Distinct roles of two RDL GABA receptors in fipronil action in the diamondback moth (<i>Plutella xylostella</i>)

Li, Ben-Jie; Wang, Kun-Kun; Chen, Dongping; Yan, Ying; Cai, Xuling; Chen, Huimin; Dong, Ke; Lin, Fei; Xu, Hanhong

doi:10.1111/1744-7917.12892

Cited by 16 publications

(25 citation statements)

References 58 publications

(72 reference statements)

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“…xylostella. − While compounds synthesized by scaffold hopping usually possessed the same target as the original compound, − the mechanism of 5a action on insects has not been well elucidated. The γ-aminobutyric acid (GABA) receptor (GABAR) together with the glutamate-gated chloride channel (GluCl) had been identified as the primary molecular targets of fipronil, , and the mutations at 2′ and 6′ positions of the GABAR subunit of resistance to dieldrin (RDL) were associated with fipronil resistance. − However, our bioassay results verified there was no cross-resistance between 5a and fipronil (Table ), which implied that 5a molecularly targets P. xylostella in a way different from fipronil.…”

Section: Introductionmentioning

confidence: 77%

“…The insecticidal activities of 5a and fipronil to P. xylostella were measured with the leaf dip method as described previously . Mortality was recorded after 48 h.…”

Section: Methodsmentioning

confidence: 99%

“…The PxRdl1 and PxRdl2 were cloned from the cDNA of susceptible and field-collected strains in the previous study . The full-length open reading frame of PxGluCl (GenBank no.…”

Section: Methodsmentioning

confidence: 99%

“… a GZ and FZ strains are two field-collected strains and show 1686- and 953-fold fipronil resistance, respectively b Lower case letters (a to c) indicate the significance between different strains.…”

Section: Introductionmentioning

confidence: 99%

“… a GZ and FZ strains are two field-collected strains and show 1686- and 953-fold fipronil resistance, respectively …”

Section: Introductionmentioning

confidence: 99%

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Mode of Action of Novel Pyrazoloquinazoline on Diamondback Moth (Plutella xylostella) Ligand-Gated Chloride Channels

Yan

Yao

et al. 2023

J. Agric. Food Chem.

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In our previous study, a series of novel pyrazoloquinazolines were synthesized. Pyrazoloquinazoline 5a showed high insecticidal activity against the diamondback moth (Plutella xylostella) and no cross-resistance to fipronil. Patch clamp electrophysiology performed on P. xylostella pupae brains and two-electrode voltage clamp electrophysiology performed on Xenopus Laevis oocytes indicated that 5a might act on the ionotropic γ-aminobutyric acid (GABA) receptor (GABAR) and glutamate-gated chloride channel (GluCl). Moreover, 5a's potency on PxGluCl was about 15-fold higher than on fipronil, which may explain why there was no cross-resistance between 5a and fipronil. Downregulation of the PxGluCl transcription level significantly enhanced the insecticidal activity of 5a on P. xylostella. These findings shed light on the mode of action of 5a and provide important insights into the development of new insecticides for agricultural applications.

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Section: Introductionmentioning

confidence: 77%

“…The insecticidal activities of 5a and fipronil to P. xylostella were measured with the leaf dip method as described previously . Mortality was recorded after 48 h.…”

Section: Methodsmentioning

confidence: 99%

“…The PxRdl1 and PxRdl2 were cloned from the cDNA of susceptible and field-collected strains in the previous study . The full-length open reading frame of PxGluCl (GenBank no.…”

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“… a GZ and FZ strains are two field-collected strains and show 1686- and 953-fold fipronil resistance, respectively …”

Section: Introductionmentioning

confidence: 99%

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Mode of Action of Novel Pyrazoloquinazoline on Diamondback Moth (Plutella xylostella) Ligand-Gated Chloride Channels

Yan

Yao

et al. 2023

J. Agric. Food Chem.

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CRISPR/Cas9‐mediated D472N substitution in the Rdl1 of Plutella xylostella confers low resistance to abamectin

Hua

Zhu

Liang

et al. 2022

Pest Management Science

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Background: Abamectin is one of the main insecticides used for the control of Plutella xylostella, a destructive pest of cruciferous crops. Target-site mutation plays an important role in insecticide resistance. A point mutation (D472N) has been reported in the Rdl1 γ-aminobutyric acid receptor (GABAR) in P. xylostella, but its roles in insecticide resistance remain unknown.Results: In this study, the D472N mutation of the Rdl1 GABAR was detected in several field populations of P. xylostella and showed a positive correlation with abamectin resistance. A knock-in homozygous mutation strain (D472N-KI) of P. xylostella was successfully constructed using CRISPR/Cas9 coupled with homology-directed repair, and the bioassay results demonstrated that compared with the susceptible strain, the D472N-KI strain had 11.1-and 3.7-fold increased resistance to abamectin and endosulfan, respectively. There was no difference in resistance to fipronil, broflanilide or isocycloseram, which also target the GABAR. In addition, the total fecundity of the D472N-KI strain was significantly reduced by 50.0%. Conclusion:Our results suggest that the homozygous D472N mutation in Rdl1 confers a low level of resistance to abamectin in P. xylostella but causes significant fecundity disadvantages, which may delay the development of resistance to some extent. These results lay a foundation for further understanding the mechanisms of abamectin resistance in insect pests.

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Design, synthesis, and biological activity of novel spiro‐pyrazolo[1,5‐a]quinazolines derivatives as potential insecticides

Yao

Wang

et al. 2022

Pest Management Science

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BACKGROUND: Arylpyrazole insecticides display broad-spectrum insecticidal activity against insect pests. However, the high toxicity toward honeybees associated with fipronil prohibits its agronomic utility. To explore reducing the toxicity of aryl pyrazole analogs to bees, a series of new spiro-pyrazolo[1,5-a]quinazoline derivatives were designed and synthesized. RESULTS: Bioassay results showed that these compounds exhibited good insecticidal activity. In particular, the insecticidal activity of compound 5f against Plutella xylostella larvae (median lethal contentration, LC 50 = 1.43 mg L −1 ) was equivalent to that of fipronil. Moreover, some compounds also showed good insecticidal activity against Solenopsis invicta. Importantly, the bee toxicity study confirmed that compound 5f had much lower acute oral toxicity, with a median lethal dose (LD 50 ) = 1.15 ∼g bee −1 that was three to four orders of magnitude greater than that of fipronil (0.0012 ∼g bee −1 ). Electrophysiological studies were conducted using honeybee γ-aminobutyric acid receptor heterologously expressed in Xenopus oocytes to explain the reduced bee toxicity of compound 5f. The inhibitory effect of compound 5f (16.29 ∼mol L −1 ) was determined to be approximately 700-fold lower than that of fipronil (0.023 ∼mol L −1 ).CONCLUSION: These spiro-pyrazolo[1,5-a]quinazoline derivatives could be potential candidates and lead structures for the discovery of novel insecticides with low bee toxicity.

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Distinct roles of two RDL GABA receptors in fipronil action in the diamondback moth (Plutella xylostella)

Cited by 16 publications

References 58 publications

Mode of Action of Novel Pyrazoloquinazoline on Diamondback Moth (Plutella xylostella) Ligand-Gated Chloride Channels

Mode of Action of Novel Pyrazoloquinazoline on Diamondback Moth (Plutella xylostella) Ligand-Gated Chloride Channels

CRISPR/Cas9‐mediated D472N substitution in the Rdl1 of Plutella xylostella confers low resistance to abamectin

Design, synthesis, and biological activity of novel spiro‐pyrazolo[1,5‐a]quinazolines derivatives as potential insecticides

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