Anti-Inflammatory, Antipyretic and Analgesic Potential of Zilla spinosa in Animal Model

2019 ◽  
Author(s):  
Riaz Ullah ◽  
Abdelaaty A Shahat ◽  
Ali S Alqahtani ◽  
Omer Mohammed Almarfad ◽  
Mohammad Sayer M Alharbi ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Tail Flick ◽  
Chloroform Fraction ◽  
Test Model ◽  
Hot Plate Test ◽  
Tail Flick Test ◽  
Antipyretic Activity ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Analgesic Activities

The anti-inflammatory, antipyretic and analgesic activities of two concentrations (250 and 500 mg/kg) of the chloroform and butanol fractions of Zilla spinosa were determined. The carrageenan-induced rat paw edema assay was exercised for assessing the anti-inflammatory activity in rats, yeast-induced hyperthermia was utilized to assess the antipyretic activity in mice and the analgesic activity was measured by three different methods (hot-plate test model in mice, tail flick test in mice and acetic acid-induced writhing in mice). The antioxidant activity was studied by using the DPPH assay. The chloroform fraction of the methanol extract of Z. spinosa (ZSC) demonstrated the maximum inhibition of inflammation (50% at 500 mg/kg; 44% at 250 mg/kg). The chloroform fraction showed significant antipyretic activities (p andlt; 0.001 at 500 mg/kg) after 60 and 120 min of administration. ZSC also exhibited significant analgesic activity (p andlt;0.001). The butanol fraction (ZSB) was inactive in all the biological screening assays.

scholarly journals Synthesis and analgesic activities of some new 5-chloro-2(3H)-benzoxazolone derivatives

2017 ◽  
Vol 1 (3) ◽  
pp. 235-240 ◽  
Author(s):  
Yusuf Mulazim ◽  
Cevdet Berber ◽  
Hakkı Erdogan ◽  
Melike Hacer Ozkan ◽  
Banu Kesanli
Keyword(s):  
Biological Activities ◽  
Inflammatory Activity ◽  
Microwave Assisted Synthesis ◽  
Tail Flick ◽  
Synthesis Methods ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Tail Flick Test ◽  
Anti Inflammatory ◽  
Analgesic Activities

Abstract Affordable and practical synthesis methods in drug development have always been very attractive. Herein, microwave assisted synthesis was utilized to prepare piperazine substituted 5-chloro-2(3H)-benzoxazolone derivatives in 5 minutes. Structural characterization of these 5-chloro-2(3H)-benzoxazolone derivatives was achieved by IR, NMR, ESI-MS and elemental analysis. Since these types of compounds have been shown to have anti-inflammatory and analgesic activities there biological activities were also examined. Indomethacin (INDO) and acetylsalicylic acid (ASA) were used as reference. Carrageenan-induced hind paw edema in mice test was used to study anti-inflammatory activity. Compound 1 (100 mg / kg dose) showed the longest anti-inflammatory activity among the title compounds synthesized. For the analgesic activities, both hot-plate and tail-flick tests were employed. Compound 3 was found to have the highest activity in the hot-plate test whereas in the tail-flick test, compounds 1 and 2 showed higher anti-nociceptive activity.

scholarly journals DESIGN AND SYNTHESIS OF NOVEL 4-(4-FLUORO-3-METHYLPHENYL)-6-(SUBSTITUTED ARYL)-1,6-DIHYDROPYRIMIDIN-2-OL DERIVATIVES AS POTENT ANTI-INFLAMMATORY AND ANALGESIC AGENTS

2019 ◽  
pp. 251-256
Author(s):  
MURALIDHARAN V ◽  
RAJA S ◽  
ASHA DEEPTI
Keyword(s):  
Pyrimidine Derivative ◽  
Cellular Level ◽  
Tail Flick ◽  
Design And Synthesis ◽  
Rat Paw Edema ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Analgesic Activities

Objective: Pyrimidine heterocycles possessing hydroxy group has a unique place in medicinal chemistry and also plays a key role in biological processes. In the biological functions at cellular level pyrimidine plays imperative roles which lead the researchers to design a variety of its derivatives. The aim of the present study was to synthesize the novel set of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydropyrimidin-2-ol derivatives. These compounds were screened for their analgesic and anti-inflammatory activities. Methods: A novel series of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were furnished in two steps starting from 4-fluoro-3-methyl acetophenone through chalcone formation. Human red blood cell membrane stabilization method and carrageenan-induced rat paw edema test were performed for screening in vitro and in vivo anti-inflammatory activity, respectively. Tail-flick technique was performed for screening analgesic activity. Results: All the synthesized 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were characterized by Fourier-transform infrared spectroscopy,1H nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. The result of biological screening revealed that many of the new derivatives were endowed with improved anti-inflammatory and analgesic activities. Conclusion: Nature of the substituent played a major role in anti-inflammatory and analgesic activities. The pyrimidine derivative with chlorophenyl substitution exhibited potent anti-inflammatory and analgesic activities. From the results, it was concluded that 6-(4-chlorophenyl)-4-(4-fluoro-3- methyl phenyl)-1,6-dihydropyrimidin-2-ol was the most active compound.

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 Synthesis, Anti-Inflammatory, and Analgesic Activities of Derivatives of 4-Hydroxy-2-benzoxazolone

2015 ◽  
Vol 2015 ◽  
pp. 1-5
Author(s):  
Guangjin Zheng ◽  
Tieyu Chen ◽  
Xing Peng ◽  
Shengjing Long
Keyword(s):  
Chinese Herb ◽  
Primary Amines ◽  
One Pot ◽  
Hot Plate Test ◽  
Rat Paw Edema ◽  
Electrophilic Reagents ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Rat Paw ◽  
Derivatives Of

Benzoxazolones are widely distributed in plants and are of increasing interest for a variety of pharmacological properties, such as detoxification, antibacterial, anti-inflammatory, and analgesic activities and tranquilizers (Michaelidou and Hadjipavlou-Litina, 2005; Doğruer et al., 1998). 4-Hydroxy-2-benzoxazolone (HBOA) is one of the major bioactive compounds in traditional Chinese herb drugAcanthus ilicifolius  (Peng and Long, 2006) which has obvious anti-inflammatory and analgesic activities (Huo et al., 2004; Mani Senthil Kumar et al., 2008; Babu et al., 2001). In this research, we used 2-nitroresorcinol as starting material to prepare HBOA with a novel “one-pot-way.” Derivatives of HBOA TC-2∼TC-4 were obtained via electrophilic reagents and reacted with corresponding primary amines to afford Schiff Base derivatives TC-5∼TC-10 for further study. Anti-inflammatory and analgesic activities of those derivatives were determined by using carrageenan-induced rat paw edema test. The analgesic activities of the derivatives were determined by the hot-plate test.

scholarly journals Assessment of pharmacological activity and bioavailability of the new derivative 1,3,4-thiadiazole

2018 ◽  
Vol 4 (2) ◽  
pp. 27-46
Author(s):  
Nikita S. Popov ◽  
Marina A. Demidova ◽  
Alexandr S. Malygin
Keyword(s):  
Pharmacological Activity ◽  
Analgesic Activity ◽  
Animal Experiments ◽  
Inflammatory Activity ◽  
Intragastric Administration ◽  
Hot Plate Test ◽  
Antipyretic Activity ◽  
Formalin Edema ◽  
Anti Inflammatory ◽  
Stimulation Of

Introduction: Acexazolamide is a new derivative of 1,3,4-thiadiazole and acexamic acid. Materials and methods: In animal experiments, acute toxicity, pharmacological activity and bioavailability of acexazolamide were evaluated. Anti-inflammatory activity was assessed on the model of formalin edema of paw and cotton pellet granuloma in rats. Assessment of analgesic activity was carried out in a hot plate test in mice, chemical pain stimulation of the peritoneum and inflammatory hyperalgesia in rats. The antipyretic activity of acexazolamide was evaluated in a model of yeast-induced hyperthermia in rats. The anti-burn activity of acexazolamide was evaluated in a thermal skin burn model in rats. Bioavailability of acexazolamide with intragastric administration was determined in rabbits. The content of acetaxazolamide in blood plasma was determined by HPLC-MS/MS method. Results and discussion: DL50 of acexazolamide after intragastric administration to mice was 860.99 (95% CIs, 462.2 to 1259.8) mg/kg. The anti-inflammatory activity of acexazolamide (21.5 mg/kg) with formalin-induced paw edema and fetal granuloma in rats was higher than that of ketoprofen (23.0 mg/kg). ED50 value for analgesic activity with acetic acid induced cortex was 24.99 (95% CIs: 15.31–34.68) mg/kg. With thermal stimulation of the paw in mice, the ED50 value was 25.56 (95% CIs: 15.13 to 35.98) mg/kg. ED50 value for antipyretic activity was 31.85 (95% CIs: 19.22–44.47) mg/kg. Acexazolamide (21.5 mg/kg) had a stimulating effect on the regeneration of damaged tissues in case of thermal skin burns. Bioavailability of acexazolamide (1 mg/kg) with intragastric administration was 37%. Conclusion: Acexazolamide has the properties of a non-steroidal anti-inflammatory agent.

scholarly journals Assessment of analgesic and anti-inflammatory potential of ethanolic extract of Gossypium arboreum leaves in experimental animals

2019 ◽  
Author(s):  
Sharad Patange ◽  
Vijay Navghare ◽  
Prashant Zagade ◽  
Akshay Kendre ◽  
Swarp Jadhav ◽  
...  
Keyword(s):  
Cotton Plant ◽  
Analgesic Activity ◽  
Ethanolic Extract ◽  
Tail Flick ◽  
Gossypium Arboreum ◽  
Paw Edema ◽  
Experimental Animals ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw

Background and objectives: Gossypium arboreum commonly known as cotton plant, this variety of cotton plant available throughout India. Cotton plant was used traditionally for the treatment of infection, diarrhea and other inflammatory conditions. The aim of present study is to evaluate analgesic and anti-inflammatory activity of Gossypium arboreum leaves extract on experimental animals. Materials and Methods: The ethanolic extract of Gossypium arboreum leaves (EEGA) was subjected to assess its antioxidant potential using DPPH radical scavenging assay; further anti-inflammatory and analgesic activity was assessed by using carrageenan-induced rat paw edema and tail flick test respectively in experimental animals. Results: It was observed that free radicals were scavenged by the EEGA in a concentration dependent manner. The Ethanolic extract showed maximum 72% scavenging activities at 200 g/ml concentration. The ethanol extract exhibited significant analgesic activity in the tail-flick model (?<0.01) by increasing the reaction time of the mice to 8.9 sec at 180min after treatment in comparison to control (3.4 sec). The EEGA (100, 200 and 400 mg/kg, p.o.) showed dose-dependent, inhibition of carrageenan-induced rat paw edema from 30 min onwards (P<0.01), Conclusions: Present study revealed that the ethanolic extract of Gossypium arboreum displayed prominent analgesic and anti-inflammatory activity in experimental animals owing to its antioxidant property.

scholarly journals Analgesic and Anti-Inflammatory Activities of Quercetin-3-methoxy-4′-glucosyl-7-glucoside Isolated from Indian Medicinal Plant Melothria heterophylla

Medicines ◽  
2019 ◽  
Vol 6 (2) ◽  
pp. 59 ◽  
Author(s):  
Arijit Mondal ◽  
Tapan Kumar Maity ◽  
Anupam Bishayee
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Tail Flick ◽  
Test Compound ◽  
Active Components ◽  
Hot Plate ◽  
Rat Paw Edema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: Melothria heterophylla (family: Cucurbitaceae), commonly known as kudari, is used in the Indian traditional medicine to treat various inflammation-associated diseases, such as asthma, arthritis and pain. However, the anti-inflammatory active components of this plant have not been identified yet. The aim of this study was to investigate the potential analgesic and anti-inflammatory activities of a compound, quercetin-3-methoxy-4′-glucosyl-7-glucoside, isolated from M. heterophylla. Methods: The anti-inflammatory activity was determined using carrageenan- and dextran-induced rat paw edema as well as cotton pellet-induced granuloma in rats, whereas the analgesic activity was analyzed using acetic acid-induced writhing, hot plate and tail flick response in mice. The test compound was orally administered at a dose of 5, 10 or 15 mg/kg. The cyclooxygenase-1 (COX-1)- and COX-2-inhibitory capacity of the test compound was studied by enzyme immunosorbent assay. Results: Quercetin-3-methoxy-4′-glucosyl-7-glucoglucoside at 15 mg/kg exhibited a maximum inhibition of carrageenan-induced inflammation (50.3%, p < 0.05), dextran (52.8%, p < 0.05), and cotton pellets (41.4%, p < 0.05) compared to control animals. At the same dose, it showed a 73.1% inhibition (p < 0.05) of the pain threshold in acetic acid-induced writhing model. It also exhibited a considerable analgesic activity by prolonging the reaction time of the animals based on hot plate as well as tail flick response. The test compound was found to inhibit COX-1 (IC50 2.76 µg/mL) and more efficiently, COX-2 (IC50 1.99 µg/mL). Conclusions: Quercetin-3-methoxy-4′-glucosyl-7-glucoside possessed substantial analgesic and anti-inflammatory activities possibly due to inhibition of prostaglandin production, supporting the ethnomedicinal application of M. heterophylla to treat various inflammatory disorders.

Effects of aloperine on acute and inflammatory pain models in mice

2015 ◽  
Vol 8 (1) ◽  
pp. 28-34 ◽  
Author(s):  
Yang Yang ◽  
Shao-Ju Jin ◽  
Hong-Ling Wang ◽  
Yu-Xiang Li ◽  
Juan Du ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Inflammatory Pain ◽  
Tail Flick ◽  
Paw Edema ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Tail Flick Test ◽  
Plate Test ◽  
Tnf Α ◽  
Anti Inflammatory

AbstractBackground and objectivesAloperine (ALO) is an alkaloid compound and presents in several medicinal plants. This study was undertaken to investigate the anti-nociceptive and anti-inflammatory activities of ALO on various chemical- and thermal-induced hypersensitivity models in mice.MethodsThe anti-nociceptive effect of ALO was evaluated using acetic acid-induced writhing test, hot plate test, tail flick test, formalin test, ear swelling test, locomotor activity test, rota-rod test and carrageenan-induced paw edema test in mice. Inflammatory cytokines including interleukin-10 (IL-10), tumor necrosis factor α (TNF-α), interleukin-1 beta (IL-1β) and prostaglandin E2 (PGE2) expression were examined in ALO- and vehicle-treated mice.ResultsThe results showed that ALO significantly attenuated acetic acid-induced writhing numbers in mice in a dose-dependent manner. ALO showed no effect on prolonging latency in the hot plate test and the tail-flick test. ALO showed analgesic activity in the inflammatory phase of formalin-induced pain. Its anti-inflammatory effect was also confirmed in the ear-swelling test. In the carrageenan-induced paw edema model, ALO significantly and dose-dependently reduced the carrageenan-induced paw edema, decreased the contents of TNF-α IL-1β and PGE2, but increased the IL-10 production. On the other hand, ALO showed no influence on the rota-rod performance time or on spontaneous locomotor activity.ConclusionIt is concluded that ALO has both anti-inflammatory and analgesic effects, especially in the field of inflammation pain.ImplicationsOur findings support the hypothesis that ALO ameliorates inflammatory pain induced by chemical and thermal stimuli and provides a scientific basis for the resource development and clinical use of aloperine.

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.

Semi-synthesis of Novel Buprenorphine Derivatives and their Anti-nociceptive Properties and Dependency Potential

2021 ◽  
Author(s):  
Zahra Hasanpour ◽  
Peyman Salehi ◽  
Lennart Bunch ◽  
Mona Khoramjouy ◽  
Morteza Bararjanian ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Analgesic Effect ◽  
Preference Test ◽  
Biological Properties ◽  
Place Preference ◽  
Tail Flick ◽  
Tail Flick Test ◽  
Active Compounds ◽  
Methyl Group ◽  
Analgesic Activities

Abstract: Novel 1,2,3-triazole-tethered N-norbuprenorphine derivatives with an OMe or OH group at the C3 position were synthesized alongside with evaluation of their analgesic properties. The analgesic activities of the resulting library were investigated via tail flick test in mice. Our results indicated that 10b and 10e were as effective as the starting compounds 8 and 9 with ED50 equal to 16.59 and 19.44 mg/kg, respectively. To investigate the effect of a methyl group at C3 on biological properties, the most active compounds were O-demethylated and their anti-nociceptive effects were assessed. The new O-demethylated derivatives (11b and 11e) showed better analgesic properties than the parent compounds with ED50 of 14.73 and 15.80 mg/kg, respectively. Naloxone prevented the analgesic effect of the synthesized compounds, indicating that the opioid receptors are highly involved in the anti-nociceptive effects of these. The potential dependency effects of the most potent derivatives were studied by condition place preference test in mice and compared to morphine and buprenorphine. Interestingly, 10b, 10e, 11b, and 11e did not show any dependency effect, similar to buprenorphine.

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