Modulatory Effects of Natural Curcuminoids on P-Glycoprotein ATPase of Insecticide-Resistant Pest Helicoverpa armigera (Lepidopetera: Noctuidae)
Modulatory Effects of Natural Curcuminoids on P-Glycoprotein ATPase of Insecticide-Resistant Pest Helicoverpa armigera (Lepidopetera: Noctuidae)
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DOI：
10.1007/s00232-010-9299-5
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发表时间：
2010-08-01
影响因子：
2.4
通讯作者：
Sreeramulu, Kuruba
中科院分区：
文献类型：
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作者：
Aurade, Ravindra M.;Jayalakshmi, Senigala K.;Sreeramulu, Kuruba
从姜黄中分离纯化了3个主要的姜黄素类化合物(I、II和III)，并研究了它们对抗药性棉铃虫P-糖蛋白ATPase功能的调节作用。姜黄素合剂在100mM浓度下对Ha-PGP-ATPase活性的抑制率为80-90%。与姜黄素I、II和III一起，它能抑制维拉帕米和乙基对氧磷刺激的Ha-PGP ATPase活性。通过猝灭纯化的Ha-PGP ATPase的本征Trp荧光来定量姜黄素的结合。使用高亲和力荧光底物四甲基罗胺(TMR)实时监测含有Ha-PGP ATPase的蛋白脂质体的转运。姜黄素混合物的加入降低了Ha-PGP ATPase产生的TMR浓度梯度。对Ha-PGP ATPase活性的抑制研究对于制定克服该害虫抗药性的策略具有重要意义。
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 mu M 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.