLC-MS. The compounds responsible for anti-inflammatory activity would be condensed tannins. The latter would consist mainly of catechin oligomers.  Keys words: Piliostigma reticulatum, bark, anti-inflammatory activity, HPLC-DAD, HPLC-MS

scholarly journals Tempol, a Superoxide Dismutase Mimetic Agent, Inhibits Superoxide Anion-Induced Inflammatory Pain in Mice

2017 ◽  
Vol 2017 ◽  
pp. 1-15 ◽  
Author(s):  
Catia C. F. Bernardy ◽  
Ana C. Zarpelon ◽  
Felipe A. Pinho-Ribeiro ◽  
Cássia Calixto-Campos ◽  
Thacyana T. Carvalho ◽  
...  
Keyword(s):  
Spinal Cord ◽  
Superoxide Dismutase ◽  
Mrna Expression ◽  
Inflammatory Pain ◽  
Superoxide Anion ◽  
Thermal Hyperalgesia ◽  
Mechanical Hyperalgesia ◽  
Antioxidant Defenses ◽  
Paw Edema ◽  
Anti Inflammatory

The present study evaluated the anti-inflammatory and analgesic effects of the superoxide dismutase mimetic agent tempol in superoxide anion-induced pain and inflammation. Mice were treated intraperitoneally with tempol (10–100 mg/kg) 40 min before the intraplantar injection of a superoxide anion donor, potassium superoxide (KO2, 30 μg). Mechanical hyperalgesia and thermal hyperalgesia, paw edema, and mRNA expression of peripheral and spinal cord mediators involved in inflammatory pain, TNFα, IL-1β, IL-10, COX-2, preproET-1, gp91phox, Nrf2, GFAP, and Iba-1, were evaluated. Peripheral and spinal cord reductions of antioxidant defenses and superoxide anion were also assessed. Tempol reduced KO2-induced mechanical hyperalgesia and thermal hyperalgesia and paw edema. The increased mRNA expression of the evaluated mediators and oxidative stress in the paw skin and spinal cord and increased mRNA expression of glial markers in the spinal cord induced by KO2 were successfully inhibited by tempol. KO2-induced reduction in Nrf2 mRNA expression in paw skin and spinal cord was also reverted by tempol. Corroborating the effect of tempol in the KO2 model, tempol also inhibited carrageenan and CFA inflammatory hyperalgesia. The present study demonstrates that tempol inhibits superoxide anion-induced molecular and behavioral alterations, indicating that tempol deserves further preclinical studies as a promising analgesic and anti-inflammatory molecule for the treatment of inflammatory pain.

scholarly journals New ibuprofen derivatives with thiazolidin-4-one scaffold with improved pharmaco-toxicological profile

2020 ◽  
Author(s):  
Ioana-Mirela Vasincu ◽  
Maria Apotrosoaei ◽  
Sandra Madalina 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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