title: Modulatory effects of natural curcuminoids on P-glycoprotein ATPase of insecticide-resistant pest Helicoverpa armigera (Lepidopetera: Noctüidae).
abstract: Three major curcuminoids (I, II and III) were purified from turmeric and tested for their ability to modulate the function of P-glycoprotein ATPase of the insecticide-resistant pest Helicoverpa armigera (Ha-Pgp). The curcumin mixture inhibited the activity of Ha-Pgp ATPase by 80-90% at 100 μM concentration. Along with curcuminoids I, II and III, it inhibited the verapamil- and ethylparaoxon-stimulated Ha-Pgp ATPase activity. Curcuminoid binding was quantitated by quenching the intrinsic Trp fluorescence of purified Ha-Pgp ATPase. Transport was monitored in proteoliposomes containing Ha-Pgp ATPase using the high-affinity fluorescent substrate tetramethylrosamine (TMR) in real time. Addition of the curcuminoid mixture collapsed the TMR concentration gradient generated by Ha-Pgp ATPase. Inhibition studies on Ha-Pgp ATPase activity are important to develop strategies to overcome insecticide resistance in this pest.
authors.affiliation: Department of Biochemistry, Gulbarga University, Gulbarga, Karnataka, India.
authors.forename: Ravindra M
authors.initials: RM
authors.lastname: Aurade
authors.forename: Senigala K
authors.initials: SK
authors.lastname: Jayalakshmi
authors.forename: Kuruba
authors.initials: K
authors.lastname: Sreeramulu
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000251:Adenosine Triphosphatases / Q000378:metabolism*; D000818:Animals; D030024:Curcuma / Q000737:chemistry*; D003474:Curcumin / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D007305:Insecticide Resistance / Q000187:drug effects / Q000502:physiology*; D009036:Moths / Q000187:drug effects / Q000378:metabolism*; D010936:Plant Extracts / Q000494:pharmacology*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D010936:Plant Extracts; D000251:Adenosine Triphosphatases; D003474:Curcumin
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