Document Detail


Inhibition of diacylglycerol acyltransferase by betulinic acid from Alnus hirsuta.
MedLine Citation:
PMID:  16534734     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
During the screening for diacylglycerol acyltransferase (DGAT) inhibitors from natural products, the lupane-type triterpenoid betulinic acid was isolated from the methanol extract of Alnus hirsuta. It potently inhibited DGAT in the rat liver microsomes with an IC (50) value of 9.6 microM. Enzyme kinetic studies showed apparent Km and Ki values of 13.3 microM and 8.1 microM using [(14)C]oleoyl-CoA as a substrate. A decrease in the apparent Vmax was observed with betulinic acid, whereas the apparent Km remained constant. Therefore, a Lineweaver-Burk plot of DGAT inhibition by betulinic acid showed a non-competitive type of inhibition. In the cell-based assay, betulinic acid inhibited triglyceride (TG) formation by human HepG2 cells. These findings suggest that betulinic acid may be a potential lead compound in the treatment of obesity.
Authors:
Mi Yeon Chung; Mun-Chual Rho; Seung Woong Lee; Hye Ran Park; Koanhoi Kim; In Ah Lee; Dong Hyun Kim; Kyung Hee Jeune; Hyun Sun Lee; Young Kook Kim
Related Documents :
3519604 - Effect of thiolactomycin on the individual enzymes of the fatty acid synthase system in...
18369234 - Thematic review series: glycerolipids. acyltransferases in bacterial glycerophospholipi...
3875494 - Synthesis of docosahexaenoyl-, arachidonoyl- and palmitoyl-coenzyme a in ocular tissues.
3948404 - An enzymatic method for calibration of serum lipase assays.
422324 - The purification of peptides by partition chromatography based on a hydrophobicity scale.
11767164 - Use of a ruthenium(iii), iron(ii), and nickel(ii) hexacyanometallate-modified graphite ...
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Planta medica     Volume:  72     ISSN:  0032-0943     ISO Abbreviation:  Planta Med.     Publication Date:  2006 Feb 
Date Detail:
Created Date:  2006-03-14     Completed Date:  2006-04-27     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0066751     Medline TA:  Planta Med     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  267-9     Citation Subset:  IM    
Affiliation:
Laboratory of Lipid Metabolism, Korea Research Institute of Bioscience and Biotechnology, Daejon.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Alnus*
Animals
Anti-Obesity Agents / administration & dosage,  pharmacology*,  therapeutic use
Diacylglycerol O-Acyltransferase / antagonists & inhibitors,  drug effects*
Enzyme Inhibitors / administration & dosage,  pharmacology*,  therapeutic use
Humans
Inhibitory Concentration 50
Male
Microsomes, Liver / drug effects,  enzymology
Phytotherapy*
Plant Extracts / administration & dosage,  pharmacology,  therapeutic use
Rats
Rats, Sprague-Dawley
Triterpenes / administration & dosage,  pharmacology*,  therapeutic use
Chemical
Reg. No./Substance:
0/Anti-Obesity Agents; 0/Enzyme Inhibitors; 0/Plant Extracts; 0/Triterpenes; 472-15-1/betulinic acid; EC 2.3.1.20/Diacylglycerol O-Acyltransferase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  New indole N-oxide alkaloids from Evodia fargesii.
Next Document:  Minor alkaloids from Guatteria dumetorum with antileishmanial activity.