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