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2006:93908 BIOSIS
DN
PREV200600097036
TI
Specific inhibition of hormone-sensitive lipase improves lipid profile while reducing plasma glucose.
AU
Claus, Thomas H.; Lowe, Derek B.; Liang, Yin; Salhanick, Arthur I.; Keiper Lubeski, Christine; Yang, Ling; Lemoine, Lynn; Zhu, Jian; Clairmont, Kevin B. [Reprint Author]
CS
Bayer Res Ctr, Dept Metab Disorders Res, 400 Morgan Lane, West Haven, CT 06516 USA kevin.clairmont.b@bayer.com
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Journal of Pharmacology and Experimental Therapeutics, (DEC 2005) Vol. 315, No. 3, pp. 1396-1402. http://www.jpet.org. CODEN: JPETAB. ISSN: 0022-3565.
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Article
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English
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Entered STN: 1 Feb 2006 Last Updated on STN: 1 Feb 2006
AB
Elevation of plasma free fatty acids has been linked with insulin resistance and diabetes. Inhibition of lipolysis may provide a mechanism to decrease plasma fatty acids, thereby improving insulin sensitivity. Hormone-sensitive lipase (HSL) is a critical enzyme involved in the hormonally regulated release of fatty acids and glycerol from adipocyte lipid stores, and its inhibition may thus improve insulin sensitivity and blood glucose handling in type 2 diabetes. In rat adipocytes, forskolin-activated lipolysis was blocked by in vitro addition of a potent and selective HSL inhibitor or by prior treatment of the animals themselves. Antilipolytic effects also were demonstrated in overnight-fasted mice, rats, and dogs with species-dependent effects on plasma free fatty acid levels but with similar reductions in plasma glycerol being observed in all species. Inhibition of HSL also reduced hyperglycemia in streptozotocin-induced diabetic rats. The data support a connection between adipose tissue lipolysis and plasma glucose levels.
CC
Cytology - Animal 02506 Biochemistry studies - General 10060 Biochemistry studies - Carbohydrates 10068 Enzymes - General and comparative studies: coenzymes 10802 Pathology - Therapy 12512 Metabolism - Metabolic disorders 13020 Blood - Blood and lymph studies 15002 Blood - Blood cell studies 15004 Endocrine - General 17002 Endocrine - Pancreas 17008 Pharmacology - General 22002 Toxicology - General and methods 22501
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Major Concepts Pharmacology; Enzymology (Biochemistry and Molecular Biophysics); Endocrine System (Chemical Coordination and Homeostasis)
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Parts, Structures, & Systems of Organisms plasma: blood and lymphatics
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Diseases insulin resistance syndrome: endocrine disease/pancreas, metabolic disease Insulin Resistance (MeSH)
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Diseases type 2 diabetes: endocrine disease/pancreas, metabolic disease, drug therapy, chemically-induced Diabetes Mellitus, Non-Insulin-Dependent (MeSH)
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Chemicals & Biochemicals glucose; glycerol; streptozotocin; hormone-sensitive lipase: inhibition; hormone-sensitive lipase inhibitor: enzyme inhibitor-drug
ORGN
Classifier Canidae 85765 Super Taxa Carnivora; Mammalia; Vertebrata; Chordata; Animalia Organism Name dog (common): breed-beagle, male Taxa Notes Animals, Carnivores, Chordates, Mammals, Nonhuman Vertebrates, Nonhuman Mammals, Vertebrates
ORGN
Classifier Muridae 86375 Super Taxa Rodentia; Mammalia; Vertebrata; Chordata; Animalia Organism Name Wistar rat (common): male rat (common): strain-Sprague-Dawley, male mouse (common): strain-Balb/C, male 3T3-L1 cell line (cell_line): murine adipocyte cells Taxa Notes Animals, Chordates, Mammals, Nonhuman Vertebrates, Nonhuman Mammals, Rodents, Vertebrates
RN
58367-01-4 (glucose) 56-81-5 (glycerol) 18883-66-4 (streptozotocin) 9001-62-1 (hormone-sensitive lipase)