Inhibition of pancreatic lipase by poloxamer 407 may provide an adjunct treatment strategy for weight loss

Journal of Pharmacy and Pharmacology

Volumn 58, Issue 8, 2006, Pages 1099-1105

  Johnston, Thomas P ^a   Goldberg, Ira J ^b  

^a UNIVERSITY OF MISSOURI KANSAS CITY   (United States)

^b New York Presbyterian Columbia University Medical Center   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DRINKING WATER; LIPID EMULSION; POLOXAMER; TRIACYLGLYCEROL; TRIACYLGLYCEROL LIPASE;

ANIMAL EXPERIMENT; ARTICLE; BODY WEIGHT; CONTROLLED STUDY; DIURESIS; DOSE RESPONSE; ENZYME ACTIVITY; ENZYME INHIBITION; FLUID INTAKE; IC 50; IN VITRO STUDY; LIPID ANALYSIS; LIPID DIET; MALE; MOUSE; NONHUMAN; PALATABILITY; TITRIMETRY; TRIACYLGLYCEROL BLOOD LEVEL; URINE VOLUME; WEIGHT GAIN; WEIGHT REDUCTION;

ANIMALS; ENZYME INHIBITORS; EXCIPIENTS; FAT EMULSIONS, INTRAVENOUS; FATS; FECES; LIPASE; MICE; OBESITY; PANCREAS; POLOXAMER; TASTE; TRIGLYCERIDES; WEIGHT LOSS;

EID: 33747073829     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.58.8.0011     Document Type: Article

References (27)

1. Ackroff, K., Sclafani, A. (1996) Effects of the lipase inhibitor orlistat on intake and preference for dietary fat in rats. Am. J. Physiol. 271: R48-R54
2. Borgstrom, B. (1988) Mode of action of tetrahydrolipstatin: a derivative of the naturally occurring lipase inhibitor lipstatin. Biochim. Biophys. Acta 962: 308-316
3. Bray, G. A. (1985) Obesity: definition, diagnosis, and disadvantages. Med. J. Aust. 142 (Suppl.): S2-S8
4. Bray, G. A. (1993) Use and abuse of appetite-suppressant drugs in the treatment of obesity. Ann. Intern. Med. 119: 707-713
5. Cerulli, J., Lomaestro, B. M., Malone, M. (1997) Update on the pharmacotherapy of obesity. Ann. Pharmacother. 337: 396-407
6. Comai, K., Sullivan, A. C. (1980) Antiobesity activity of pluronic L-101. Int. J. Obes. 4: 33-42
7. Dollinger, L. M., Howell, A. R. (1998) A 2-methyleneoxetane analog of orlistat demonstrating inhibition of porcine pancreatic lipase. Bioorg. Med. Chem. Lett. 8: 977-978
8. Garfinkel, L. (1985) Overweight and cancer. Ann. Intern. Med. 103: 1034-1036
9. Hadvary, P., Lengsfeld, H., Wolfer, H. (1988) Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin. Biochem. J. 256: 357-361
10. Hadvary, P., Sidler, W., Meister, W., Vetter, W., Wolfer, H. (1991) The lipase inhibitor tetrahydrolipstatin binds covalently to the putative active site serine of pancreatic lipase. J. Biol. Chem. 266: 2021-2027
11. Han, L. K., Zheng, Y. N., Yoshikawa, M., Okuda, H., Kimura, Y. (2005) Anti-obesity effects of chikusetsusaponins isolated from Panax japonicus rhizomes. BMC Compliment Alternative Med. 5: 1-10
12. Hogan, S., Fleury, A., Hadvary, P., Lengsfeld, H., Meier, M. K., Triscari, J., Sullivan, A. C. (1987) Studies on the anti-obesity activity of tetrahydrolipstatin, a potent and selective inhibitor of pancreatic lipase. Int. J. Obes. 11 (Suppl. 3): 35-42
13. Johnston, T. P., Palmer, W. K. (1993) Mechanism of poloxamer 407-induced hyper-triglyceridemia in the rat. Biochem. Pharmacol. 46: 1037-1042
14. Lethbridge-Cejku, M., Schiller, J. S., Bernadel, L. (2004) Summary health statistics for U.S. adults: National Health Interview Survey, 2002. Vital Health Stat. 222: 1-151
15. Lookene, A., Skottova, N., Olivecrona, G. (1994) Interactions of lipoprotein lipase with the active-site inhibitor tetrahydrolipstatin (Orlistat). Eur. J. Biochem. 222: 395-403
16. Luthi-Peng, Q., Maerki, H. P., Hadvary, P. (1992) Identification of the active-site serine in human pancreatic lipase by chemical modification with tetrahydrolipstatin. FEBS Lett. 299: 111-115
17. NIH Consensus Statement Covers Treatment of Obesity (1991) Am. Fam. Phys. 44: 305-306
18. Pi-Sunyer, F. X. (1993) Medical hazards of obesity. Ann. Intern. Med. 119: 655-660
19. Roche Pharmaceuticals, Inc. (2003) Complete product information for Xenical® (orlistat) capsules. Technical Report No. 27898691: 1-17
20. Sakata, Y., Ishigure, S., Shimbo, S. (2000) Weight of feces and its daily fluctuations in young women. Part I. A survey of the relation between fecal weight, dietary habits, and life-styles. Nippon Koshu Eisei Zasshi 47: 385-393
21. Smith, G. M., Garton, A. J., Aitken, A., Yeaman, S. J. (1996) Evidence for a multi-domain structure for hormone-sensitive lipase. FEBS Lett. 396: 90-94
22. Ueshima, K., Akihisa-Umeno, H., Nagayoshi, A., Takakura, S., Matsuo, M., Mutoh, S. (2004) A gastrointestinal lipase inhibitor reduces progression of atherosclerosis in mice fed a western-type diet. Eur. J. Pharmacol. 501: 137-142
23. United States National Commission on Diabetes (1975) Report of the National Commission on Diabetes to the Congress of the United States. Bethesda (MD): U.S. Department of Health, Education, and Welfare. Publication No. 76-1021; Vol. 1
24. Van Itallie, T. B. (1985) Health implications of overweight and obesity in the United States. Am. Intern. Med. 103: 983-988
25. Wasan, K. M., Subramanian, R., Kwong, M., Goldberg, I. J., Wright, T., Johnston, T. P. (2003) Poloxamer 407-mediated alterations in the activities of enzymes regulating lipid metabolism in rats. J. Pharm. Pharmaceut. Sci. 6: 108-116
26. Worthington, C. C. (1988) In: Worthington, C.C. (ed.) Worthington enzyme manual. Freehold: Worthington Biochemical Corporation, pp 212-214
27. Wybenga, D. R., Inkpen, J. A. (1974) Lipids. In: Henry, R. J., Cannon, D. C., Winkelman, J. W. (eds) Clinical chemistry. Harper & Row, New York, pp 1475-1482