scholarly journals The Study of the Effect of Histidine Derivatives as a Novel Antinociceptive and Anti-Inflammatory Activity

2011 ◽  
Vol 8 (4) ◽  
pp. 1832-1842 ◽  
Author(s):  
Usama H. Ramadhan ◽  
Niran J. Al-Salihi

This study explains the biochemical activity of histidine derivatives The compounds were identified by CHN analysis, FT-IR and H1NMR. The results certified that the chemical structures of the prepared compounds. The anti-inflammatory and antinociceptive activity was studied by two different tests; the hot plate test and writhing test for analgesic activity and two tests for anti-inflammatory activity they are formalin induced inflammation test and carrageen an induced inflammation test. The histidine derivatives were found to have potent activity as anti-inflammatory and antinociceptive. The active compounds were tested to acute toxicity. It was found that they are safety to the dose 5 g/kg orally in mice without any mortality.

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Anansa Bezerra de Aquino ◽  
Luiz Henrique Agra Cavalcante-Silva ◽  
Carolina Barbosa Brito da Matta ◽  
Willians Antônio do Nascimento Epifânio ◽  
Pedro Gregório Vieira Aquino ◽  
...  

We investigated the antinociceptive and anti-inflammatory activities of the crude ethanolic extract (CEE), its fractions, and the flavonoid isorhamnetin fromAspidosperma tomentosumusing models of nociception and inflammation in mice. In the writhing test, the CEE and its fractions (except for soluble phase, CHCl3100% and EtAcO 100%) at 100 mg/kg p.o. induced antinociceptive activity. Isorhamnetin (100 μmol/kg, p.o.) was also active. In the hot plate test, only the treatment with the fractions Hex : CHCl350%, CHCl3100%, and CHCl3 : MeOH 5% (100 mg/kg, p.o.) increased the latency time, reversed by the opioid antagonist naloxone. Fractions that were active in the hot plate test did not show catalepsy condition. It was observed that CEE, all fractions, and isorhamnetin reduced the formalin effects in the neurogenic phase. In the inflammatory phase, only CEE, isorhamnetin, and CHCl3100% and CHCl3 : MeOH 5% fractions were active. CEE and all fractions, except for CHCl3 : MeOH 10% fraction, isorhamnetin, and soluble fraction were able to produce an antioedematogenic activity in the ear capsaicin-induced edema test. In the thioglycolate-induced peritonitis, only EtAcO 100% fraction was not active. The results demonstrate thatA. tomentosumhas antinociceptive and anti-inflammatory activities in animal models.


2019 ◽  
Vol 10 (3) ◽  
pp. 1763-1769 ◽  
Author(s):  
Raghdah M. Alwiswasy ◽  
Raheem Jameel M ◽  
Basim Jasim Hameed

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.


2019 ◽  
Vol 26 (1) ◽  
pp. 77-87
Author(s):  
Evgeniya A. Beskhmelnitsyna ◽  
Mikhail V. Pokrovskii ◽  
Aleksandr A. Dolzhikov ◽  
Tat’yana V. Avtina ◽  
Nina I. Zhernakova ◽  
...  

The aim is to study the analgesic and anti-inflammatory activity of an innovative molecule under the ZC02-0012 laboratory code belonging to the group of selective blockers of the TRPA1 ion channel.Materials and methods. The study of the ZC02-0012 analgesic activity was carried out by the hot plate and acetic acid writhing tests. The hot plate test was performed on white laboratory mice. ZC02-0012 substance was administered in doses of 1, 3 and 9 mg/kg. Ketorol at a dose of 3.48 mg/kg was chosen as the reference drug. To study the analgesic effects in the hot plate test, intact white laboratory mice were placed on a preheated at 55°C plate to determine the base level of pain sensitivity. Then the test substances were administered to the animals divided into groups, and the hot plate test was repeated after 30, 60, 90 and 120 minutes. To study the analgesic effects in the test of acetic acid writhing, white laboratory rats were injected with the ZC02-0012 substance at doses of 0.46, 1.38, and 4.15 mg/kg. Ketorol at a dose of 1.6 mg/kg was chosen as the reference drug. 30 minutes after intramuscular injection and 60 minutes after intragastric administration, the intraperitoneal administration of a 0.75% solution of acetic acid was carried out at the rate of 1 ml per 100 g of animal weight. Counting the number of writhings started 15 minutes after the injection of acetic acid and continued for 30 minutes. The anti-inflammatory effects of the ZC02-0012 substance were studied using a model of acute exudative inflammation in response to the subplantar introduction of 0.02 ml of 2% formaldehyde aqueous solution into the right hind paw of the mouse. 4 hours after the phlogistic introduction, the mass of the edematous paw was evaluated. ZC02-0012 substance at doses of 1, 3 and 9 mg/kg and the Diclofenac reference drug at a dose of 13.91 mg/kg were administered intragastrically or intramuscularly 45 minutes before the introduction of phlogistic. The presence and severity of anti-inflammatory activity was judged by the inhibitory effect, expressed in percentage.Results. The analgesic activity of ZC02-0012 is found to exceed that for Ketorol in both the intramuscular and intragastric ways of administration according to the results of hot plate tests in doses of 3 and 9 mg/kg and acetic acid writhing in doses of 1.38 and 4.15 mg/kg, while the anti-inflammatory activity of ZC02-0012 at doses of 3 and 9 mg/kg is shown to be comparable to that of Diclofenac. Conclusion. The innovative molecule under the ZC02-0012 laboratory code is established to exhibit a pronounced analgesic and anti-inflammatory activity, thus being prospective for further research.Conflict of interest: the authors declare no conflict of interest.


2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Akinyinka O. Alabi ◽  
Abayomi M. Ajayi ◽  
Osarume Omorogbe ◽  
Solomon Umukoro

Abstract Background To investigate the antinociceptive and anti-inflammatory activities of aqueous extract of a blended mixture of dried leaves of Ocimum gratissimum and Psidium guajava, a traditional analgesic drug polyherbal (TADP) used as a remedy for pain-related conditions. Methods Antinociceptive activity of TADP (100, 200 and 400 mg/kg) was evaluated in the hot plate test and acetic acid-induced nociception in mice while the anti-inflammatory was evaluated in carrageenan-induced paw oedema in rats. Levels of nitrite, myeloperoxidase, glutathione and malondialdehyde were assayed in carrageenan-induced paw tissue. Results TADP (200 and 400 mg/kg) significantly prolong the latency time in the hot-plate test. TADP (100–400 mg/kg) produced a dose-dependent significant inhibition of the acetic-acid induced abdominal constriction. The antinociceptive activity of TADP in the presence of naloxone and atropine was not reversed whereas yohimbine and glibenclamide significantly reversed it. TADP (100, 200 and 400 mg/kg) significantly reduced the swelling in the carrageenan-induced oedema model and also produced a reduction in the nitrite and myeloperoxidase level. TADP (400 mg/kg) significantly reduced malondialdehyde concentration and increase glutathione level in the carrageenan-induced rat paw. TADP significantly decrease the number of cellular infiltrates in the histopathological assessment. Conclusion These results indicate that polyherbal product containing blended leaves of Ocimum gratissimum and Psidium guajava possess antinociceptive and anti-inflammatory properties, hence represents a promising alternative remedy in inflammation-induced pain.


2010 ◽  
Vol 9 (3) ◽  
pp. 28
Author(s):  
Sh. M. Al-khazrji , and I. K. Khalil

The present study was aimed to investigate the analgesic effects of the aqueous extract of Artemisia herba alba Arial part in rats and mice ( AEAHA ). The AEAHA (400- 700 mg/kg; p.o.) was evaluated for its analgesic activity by employing acetic acid-induced writhing test, hot plate test and tail immersion tests i.e. in hot and cold water. AEAHA (400- 700 mg/kg; p.o.) showed significant (P<0.01) reduction in the number of writhing induced by acetic acid,increased reaction time in hot plate test and elevated pain threshold in hot and cold water tests. AEAHA exhibited the dose-dependent analgesic effects


2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Jackson Roberto Guedes da Silva Almeida ◽  
Grasielly Rocha Souza ◽  
Juliane Cabral Silva ◽  
Sarah Raquel Gomes de Lima Saraiva ◽  
Raimundo Gonçalves de Oliveira Júnior ◽  
...  

Borneol, a bicyclic monoterpene, has been evaluated for antinociceptive and anti-inflammatory activities. Antinociceptive and anti-inflammatory activities were studied by measuring nociception by acetic acid, formalin, hot plate, and grip strength tests, while inflammation was prompted by carrageenan-induced peritonitis. The rotarod test was used to evaluate motor coordination. Borneol produced a significant (P<0.01) reduction of the nociceptive behavior at the early and late phases of paw licking and reduced the writhing reflex in mice (formalin and writhing tests, resp.). When the hot plate test was conducted, borneol (in higher dose) produced an inhibition (P<0.05) of the nociceptive behavior. Such results were unlikely to be provoked by motor abnormality. Additionally, borneol-treated mice reduced the carrageenan-induced leukocytes migration to the peritoneal cavity. Together, our results suggest that borneol possess significant central and peripheral antinociceptive activity; it has also anti-inflammatory activity. In addition, borneol did not impair motor coordination.


Author(s):  
Mavuto Gondwe ◽  
Anda Mpalala ◽  
Lusanda Zongo ◽  
David Kamadyaapa ◽  
Eugene Ndebia ◽  
...  

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.


2012 ◽  
Vol 67 (1-2) ◽  
pp. 15-21 ◽  
Author(s):  
Leonardo R. Bonjardim ◽  
Edisleide S. Cunha ◽  
Adriana G. Guimarães ◽  
Michele F. Santana ◽  
Makson G. B. Oliveira ◽  
...  

We attempted to identify the antinociceptive and anti-inflammatory actions of the monoterpene p-cymene. Firstly, behavioural screening was carried out to verify the influence of p-cymene [25, 50, and 100 mg/kg intraperitoneal (i.p.)] on the central nervous system (CNS) activity. The antinociceptive activity of p-cymene was evaluated by the acetic acidinduced writhing response, formalin, and hot-plate test, respectively. The leukocyte migration induced by injection of carrageenan was used to assess the anti-inflammatory activity. p-Cymene showed depressant activity on CNS after 4 h of treatment and also a possible action on the autonomous nervous system (ANS), mainly at the dose of 100 mg/kg (i.p.). It was found that p-cymene (50 and 100 mg/kg, i.p.) significantly (p < 0.05) reduced the writhing responses induced by acetic acid. p-Cymene also decreased the licking time in the first and second phase, respectively, of the formalin test. The results of the hot-plate test showed that all doses of p-cymene increased significantly the latency time of the response to the thermal stimulus in both licking and jumping parameters. In addition, there was a significantly (p < 0.05) decreased leukocyte migration at all doses of p-cymene. The experimental data demonstrate that p-cymene possesses antinociceptive and anti-inflammatory activities


2019 ◽  
Vol 17 (1) ◽  
pp. 1034-1042
Author(s):  
Riaz Ullah ◽  
Mansour S. Alsaid ◽  
Ali S. Alqahtani ◽  
Abdelaaty A. Shahat ◽  
Almoqbil A. Naser ◽  
...  

AbstractThe medicinal plant Haloxylon salicornicum is utilized for therapeutic purposes. We previously reported the antioxidant potential of hexane fraction and methanol extracts of the same species. However, since these solvents could be clinically toxic, the current findings investigated the pharmacological effects of the water fraction. The pain relieving, antioxidant, anti-inflammatory, and antipyretic potential of H. salicornicum water extract (HEW) were studied at two concentrations (250 and 500 mg/kg) in rodents. The carrageenan stimulated rat paw edema assay was exercised to assess anti inflammatory potential in rats; yeast-stimulated hyperthermia was utilized to test antipyretic activity in mice; analgesic properties were assessed based on acetic acid-induced writhing, tail flicking, and hot-plate test; and antioxidant potential was examined with the 2,2-diphenyl-1-picrylhydrazyl assay. We found that 500 mg/kg HEW inhibited edema by 44.03%. Yeast-induced hyperthermia in mice was reduced by 250 and 500 mg/kg HEW after 30, 60, and 120 min with significant level of (P < 0.001) compared to rectal temperature of yeast administered group. The high dose of HEW (500 mg/kg) improved the reaction time of mice in the hot-plate test from 6.66 ± 0.33 to 11.33 ± 0.49 s after 120 min. In the acetic acid-stimulated writhing test, 250 and 500 mg/kg HEW decreased writhing by 32.71% and 51.40%, respectively, after 20 min. HEW also showed antioxidant effects. These results demonstrate that HEW is bioactive and has therapeutic potential for treating a variety of ailments.


2005 ◽  
Vol 33 (01) ◽  
pp. 29-40 ◽  
Author(s):  
Hyun-Ae Eum ◽  
Woo-Yong Lee ◽  
Sung-Ho Kim ◽  
Joo-Young Kim ◽  
Sang-Won Park ◽  
...  

CML-1 is a purified extract from a mixture of 13 Oriental herbs (Achyranthis Radix, Angelicae Gigantis Radix, Cinnamomi Cortex Spissus, Eucommiae Cortex, Glycyrrhizae Radix, Hoelen, Lycii Fructus, Paeoniae Radix, Rehmanniae Radix Preparata and Atractylodis Rhizoma, Zingiberis Rhizoma, Zizyphi Semen, Acori Graminei Rhizoma) that have been widely used for the treatment of inflammatory diseases in Asia. The aim of this study was to investigate the anti-inflammatory and analgesic potential of CML-1. The animals used in this study were administered either vehicle or CML-1 (30, 100, 300 and 600 mg/kg) orally. The vascular permeability induced by acetic acid was significantly reduced by CML-1 in all doses. The swelling of the rat's hind paw induced by carrageenan was significantly inhibited by CML-1 in doses of 100, 300 and 600 mg/kg. In the case of rheumatoid arthritis induced by complete Freund's adjuvant in rats, the treatment with CML-1 at a dose level of 300 mg/kg inhibited edema. CML-1 at a dose level of 600 mg/kg inhibited acetic acid-induced writhing syndrome, however it did not have any anti-nociceptive action in the Randall-Selitto assay or the hot plate test. Our findings suggest that CML-1 has a potent anti-inflammatory activity.


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