Peripheral Analgesic Activity Research Articles

Screening of novel 2-4methylphenylimino-3-carboxamide substituted thiophene compound for peripheral analgesic activity

Background: Pain is an unpleasant sensation that can range from mild, localized discomfort to agony. The mechanism of pain perception involves dedicated subsets of peripheral and central neurons. For management of pain, currently, available treatment regimens are opioid analgesics and NSAIDs which are easily available over the counter drugs. Long term use of analgesics can lead to significant impact on human renal system, cardiovascular system and analgesic abuse etc. So, there is a need for novel, safe and cost effective analgesic compound. Hence a study on 2-4methylphenylimino-3-carboxamide substituted thiophene compound, a novel thiophene compound has been carried out in different experimental animal models.Methods: Two methods were used to evaluate the peripheral analgesic activity of 2-4methylphenylimino-3-carboxamide substituted thiophene compound. First method was Acetic acid induced writhing and compared to standard drug aspirin. Second method was late phase of formalin induced paw licking in mice and compared to a standard drug, aspirin.Results: With Acetic acid induced writhing, 40mg/kg dose of 2-4methylphenylimino-3-carboxamide substituted thiophene compound has shown maximum Pain Inhibition Percentage (PIP) of 78 % compared to 91% by Aspirin. Whereas with late phase of Formalin test, 40mg/kg dose of 2-4methylphenylimino-3-carboxamide substituted thiophene compound has shown maximum PIP of 58% in late phase compared to 86% by aspirin. The results were statistically significant with p<0.05.Conclusions: It can be concluded that 2-4methylphenylimino-3-carboxamide substituted thiophene compound found to have moderate peripheral analgesic activity as evident in acetic acid induced writhing and late phase of formalin tests.

RETRACTED: Dobera glabra (Forssk.) Poir. (Salvadoraceae); phenolic constituents of the aqueous leaves extract and evaluation of its anti-inflammatory, analgesic activities

BackgroundThe plant kingdom is considered one of the most common sources for structural and biological diversity. In particular, the wild category acquires our attention to investigate the phytochemical and the biological evaluations. MethodsDobera glabra was exposed to phytochemical examination using HPLC-ESI-MS analysis. Furthermore, the anti-inflammatory activity was evaluated using carrageenan-induced rat paw edema model, whereas both the central and peripheral analgesic activities were tested via hot plate test in rats and acetic acid-induced writhing in mice, respectively. ResultsTwenty phenolic compounds of D. glabra aqueous leaves extract were emphasized by liquid chromatography coupled with mass spectrometry. Moreover, D. glabra exhibited both anti-inflammatory and peripheral analgesic activities. Furthermore, D. glabra significantly decreased the immune expression of MMP-9, TNF-α and TGF-β1 in the hind paw of rats. ConclusionD. glabra possess peripheral anti-nociceptive and anti-inflammatory effects in rats mediated through its anti-oxidant and anti-inflammatory activities. The activity of D. glabra leaves extract might be attributed to the presence of hydroxy and keto structures.

Pharmacological investigation of Thespesea populnea bark extract for analgesic activity

Background: Pain is an unpleasant and distressing common problem with profound impact on individuals and society. Existing treatment modalities used for pain management are either less effective or exhibits several side effects. The aim of current study is to investigate the analgesic activity of stem bark extract of Thespesea populnea for pain management.Methods: Thirty Swiss albino were divided into five groups including control, standard and three tests groups (different doses of Thespesea populnea bark extract). Groups were investigated for analgesic activity using hot plate induced paw withdrawal, acetic acid induced writhing and formalin induced paw licking models.Results: Findings of hot plate model revealed that, percent increase in reflex latency of paw licking response in mice for test drug (10 mg/kg), attained peak effect of 136% at 180 minutes, whereas for standard pentazocine peak effect of 125% was attained at 180 minutes. In acetic acid model, the maximum percent inhibition in number of writhings for the test drug (30 mg/kg) was 68% and for standard diclofenac, it was 80%. In formalin model, percent inhibition in licking response in early and late phases for test drug (30 mg/kg) were 81% and 91% and for standard diclofenac it was 56% and 94% respectively. It was thus depicted that analgesic activity of test drug was significantly more than the standard in early phase and equivalent to standard in late phase.Conclusions: It was concluded that Thespesea populnea bark extract at a dose of 10 mg/kg showed potential peripheral and central analgesic activity.

Evaluation of analgesic activity of ethanolic extract of alpinia galanga rhizomes in experimental animal models

Introduction: Alpinia galanga Linn is a widely used medicinal plant. It is also known as Greater Galangal and belongs to family Zingiberaceae. The plant is a perennial rhizomatous herb and has been claimed to possess analgesic activity apart from many medicinal properties. Objectives: The aim of the present study was to evaluate the analgesic activity of ethanolic extract of alpinia galanga rhizomes (EEAGR) in experimental animals. Methods: Acute toxicity test was done following the Organization of Economic Cooperation and Development guidelines.100 mg/kg, 200 mg/kg, and 400 mg/kg body weight [b.w] of ethanolic extract of alpinia galanga rhizomes was given orally to experimental animals. EEAGR was evaluated for central analgesic activity by using the tail flick method and peripheral analgesic activity by using the acetic acid induced writhing test using aspirin (300 mg/kg b.w and 100 mg/kg b.w orally) as the standard drug respectively. Results: EEAGR at 400mg/kg produced highly significant and greater analgesic activity than Aspirin (standard drug) in tail flick method. EEAGR at dose 400mg/kg has shown comparable reduction in mean total number of writhings which is equivalent to that of Aspirin (standard drug) in writhing test. Conclusion: EEAGR has significant central and peripheral analgesic activity. Keywords: Alpinia galanga, Analgesic, Pain, Tail flick, Writhing.

Analgesic activity of Terminalia bellerica fruit pulp aqueous extract by using acetic acid induced writhing test in Swiss albino mice by peripheral mechanism

Objective: To evaluate analgesic activity of Terminalia bellerica fruit pulp aqueous extract by acetic acid induced writhing reflex test in Swiss albino mice by peripheral mechanism. Materials and Methods:Albino mice of Swiss strain (Male / Female-equal number), were `selected for the study and each mouse weighed about 15-30gms. Five experimental groups made assigned as Control, Standard and three groups of test drugs at different doses, and the doses were Gum acacia (1%), 10ml/kg, Diclofenac sodium (30mg/kg), Terminalia bellerica 9, 18 and 36 mg/kg respectively. All the drugs were administered orally one hour before commencing the experiment followed by injecting 0.1 ml of 0.6% acetic acid intraperitoneally and writhing reflex was observed for next five minutes. Observations recorded as mean ± SD. Results obtained were analyzed by using ANOVA (one-way) statistical test followed by Dunnet’s multiple comparison test and if p value Results: Our study reveals that aqueous extract of Terminalia bellerica fruit pulp in the dose of 9mg/kg (4.83±1.47=p Conclusion:Aqueous extract of Terminalia bellerica fruit pulp exhibited peripheral action in all the dose of 9, 18 and 36 mg/kg by acetic acid induced writhing reflex test in Swiss albino mice. Keywords: Aqueous extract, Fruit pulp, Peripheral analgesic activity, Terminalia bellerica, Writhing test

COMPARATIVE STUDIES ON ANTIDIABETIC, ANALGESIC, AND CYTOTOXIC EFFECT OF ETHANOLIC EXTRACTS OF AMARANTHUS GANGETICUS L. AND ALTERNANTHERA SESSILIS L.

Objective: The present study was designed to evaluate and compare antidiabetic, analgesic, and cytotoxic properties of Lal shak (Amaranthus gangeticus L.) and Chanchi shak (Alternanthera sessilis L.). We carried out this work to explore the medicinal uses of very common and cheap leafy plant vegetables among the people of all classes.
 Methods: The antidiabetic activity was evaluated and compared by studying the effect of ethanolic extract of A. gangeticus (EEAG) and ethanolic extract of A. sessilis (EEAS) against blood glucose level of alloxan-induced diabetic mice in every 6 h for 24 h. To evaluate and compare analgesic and cytotoxic activity, different tests such as acetic acid-induced writhing test, hot plate test, and brine shrimp lethality bioassay test had been performed.
 Results: The mice were treated with both plants extract at a dose of 200 mg/kg body weight in case of antidiabetic activity test. Blood glucose level was examined and found that there was a significant reduction of blood glucose level with EEAG (p<0.05) and EEAS (p<0.001) in comparison with their respective diabetic control group. Although both plant extracts reduced the blood glucose level, the glucose reducing effect was higher in EEAS. Both the plants showed significant (p<0.05) peripheral analgesic activity in treated mice but no significant central analgesic activity. EEAG showed higher peripheral analgesic activity than EEAS. In brine shrimp lethality bioassay, both the plants showed higher LC50 value thus cytotoxicity occurs at very higher dose and safe to administer.
 Conclusion: In this study, both the plants showed sufficient antidiabetic property and higher LC50 value, thus administration of leafy vegetable Lal shak and Chanchi shak may be useful for diabetic people. Chanchi shak may be more helpful for diabetic people than Lal shak.

Acute toxicity and central and peripheral analgesic activity of flowers and leaves essential oils of Asteriscus graveolens from South-West Algeria

The objective of this study is the evaluation of the central and peripheral analgesic activity of the leaves and flowers Essential Oils (EOs) of Asteriscus graveolens as well as their acute toxicity. The pharmacological tests were performed using an animal model. Acute toxicity was determined by Lorke's method. Central analgesic activity was evaluated by the hot plate test, and peripheral analgesic activity was conducted by the writhing test. The results showed that the EOs of A. graveolens from both organs are weakly toxic. For the central analgesic activity, the results revealed that leaf EO have a remarkable antinociceptive effect compared to flowers EO with a maximum latency time of the animals on the hot plate on the order of 22.5 seconds. Finally, the peripheral analgesic activity revealed a maximum inhibition of abdominal writhing of 99% for flowers EO and 96% for leaves EO. Keywords: Asteriscus graveolens, analgesic activity, toxicity.

Screening for anti-inflammatory and peripheral analgesic activity of Coleus amboinicus leaves using wistar albino rats

We have abundant plant resources with many health benefits. Use of plant material for health benefits will help in reduce the cost of drugs and also provide a substitute drug that is less expensive. Coleus amboinicus is plant largely distributed in Dakshina kannada and is used for its medicinal properties as household cure. We planned to find out the anti-inflammatory and peripheral analgesic activity of Aqueous Extract of leaves of Coleus amboinicus. Wistar albino rats were randomly selected and tests were performed by dividing the animals into three groups- control, standard, test.Aqueous extract of leaves of Coleus amboinicus was prepared using soxhlet apparatus. The dose of leaf extract used was 500mg/kg. Data was analysed by applying one way ANOVA followed by Dunnets multiple comparison test using Graphpad Instat.The results obtained were statistically significant. In Carragenan induced inflammation model significant inhibition of inflammation was shown by the test drug at the end of 3 hrs and in Acetic acid induced writing test significant inhibition of occurrence of writhes was noted by the test drug.This study validates the folkloric use of aqueous extract of leaves of Coleus amboinicus (AECA) at the dose of 500mg/kg for its anti-inflammatory and peripheral analgesic activity.

Evaluation of the analgesic activity of ethanolic extract of Populus deltoides leaves in mice

The ethanolic leaves extract of Populus deltoides was tested for the presence of various phytoconstituents and designed to evaluate the analgesic activity in mice. The peripheral analgesic activity of ethanolic leaves extract of P.deltoides (250 and 500 mg/kg) was studied by using acetic acid stimulated writhing test and central analgesic activity of P.deltoides was studied by using hotplate process. The ethanolic leaves extract of P.deltoides professed the existence of a variety of chemical constituents like alkaloids, saponins, flavonoids, terpenes and steroids. Leaves extract of P.deltoides appreciably decreased the writhing actions in acetic acid-induced writhing test in mice and amplified the respond time in hotplate test. These results suggest that the extract may have NSAIDs like activity through the peripheral mechanism and central analgesic activities via opioid receptors. From our study, we endowed that leaves extract of P.deltoides has feasible to analgesic activity. This study reveals that it can be used in the management of pain and provide a scientific basis for its traditional use.

Antinociceptive, antiinflammatory, and antipyretic effects induced by the venom of Egyptian scorpion Androctonus amoreuxi

BackgroundScorpion venom is a very complicated mixture of various peptides/proteins which could induce toxicological and pharmacological responses. This investigation was conducted to evaluate the possible pharmacological properties (analgesic, antipyretic, and antiinflammatory effects) of the Egyptian scorpion venom Androctonus amoreuxi in mice and rats injected intraperitoneally with 1/10 and 1/5 LD50 (0.11 and 0.22 mg/kg for mice; 0.385 and 0.77 mg/kg for rats, respectively).ResultsThe peripheral and central analgesic effect of A. amoreuxi venom was determined using the tests of mice-abdominal writhing and tail immersion of rats, respectively. The antipyretic and antiinflammatory activities were examined using the pyrexia rats model induced by Brewer’s yeast and the paw mice edema induced by carrageenan, respectively. The venom of A. amoreuxi produced significant (p < 0.05) peripheral and central analgesic activity in both animal models. Also, treatment with the scorpion venom showed significant (p < 0.05) dose-independent reduction in pyrexia of rats. More importantly, the venom significantly inhibited mice paw edema induced by carrageenan.ConclusionAccordingly, the present results showed that the venom of this scorpion possesses remarkable pharmacological properties (analgesic, antipyretic, and antiinflammatory activities) on animal models, and might be contain certain peptides responsible for the reported activities.

Evaluation of Analgesic and Anti-Inflammatory Activities of 80% Methanol Root Extract of Echinops kebericho M. (Asteraceae).

BackgroundPain and inflammation are the major devastating health problems commonly treated with traditional medicinal plants in Ethiopia. Echinops kebericho M. (Asteraceae) is the one which is frequently used to treat pain and inflammation by traditional healers in Ethiopian folk medicine. However, the plant has not been scientifically evaluated for its traditionally claimed use. The present study aimed at the investigation of analgesic and anti-inflammatory activities of 80% methanol root extract of Echinops kebericho M. in mice model.MethodsSuccessive maceration was used as a method of extraction using solvents of increasing polarity: methanol and water. After extraction of the roots with 80% hydro methanol, the crude extract was evaluated for its peripheral and central analgesic activities using acetic acid-induced writhing test and hot plate method, respectively, while its anti-inflammatory activity was evaluated using carrageenan- and formalin-induced paw edema. The extract was evaluated at 100, 200 and 400 mg/kg doses. The positive control groups were treated with ASA 150 mg/kg for writhing test, morphine 10 mg/kg for hot plat method, indomethacin 25 mg/kg and diclofenac 10 mg/kg for paw edema tests and vehicle, distilled water (10 mL/kg) treated mice were assigned as negative controls. All treatment administrations were performed orally.ResultsE. kebericho extract at all test doses showed statistically significant antinociceptive activity in both chemicals-induced peripheral and thermal-induced central pain in a dose dependent manner (p < 0.01 and p < 0.001). The greater analgesic activity was observed by the maximum dose of the extract (400 mg/kg) in both acetic acids-induced writhing test (57.84%) and hot plate method (69.40%). The effect of the extract was also statistically significant (p < 0.01 and p < 0.001) in both carrageenan and formalin-induced paw edema in dose dependent manner. Greater edema inhibition was observed by the highest dose (400 mg/kg) in both observations with the respective percentage values of 70.00% and 79.87%, respectively.ConclusionIn general, the data obtained from the present study elucidated that the extract possessed a significant analgesic and anti-inflammatory activities and recommended for further studies.

Anti-Nociceptive and Anti-Inflammatory Activity of Hygrophila schulli Leaves.

PurposeThe management of pain and inflammation with non-steroidal anti-inflammatory drugs and opioid analgesics are currently encountering severe adverse reactions. To overcome these problems, herbal remedies may offer new alternative medicines. Hygrophila schulli is a medicinal plant traditionally used for the treatment of pain and inflammation-related disorders; yet, these claims are not scientifically validated. Hence, this study was aimed to validate the traditional use of Hygrophila schulli leaves as anti-inflammatory and analgesic remedy.MethodsIn vitro anti-hyaluronidase assay and in vivo carrageenan-induced hind paw oedema model were used to evaluate the anti-inflammatory property of ethanolic leaf extract of Hygrophila schulli. Tail immersion and acetic acid-induced writhing tests were performed to determine the central and peripheral analgesic activity of the leaf extract, respectively.ResultsThe ethanolic leaf extract exhibited significant anti-hyaluronidase activity (P<0.001) and significant inhibition of carrageenan-induced paw oedema (P<0.05) compared to untreated controls. Similarly, the extract significantly prolonged the reaction time of mice (P<0.05) for the hot-water stimuli. Furthermore, an oral dose of the extract showed significant inhibition (P<0.01) of acetic acid-induced abdominal contractions of mice. Besides, the ethanolic leaf extract did not cause any obvious sign of acute toxicity at a single oral dose of 2 g/kg.ConclusionThe findings of this study may partially support the acclaimed traditional use of Hygrophila schulli leaves for the treatment of pain and inflammatory conditions.

Investigation of the Peripheral Analgesic Activity of Oxicams and Their Combinations with Caffeine.

Therapy of pain syndromes involves exposure to its source, receptors, and peripheral fibers. Treatment of acute pain and inflammation involves the use of nonsteroidal anti-inflammatory drugs and nonnarcotic analgesics. An alternative to obsolete analgesics is combined compositions. Experimental results clearly indicates that caffeine effectively enhances the peripheral analgesic activity when combined in an analgesic. The aim of the present study was to evaluate the peripheral analgesic activity of meloxicam, piroxicam, and their pharmacological combinations with caffeine. The peripheral analgesic activity of piroxicam, meloxicam, and their combinations with caffeine was studied using the abdominal writhing test. This method was used to induce pain of peripheral origin by intraperitoneal injection of 0.6% acetic acid solution. The investigated drugs, their combinations, and 3% starch mucilage were administrated 1 h before the introduction of the algogen. The cumulative number of writhing responses induced by acetic acid was determined over the subsequent 20 min. All investigated drugs supplied a decrease in writhing in rats. Meloxicam and caffeine showed peripheral analgesic activity of 63.6% and 64.5%, respectively (p<0.05). The pharmaceutical combination of meloxicam and caffeine showed analgesic potential of 76.4%. Thus, caffeine potentiates the analgesic activity of meloxicam. The results exceeded the corresponding value of diclofenac sodium (67.3%). Experimental results clearly indicates that caffeine effectively enhances the peripheral analgesic action of meloxicam when combined in a pharmaceutical composition. These results can serve as a basis for the development of new domestic combined drugs.

In vivo Analgesic, Anti-hyperglycaemic and CNS Depressant Studies of Commelina paludosa Blume

The methanol extract of whole plant of Commelina paludosa Blume (family: Commelinaceae) has been screened to explore its in vivo central and peripheral analgesic, hypoglycaemic and central nervous system depressant activities in Swiss Albino mice. The crude extract significantly increased the latent response time in tail-flick method (p&lt;0.001) at the doses of 200 and 400mg/kg body weight for a 90 minute period when compared to control group. The peripheral analgesic activity was evaluated by acetic acid-induced writhing method and the extract showed significant results (p&lt;0.001) with 51.72 and 67.24% inhibition at 200- and 400-mg/kg body weight, respectively. In addition, a dose dependant blood glucose lowering and CNS depressant activities were also observed by the crude extract. Bangladesh Pharmaceutical Journal 23(2): 103-108, 2020

Vachellia farnesiana (L.) Wight &amp; Arn. Growing in Bangladesh Exerts In-vitro Antioxidant and In-vivo Analgesic and Anti-diarrheal Activities

The present study was conducted to evaluate the antioxidant, antidiarrheal and analgesic activities of Vachellia farnesiana (L.) Wight &amp; Arn. The methanol extract of V. farnesiana and its different fractionates were subjected to in-vitro assay for the determination of total phenolic content and antioxidative potential. The ethyl acetate soluble fraction (EASF) exhibited the highest free radical scavenging capacity (IC50 value of 21.49 ± 1.04 μg/ml) as compared to that exhibited by the standard butylated hydroxyl toluene (BHT) (IC50 value of 20.41 ± 0.05 μg/ml). Such prominent antioxidative potential was further reinforced by a phenolic content of 39.26 ± 0.85 mg of gallic acid equivalent per gram of extract. The plant extract, at the dose of 400 mg/kg body weight, reduced castor oil-induced diarrhea in mice model by a statistically significant (p &lt; 0.05) margin of 47.62%, while the standard loperamide produced 66.67% reduction of diarrheal feces. The central and peripheral analgesic activities of the crude methanol extract of V. farnesiana (MEVF) was determined by tail flick- and acetic acidinduced writhing methods, respectively, in Swiss albino mice. In the tail flick method, oral administration of MEVF at doses of 200 and 400 mg/kg body weight exhibited 221.09 and 237.09% elongation of pain response time, respectively, after 90 minutes of administration whereas the standard morphine effectuated 518.34% elongation within the same time. Furthermore, the same doses of the extract illustrated 63.27 and 69.39% reductions, respectively, in the acetic acid-induced abdominal constrictions in mice. Compared to the standard acetylsalicylic acid with 75.51% inhibition, statistically significant (p &lt; 0.05) peripheral analgesic activity was established. The results of the present investigations suggest that methanol extract of V. farnesiana possesses antioxidant, antidiarrheal and analgesic activities which eventually indicates the presence of biologically important phytoconstituents within the plant that needs further exploration. Bangladesh Pharmaceutical Journal 23(2): 181-186, 2020

Bioactivities of Stixis suaveolens (Roxb.) Fruit Extract: An Evaluation in Mice Model

The fruits of Stixis suaveolens (Roxb.) have been a popular folk medicine among traditional practitioners. However, there are questions about its traditional uses due to lack of scientific evidence. This study was aimed to evaluate the effects of crude methanol extract of fruits of S. suaveolens in mice model. The central and peripheral analgesic activity were evaluated using the ‘tail flick’ and ‘writhing’ assay respectively. The anti-hyperglycemic potential was assessed by the ability of the crude extract in reducing blood glucose level in mice after oral administration of glucose. Oral administration (400 mg/kg bw) of the extract showed significant (p&lt;0.001) delay in pain sensation and inhibition of acetic acid induced writhing response in mice model. The results were compared with the respective standard morphine (2 mg/kg bw) and diclofenac (50 mg/kg bw). Likewise, in anti-hyperglycemic assay, maximum reduction (p&lt;0.001) of blood glucose level (39.6%) was observed 120 min after oral intake (400 mg/kg bw) of the extract as compared that exhibited by the standard drug, glibenclamide (46.83%). The in vivo bioassays confirmed that the crude methanolic extract of fruits of S. suaveolens possesses significant central- and peripheral-analgesic as well as anti-hyperglycemic activities. These findings justify its popularity as a traditional medicine and hence demands future study involving isolation and characterization of its bioactive compounds. Bangladesh Pharmaceutical Journal 23(2): 135-140, 2020

Antidiarrheal and Analgesic Activities of Bouea oppositifolia (Roxb.) Adelb. in Experimental Animal Model

The current study was designed to evaluate the antidiarrheal and analgesic activities of the methanol extract of Bouea oppositifolia (Roxb.) Adelb. leaves through iv vivo studies in Swiss Albino mice. Oral administration of the extract at doses of 200- and 400-mg/kg of body weight demonstrated statistically significant (p &lt; 0.05) antidiarrheal activities in castor oil-induced diarrheal mice. The extracts and standard loperamide alleviated diarrhea by margins of 31.82-, 45.45- and 68.17%, respectively. Potential of the plant extract to effectuate analgesia was ascertained both centrally and peripherally. In tail immersion method for the determination of central analgesic activity, the plant extract at both doses enhanced pain tolerance to maximum extents of 192.76% and 221.09%, respectively, compared to standard morphine (419.57%) after 90 minutes of sample administration. Comparable levels of central analgesia were also observed for both doses of the plant extracts at 30 and 60 minutes of pharmacological intervention and the p value of less than 0.05 illustrated statistical significance of the activity. On a similar note, potent peripheral analgesic activities were observed for both doses of the extract as evident by 45.45- and 54.55% inhibitions of acetic acid induced writhing responses, respectively. Compared to the standard acetylsalicylic acid characterized by 78.18% inhibition, the peripheral analgesic activity of the plant was found to be statistically significant (p &lt; 0.05). The results of the study are indicative of the presence of potentially bioactive phytoconstituents with antidiarrheal and analgesic properties which might lead to newer drug candidates in future. Bangladesh Pharmaceutical Journal 23(2): 167-171, 2020

Analgesic, Antidiarrheal and CNS-depressant Activities of Flemingia macrophylla (Willd.)

Plants are the priceless sources of bioactive natural compounds. Medicinal plants have been used since time immemorial in both developing and developed countries. Flemingia macrophylla (Willd.) is widely used as a hereditary medicines. The current study was designed to observe the analgesic, antidiarrheal and CNS depressant activities of methanol extract of the leaves of F. macrophylla (MEFM) and its petroleum ether (PEFM), dichloromethane (DFM), chloroform (CFM) and aqueous (AFM) fractions. The analgesic activities was assessed by acetic acid induced writhing method at doses 200- and 400- mg/kg body weight. The CNS-depressant effect was assayed by phenobarbitone sodium-induced sleeping time test. The anti-diarrheal activity of the extract was evaluated using castor oil-induced diarrhea in mice. The crude extract displayed significant peripheral analgesic activity at both test doses with 56.72- to 59.70-% inhibition of writhing responses, respectively. In CNS-depressant test, the extract revealed its activity in a dose dependent manner. In screening for antidiarrheal activity, the extract exhibited 20.83 and 41.67 % inhibition of defecation at 200- and 400-mg/kg bw, respectively whereas the standard loperamide (50 mg/kg bw) displayed 70.83 % inhibition of defecation. Bangladesh Pharmaceutical Journal 23(2): 141-145, 2020

Synthesis of new ibuprofen hybrid conjugates as potential anti-inflammatory and analgesic agents.

Background: A new set of hybrid conjugates derived from 2-(4-isobutylphenyl)propanoic acid (ibuprofen) is synthesized to overcome the drawbacks of the current non-steroidal anti-inflammatory drugs. Results &methodology: Synthesized conjugates were screened for their anti-inflammatory, analgesic and ulcerogenic properties. Few conjugates were found to have significant anti-inflammatory properties in the carrageenan-induced rat paw edema test, while a fair number of conjugates showed promising peripheral analgesic activity in the acetic acid-induced writhing test as well as central analgesic properties in the in vivo hot plate technique. The newly synthesized conjugates did not display any ulcerogenic liability. Conclusion:In vitro, COX-1 and COX-2 enzyme inhibition studies raveled compound 7e is more selective toward COX-2 compared with ibuprofen.

INVESTIGATING THE ROLE OF NF-κB, COX-1, COX-2, COMT, IL-10, IL-6 AND TNF-α IN MODULATING ANTI-NOCICEPTIVE ACTIVITY OF METHANOLIC EXTRACT OF ENTADA PHASEOLOIDES

Objective: To investigate the analgesic activity of methanolic extract of Entada phaseoloides (MEEP) along with its molecular mechanistic pathway.&#x0D; Methods: Swiss albino female mice and Wistar rats of either sex were administered orally with MEEP extracts (100, 200 and 400 mg/kg) and pentazocine, tramadol and diclofenac sodium, as standard drugs. Following administration, anti-nociceptive activity was evaluated using an acetic acid-induced writhing test, Eddy’s hot plate, and hot water immersion test. Serum was collected for molecular expression of various proteins and genes using Reverse Transcriptase PCR and Western Blotting.&#x0D; Results: Acetic acid writhing test, a frequently used method to assess peripheral analgesic activity, revealed that MEEP reduced peripherally induced pain in a dose-dependent manner. Likewise, Eddy’s hot plate and hot water immersion methods, often implicated for testing central analgesic activities, showed that MEEP is bestowed with the capability to counteract analgesia in a dose and time-dependent manner. Pro-inflammatory cytokines and factors like COX-2, IL-6, TNF-α, and NF-κB that cause inflammatory responses and pain were significantly reduced, suggesting its analgesic and anti-inflammatory potential. This analgesic and the anti-inflammatory role played by MEEP is also supported by the up-regulation of anti-inflammatory cytokine IL-10 and COMT and COX-1 enzyme demonstrated no significant difference between the groups.&#x0D; Conclusion: The study revealed the weak peripheral and potent central analgesic property MEEP by modulating pro-inflammatory and anti-inflammatory pathways.