scholarly journals Screening of N-Benzoyl Isoserine Methyl Ester (N-bime) for anti-inflammatory analgesic activity and toxicity profile in animals

2018 ◽  
Vol 7 (7) ◽  
pp. 1319
Author(s):  
Maliha Niroomand ◽  
Kalpana U. Shah ◽  
Balasaheb B. Ghongane
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Methyl Ester ◽  
Analgesic Activity ◽  
Dose Range ◽  
Biological Data ◽  
Toxicity Profile ◽  
National Chemical Laboratory ◽  
Tail Pinch ◽  
Anti Inflammatory

Background: Pain and inflammation are the basic processes involved in the pathogenesis of many diseases. Non-steroidal anti-inflammatory drugs are often used to treat rheumatic diseases. The study compound N-Benzoyl Isoserine Methyl Ester (N-bime) is a newly synthesized propionic acid derivative by National Chemical Laboratory, Pune. Since the biological data of this compound is not available, the present study has been planned to screen this compound for anti-inflammatory, analgesic activity and its toxicity profile in animals.Methods: Single dose toxicity study was carried out in rats. Anti-inflammatory activity was tested by Rat Hind Paw Oedema and Cotton Pellet Implantation method. For Analgesic activity, Acetic acid induced writhing and Tail Pinch method was used. Yeast induced Pyrexia was used for evaluation of anti-pyretic activity. Ibuprofen was the positive control. Data are presented as mean±SEM. Statistical analysis was performed by analysis of variance and students unpaired‘t’ test.Results: The test compound N-bime did not show any apparent adverse effects or mortality in the dose range 1mg - 500mg / 100gm body weight in animals. It showed better anti-inflammatory actions in higher doses as compared to Ibuprofen (p˂ 0.05). In acetic acid induced writhing test N-bime offered better protection against writhes, than Ibuprofen. But, both failed to demonstrate analgesic activity in the Tail Pinch method. N-bime showed a gradual decrease in temperature in the anti-pyretic test (P<0.001).Conclusions: The present study indicates that N-bime does possess anti-inflammatory, analgesic and weak anti-pyretic properties like the NSAIDs. It has proved to be safe in the dose range of 1mg - 500mg / 100gm body weight in rats and mice.

scholarly journals Characterization of fluoroquinolone-induced Achilles tendon toxicity in rats: comparison of toxicities of 10 fluoroquinolones and effects of anti-inflammatory compounds.

1997 ◽  
Vol 41 (11) ◽  
pp. 2389-2393 ◽  
Author(s):  
Y Kashida ◽  
M Kato
Keyword(s):  
Nitric Oxide ◽  
Body Weight ◽  
Methyl Ester ◽  
Achilles Tendon ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
High Dose ◽  
Juvenile Rats ◽  
Anti Inflammatory

Fluoroquinolone antibacterial agents have been reported to induce tendon lesions in juvenile rats. In the present study, we characterized fluoroquinolone-induced Achilles tendon lesions by comparing the effects of 10 fluoroquinolones and examining the potential of one of these antimicrobial agents, pefloxacin, to induce tendon lesions when coadministered with one of nine anti-inflammatory compounds. Among the 10 fluoroquinolones tested, fleroxacin and pefloxacin were the most toxic, inducing lesions at a dose of 100 mg/kg of body weight or more, while lomefloxacin, levofloxacin, and ofloxacin or sparfloxacin and enoxacin induced lesions at 300 mg/kg or more and 900 mg/kg, respectively. In contrast, norfloxacin, ciprofloxacin, and tosufloxacin had no effect even at the high dose of 900 mg/kg. The severity of the Achilles tendon lesions appeared to correlate with the structure of the substituent at the seventh position. Furthermore, pefloxacin-induced tendon lesions were inhibited by coadministration with dexamethasone and N-nitro-L-arginine methyl ester. Phenidone (1-phenyl-3-pyrazolidinone) and 2-(12-hydroxydodeca-5,10-diynyl)3,5,6-trimethyl-1,4-benzoqui none (AA861) also decreased the incidence of tendon lesions. In contrast, catalase, dimethyl sulfoxide, indomethacin, pyrilamine, and cimetidine did not modify these tendon lesions. These results suggest that nitric oxide and 5-lipoxigenase products partly mediate fluoroquinolone-induced tendon lesions.

The Role of Andrographolide in Andrographis paniculata as a Potential Analgesic for Herbal Medicine based Drug Development

2021 ◽  
pp. 6269-6274
Author(s):  
Lidya Tumewu ◽  
Irfan Rayi Pamungkas ◽  
Hilkatul Ilmi ◽  
Achmad Fuad Hafid ◽  
Indah Setyawati Tantular ◽  
...  
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Herbal Medicine ◽  
Drug Development ◽  
Analgesic Activity ◽  
Active Ingredient ◽  
Active Substance ◽  
Ethanol Extract ◽  
Positive Control ◽  
Andrographis Paniculata

Background: Andrographis paniculata is a herbaceous plant in the Acanthaceae family, that is widely used as a traditional medicine in Asian countries and known to exhibit a wide range of pharmacological effects. Recent studies have provided an overview of the great potential of A. paniculata as an analgesic. The ethanol extract and ethyl acetate (EA) fraction of A.paniculata were shown to contain diterpene lactone compounds, which may be useful as a potential active ingredient in analgesic drugs. The development of a herbal medicine based drug requires an effective and high quality active ingredient. Therefore, this research was aimed to compare the analgesic activity of ethanol extract and EA fraction based on their andrographolide content and further to determine the more viable active substance for analgesic herbal medicine based drug development. Method: The andrographolide content in the ethanol extract and EA fraction was determined by High Pressure Liquid Chromatography (HPLC). Measurement of analgesic activity was performed by writhing test. The experimental animals were randomly divided into eight groups consisting of 5 mice in each. Group 1 (negative control) received 1% Tween-80 in normal saline. Group 2 (positive control) received a standard analgesic drug (diclofenac sodium) at a dose of 40 mg/kg body weight. Group 3, 4, and 5 received ethanol extract while Group 6, 7, and 8 received EA fraction, each at a dose of 12.5, 25, and 50 mg andrographolide/kg body weight, respectively. Each mouse was injected intraperitoneally with 1% acetic acid at a dose of 10 ml/kg body weight 30 minutes after oral administration of the treatments. The number of writhes were counted 5 min after acetic acid injection over a period of 45 min. Results: Andrographolide content in ethanol extract and EA fraction was 15.66±0.28 and 21.25±1.08 % w/w, respectively. Ethanol extract and EA fraction displayed analgesic activity of 67.68% and 70.91% respectively, at a dose of 50 mg andrographolide/kg body weight. The positive control at a dose of 40 mg/kg body weight showed an analgesic activity of 74.33%. Statistical analysis showed no significant differences between EA fraction at a dose of 50 mg andrographolide/kg body weight and ethanol extract at the same dose as well as the positive control (P> 0.05). The effective dose 50% (ED50) of the ethanol extract and EA fraction was determined to be 29.49 and 25.55 mg/kg body weight, respectively. Conclusion: It was possible to use andrographolide content as an indicator for the analgesic activity of A.paniculata. Ethanol extract and EA fraction of A. paniculata at the same dose of andrographolide showed similar analgesic activity. The amount of ethanol extract which needed to reach similar analgesic activity was higher than EA fraction. Therefore, EA fraction likely has greater potential as an analgesic active substance due to its higher content of andrographolide; however further study is needed to develop it as a dosage form.

scholarly journals In vivo and in vitro pharmacological activities of Tacca integrifolia rhizome and investigation of possible lead compounds against breast cancer through in silico approaches

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Shahriar Ahmed ◽  
Ahmed Rakib ◽  
Md. Ashiqul Islam ◽  
Bibi Humayra Khanam ◽  
Farhana Binta Faiz ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Acetic Acid ◽  
Molecular Docking ◽  
Analgesic Activity ◽  
In Silico ◽  
Antineoplastic Activity ◽  
Paw Edema ◽  
Writhing Test ◽  
Antipyretic Activity ◽  
Anti Inflammatory

Abstract Background The study was conducted to evaluate the analgesic, anti-inflammatory, antipyretic properties of ethanolic extract of Tacca integrifolia rhizome (EETI) in mice and cytotoxic effects in brine shrimp nauplii followed by a PASS prediction study for some isolated compounds of T. integrifolia. Additionally, this experiment included the in silico molecular docking and ADME/T property analyses of some phytochemicals. Methods Formalin- induced paw licking test and acetic acid-induced writhing test for analgesic activity, carrageenan-induced paw edema test for anti-inflammatory potential and Brewer’s yeast-induced pyrexia test for antipyretic activity were applied. Antinociceptive and antineoplastic activity for breast cancer were revealed with PASS program. Schrodinger suite 2015 was used to evaluate the binding interaction and ADME/T properties of selected phytoconstituents with estrogen receptor alpha. Results In formalin-induced paw licking test, EETI at the doses of 200 and 400 mg/kg BW showed highly significant inhibition of writhing in both neurogenic and inflammatory phases. While EETI also exhibited highly significant, compared to control, writhing inhibition for both the doses in acetic acid-induced writhing test. Moderate anti-inflammatory effect at a dose of 400 mg/kg BW was noticed in paw-edema test. It also showed 77.51% of maximum antipyretic effect which was significantly effective compared to standard drug paracetamol (150 mg/kg) in Brewer’s yeast-induced pyrexia test. The EETI showed potential cytotoxic activity with LC50 value of 114.46 μg/mL. The PASS prediction revealed the potential antinociceptive and antineoplastic activity of target compounds. The compounds betulinic acid, quercetin-3-α-arabinoside, catsanogenin were found to be effective in molecular docking study. Conclusion It is evident that the EETI possesses highly significant analgesic activity with remarkable anti-inflammatory and antipyretic activity. The phytoconstituents have potential antinociceptive and antineoplastic (breast cancer) activity. Graphical abstract

scholarly journals Evaluation of Analgesic and Anti-inflammatory Activities of Polyalthia simiarum (Hook. F. &Thomson)

2019 ◽  
Vol 5 (1) ◽  
pp. 18-23
Author(s):  
Selina Kabir ◽  
Ronok Zahan ◽  
Abdullah Mohammad Sarwaruddin Chowdhury ◽  
Choudhury Mahmood Hasan ◽  
Mohammad Abdur Rashid
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Biological Activities ◽  
Dependent Manner ◽  
Paw Edema ◽  
Immersion Method ◽  
Ongoing Research ◽  
Tail Immersion ◽  
Anti Inflammatory ◽  
Dose Dependent

Background: Polyalthia simiarum (Hook. F. &Thomson) exhibits different effects in human body. Objective: As a part of ongoing research on medicinal plants of Bangladesh, the present study is focused to investigate the analgesic and anti-inflammatory activities of stem bark of Polyalthia simiarum (Annonaceae). Methodology: The ethyl acetate (EA) and petroleum ether (PE) extracts were subjected to qualitative chemical investigation for the identification of different phytoconstituents. The analgesic activity was determined for its central and peripheral pharmacological actions using tail immersion method and acetic acid-induced writhing test. The anti-inflammatory activity was evaluated by carrageenan induced paw edema in rats. Analgesic and anti-inflammatory data were evaluated statistically analysed by Dunnett’s-T test. Result: Both extracts at the dose of 50- and 100 mg/kg b.w., produced significant increase in pain threshold in tail immersion method whereas significantly reduced the writhing caused by acetic acid in a dose dependent manner. The EA and PE extracts showed anti-inflammatory activities at 50- and 100 mg/kg body weight. Among all the extracts, the EA extract showed a dose dependent and comparable analgesic activity in all the tested methods and also reduced the paw edema considerably (27.5% and 39.1% inhibition after 4h), in dose dependent manner when compared to carrageenan induced control rat. Conclusion: Therefore, the EA and PE extracts of Polyalthia simiarum were capable to exhibit moderate analgesic and anti-inflammatory activities. This is the first report of analgesic and anti-inflammatory potential of Polyalthia simiarum and can be further investigated to isolate the active compounds responsible for the biological activities. Journal of National Institute of Neurosciences Bangladesh, 2019;5(1): 18-23

scholarly journals Analgesic and Antidiarrheal Activities of Leaf of Podocarpus neriifolius D. Don

2016 ◽  
Vol 19 (2) ◽  
pp. 215-218
Author(s):  
Md Rahatullah Razan ◽  
Muhammed Mahfuzur Rahman ◽  
Faiza Tahia ◽  
Md Khalid Hossain ◽  
Mohammad A Rashid
Keyword(s):  
Body Weight ◽  
Acetic Acid ◽  
Analgesic Activity ◽  
Castor Oil ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Pharmaceutical Journal ◽  
Activity Assay ◽  
Swiss Albino Mice

The methanol extract of leaf of Podocarpus neriifolius D. Don exhibited in vivo peripheral analgesic and antidiarrheal activities in Swiss Albino mice. In the peripheral analgesic activity assay, the methanolic extract showed 50.00 ± 8.57% and 70.25 ± 1.18% inhibition of acetic acid-induced writhing at 200 and 400 mg/kg body weight, respectively. In addition, the extract also revealed a dose dependant inhibition of castor oil- induced diarrhea with 43.77 ± 3.13% and 56.23 ± 6.49% inhibition of feces at 200 and 400 mg/kg body weight, respectivelyBangladesh Pharmaceutical Journal 19(2): 215-218, 2016

Cassiaindoline, a New Analgesic and Anti-Infl ammatory Alkaloid from Cassia alata

2009 ◽  
Vol 64 (5-6) ◽  
pp. 335-338 ◽  
Author(s):  
Irene M. Villaseñor ◽  
Arlyn C. Sanchez
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Indole Alkaloid ◽  
Inflammatory Activity ◽  
Cassia Alata ◽  
Spectroscopic Analyses ◽  
Anti Inflammatory

Cassiaindoline is a new dimeric indole alkaloid isolated from Cassia alata L. leaves whose structure was elucidated through spectroscopic analyses. It exhibited analgesic activity at a dosage of 125.0 mg/kg mouse and decreased the number of writhings induced by acetic acid by 49.4%. It also showed a 57.1% anti-inflammatory activity at a dosage of 75 mg/kg mouse

Evaluation of the Anti-Inflammatory and Analgesic Activities of the Total Saponins Extracted from Fermented Polygala japonica Houtt

2013 ◽  
Vol 641-642 ◽  
pp. 931-934
Author(s):  
Ming Xing Liu ◽  
Ting Zhu ◽  
She Ne Guo ◽  
Hong Da Zhu
Keyword(s):  
Experimental Study ◽  
Acetic Acid ◽  
Vascular Permeability ◽  
Analgesic Activity ◽  
Inflammatory Activity ◽  
Hot Plate ◽  
Plate Models ◽  
Anti Inflammatory ◽  
Analgesic Activities

This study was to investigate the anti-inflammatory and analgesic activities of the total saponins extracted from fermented Polygala japonica Houtt (FPH) compared with that of unfermented Polygala japonica Houtt (UFPH). The total saponins extracted from FPH and UFPH were evaluated for anti-inflammatory activity in xylene-induced ear swelling and acetic acid-induced vascular permeability models in mice, analgesic activity in acetic acid-induced writhing and hot plate models in mice. The total saponins extracted from FPH had the significant anti-inflammatory (p<0.001) and analgesic (p<0.01) activities with the doses of 6 g/kg b.w. in mice. The results of this experimental study thus strongly support the potential significant use of the total saponins extracted from FPH for pain and inflammatory.

scholarly journals Assessment of Analgesic, Anti-Inflammatory And Anti-Pyretic Activities of Malva Neglecta Wallr. In Animal Model

2021 ◽  
Vol 50 (3) ◽  
pp. 577-583
Author(s):  
Rahma Hamayun ◽  
Muhammad Shahid Iqbal ◽  
Muhammad Imran Qadir
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Aqueous Ethanol ◽  
Mice Model ◽  
Hot Plate ◽  
Standard Drug ◽  
Antipyretic Activity ◽  
Ethanolic Extracts ◽  
Anti Inflammatory ◽  
Ethanol Extracts

Analgesic, anti-inflammatory and anti-pyretic activities of n-hexane and aqueous ethanolic extracts of Malva neglecta in Swiss albino mice was evaluated. For each activity, the mice were divided into 4 groups: Group 1 served as control, Groups 2 and 3 were given n-hexane and aqueous ethanol extracts, respectively whereas Group 4 was treated with the standard drug. Analgesic activity was evaluated against acetic acid induced writhing, Eddy's hot plate method, and Formalin induced paw licking. Anti-inflammatory activity was evaluated by carrageenan-induced paw edema. The extracts were also examined for their anti-pyretic activities against yeast-induced pyrexia. Results showed that the n-hexane (p < 0.05) and aqueous ethanolic (p < 0.005) extracts of M. neglecta exhibited analgesic activity by reducing acetic acid-induced writhing, mean reaction time on hot plate model and formalin-induced paw licking in mice as compared to the control. The n-hexane extract (p < 0.05) as well as aqueous ethanolic (p < 0.005) extracts produced significant antiinflammatory activity as compared to the control. Both the n-hexane and aqueous ethanolic extracts revealed significant antipyretic activity (p < 0.005 and p < 0.05, respectively) in mice model. The results of the present study demonstrated that the n-hexane and aqueous ethanol extracts of M. neglecta possess analgesic, antiinflammatory and anti-pyretic activities. Bangladesh J. Bot. 50(3): 577-583, 2021 (September)

scholarly journals “EVALUATION OF GALPHIMIA GLAUCA STEM METHANOL EXTRACT FRACTIONS FOR ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES”

2019 ◽  
pp. 266-272
Author(s):  
GARIGE BABA SHANKAR RAO ◽  
SRISAILAM K ◽  
V UMA MAHESHWARA RAO ◽  
VASUDHA B
Keyword(s):  
Acetic Acid ◽  
Methanol Extract ◽  
Dose Range ◽  
Experimental Studies ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Methanol Fraction ◽  
Cotton Pellet ◽  
Anti Inflammatory

Objective: This current investigation assesses in vivo central and peripheral analgesic effects and anti-inflammatory properties of fractions obtained from Galphimia glauca (GG) stem methanol extract. Methods: The laboratory models such as Swiss albino mice and Wistar albino rats were employed in the studies. The GG stem methanol extract was subjected to fractionation with solvents such as hexane, chloroform, ethyl acetate, and methanol. Orally, the dose range of 100, 200, and 400 mg/kg was given for 1 day for evaluating analgesic (hotplate test, tail clip test, writhing test, and formalin test) and weekdays for assessing anti-inflammatory activity (carrageenan and cotton pellet test methods), respectively. The experimental studies were further conducted for determining the involvement of central and peripheral receptor actions in the analgesic activity of the extract by prechallenging it with naloxone and acetic acid, respectively. The in vivo anti-inflammatory studies were conducted using carrageenan-induced rat paw edema model and cotton pellet granuloma test. Results: The LD50 of the extract was found to be >2000 mg/kg b.w. The methanol fraction of 400 mg/kg dose exhibited significant (p≤0.001) and dose-dependent analgesic and anti-inflammatory activity. It also exhibited central and peripheral analgesic actions when treated with naloxone and acetic acid, respectively. Conclusion: The results revealed that the stem methanol fraction has more potential in terms of analgesic and anti-inflammatory properties.

Sign in / Sign up

Export Citation Format

Share Document