Isocoumarin-based inhibitors of pancreatic cholesterol esterase
نویسندگان
چکیده
منابع مشابه
A new synthesis of fully phosphorylated flavones as potent pancreatic cholesterol esterase inhibitors.
Five flavones possessing one to four phenolic groups were fully phosphorylated efficiently and the obtained compounds showed excellent pancreatic cholesterol esterase (CEase) inhibitory activities with IC(50) in the nanomolar range, which were much more potent than their parent compounds. The inhibition mechanism and kinetic characterization studies indicate that they are irreversible competiti...
متن کاملDiscovery of potential pancreatic cholesterol esterase inhibitors using pharmacophore modelling, virtual screening, and optimization studies.
Pancreatic cholesterol esterase (CEase) is a serine hydrolase involved in the hydrolysis of variety of lipids and transport of free cholesterol. In this study, pharmacophore hypotheses based on known inhibitors were generated using common feature pharmacophore generation protocol available in Discovery Studio program. The best pharmacophore model containing two hydrogen bond acceptor and three ...
متن کاملPlant sterol and stanol substrate specificity of pancreatic cholesterol esterase.
Consumption of plant sterols or stanols (collectively referred to as phytosterols) and their esters results in decreased low-density lipoprotein cholesterol, which is associated with decreased atherosclerotic risk. The mechanisms by which phytosterols impart their effects, however, are incompletely characterized. The objective of the present study is to determine if pancreatic cholesterol ester...
متن کاملPurification and properties of pancreatic juice cholesterol esterase.
Rat pancreatic juice cholesterol ester hydrolase (EC 3.1.1.13) has been purified 600-fold by sequential precipitation with 35 % acetone, diethylaminoethyl cellulose chromatography, and hydroxylapatite chromatography. The purified enzyme gives a single band on polyacrylamide disc electrophoresis and will not hydrolyze methyl butyrate, triolein, or secondary alcohol esters. Data are presented tha...
متن کاملManometric assay and properties of pancreatic cholesterol esterase.
It has long been known that enzymically catalysed synthesis and hydrolysis of cholesterol esters occurs in the presence of certain tissues (Kondo, 1910a, b; Schultz, 1912; Cytronberg, 1912; Gardner & Lander, 1913; Mueller, 1916a, b; Porter, 1916; Nomura, 1924a, b; Shope, 1928; Nedswedski, 1935, 1936; Klein, 1939; Sperry, 1935; Sperry & Stoyanoff, 1937, 1938). The most extensive recent studies, ...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2008
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2008.03.016