View source for BIOSIS / 2002:429399

AN   
     2002:429399  BIOSIS
DN   
     PREV200200429399
TI   
     Cyclipostins, Novel hormone-sensitive lipase inhibitors from
     Streptomyces sp. DSM 13381: II. Isolation, structure elucidation and
     biological properties. 
AU   
     Vertesy, Laszlo [Reprint author]; Beck, Bernd; Broenstrup, Mark; Ehrlich,
     Klaus; Kurz, Michael; Mueller, Guenter; Schummer, Dietmar; Seibert,
     Gerhard
CS   
     LG Natural Products Research, H 780, Frankfurt/Main, Germany
     Laszlo.Vertesy@aventis.com
SO   
     Journal of Antibiotics (Tokyo), (May, 2002) Vol. 55, No. 5, pp. 480-494.
     print. 
     CODEN: JANTAJ. ISSN: 0021-8820. 
DT   
     Article
LA   
     English
ED   
     Entered STN: 7 Aug 2002
     Last Updated on STN: 23 Sep 2002
AB   
     Hormone-sensitive lipase (HSL) is a key enzyme of lipid metabolism
     and its control is therefore a target in the treatment of diabetes
     mellitus.  Cultures of the Streptomyces species DSM 13381 have been shown
     to potently inhibit HSL.  Ten inhibitors of HSL, termed cyclipostins,
     have been isolated from the mycelium of this microorganism and a further
     nine related compounds detected.  Their structures were characterized by
     2-D NMR experiments and by mass spectrometry and were found to comprise
     neutral cyclic enol phosphate esters with an additional gamma-lactone
     ring.  On account of their ester-bound fatty alcohol side chain, the
     cyclipostins have physicochemical properties similar to those of
     triglycerides.  The outstanding characteristic of the cyclipostins is
     their strong anti-HSL activity, with IC50 values in the nanomolar range.
CC   
     Biochemistry studies - Lipids   10066
     Pathology - Therapy   12512
     Metabolism - General metabolism and metabolic pathways   13002
     Metabolism - Metabolic disorders   13020
     Endocrine - Pancreas   17008
     Pharmacology - General   22002
     Pharmacology - Endocrine system   22016
     Physiology and biochemistry of bacteria   31000
IT   
     Major Concepts
        Metabolism; Pharmacology
IT   
     Parts, Structures, & Systems of Organisms
        mycelium
IT   
     Diseases
        diabetes mellitus: endocrine disease/pancreas, metabolic disease,
        drug therapy
        Diabetes Mellitus (MeSH)
IT   
     Chemicals & Biochemicals
        cyclic enol phosphate esters; cyclipostins: antidiabetic-drug, enzyme
        inhibitor-drug, biological properties, structure; hormone-sensitive
        lipase; triglycerides
IT   
     Methods & Equipment
        mass spectrometry: Spectrum Analysis Techniques, analytical method;
        two-dimensional NMR: analytical method
IT   
     Miscellaneous Descriptors
        lipid metabolism
ORGN 
     Classifier
        Streptomycetes and Related Genera   08840
     Super Taxa
        Actinomycetes and Related Organisms; Eubacteria; Bacteria;
        Microorganisms
     Organism Name
        Streptomyces sp.: strain-DSM 13381
     Taxa Notes
        Bacteria, Eubacteria, Microorganisms
RN   
     372092-03-0 (CYCLIPOSTINS)