Afidopyropen: New and potent modulator of insect transient receptor potential channels

Kandasamy, Ramani A.; London, D. O.; Stam, Lynn F.; Deyn, Wolfgang von; Zhao, Xilong; Salgado, Vincent L.; Nesterov, Alexandre

doi:10.1016/j.ibmb.2017.03.005

Cited by 101 publications

(74 citation statements)

References 18 publications

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“…Kandasamy et al [10] investigated the mode of action of chordotonal organ modulators on TRP channels, but both flonicamid and TFNA-AM were inactive on this target. A number of metabolizing enzymes and neurological receptors have been ruled out as targets of flonicamid [12], and…”

Section: Accepted Manuscriptmentioning

confidence: 99%

“…In the most recent classification, flonicamid was re-classified to group 29, to which it is the lone member and mode of action is linked to chordotonal organ modulation, but 'the specific target protein(s) responsible for biological activity are distinct from Group 9 and remain undefined' [9]. A recent paper by Kandasamy et al [10] investigated the mode of action of chordotonal organ modulators on TRP channels, but both flonicamid and TFNA-AM were inactive on this target. Morita et al…”

Section: Introductionmentioning

confidence: 99%

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Toxicity, mode of action, and synergist potential of flonicamid against mosquitoes

Taylor-Wells

Gross

Jiang

et al. 2018

Pesticide Biochemistry and Physiology

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The present study focused on the toxicity of the aphid anti-feedant flonicamid and its main metabolite, 4-trifluoromethylnicotinamide (TFNA-AM) to Aedes aegypti and Anopheles gambiae mosquitoes.The compounds were toxic to both species via topical application, resulting in un-coordinated locomotion and leg splaying, with a favorable An. gambiae LD 50value of 35 ng/mg for TFNA-AM, but no significant lethality to Ae. aegypti at 10 μg/female.There was mild cross resistance in the Akron-kdr (Akdr) strain of An. gambiae. Both compounds were non-toxic to intact larvae (LC 50 >300 ppm); however, headless Ae. aegypti larvae displayed spastic paralysis, with PC 50 values of 2-4 ppm, indicating that the cuticle is a significant barrier to penetration. TFNA-AM showed low mammalian toxicity, with an LD 50 of >2000 mg/kg in mice. Electrophysiological experiments showed larval Aedes muscle depolarization and Kv2 channel blocking activity that required near mM concentrations, suggesting that this potassium channel is not the main target for flonicamid nor its metabolite.However, TFNA-AM was a potent blocker of evoked body wall sensory discharge in dipteran larvae, suggesting that some component of the chordotonal organ system may be involved in its toxicity. Finally, flonicamid and TFNA-AM showed about 2-fold synergism of permethrin toxicity against An. gambiae adult females whose mechanism should become more clear once the mode of action of these compounds is better defined.

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Section: Accepted Manuscriptmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Toxicity, mode of action, and synergist potential of flonicamid against mosquitoes

Taylor-Wells

Gross

Jiang

et al. 2018

Pesticide Biochemistry and Physiology

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“…This insecticide is a semi‐synthetic derivative of a fermentation product called pyripyropene, which is produced by the microbe Aspergillus fumigatus Fresenius (Eurotiales: Trichocomaceae) . Afidopyropen acts on the vanilloid‐type transient receptor potential (TRPV) channels of the chordotonal stretch receptor neurons of insects . Chordotonal receptors serve a mechanosensory role in insects by detecting movement at articulations .…”

Section: Introductionmentioning

confidence: 99%

Efficacy of afidopyropen against soybean aphid (Hemiptera: Aphididae) and toxicity to natural enemies

Koch

Queiroz

Aita

et al. 2019

Pest Management Science

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BACKGROUND Soybean aphid, Aphis glycines (Hemiptera: Aphididae), remains the most significant soybean insect pest in the North Central Region of the USA. The sustainability of reliance on only a few insecticide groups for this pest is questionable. We evaluate afidopyropen, a novel pyropene insecticide (Group 9D), for efficacy against A. glycines in field and greenhouse experiments and toxicity to common natural enemies in laboratory experiments. RESULTS Across 4 site‐years of field experiments and a greenhouse experiment, afidopyropen reduced A. glycines populations similar to commonly used broad‐spectrum [i.e. lambda‐cyhalothrin (Group 3A) and chlorpyrifos (Group 1B)] insecticides and potential selective insecticides [i.e. sulfoxaflor (Group 4C) and flupyradifurone (Group 4D)]. In the greenhouse, however, A. glycines mortality was delayed slightly for afidopyropen compared to the other insecticides. In laboratory experiments with natural enemies of A. glycines, afidopyropen was not toxic to adult or third instar Hippodamia convergens (Coleoptera: Coccinellidae) or adult Orius insidiosus (Hemiptera: Anthocoridae), and was only moderately toxic to Aphelinus certus (Hymenoptera: Aphelinidae). CONCLUSION Afidopyropen is effective against A. glycines and relatively non‐toxic to natural enemies, and appears to be an effective option for integrated pest management and insecticide resistance management programs for A. glycines. © 2019 Society of Chemical Industry

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“…Afidopyropen is a new potent and specific modulator of insect transient receptor potential vanilloid (TRPV) cation channels, exhibiting unique binding (Kandasamy et al 2017;Nilius and Owsianik 2011). It is derived from natural products (Jeschke 2017;Leichter et al 2013).…”

mentioning

confidence: 99%

“…The insecticidal activity of chordotonal organ TRPV channel modulators is likely related to species selectivity at the target level and the importance of chordotonal organs for insect survival. Their mode of action involves stimulating heterologously expressed transient receptor potential channels that act by targeting nanchung (NAN) and inactive (INA) proteins (Kandasamy et al 2017). Afidopyropen is a semi-synthetic analog of pyropropen, and was developed to target sap-feeding insects such as the pea aphid Acyrthosiphon pisum Harris (Hemiptera: Aphididae) by causing mortality through starvation and desiccation (Gerwick and Sparks 2014;Leichter et al 2013).…”

mentioning

confidence: 99%

Susceptibility of Asian citrus psyllid, Diaphorina citri (Hemiptera: Liviidae), to the insecticide afidopyropen: a new and potent modulator of insect transient receptor potential channels

2018

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A relatively new insecticide chemistry for controlling sucking insects, afidopyropen, was investigated for toxicity against Asian citrus psyllid, Diaphorina citri Kuwayama (Hemiptera: Liviidae). We evaluated the mortality of D. citri eggs, nymphs, and adults treated with afidopyropen using both laboratory-reared and field populations. We also quantified the effects of sublethal doses of afidopyropen on D. citri feeding, host choice selection, and fecundity. For laboratory susceptible adults, the contact LC 50 , topical application LD 50 , and leaf dip LC 50 were 2.13, 2.00, and 3.08 ng/µL, respectively. For adults collected from a commercially managed citrus grove in Florida, the contact LC 50 , topical application LD 50 , and leaf dip LC 50 were 1.37, 1.92, and 4.89 ng/µL, respectively. Egg hatch was significantly reduced following exposure to afidopyropen at 100 ng/µL. Furthermore, afidopyropen reduced D. citri nymph survival and adult emergence at concentrations ranging between 0.01 and 100 ng/µL. Diaphorina citri adult feeding decreased on citrus leaves treated with afidopyropen in a concentration-dependent manner as measured indirectly by honeydew excretion, and appeared almost completely inhibited after treatment with 10 and 100 ng/µL solutions of afidopyropen. In choice tests, significantly fewer D. citri adults settled on afidopyropen-treated plants than on control plants at 24, 48, and 72 h after release, with no differences in settling between males and females. Afidopyropen reduced the fecundity of D. citri in a concentration-dependent manner. Collectively, the results suggest that afidopyropen could contribute to the integrated management of D. citri and may therefore be useful in rotational programs to improve resistance management.

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Afidopyropen: New and potent modulator of insect transient receptor potential channels

Cited by 101 publications

References 18 publications

Toxicity, mode of action, and synergist potential of flonicamid against mosquitoes

Toxicity, mode of action, and synergist potential of flonicamid against mosquitoes

Efficacy of afidopyropen against soybean aphid (Hemiptera: Aphididae) and toxicity to natural enemies

Susceptibility of Asian citrus psyllid, Diaphorina citri (Hemiptera: Liviidae), to the insecticide afidopyropen: a new and potent modulator of insect transient receptor potential channels

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