DOI: http://dx.doi.org/10.18203/2319-2003.ijbcp20182676

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

Maliha Niroomand, Kalpana U. Shah, Balasaheb B. Ghongane

Abstract


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.


Keywords


Anti-inflammatory activity, Analgesic activity, Anti-pyretic activity, N-Benzoyl Isoserine Methyl Ester (N-bime), Toxicity profile

Full Text:

PDF

References


Bielefeldt K, Davis B, Binion DG. Pain and inflammatory bowel disease. Inflamm Bowel Dis. 2009;15:778-88.

Amaya-Amaya J, Botello-Corzo D, Calixto OJ, Calderón-Rojas R, Domínguez AM, Cruz-Tapias P, et al. Usefulness of patients-reported outcomes in rheumatoid arthritis focus group. Arthritis. 2012 Sep 28;2012.

Grosser T, Smyth Emer, Fitzgerald GA. Anti-inflammatory, Antipyretic and Analgesic agents; Pharmacotherapy of Gout. In: Brunton LB, Chabner BA, Knollman BC, eds. Goodman and Gilman’s The Pharmacological Basis of Therapeutics. 12th ed. Newyork, NY: Mc Graw Hill;2011:959-1004.

Wani MC, Taylor HL, Wall HE, Coggon P, McPhail AT. Plant anti-tumor agents Ⅵ. The isolation and structure of taxol, a novel anti-leukemic and anti-tumor agent from Taxus brevifolia. J Am Chem Soc, 1971: 2325-2327. Cited in: Banerjee A, Hamberger B. P450s controlling metabolic bifurcations in plant terpene specialized metabolism. Phytochem Rev. 2018;17(1):81-111.

Denis JN, Correa A, Greene EA. An improved synthesis of the Taxol side chain and of RP56976. J Org Chem. 1989;55:1957-9.

Ghosh MN. Fundamentals of Experimental Pharmacology. 6th Ed. Hilton and company, Calcutta; 2015:1-287.

Ratheesh M, Helen A. Anti-inflammatory activity of Ruta graveolens Linn on carrageenan induced paw edema in wistar male rats. African J of Biotech. 2007;6(10):1209-11.

Buttle GAH, D’Arcy PF, Howard EM, Kellett DN. Plethysmometric measument of swelling in the feet of small laboratory animals. Nature; 1957:179:629.

Bourget P, Delouis JM. Review of a technique for the estimation of area under the concentration curve in pharmacokinetic analysis. France. Therapie. 1993;48:1-5.

Romay C, Ledo´n N, Gonza´lez R. Further studies on anti-inflammatory activity of phycocyanin in some animal models of inflammation. Inflamm Res. 1998;47:334-8.

Gawade SP. Acetic acid induced painful endogenous infliction in writhing test on mice. J of Pharma and Pharmacoth. 2012;3(4):348.

Loux JJ, DePalma PD, Yankell SL. Anti-pyretic testing of Aspirin in rats. Toxic Appl Pharmac. 1972;22:672-5.

Adams SS, McCullough KF, Nicholson JS. The pharmacological properties of ibuprofen, an anti-inflammatory, analgesic and antipyretic agent. Arch Intern Pharmacodyn. 1969;178(1):115-29.

Kulkarni SD. Statistic in Medical Research. In Souvenir, Sixth Annual Conference of The Pharmacologists of Maharashtra. Dept. of Pharmacology, B.J. Medical College, Pune. 1980;44-65.