Specific Synergist for Neonicotinoid Insecticides: IPPA08, a cis-Neonicotinoid Compound with a Unique Oxabridged Substructure.
Insecticide synergists are key components to increase the control efficacy and reduce active ingredient use. Here, we describe a novel insecticide synergist with activity specific for insecticidal neonicotinoids. The synergist IPPA08, a cis configuration neonicotinoid compound with a unique oxabridged substructure, could increase the toxicity of most neonicotinoid insecticides belonging to the Insecticide Resistance Action Committee (IRAC) 4A subgroup against a range of insect species, although IPPA08 itself was almost inactive to insects at synergistic concentrations. Unfortunately, similar effects were observed on the honey bee (Apis mellifera) and the brown planthopper (Nilaparvata lugens), resistant to imidacloprid. IPPA08 did not show any effects on toxicity of insecticides with different targets, which made us define it as a neonicotinoid-specific synergist. Unlike most insecticide synergists, by inhibition of activities of detoxification enzymes, IPPA08 showed no effects on enzyme activities. The results revealed that IPPA08 worked as a synergist through a distinct way. Although the modulating insect nicotinic acetylcholine receptors (nAChRs, targets of neonicotinoid insecticides) were supposed as a possible mode of action for IPPA08 as a neonicotinoid-specific synergist, direct evidence is needed in further studies. In insect pest control, IPPA08 acts as a target synergist to increase neonicotinoid toxicity and reduce the amount of neonicotinoid used. Combinations of IPPA08 and insecticidal neonicotinoids may be developed into new insecticide formulations. In summary, combining an active ingredient with a "custom" synergist appears to be a very promising approach for the development of effective new insecticide products.
Key Laboratory of Integrated Management of Crop Diseases and Pests (Ministry of Education), College of Plant Protection, Nanjing Agricultural University , Weigang 1, Nanjing, Jiangsu 210095, People's Republic of China.
Haibo
H
Bao
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology , Meilong Road 130, Shanghai 200237, People's Republic of China.
Xusheng
X
Shao
Key Laboratory of Integrated Management of Crop Diseases and Pests (Ministry of Education), College of Plant Protection, Nanjing Agricultural University , Weigang 1, Nanjing, Jiangsu 210095, People's Republic of China.
Yixi
Y
Zhang
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology , Meilong Road 130, Shanghai 200237, People's Republic of China.
Yayun
Y
Deng
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology , Meilong Road 130, Shanghai 200237, People's Republic of China.
Xiaoyong
X
Xu
Key Laboratory of Integrated Management of Crop Diseases and Pests (Ministry of Education), College of Plant Protection, Nanjing Agricultural University , Weigang 1, Nanjing, Jiangsu 210095, People's Republic of China.
Zewen
Z
Liu
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology , Meilong Road 130, Shanghai 200237, People's Republic of China.
Zhong
Z
Li
D000691:Anabasine / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001516:Bees / Q000187:drug effects; D004357:Drug Synergism; D006430:Hemiptera / Q000187:drug effects; D007305:Insecticide Resistance; D007306:Insecticides / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D013237:Stereoisomerism
D007306:Insecticides; D000691:Anabasine
detoxification enzyme; insecticide synergist; neonicotinoid; nicotinic acetylcholine receptors