Modulation of P-glycoprotein ATPase of Helicoverpa armigera by cholesterol: effects on ATPase activity and interaction of insecticides.

Abstract:

:Purified P-glycoprotein ATPase from Helicoverpa armigera (Ha-Pgp), reconstituted in proteoliposomes composed of phospholipids and cholesterol, shows higher ATPase activity in the presence of cholesterol than in its absence. The Ha-Pgp ATPase activity was increased 30-40% with cholesterol. The KM for ATP was found to be 1 and 0.8 mM in the absence and presence of cholesterol, respectively. The insecticide-stimulated Ha-Pgp ATPase activity was increased by 10-20% for all the insecticides in the reconstituted proteoliposomes containing cholesterol compared to those with no cholesterol. The effects of cholesterol on KM and Vmax values of insecticide-stimulated Ha-Pgp ATPase activity were unrelated to the size of the insecticide. Ha-Pgp tryptophan fluorescence displayed a red shift of 3 and 8 nm in emission spectra upon binding of insecticides. Cholesterol enhances the interaction of insecticides with Ha-Pgp. Kd values of different insecticides for binding to Ha-Pgp were found to be lower in the presence of cholesterol in the proteoliposomes compared to its absence. Results suggest that cholesterol plays a role in the recognition and interaction of insecticides by modulating Ha-Pgp ATPase and may be involved in efflux of insecticides from cells by the transporter.

authors

Aurade RM,Jayalakshmi SK,Udikeri SS,Sreeramulu K

doi

10.1002/arch.21004

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

47-60

issue

1

eissn

0739-4462

issn

1520-6327

journal_volume

79

pub_type

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