Synthesis of 8-alkoxy-1,3-dimethyl-2, 6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides as analgesic and anti-inflammatory agents

2015 ◽  
Vol 21 (5) ◽  
pp. 273-278 ◽  
Author(s):  
Grażyna Chłoń-Rzepa ◽  
Agnieszka W. Jankowska ◽  
Małgorzata Zygmunt ◽  
Krzysztof Pociecha ◽  
Elżbieta Wyska
Keyword(s):  
Analgesic Activity ◽  
Structural Element ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Peripheral Mechanism ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Necrosis Factor ◽  
Inhibit Tumor Necrosis Factor

AbstractA series of new 8-alkoxy-1,3-dimethyl-2,6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides 6–12 was synthesized and evaluated for the analgesic activity in two in vivo models: the writhing syndrome and the hot-plate tests. Among the investigated derivatives, compounds with N′-arylidenehydrazide moiety 9–12 show analgesic activity significantly higher than that of acetylsalicylic acid, which may indicate the importance of this structural element for analgesic properties. The lack of the activity in the hot-plate test may suggest that the analgesic activity of the newly synthesized compounds is mediated by a peripheral mechanism. The selected compounds 7 and 12 inhibit tumor necrosis factor α production in a rat model of lipopolysaccharide-induced endotoxemia, similarly to theophylline, which may confirm their anti-inflammatory properties.

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 Evaluation In Vivo and In Vitro of the Antioxidant, Antinociceptive, and Anti-Inflammatory Activities of Biflavonoids From Ouratea hexasperma and O. ferruginea

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1985680 ◽  
Author(s):  
Poliana de Araujo Oliveira ◽  
Queli Cristina Fidelis ◽  
Thayane Ferreira da Costa Fernandes ◽  
Milene Conceição de Souza ◽  
Dayane Magalhães Coutinho ◽  
...  
Keyword(s):  
Type I Collagen ◽  
In Vivo Model ◽  
Type I ◽  
Anti Inflammatory ◽  
Vitro Model ◽  
Factor Α ◽  
Necrosis Factor

Ouratea species are used for the treatment of inflammation-related diseases such as rheumatism and arthritic disorders. The Ouratea genus is a rich source of flavonoids and bioflavonoids and for this reason we evaluated the effects of the biflavonoid fractions from the leaves of O. hexasperma (OHME) and O. ferruginea (OFME) in the in vivo model of complete Freund’s adjuvant (CFA)-induced arthritis and in the in vitro model of oxidative stress and cellular viability. The CFA-induced arthritis model in rats was followed by paw volume, articular incapacitation and Randall-selitto models, as well as quantification of cytokines and serum C-terminal telopeptide of type I collagen levels. OHME and OFME demonstrated antinociceptive and anti-inflammatory activities, as well as improvement in articular incapacity and reduction in levels of interleukin 1β (IL-1β), IL-6, tumor necrosis factor α, and type 1 collagen, and increased cell viability. No adverse effects were observed. The results suggest that OHME and OFME can reduce inflammation and bone resorption besides their antioxidant action.

scholarly journals Blackberry phenolic and volatile extracts inhibit cytokine secretion in LPS-inflamed RAW264.7 cells

2021 ◽  
Vol 16 ◽  
Author(s):  
Pauline Morin ◽  
Luke Howard ◽  
John Tipton ◽  
Laura Lavefve ◽  
Cindi Brownmiller ◽  
...  
Keyword(s):  
Preventive Treatment ◽  
Inflammatory Activity ◽  
Total Phenolic ◽  
Total Volatile ◽  
Phenolic Contents ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Necrosis Factor

The anti-inflammatory activity of blackberries has been attributed to phenolic compounds, especially anthocyanins. The present study hypothesized that volatiles could contribute to anti-inflammatory activity as well. The anti-inflammatory properties of three blackberry genotypes varying in total volatile and phenolic contents were assessed by measuring concentrations of nitric oxide (NO), interleukin-6 (IL-6) and tumor necrosis factor -α  (TNF-α) within LPS-inflamed RAW264.7 murine macrophage cells after a preventive treatment of either a phenolic or a volatile extract. Extracts from blackberry genotypes A2528T, A2587T and Natchez had total phenolic contents of 4315, 3369 and 3680 µg/mL, respectively, and total volatile contents of 283, 852 and 444 ng/mL, respectively. Phenolic and volatile extracts of all genotypes significantly lowered the secretion of NO, IL-6 and TNF-α in ranges varying between 20-42%, 34-60% and 28-73% inhibition, respectively. Volatile extracts exhibited greater anti-inflammatory properties than phenolic extracts, despite being present at much lower concentrations in the berries. Further research is needed to assess bioavailability and anti-inflammatory effect of blackberry volatiles in vivo.

Synthesis and Analgesic Activity of Monoterpenoid Aldehyde-derived Hydro-2H-chromeneols

2019 ◽  
Vol 17 (1) ◽  
pp. 68-78 ◽  
Author(s):  
Irina Il'ina ◽  
Ekaterina Morozova ◽  
Dina Korсhagina ◽  
Konstantin Volсho ◽  
Tat'yana Tolstikova ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Topical Issue ◽  
Hot Plate ◽  
One Pot ◽  
Hot Plate Test ◽  
Writhing Test ◽  
Structural Types ◽  
In Vivo Tests ◽  
Low Toxicity

Background: Despite a variety of drugs used to stop acute pain, problems related to their insufficient efficacy and undesirable side effects have remained unresolved. Therefore, the search for analgesics of new structural types, which combine high activity with low toxicity, is a topical issue. It is known that a number of compounds with a hydrogenated 2H-chromene skeleton exhibit significant analgesic activity in in vivo tests. Methods: New hydro-2H-chromenols containing monoterpenoid moieties were obtained via one-pot synthesis by the interaction between para-menthane alcohols and commercially available monoterpene aldehydes: Citral, hydroxycitronellal, myrtenal, and perillaldehyde. The analgesic activity of these compounds wаs studied in the acetic acid-induced writhing test and hot plate test. Results: The target compounds were characterized using NMR and HR-MS. Most of them exhibited pronounced analgesic activity. Conclusion: Due to high analgesic activity, (2S,4aR,8R,8aR)-2-((E)-2,6-dimethylhepta-1,5-dien-1- yl)-4,7-dimethyl-3,4,4a,5,8,8a-hexahydro-2H-chromene-4,8-diol is considered as candidate compound to participate in further research.

scholarly journals Evaluation of Analgesic and Anti-Inflammatory Activities of Water Extract of Galla Chinensis In Vivo Models

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Kai Sun ◽  
Xu Song ◽  
RenYong Jia ◽  
Zhongqiong Yin ◽  
Yuanfeng Zou ◽  
...  
Keyword(s):  
Capillary Permeability ◽  
Water Extract ◽  
Control Group ◽  
Paw Edema ◽  
Hot Plate ◽  
Hot Plate Test ◽  
In Vivo Models ◽  
Ear Edema ◽  
Anti Inflammatory

Aim. Pain and inflammation are associated with many diseases in humans and animals. Galla Chinensis, a traditional Chinese medicine, has a variety of pharmacological properties. The purpose of this study was to evaluate analgesic and anti-inflammatory activities of Galla Chinensis through different animal models. Method. The analgesic activities were evaluated by hot-plate and writhing tests. The anti-inflammatory effects were assessed by ear edema, capillary permeability, and paw edema tests. The contents of cytokines (NO, iNOS, PGE2, and IL-10) in serum of rats in paw edema test were inspected by ELISA assays. Results. In the hot-plate test, Galla Chinensis could significantly extend pain threshold when compared to control group. The inhibitory rates of writhes ranged from 36.62% to 68.57% in Galla Chinensis-treated mice. Treatment with Galla Chinensis (1 and 0.5 g/kg) could significantly inhibit ear edema (47.45 and 36.91%, resp.; P < 0.01). Galla Chinensis (1 g/kg) had significant (P < 0.05) anti-inflammatory activity in capillary permeability test (29.04%). In carrageenan-induced edema test, the inhibitory rates were 43.71% and 44.07% (P < 0.01) at 1 h and 2 h after administration of Galla Chinensis (1 g/kg), respectively, and the levels of proinflammatory cytokines were significantly reduced. Conclusion. These results suggest that Galla Chinensis has analgesic and anti-inflammatory effects, which may be a candidate drug for the treatment of inflammation and pain.

scholarly journals The analgesic activity of new sulfur-containing di- and tetrahydropyridine derivatives in the hot plate test

2021 ◽  
pp. 45-55
Author(s):  
E.Yu. Bibik ◽  
◽  
L.I. Kurbanov ◽  
S.A. Grygoryan ◽  
D.S. Krivokolysko ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
High Efficiency ◽  
Pain Syndrome ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Reference Drug ◽  
Plate Test ◽  
Metamizole Sodium ◽  
Sulfur Containing

Nowadays the search of new high-efficiency and safe drugs for the pharmacotherapy of diseases accompanied by pain syndrome is an active area of modern pharmacological research. 170 new derivatives of di- and tetrahydropyridines synthesized on the basis of the Chemex Research Laboratory, Vladimir Dahl Lugansk State University were exposed to the virtual bioscreening using the Swiss Target Prediction software. The paper describes screening studies in vivo of 5 samples of sulfur-containing di- and tetrahydropyridines (laboratory codes d02-138, as-262, f02-079, cv-074, cv-143) in the standard hot plate test in comparison with the reference drug — metamizole sodium. The compounds in the dose of 5 mg/kg were given intragastrically 1 hour and a half before placing the rats on the hot plate, the reference drug in the dose of 7 mg/kg also was given intragastrically 1 hour and a half before placing the rats on the hot plate. The compounds with laboratory codes as-262 (allyl 6-({2-[(4-acetylphenyl)amino]-2-oxoethyl}thio)-5-cyano-4-(2-furyl)-2-methyl-1,4-dihydropyridine-3-carboxylate) and d02-138 (ethyl 4-[({[3-cyano-5-{[(2,4-dichlorophenyl)amino]carbonyl}-4-(2-furyl)-6-methyl-1,4-dihydropyridinе-2-yl]thio}acetyl)amino]benzoate) possess the most pronounced analgesic activity in the dose of 5 mg/kg, they demonstrated 2.03 and 1.9-fold efficiency in comparison to metamizole sodium respectively. The rest three specimens demonstrated metamizole sodium-like analgesic activity.

scholarly journals Synthesis, characterization and pharmacological activity of new 2- imino –thiazolidine-4-one derivatives

2019 ◽  
Vol 10 (3) ◽  
pp. 1763-1769 ◽  
Author(s):  
Raghdah M. Alwiswasy ◽  
Raheem Jameel M ◽  
Basim Jasim Hameed
Keyword(s):  
Acetic Acid ◽  
Pharmacological Activity ◽  
Analgesic Activity ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Plate Test ◽  
Edema Model ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Analgesic Activities

A new 2-iminothiazolidin-4-ones compound and its derivatives were synthesized and characterized by FT-IR, CHN, and 1HNMR techniques. The target compounds were assessed for their anti-inflammatory and analgesic activities, and the study was performed using Swiss albino mice (25-30 g) for investigation. A hind edema model caused by , while the analgesic activity was assessed using an acetic acid-induced writhing and a hot plate test evaluated the anti-inflammatory activity.

scholarly journals Anti-inflammatory, analgesic and acute toxicity effects of fermented soybean

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Hamidah Mohd Yusof ◽  
Norlaily Mohd Ali ◽  
Swee Keong Yeap ◽  
Wan Yong Ho ◽  
Boon Kee Beh ◽  
...  
Keyword(s):  
Body Weight ◽  
Acute Toxicity ◽  
Latency Period ◽  
Raw 264.7 ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Tnf Α ◽  
Anti Inflammatory

Abstract Background Tempeh is a widely known fermented soybean that contains elevated level of bioactive contents. Our previous study has shown that anaerobic fermented Nutrient Enriched Soybean Tempeh (NESTE) with increase amino acid and antioxidant levels possessed better hepatoprotective effect than raw soybean. Methods In this study, the anti-inflammatory effect of the NESTE aqueous extract and raw soybean aqueous extract (SBE) were evaluated by quantifying the inhibition of IL-1β, TNF-α and nitric oxide (NO) secretion in LPS treated RAW 264.7 cell in vitro. On the other hand, in vivo oral acute toxicity effect of the extract was tested on mice at the dose of 5000 mg/kg body weight. In vivo oral analgesic effect of both aqueous extracts at 200 and 1000 mg/kg body weight was evaluated by the hot plate test. Results In the in vitro anti-inflammatory study, 5 mg/mL NESTE was able to inhibit 25.50 ± 2.20%, 35.88 ± 3.20% and 28.50 ± 3.50% of NO, IL-1β and TNF-α production in LPS treated RAW 264.7 cells without inducing cytotoxic effect on the cells. However, this effect was lower than 4 μg/mL of curcumin, which inhibited NO, IL-1β and TNF-α production by 89.50 ± 5.00%, 78.80 ± 6.20% and 87.30 ± 4.00%, respectively. In addition, 1.5 to 2.5-fold increase of latency period up to 120 min for mice in the hot plate test was achieved by 1000 mg/kg NESTE. The analgesic effect of NESTE was better than 400 mg/kg of acetyl salicylic acid, which only increased ~ 1.7-fold of latency period up to 90 min. Moreover, NESTE did not show acute toxicity (no LD50) up to 5000 mg/kg body weight. Conclusion NESTE is a nutritious food ingredient with potential anti-inflammatory and analgesic effects.

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