Document Detail

PEGylation of cholecystokinin prolongs its anorectic effect in rats.
MedLine Citation:
PMID:  17379357     Owner:  NLM     Status:  MEDLINE    
The anorectic compound CCK-9 was coupled to polyethylene glycol 5 kDa, 10 kDa, 20 kDa and 30 kDa, under different reaction conditions. Conjugates were purified by HPLC and characterized by MALDI-TOF MS. A 96% PEGylation yield was obtained in buffer pH 7.5 after 6h reaction at 20 degrees C. The anorectic activity was tested in vivo in rats. A single bolus intra-peritoneal injection of non-modified CCK-9 resulted in a significant initial food intake reduction 30 min after food presentation (87% compared to paired control group). When PEG-CCK-9 conjugates modified with polymers of molecular weight up to 20 kDa were injected, lower but statistically significant initial food intake reductions were obtained (76% for PEG 10 kDa-CCK-9 conjugate compared to control group). The cumulative food intake reduction of non-modified CCK-9 is normalized within 1-2h, whereas the PEG-CCK-9 molecules showed a prolonged anorectic activity lasting for 6h for PEG 5 kDa-CCK-9; 23 h for PEG 10 kDa-CCK-9 and between 8h and 23 h for PEG 20 kDa-CCK-9. For PEG 30 kDa-CCK-9 conjugate, neither an initial nor a cumulative FI reduction was observed. PEG-CCK-9 conjugates show a significantly prolonged anorectic activity in comparison to the non-modified peptide. This effect is most evident for the PEG 10 kDa-CCK-9 conjugate.
Fabián León-Tamariz; Isabelle Verbaeys; Maurits Van Boven; Marcel De Cuyper; Johan Buyse; Elke Clynen; Marnix Cokelaere
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-02-15
Journal Detail:
Title:  Peptides     Volume:  28     ISSN:  0196-9781     ISO Abbreviation:  Peptides     Publication Date:  2007 May 
Date Detail:
Created Date:  2007-05-02     Completed Date:  2007-08-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8008690     Medline TA:  Peptides     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1003-11     Citation Subset:  IM    
Laboratory of Toxicology and Bromatology, Faculty of Pharmaceutical Sciences, Katholieke Universiteit Leuven, Leuven, Belgium.
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MeSH Terms
Anorexia / chemically induced,  physiopathology
Cholecystokinin / administration & dosage,  chemistry,  pharmacology*
Chromatography, High Pressure Liquid
Chromatography, Thin Layer
Drug Stability
Eating / drug effects*,  physiology
Injections, Intraperitoneal
Molecular Structure
Molecular Weight
Peptide Fragments / administration & dosage,  chemistry,  pharmacology*
Polyethylene Glycols / administration & dosage,  chemistry,  pharmacology*
Rats, Wistar
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Structure-Activity Relationship
Time Factors
Reg. No./Substance:
0/Peptide Fragments; 0/Polyethylene Glycols; 108050-84-6/cholecystokinin 9; 9011-97-6/Cholecystokinin

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