جستجوی مقالات مرتبط با کلیدواژه « Analgesic activity » در نشریات گروه « پزشکی »

Albuca amoena is a Moroccan-Algerian endemic medicinal plant with various implications. The aim of this study is to identify phytochemical compounds of the plant, check its acute toxicity, and test its anti-depressive, anxiolytic, and analgesic effects on the central nervous system (CNS).

The estimation of chemical compounds was carried out according to coloring and precipitation reactions. The Organization of Economic Cooperation and Development guidelines 423 and 402 made it possible to verify the acute toxicity of the plant orally and dermally. The sedative activity was performed according to 4 tests: rotarod, hole-board, traction, and chimney tests. The anti-depressive, anxiolytic, and analgesic effects were evaluated by forced swimming, light/dark, and writhing tests, respectively.

The phytochemical analysis showed that A. amoena contained a mixture of phytochemical compounds like terpenes, alkaloids, and polyphenols. According to the acute toxicity tests, the lethal dose of 50% (LD50) of A. amoena hydroalcoholic extract was between 300 and 2000 mg/kg orally and higher than 2000 mg/kg dermally. Moreover, the result of the behaviour tests of sedative and analgesic activities revealed that A. amoena hydroalcoholic extract exerted positive effects on the CNS.

These results show the anti-depressive, anxiolytic, and analgesic effects of the bioactive substances present in A. amoena on the CNS and provide access to further investigations to highlight the main compounds of this plant and their mechanisms of actions.

Salvia reuterana, commonly known as Maryam Goli Esfahani, is a member of the Labiateae family. In Iranian folk medicine, aerial parts of S. reuterana have been used as sedative and anxiety. Evaluation of various extracts of the plant for their analgesic activity revealed that treatment of mice with n-hexane extract (500 mg/kg, i.p.) significantly increased the latency time as compared to the control group. Fractionation of the hexane extract of S. reuterana led to the isolation of sclareol as the main compound (0.19% w/w). Column chromatography was used to isolation of compounds from S. reuterana and spectroscopic method including NMR was used to identification of the isolated compound. Evaluation the analgesic effect of sclareol using hot plate, tail flick and formalin tests in mice confirmed the potent analgesic effect of sclareol as an effective compound of S. reuterana. These results showed that the n-hexane extract of aerial parts of S. reuterana and its main constituent sclareol showed significant analgesic activity in different rodent nociceptive behavioral tests.

The objective of the current study was to develop Ibuprofen (IBP) gel using different polymers individually and in combination and then to select best gel formulation based on various in-vitro evaluation parameters such as bioadhesive strength, gel strength, spreadability, viscosity and drug release study. The selected gel formulation was found to be composed of 1% (w/w) each of hydroxypropyl methylcellulose (HPMC K100M) and sodium carboxy methylcellulose (NaCMC). Two techniques such as chemical method using 1,8-cineole as chemical penetration enhancer (CPE) and physical technique using microneedle were employed to improve IBP permeation across the abdominal skin of rat. Out of the two techniques, the later technique showed higher (2.865-fold) permeation enhancement compared to control. Furthermore, a synergistic effect was also observed when both the techniques were used simultaneously with 3.307-fold increase in permeation enhancement. In-vivo anti-inflammatory study on rats induced with carrageenan paw oedema and analgesic activity investigation by tail flick method in rat model exhibited sustained effect up to 8 h compared to orally treated group. The stability study at room and accelerated conditions for three months did not show any sign of instability. Thus, the developed IBP gel is stable and have potential to illicit both anti-inflammatory and analgesic effect when administered transdermally.

Scorpion venom contains different toxins with multiple biological functions. IMe-AGAP is the first Analgesic-Antitumor like Peptide (AGAP) isolated from Iranian scorpion Mesobuthus eupeus. This peptide is similar to AGAP toxin with high analgesic activity, extracted from Chinese scorpion and inhibits NaV1.8 and NaV1.9 voltage-gated sodium channels involved in the pain pathway. In this study, IMe-AGAP was cloned in a prokaryotic expression vector; expression of toxin in Escherichia coli (E. coli) was assayed and then purified. In in-silico studies, peptide sequence was compared with other scorpion analgesic toxins. The structures of IMe-AGAP and sodium channels were modeled using homology modeling. Structural evaluation and stereo-chemical analysis of modeled structures were performed using RAMPAGE web server Ramachandran plots. Hex Server was used to investigate the interactions between IMe-AGAP and S3-S4 and also S5-S6 segments of Nav1.8 and NaV1.9. Binding energies calculation was used for evaluation of protein docking. Soluble expression of IMe-AGAP in bacteria was investigated by SDS-PAGE analysis. Pure recombinant protein was obtained by Ni-NTA affinity chromatography. The results of three-dimensional structure prediction showed βαββ topology for the toxin that is similar to the conserved structure of α-toxins. Comparison analysis between IMe-AGAP and AGAP toxins exhibited high similarity in homology modeling. Docking analysis demonstrated that IMe-AGAP can interact with NaV1.8 and NaV1.9 domains involved in pain. According to the results of homology studies and docking, IMe-AGAP might be a novel potential drug for pain treatment.

Otostegia fruticosa is traditionally used to treat tonsillitis, stomach ache, asthma, arthritis, and febrile illness in different parts of Ethiopia and other countries. In this experiment 70% ethanolic crude extract and fractions of the leaf of Otostegia fruticosa (Forssk.) Schweinf. ex Penzig were evaluated for their in-vivo anti-inflammatory and analgesic activities and in-vitro hyaluronidase inhibition properties at different concentrations. Tail immersion, acetic acid induced writhing and carrageenan-induced paw edema model were used to assess the in-vivo analgesic and anti-inflammatory activities, respectively. Swiss albino mice of either sex were randomly divided into five groups of six mice per group and for evaluation of the fractions randomly divided into six groups of six mice per group. The test groups were treated with hydroalcoholic extract of O. fruticosa at doses of 100, 200, and 400 mg/kg. The positive control groups received either pethidine 5 mg/kg or aspirin at 100 mg/kg or 150 mg/kg. The negative control groups were orally given sunflower oil. All the fractions were administered at the dose of 400 mg/kg. In all models, the higher dose (400 mg/kg) of the crude extract and chloroform fraction showed a significant central and peripheral analgesic and anti-inflammatory activities with comparable effects to standards used.  The hyaluronidase inhibition assay result showed that the test samples displayed concentration-dependent inhibitory activities. These findings indicate that 70% ethanol extract and organic solvent fractions of O. fruticosa leaves have potential analgesic, anti-inflammatory, and enzyme inhibitory activities.

Ficus palmata (FI) is an important and widely used medicinal plant. It is principally used as an item of diet in the treatment of constipation and diseases of the lungs and bladder. The sap is used in the treatment of warts. Ficus palmata plant is used in various disease e.g. gastrointestinal, hypoglycemic, antitumor, anti-ulcer, anti-diabetic, lipid lowering and antifungal activities. This study evaluates both the central and peripheral analgesic effect of the different extracts of Ficus palmata in the experimental animals. Acute toxicity test was done following the Organization of Economic Co-operation and Development guidelines. Ficus palmata extracts (250 mg/kg, 500 mg/kg) body weight was evaluated for central analgesic activity by the hot plate method, tail immersion method and formalin test models using tramodol (20 mg/kg b.w.) as the standard drug. In all the models, chloroform extract showed significant inhibition as well as the elongation of time at a dose of 500 mg/kg body weight. A linear dose response relationship was also observed which was comparable with that of the standard drug tramodol (p<0.01, p<0.05). The study showed significant central and peripheral analgesic activity of Ficus palmata which may be attributed to the inhibition of prostaglandin synthesis, phospholipase A2, and tumor necrosis factor alpha. Ficus plamata as a commercial source of analgesic drug should be subjected to further research.

Numerous proteins and peptides in venomous marine animals are potentially active molecules with pharmacological properties. Particular condition of the Persian Gulf as a closed ecosystem is a good opportunity to study of biological activities and toxicity of venomous animals. In this study, Stichodactyla haddoni (S. haddoni), a sea anemone, selected to tracing for possible pharmaceutical agents and toxicological characterization. Analgesic, edematic, dermonecrotic, LD50, phospholipase, and proteolytic activities of the venom were estimated. LD50 was recorded at 675µg by intraperitoneal injection. Analgesic activitiy of crude venom on Balb/c mice at both 100 and 150 µg were dose dependent as a linear trend. Three folds increase of activity was seen at both 100 and 150 µg after 240 min comparing to activity of morphine at 200 µg. The crude venom at amount of 0.23 µg produced 50% hemolysis. The highest edematogenic activity was seen on Balb/c mice just two hours after injection for both 168 µg (157%) and 335 µg (247%). The crude venom at 675 µg made 4 mm inflammation area on rabbit skin after 3 h but the amount of 1000 µg induced 8 mm necrosis area. Potent analgesic activity of the venom was seen below its toxic dose that was very greater than the other sea anemones in the other geographical areas. The results indicate that a persistent edematogenic activity could be happened after envenomation. Instant potent edematogenic and rapid dermonecrotic activity were significant phenomena. HD50 at 0.23 µg indicates that a very potent hemolytic agent exists in the venom. The results would also be of high value to better management of envenomation. This study confirmed the great value of further studies on the Persian Gulf S. haddonivenom.

Leptadenia reticulata was reported to be used for several medicinal purposes. The present study was undertaken to evaluate anti-inflammatory, analgesic and lipid peroxidation inhibition activities of L. reticulata. The anti-inflammatory assay was performed by λ-carrageenan and formalin induced paw edema test. Pro inflammatory mediators (IL2, IL6, TNF-α) in serum of treated and control organism were analyzed by quantitative ELISA. Lipid peroxidation inhibition was measured by thiobarbituric acid reactive substances (TBARS) assay. Analysis of the most active fraction revealed the presence of one phenolic compound (p-coumaric acid), two flavonoids (rutin and quercetin) which also determined quantitatively. The ethyl acetate fraction at 600 mg/kg significantly inhibited λ-carrageenan and formalin induced paw edema by 60.59% and 59.24% respectively. Notable reduction in percentage of writhing (76.25%), induced by acetic acid signifies the potent analgesic activity. Lower level of pro-inflammatory cytokines (IL-2, IL-6, TNF-α) in serum at the 4th hour of λ-Carrageenan injection indicated the inhibition of cyclooxigenase-2 (Cox-2), Nitric oxide (NO) and release of prostaglandin to prevent inflammation. The study also demonstrated the decrease in malonaldehyde (MDA) concentration which revealed the lipid peroxidation inhibition potential of the plant. Our finding provides evidence for potent biological activities in tested model which is supported by its characterized bioactive compounds and ethnomedicinal relevance.

The uses of non-steroidal anti-inflammatory drugs (NSAIDs) are limited by a variety of side effects. So research on preparing new analgesic agents is important. According to some reports about the analgesic activity of hydrazide and hydrazine derivatives a new series of these compounds were synthesized in order to obtain new analgesic compounds. The final compounds 10a-10e and 15a-15d were prepared by condensation of corresponding hydrazides 7 and 8with different aldehydes 9a-9e. The structures of all synthesized compounds were confirmed by means of FT-IR, 1H-NMR and Mass spectra. All compounds were evaluated for their analgesic activities by abdominal constriction test (writhing test). Most of the synthesized compounds induced significant reduction in the writhing response when compared to control and compound 15was more potent than mefenamic acid in the writhing test.

A series of phenoxybenzylidene aroylhydrazine derivatives were synthesized and their structures were confirmed using FT-IR and 1H-NMR spectroscopy. Analgesic profiles of all compounds were examined using abdominal constriction test (writhing test). Most of synthesized compounds induced significant reduction in the writhing response as compared with controls. The most active compounds exhibited an analgesic activity comparable with that of mefenamic acid.

There is the need for new drugs with better action and lesser side effects. A lot of research is being undertaken to find out new plant drugs, their extraction and pharmacological evaluation. One of such plant is Curcuma aromatica whichbelongs to the genus Curcuma and reported to have high ethno-botanical values in traditional medicine. The present study evaluates comparative pharmacological activity of four different extracts of Curcuma aromatica in healthy Wistar strain albino rats.Extraction of active constituents from powdered plant rhizomes was done by cold maceration technique using water, ethanol, hydroalcohol and toluene as solvents separately to get respective extracts. Acute oral toxicity study was performed to determine toxicity or side effects associated with the prepared plant extracts. The extracts were evaluated for anti-diabetic, anti-oxidant, anti-inflammatory and analgesic activity. Anti-diabetic activity was comparatively evaluated in alloxan induced diabetic rat models. Toluene extract was found to have relatively higher anti-diabetic activity. In vitro antioxidant potential of different extracts of was evaluated by DPPH radical scavenging activity. The results show anti-oxidant potency in toluene extract slightly better than other extracts. Aqueous extract of Curcuma aromatica rhizomes was found to have more potency in treatment of carrageenan induced paw oedema and also in its anti-nociceptive action against heat induced pain by Eddy’s hot plate method in rats.Though the anti-diabetic and anti-oxidant activities were slightly superior in toluene extract, the risk of residual amount of toluene remained in the final extract and its teratogenic property subdues its benefits of treatment.Findings of this research prove our hypothesis that oral administration of aqueous rhizome extract has potential anti-diabetic, anti-oxidant, anti-inflammatory and analgesic activities.

In the present study in vivo analgesic activity of some previously synthesized 1,2,4-triazole derivatives containing pyrazole, tetrazole, isoxazole and pyrimidine ring have been evaluated. Acetic acid induced writhing method and Hot plate method has been described to study analgesic activity of some 1,2,4-triazole derivatives containing pyrazole, tetrazole, isoxazole and pyrimidine as a pharmacological active lead. Thirty six different derivatives containing 1,2,4-triazole ring were subjected to study their in vivo analgesic activity. Chloro, nitro and methoxy, hydroxy and bromo substituted derivatives showed excellent analgesic activity and dimethylamino, furan and phenyl substituted derivatives showed moderate analgesic activity in both of the methods. Compounds IIIa, IIId, IIIf, IIIi, IIIj, IVa, IVb, IVd, IVf, IVh, IVj IV3a and IIj were found to be superior analgesic agents after screening by Acetic acid induced writhing method. Compounds IIIb, IIId, IIIf, IIIh, IIIj, IVa, IVb, IVd, IVf, IVh, IVi, IV3c, IV3e and IIj were showed analgesic potential after screening of Hot plate method. All tested compounds containing 1,2,4-triazole were found to be promising analgesic agents, for this activity pyrazole, tetrazole, isoxazole and pyrimidine leads might be supported.

Present study reports analgesic activity of petroleum ether, chloroform, ethyl acetate and methanolic extracts of leaves and seeds of Trigonella foenum-graecum Linn. (Fabaceae) using hot plate method for evaluation of central analgesic activity and acetic acid induced writhing test for evaluation of peripheral analgesic activity in mice. All the extracts of Trigonella foenum-graecum showed significant central and peripheral analgesic activity at the dose of 50 mg/kg intraperitoneally. Amongst all the extract methanolic extract of leaves of Trigonella foenum-graecum showed highest increase in reaction time in hot plate method and more inhibitory effect on writhing induced by acetic acid. Pentazocin and paracetamol was taken as standard drug for hot plate and writhing model respectively.