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.

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.

Microwave-Assisted Synthesis and Anti-inflammatory Activity Evaluation of α-Aminophosphonates

2019 ◽  
Vol 4 (1) ◽  
pp. 14-19
Author(s):  
B. Sujatha ◽  
P. Kamala
Keyword(s):  
Present Report ◽  
Inflammatory Activity ◽  
Microwave Assisted Synthesis ◽  
Synthetic Approach ◽  
One Pot ◽  
Rat Paw Edema ◽  
Solvent Free Conditions ◽  
Three Component Reaction ◽  
Anti Inflammatory ◽  
Rat Paw

In the present report, an expeditious green synthetic approach was developed for the synthesis of α-aminophosphonates 5(a-j) in good yields through one-pot three component reaction (Kabachnik-Fields reaction) in solvent-free conditions under microwave irradiation. The newly synthesized compounds were characterized by IR, NMR (1H, 13C and 31P), mass and C, H, N analysis. The synthesized compounds were screened for their anti-inflammatory activity using rat paw edema method. Most of the compounds from the series showed significant (p < 0.05) anti-inflammatory activity.

scholarly journals Thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives of isonicotinic acid hydrazide: Synthesis and their biological evaluation

2011 ◽  
Vol 76 (8) ◽  
pp. 1057-1067 ◽  
Author(s):  
Sadaf Gilani ◽  
Suroor Khan ◽  
Ozair Alam ◽  
Vijender Singh ◽  
Alka Arora
Keyword(s):  
Lipid Peroxidation ◽  
Acid Hydrazide ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
New Compounds ◽  
Derivatives Of ◽  
Ulcerogenic Action

A series of thiazolidin-4-one (2a-h, 3a-h), azetidin-2-one (4a- h) and 1,3,4-oxadiazole (5a-h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1H-NMR and mass spectral data. All compounds were evaluated for their anti-inflammatory activity by the carrageenan-induced rat paw edema test method. Eleven of the new compounds, out of 32, showed very good anti-inflammatory activity in the carrageenan-induced rat paw edema test, with significant analgesic activity in the tail immersion method together with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde content (MDA), which is one of the by-products of lipid peroxidation. The study showed that the compounds inhibited the induction of gastric mucosal lesions and it can be suggested from the results that their protective effects may be related to inhibition of lipid peroxidation in the gastric mucosa.

scholarly journals Antinociceptive and anti-inflammatory effects of a Geissospermum vellosii stem bark fraction

2016 ◽  
Vol 88 (1) ◽  
pp. 237-248 ◽  
Author(s):  
JOSÉLIA A. LIMA ◽  
THIAGO W.R. COSTA ◽  
LEANDRO L. SILVA ◽  
ANA LUÍSA P. MIRANDA ◽  
ANGELO C. PINTO
Keyword(s):  
Formalin Test ◽  
Ethanolic Extract ◽  
Stem Bark ◽  
Second Phase ◽  
Murine Models ◽  
Hot Plate Test ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Abdominal Constriction

ABSTRACT Geissospermum vellosii (Pao pereira) is a Brazilian tree whose stem barks are rich in indole alkaloids that present intense anticholinesterase activity. The present study evaluated the effects of a stem bark fraction (PPAC fraction) and ethanolic extract (EE) of Pao pereira in classic murine models of inflammation and pain. The EE and PPAC fraction, both at a dose of 30 mg/kg, significantly reduced mice abdominal constriction induced by acetic acid by 34.8% and 47.5%, respectively. In the formalin test, EE (30 mg/kg) and PPAC fraction (30 and 60 mg/kg) inhibited only the second phase, by 82.8%, 84.9% and 100%, respectively. Compared with indomethacin, similar doses of EE or PPAC fraction were approximately twice as effective in causing antinociception. PPAC fraction was not effective in the hot plate test but reduced the inflammatory response at the second (50.6%) and third (57.8%) hours of rat paw edema induced by carrageenan. Antihyperalgesic activity was observed within 30 min with a peak at 2 h (60.1%). These results demonstrate that compounds in PPAC fraction have anti-inflammatory and antinociceptive activity by a mechanism apparently unrelated to the opioid system. Regardless of similar responses to indomethacin, the effects of PPAC fraction are mainly attributed to acetylcholine actions.

scholarly journals Antioxidant, analgesic and anti-inflammatory activities of Leucas cephalotes (Roxb.ex Roth) Spreng

2010 ◽  
Vol 46 (3) ◽  
pp. 525-529 ◽  
Author(s):  
Bhukya Baburao ◽  
Anreddy Rama Narsimha Reddy ◽  
Gangarapu Kiran ◽  
Yellu Narsimha Reddy ◽  
Gottumukkala Krishna Mohan
Keyword(s):  
Methanolic Extract ◽  
Maximum Activity ◽  
Dependent Manner ◽  
Hot Plate Test ◽  
Rat Paw Edema ◽  
Whole Plant ◽  
Ic50 Value ◽  
Dpph Method ◽  
Anti Inflammatory ◽  
Rat Paw

The whole plant of the methanolic extract from Leucas cephalotes was screened for invitro antioxidant (using the DPPH method), invivo analgesic (using hot plate test in mice) and anti-inflammatory (using rat paw edema test) activities. The methanolic extract of Leucas cephalotes (MELC) scavenged the DPPH radicals in a dose-dependent manner. The IC50 value to scavenge DPPH radicals was found to be 421.3µg/ml. A significant (p<0.0005) analgesic activity was observed at 60 min with 200 mg/kg, and 400 mg/kg exhibited maximum activity. The maximum anti-inflammatory response was produced at 3 hr and 2 hr with doses of 200 and 400 mg/kg, respectively. These results suggest that the methanolic extract from Leucas cephalotes exerts significant analgesic and anti-inflammatory effects, which were comparable with standard drugs.

ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF METHANOLIC EXTRACT FROM JATROPHA CURCAS (EUPHORBIACEAE) LEAVES ON EXPERIMENTAL ANIMALS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (08) ◽  
pp. 32-38
Author(s):  
P Chandra ◽  
◽  
N Sachan ◽  
R Yadav ◽  
K. Kishore ◽  
...  
Keyword(s):  
Jatropha Curcas ◽  
Pain Threshold ◽  
Methanolic Extract ◽  
Paw Edema ◽  
Traditional Use ◽  
Analgesic Effects ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Rat Paw

The present study evaluates the analgesic and anti-inflammatory activities of the methanolic extract from Jatropha curcas (Euphorbiaceae) leaves to provide experimental evidence for its traditional use. Investigations on the analgesic effects and anti-inflammatory activities of J. curcas were carried out by utilizing the different animal models. It has been shown that the methanolic extract from Jatropha curcas leaves significantly increased pain threshold and reduced writhing response as well as inhibited the increase in vascular permeability. Also, it significantly decreased the carrageenan-induced rat paw edema. The results show that the methanolic extract from Jatropha curcas leaves have both central and peripheral analgesic activities and as anti-inflammatory effects, supporting the traditional application of this herb in treating various diseases associated with inflammation and pain.

scholarly journals Novel 1,3,4-Oxadiazole Derivatives of Pyrrolo[3,4-d]Pyridazinone Exert Anti-Inflammatory Activity without Acute Gastrotoxicity in the Carrageenan-Induced Rat Paw Edema Test

2021 ◽  
Vol Volume 14 ◽  
pp. 5739-5756
Author(s):  
Marta Szandruk-Bender ◽  
Anna Merwid-Ląd ◽  
Benita Wiatrak ◽  
Maciej Danielewski ◽  
Stanisław Dzimira ◽  
...  
Keyword(s):  
Inflammatory Activity ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Derivatives Of

scholarly journals Bioactivity-Guided Investigation of the Anti-Inflammatory Activity of Hippophae rhamnoides Fruits

Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 26-33 ◽  
Author(s):  
Dóra Rédei ◽  
Norbert Kúsz ◽  
Nikoletta Jedlinszki ◽  
Gábor Blazsó ◽  
István Zupkó ◽  
...  
Keyword(s):  
Hippophae Rhamnoides ◽  
Inflammatory Activity ◽  
Hippophaë Rhamnoides ◽  
Rat Paw Edema ◽  
In Vivo Animal Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
First Time ◽  
Peel Extract

AbstractAccording to modern ethnobotanical records, the fruit of Hippophae rhamnoides is effective in the treatment of different allergic symptoms. In order to obtain pharmacological evidence for this observation, the fruit was investigated for anti-inflammatory activity using in vivo animal models. Aqueous and 70% MeOH extracts were tested in 48/80-induced rat paw edema assay after oral administration, and it was found that the 70% MeOH extract (500 mg/kg) reduced significantly edema volume (0.660 ± 0.082 mL vs. control 0.935 ± 0.041 mL). Extracts of different parts of the fruit (pulp, peel, seed) were investigated in the same assay, and the peel extract was shown to exhibit maximum edema-reducing effect (0.470 ± 0.124 mL vs. control 0.920 ± 0.111 mL). This extract was used to elucidate the mode of action. Different inflammation inducers (serotonin, histamine, dextran, bradykinin, and carrageenan) were applied in the rat paw model, but the extract inhibited only the compound 48/80 elicited inflammation. The active extract was then fractionated by solvent-solvent partitioning and chromatographic methods with the guidance of the 48/80-induced anti-inflammatory assay, and the main compounds responsible for the activity were identified as ursolic acid and oleanolic acid. Our data suggest that the activity is most probably based on a membrane stabilizing effect caused by the inhibition of degranulation of mast cells. Moreover, previously unknown 2,5-bis-aryl-3,4-dimethyltetrahydrofuran lignans, nectandrin B, fragransin A2, and saucernetindiol were isolated and identified from H. rhamnoides for the first time.

scholarly journals Retraction Note: Release-Active Dilutions of Diclofenac Enhance Anti-inflammatory Effect of Diclofenac in Carrageenan-Induced Rat Paw Edema Model

Inflammation ◽  
2020 ◽  
Author(s):  
Sachin S. Sakat ◽  
Kamaraj Mani ◽  
Yulia O. Demidchenko ◽  
Evgeniy A. Gorbunov ◽  
Sergey A. Tarasov ◽  
...  
Keyword(s):  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inflammatory Effect
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