An Overview on the Methods of Screening Antiobesity Activity

Danilae George; Y  Jyothi

doi:10.18579/jpcrkc/2016/15/2/88727

Article

An Overview on the Methods of Screening Antiobesity Activity

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Journal of Pharmaceutical Research

DOI: 10.18579/jpcrkc/2016/15/2/88727

Year: 2016, Volume: 15, Issue: 2, Pages: 38-44

Original Article

An Overview on the Methods of Screening Antiobesity Activity

Danilae George 1*, Y. Jyothi 2

Krupanidhi College of Pharmacy, No 12/1, Carmelaram Post, Chikka Bellandur, Varthur Hobli, Bengaluru, Karnataka - 560035, India
Dept. of Pharmacology, Krupanidhi College of Pharmacy, Bangalore - 560 035, India

This work is licensed under a Creative Commons Attribution 4.0 International License.

Abstract

Purpose: The incidence of obesity around the world continues to increase and is considered a major cause of morbidity and mortality through various diseases. Various animal models can be used for the study of various compounds for the discovery of a novel treatment for the obesity. It can range from food intake studies in lean rodents to studies in obese animals due to high fat diet. The use of these animals helps us to determine whether the weight loss is due to fat loss or due to changes in other parameters. Various behavioral models can be used to study the food intake pattern and the effect of the drug on that pattern. These animal models have very good predictive validity as the effect of the drug on the animal models form the basis for the effect of the drug in humans. The drug induced weight loss in humans can be predicted to an extent from the studies carried out on these animal models.Approach: The published articles from Pubmed and other standard resources are used to study, review and compile the overview on screening methods used in Anti-obesity activity.Findings: The animal models of obesity can be used to study about the effects of parameters like insulin level, resistance and leptin levels in obesity. Acute and chronic feeding studies can be carried out. While studying about anti-obesity drugs the factors that lead to weight gain has to be considered.Conclusion: The obesity can be genetic or may be due to some other reason. The common cause for obesity is food intake with high calories and fat. So diet induced obese animal models are an important part of the studies. The animal models for the drug induced weight gain helps in the study of the effect of antiobesity drugs on the drug induced weight gain. All these models have been found to have utility in predicting the weight loss in obesity in man.

References

National institute of health: Clinical Guidelines on the Identification, Evaluation, and Treatment of Overweight and Obesity in adults- The Evidence Report.Ode Res.1998;6(2):2209-51.

Li S, Zhang HY, Hu CC, Lawrence F, Gallagher KE, Surapaneni A,Estrem ST, et al. Assessment of diet-induced obese rats as an obesity model by comparative functional genomics. Obesity. 2008 April;16(4):811-8.

Apfelbaum M, Vague P, Ziegler O, Hanotin C, Thomas F, Leutenegger E. Long-term maintenance of weight loss after a very-lowcalorie diet: a randomized blinded trial of the efficacy and tolerability of sibutramine.Am J Med. 1999 Feb;106(1):179-84.

Clapham JC, Arch JRS. Thermogenic and metabolic antiobesity drugs: rationale and opportunities. Diabetes ObesMetab. 2007 May;9(3):259-75.

Bradbury MJ, Campbell U, Giracello D, Chapman D, King C, Tehrani L et al. Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J PharmacolExpTher.2005;313:395-402.

Benoit SC, Air EL, Wilmer K, Messerschmidt P, Hodge KM, Jones MB et al.Two novel paradigms for the simultaneous assessment of conditioned taste aversion and food intake effects of anorexic agents.PhysiolBehav.2003;79:761-6.

Elangbam CS. Review paper: current strategies in the development of anti-obesity drugs and their safety concerns. Vet Pathol. 2009 Jan;46(1):1024.

Halford JCG, Boyland EJ, Blundell JE, Kirkham TC, Harrold JA.Pharmacological management of appetite expression in obesity. Nat Rev Endocrinol.2010 May;6(5):255-69.

Clegg DJ, Benoit SC, Fisher ME, Barrera JG, Seeley RJ, Woods SC. Sex hormones determine body fat distribution and sensitivity to adiposity signals.Appetite.2003 Sep;52(1)324-40.

Clegg DJ, Riedy CA, Smith KA, Benoit SC, Woods SC. Differential sensitivity to central leptin and insulin in male and female rats. Diabetes. 2003 Mar;52(3):682-7.

Buettner R., Scholmerich J. and Bollheimer L.C. High-fat diets: modelingthe metabolic disorders of human obesity in rodents. Obesity (Silver Spring) 2007 April;15(4):798-808.

Warden CH, Fisler JS.Comparisons of diets used in animal models of high-fat feeding. Cell Metab. 2008;7(4):277.

Fisas A, Codony X, Romero G, Dordal A, Giraldo J, Merce R et al. Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats. Br J Pharmacol.2006;148(1):973-83.

Jackson HC, Pleasance IM, Mitchell JM, Heal DJ. Observational analysis of the effects of sibutramine, phentermine and aminorex on food intake in rats.Obes.2000;8(1):95.

Jackson HC, Cheetham SC, Gregory PC, Antel J. Effect of chronic administration of topiramate and phentermine, alone and in combination, in an animal model of dietary-induced obesity. 629.15. Neuroscience. 2007 Program No 629.15 Neuroscience Meeting Planner, Society for Neuroscience:San Diego, CA.Online.

Moore BJ. Cafeteria diet-an inappropriate tool for studies of thermogenesis. J Nutr1987 Feb;117(2):227-31.

Kris-Etherton PM, Dietschy J. Design criteria for studies examining individual fatty acid effects on cardiovascular disease risk factors: human and animal studies.Am J ClinNutr.1997;165(1):15906.

Harrold JA, Widdowson PS, Clapham JC, Williams G. Individual severity of dietary obesity in unselected Wistar rats: relationship with hyperphagia. Am J PhysiolEndocrinolMetab. 2000;279(2):340-7.

Mutch DM, Cl�ment K. Unraveling the genetics of human obesity. PloS Genet. 2006 Dec;2(12):188.

Hegsted, DM, McGandy, RB, MyersML, StareFJ. Quantitative effects of dietary fat on serum cholesterol in man. Am J ClinNutr1965 Nov;17(5):281-95.

Plump AS, Smith JD, Hayed T. Severe hypercholesterolemia and atherosclerosis in apolipoprotein E-deficient mice created by homologous recombination in ES cells. Cell, 1992 Oct 16;71(2):343-53.

Warden CH., Fisler JS. Comparisons of diets used in animal models of high-fat feeding. Cell Metab2008 April;7(4):277.

Zhang Y, Proenca R, Maffei M, Barone M, Leopold L, Friedman JM.Positional cloning of the mouse obese gene and its humanhomologue. Nature 1994 Dec 1;372(6505):425�32.

Mohapatra J, Sharma M, Singh S, Pandya G, Chatterjee A, Balaraman R et al. Involvement of adipokinesinrimonabant-mediated insulin sensitivityinob/obmice.JPharmPharmacol2009 Nov;61(11):1493-8

Vickers SP, Webster LJ, Wyatt A, Dourish CT, Kennett GA. Preferential effects of the cannabinoid CB1 receptor antagonist, SR141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats. Psychopharmacology (Ber l) 2003 Mar 11;167:103-11.

Su W, Guo Z, Randall DC, Cassis L, Brown DR, Gong MC.Hypertension and disrupted blood pressure circadian rhythm intype 2 diabetic db/db mice. Am J Physiol Heart CircPhysiol2008 Oct;295(4):1634-41.

Heal et al. Metabolic consequences of antipsychotic therapy: preclinical and clinical perspectives on diabetes, diabetic ketoacidosis, and obesity. In: Current Antipsychotics, HandbExpPharmacol, G Gross and MA Geyer (Eds), Springer,2012;212:135-64.

Maffei M, Halaas J, Ravussin E, Pratley RE, Lee GH, Zhang Y et al. Leptin levels in human and rodent: measurement of plasmaleptin and ob RNA in obese and weight-reduced subjects. Nat Med1995 Nov;1(11):1155-61.

Montague CT, Farooqi IS, Whitehead JP, Soos MA, Rau H, Wareham NJ et al. Congenital leptin deficiency is associated with severe early-onset obesity in humans. Nature. 1997 Jun 26;387(6636):903-8.

Harrold JA, Widdowson PS, Clapham JC, Williams G. Individual severity of dietary obesity in unselected Wistar rats: relationship with hyperphagia. Am J PhysiolEndocrinolMetab 2000;279(2):340-7.

Halford JCG, Boyland EJ, Blundell JE, Kirkham TC, Harrold JA.Pharmacological management of appetite expression in obesity. Nat Rev Endocrinol2010 May;6(5):255-69

Hansen DL, Toubro S, Stock MJ, Macdonald IA, AstrupA. The effect of sibutramine on energy expenditure and appetite during chronic treatment without dietary restriction. Int J ObesRelatMetabDisord1999 Oct 23;23(10): 1016-24

Halford JC, Wanninayake SC, Blundell JE. Behaviouralsatiety sequence (BSS) for the diagnosis of drug action on food intake. PharmacolBiochemBehav1998 Oct;61(2):15968.

Antin J, Gibbs J, Holt J, Young RC, Smith GP.Cholecystokinin elicits the complete behavioral sequence of satiety in rats. J Comp PhysiolPsychol1975 Sep;89(7):784-90.

Takeda N, Hasegawa S, Morita M, Matsunaga T. Pica in rats is analogous to emesis: an animal model in emesis research. PharmacolBiochemBehav1993 Aug;45(4):817-21.

Takeda N, Hasegawa S, Morita M, Horii A, Uno A, Yamatodani A, et al. Neuropharmacological mechanisms of emesis. I. Effects of antiemetic drugs on motion- and apomorphine-induced pica in rats. Methods Find ExpClinPharmacol. 1995;17(9):589-96.

Zlot A, Newell A, Silvey K, Arail K. Addressing the obesity epidemic: a genomics perspective. Prev Chronic Dis 2007;4:1-6.

Mao P. Recent advances in obesity: genetics and beyond. ISRN Endocrinology 2012 march 5;2012.

Paquot N, De Flines J, Rorive M.Obesity:a model of complex interactions between genetics and environment]. Revue m�dicale de Li�ge 2012;67(5-6):332-36.

Arita Y, Kihara S, Ouchi N, Takahashi M, Maeda K, Miyagawa J-i, et al.Paradoxical decrease of an adipose-specific protein, adiponectin, in obesity. BiochemBiophys Res Commun 1999 April 2;257(1):79-83.

Bouchard L, Tchernof A, Deshaies Y, Marceau S, Lescelleur O, Biron S. ZFP36: a promising candidate gene for obesity-related metabolic complications identified by converging genomics. ObesSurg 2007 Mar;17(3):372-82.

Gutierrez-Aguilar R, Kim DH, Woods SC, Seeley RJ. Expression of new loci associated with obesity in diet induced obese rats: from genetics to physiology.Obesity 2012 Feb;20(2):306-12.

Rask-Andersen M. Obesity Genetics: Functional of Four Genetic Loci Associated with Obesity and Body Mass [Dissertation]. ActaUniversitatisUpsaliensis. Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Medicine 2013;921:48.

Ores ie M. Obesity and psychotic disorders: uncovering common mechanisms through metabolomics.Dis Model Mech 2012;5:614-20.

Zhang A, Sun H, Wang X.Power of metabolomics in biomarker discovery and mining mechanisms of obesity.Obes Rev 2013;14:344-49.

Welthagen W, Shellie RA, Spranger J, Ristow M, Zimmermann R, Fiehn O. Comprehensive twodimensional gas chromatography�time-offlight mass spectrometry (GC� GC-TOF) for high resolution metabolomics: biomarker discovery on spleen tissue extracts of obese NZO compared to lean C57BL/6 mice.Metabolomics 2005;1:65-73.

Kirkwood JS, Legette LL, Miranda CL, Jiang Y, Stevens JF.A metabolomics driven elucidation of the anti-obesity mechanisms of xanthohumol. J Biol Chem.2013 jun;288(26):19000-13.

Wahl S, Holzapfel C, Yu Z, Breier M, Kondofersky I, Fuchs C, et al. Metabolomics reveals determinants of weight loss during lifestyle intervention in obese children. Metabolomics 2013:1-11.

Renes J, Mariman E. Application of proteomics technology in adipocyte biology. MolBioSyst 2013 jun;9(6):1076-91.

Hittel DS, Hathout Y, Hoffman EP.Proteomics and systems biology in exercise and sport sciences research.Exerc Sport Sci.2007;35(1):5-11.

Peral B, Camafeita E, Fern�ndez-Real J-M, L�pez JA. Tackling the human adipose tissue proteome to gain insight into obesity and related pathologies. Expert Rev Proteomics 2009;6:35361.

Kim OY, Shin M-J, Moon J, Chung JH. Plasma ceruloplasmin as a biomarker for obesity: a proteomic approach. ClinBiochem 2011;44:35156.

Tvarijonaviciute A, Gutierrez A, Miller I, RazzaziFazeli E, Tecles F, Ceron J.A proteomic analysis of serum from dogs before and after a controlled weightloss program. DomestAnimEndocrin 2012;43(4):271-77.

Moest H, Frei AP, Bhattacharya I, Geiger M, Wollscheid B, Wolfrum C. Malfunctioning of adipocytes in obesity is linked to quantitative surfaceome changes. BiochimBiophysActa 2013;1831(7):1208-16.