In vitro and in vivo inhibitory actions of morin on rat brain phosphatidylinositolphosphate kinase activity
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AbstractPhosphatidylinositol-4,5-bisphosphate occupies a central ro le in signal transduction and in cellular transformation. Phosphatidylinositol-4,5-bisphosphate is produced by the enzymatic phosphorylation of phosphatidylinositol-4-phosphate by phosphatidylinositolphosphate kinase (EC Inhibition of this enzyme might conceivably lowers the cellular pool of phosphatidylinositol-4,5-bisphosphate, thus constituting a feasible control point in regulating signal transduction and cellular transformation. Morin, a plant flavonoid, was demonstrated to exhibit in vitro inhibitory action on phosphatidylinositolphosphate kinase extracted from rat brain. This inhibition of enzymatic activity was found to be dose-dependent, with an IC50 value of approximately 10 mu M morin. Lineweaver-Burk transformation of the inhibition data indicates that inhibition was competitive with respect to ATP. The Ki was calculated to be 5.15x10(-6)M. Inhibition was uncompetitive with respect to phosphatidylinositol-4-phosphate. The Ki was determined to be 0.94 x 10(-5)M. Administration of morin to rats led to a decrease in phosphatidylinositolphosphate kinase activity in brain extracts. This in vivo action of morin was found to be dose-dependent and time-dependent. These effects of morin on rat brain phosphatidylinositolphosphate kinase activity are discussed in relation to the other reported biological actions of this flavonoid.
All Author(s) ListCheng CHK
Journal nameLife Sciences
Volume Number61
Issue Number20
Pages2035 - 2047
LanguagesEnglish-United Kingdom
Keywordsflavonoid; morin; phosphatidylinositolphosphate kinase
Web of Science Subject CategoriesMedicine, Research & Experimental; MEDICINE, RESEARCH & EXPERIMENTAL; Pharmacology & Pharmacy; PHARMACOLOGY & PHARMACY; Research & Experimental Medicine

Last updated on 2020-12-10 at 01:11