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role of dSC1 in drosophila melanogaster synaptic activities in response to haedoxan A

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Insect Science 2023年第6期30卷 1677-1688页

作者： Xingtao Qie Yaxin ren Xueting Chen Yuzhe du Ke dong Zhaonong Hu Institution of pesticide Science College of Plant ProtectionNorthwest A&F UniversityYanglingShaanxi ProvinceChina Key Laboratory of Botanical Pesticide R&D in Shaanxi Province YanglingShaanxi ProvinceChina department of Plant Protection College of Plant ProtectionShanxi Agricultural UniversityTaiguShanxi ProvinceChina Southern Insect Management research Unit Agricultural Research ServiceUnited States Department of AgricultureStonevilleMSUSA department of Biology Duke UniversityDurhamNCUSA key laboratory of Integrated Pest Management on Crops in Northwestern Loess Plateau Ministry of AgricultureNorthwest A&F UniversityYanglingShanxi ProvinceChina

drosophila sodium channel 1 (dSC1) encodes a voltage-gated divalent cation channel that mediates neuronal excitability in insects. Previous research revealed that dSC1 knockout drosophila melanogaster conferred different susceptibility to insecticides, which indicated the vital regulation role of dSC1 under insecticide stress. Haedoxan A (HA) is a lignan compound isolated from Phryma leptostachya, and we found that HA has excellent insecticidal activity and is worthy of further study as a botanical insecticide. Herein, we performed bioassay and electrophysiological experiments to test the biological and neural changes in the larval drosophila with/without dSC1 knockout in response to HA. Bioassay results showed that knockout of dSC1 reduced the sensitivity to HA in both w1118 (a common wild-type strain in the laboratory) and parats1 (a pyrethroid-resistant strain) larvae. Except for parats1/dSC1−/−, electrophysiology results implicated that HA delayed the decay rate and increased the frequency of miniature excitatory junctional potentials of drosophila from w1118, parats1, and dSC1−/− strains. Moreover, the neuromuscular synapse excitatory activities of parats1/dSC1−/− larvae were more sensitive to HA than dSC1−/− larvae, which further confirmed the functional contribution of dSC1 to neuronal excitability. Collectively, these results indicated that the dSC1 channel not only regulated the insecticidal activity of HA, but also maintained the stability of neural circuits through functional interaction with voltage-gated sodium channels. Therefore, our study provides useful information for elucidating the regulatory mechanism of dSC1 in the neural system of insects involving the action of HA derived from P. leptostachya.

关键词： botanical insecticide drosophila sodium channel 1(dSCI) insect nervous system neuromuscular synapse activity regulatory

discovery of novel ursolic acid derivatives as effective antimicrobial agents through a rOS-mediated apoptosis mechanism

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Frontiers of Chemical Science and Engineering 2023年第12期17卷 2101-2113页

作者： Yihong Yang Siyue Ma Ting Li Jingjing He Shitao Liu Hongwu Liu Jiaojiao Zhang Xiang Zhou Liwei Liu Song Yang National key laboratory of Green pesticide Key Laboratory of Green Pesticide and Agricultural Bioengineering(Ministry of Education)Center for R&D of Fine Chemicals of Guizhou UniversityGuiyang 550025China

In response to the reduction of food production and economic losses caused by plant bacterial diseases, it is necessary to develop new, efficient, and green pesticides. Natural products are rich and sustainable source for the development of new pesticides due to their low toxicity, easy degradation, and eco-friendliness. In this study, we prepared three series of ursolic acid derivatives and assessed their antibacterial ability. Most target compounds exhibited outstanding antibacterial activities. Among them, the relative optimal EC50 values of Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri were 2.23 (A17) and 1.39 (A16) μg·mL^(-1), respectively. The antimicrobial mechanism showed that compound A17 induced an excessive accumulation and production of reactive oxygen species in bacteria and damaged the cell membrane integrity to kill bacteria. More interestingly, the addition of low concentrations of exogenous hydrogen peroxide enhanced the antibacterial efficacy of compound A17 against Xanthomonas oryzae pv. oryzae. These entertaining results suggested that compound A17 induced an apparent apoptotic behavior in the tested bacteria. Overall, we developed the promising antimicrobial agents that destroyed the redox system of phytopathogenic bacteria, further demonstrating the unprecedented potential of ursolic acid for agricultural applications.

关键词： ursolic acid antibacterial activities reactive oxygen species apoptosis

Bactericidal bissulfone B7 targets bacterial pyruvate kinase to impair bacterial biology and pathogenicity in plants

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Science China(Life Sciences) 2024年第2期67卷 391-402页

作者： Awei Zhang Haizhen Zhang ronghua Wang Hongfu He Baoan Song runjiang Song National key laboratory of Green pesticide Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationCenter for R&D of Fine Chemicals of Guizhou UniversityGuiyang 550025China

The prevention and control of rice bacterial leaf blight(BLB)disease has not yet been achieved due to the lack of effective agrochemicals and available targets.Herein,we develop a series of novel bissulfones and a novel target with a unique mechanism to address this challenge.The developed bissulfones can control Xanthomonas oryzae pv.oryzae(Xoo),and 2-(bis(methylsulfonyl)methylene)-N-(4-chlorophenyl)hydrazine-1-carboxamide(B_(7))is more effective than the commercial drugs thiodiazole copper(TC)and bismerthiazol(BT).Pyruvate kinase(PYK)in Xoo has been identified for the first time as the target protein of our bissulfone B_(7).PYK modulates bacterial virulence via a CrP-like protein(Clp)/two-component system regulatory protein(reg r)axis.The elucidation of this pathway facilitates the use of B_(7)to reduce PYK expression at the transcriptional level,block PYK activity at the protein level,and impair the interaction within the PYK-Clp-reg r complex via competitive inhibition,thereby attenuating bacterial biology and pathogenicity.This study offers insights into the molecular and mechanistic aspects underlying anti-Xoo strategies that target PYK.We believe that these valuable discoveries will be used for bacterial disease control in the future.

关键词： 2-bissulfone-N-phenylhydrazine-1-carboxamide derivatives Xoo antibacterial activities pyruvate kinase regulatory mechanism

Knockin of the G275E mutation of the nicotinic acetylcholine receptor (nAChr) α6 confers high levels of resistance to spinosyns in Spodoptera exigua

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Insect Science 2022年第2期29卷 478-486页

作者： Ya-Yun Zuo Yu-Xin Xue Ze-Yu Wang Xuan ren Ahmed A.A.Aioub Yi-dong Wu Yi-Hua Yang Zhao-Nong Hu Institute of pesticide Science College of Plant ProtectionNorthwest A&F UniversityYanglingShaanxi712100 China College of Plant Protection Nanjing Agricultural UniversityNanjing210095 China key laboratory of Crop Pest Integrated Pest Management on the Loess Plateau of Ministry of Agriculture College of Plant ProtectionNorthwest A&F UniversityYanglingShaanxi712100 China key laboratory for botanical pesticide r&d of shaanxi province YanglingShaanxi712100 China Plant Protection department Faculty of AgricultureZagazig UniversityZagazig44511 Egypt

Spinosyns,including spinosad and spinetoram,act on the insect central nervous system,gradually paralyzing or destroying the target insect.Spinosad resistance is associated with loss-of-function mutations in the nicotinic acetylcholine receptor(nAChr)α6 subunit in a number of agricultural pests.Using gene editing,nAChrα6 has been verified as a target for spinosyns in five insect species.recently,a point mutation(G275E)in exon 9 of nAChrα6 was identified in spinosad-resistant strains of Thrips palmi and Tuta absoluta.To date,no in vivo functional evidence has been obtained to support that this mutation is involved in spinosyn resistance in lepidopteran pests.In this study,the G275E mutation was introduced into the nAChr of Spodoptera exigua using clustered regularly interspaced short palindromic repeats(CrISPr)/CrISPr-associated protein 9(Cas9)gene-editing technology.reverse transcriptase-polymerase chain reaction and sequencing confirmed that this mutation was present in exon 9 of the nAChr transcripts in the edited 275E strain.The results of bioassays showed that the 275E strain was highly resistant to spinosad(230-fold)and spinetoram(792-fold)compared to the unedited background strain,directly confirming that the G275E mutation of the nAChrα6 subunit confers high levels of spinosyn resistance in S.exigua.Inheritance analysis showed that the resistance trait is autosomal and incompletely recessive.This study employs a reverse genetics approach to validate the functional role played by the G275E mutation in nAChrα6 of S.exigua in spinosyns resistance and provides another example of the use of CrISPr/Cas9 gene-editing technology to confirm the role played by candidate target site mutations in insecticide resistance.

关键词： beet armyworm CrISPr G275E mutation nicotinic acetylcholine recep・tor spinosyns insecticides target resistance

Negative cross-resistance of a pyrethroid-resistant drosophila mutant to Phryma leptostachya-derived haedoxan A

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Insect Science 2022年第3期29卷 817-826页

作者： Xingtao Qie Yuzhe du Ahmed A.A.Aioub Ke dong Zhaonong Hu Institution of pesticide Science College of Plant ProtectionNorthwest A&F UniversityYanglingShaanxi 712100China Key Laboratory of Botanical Pesticide R&D in Shaanxi Province YanglingShaanxi 712100China Southern Insect Management research Unit Agriculture Research ServiceUnited States Department of Agriculture141 Experiment Station RoadStonevilleMS 38776USA Plant Protection department Faculty of AgricultureZagazig UniversityZagazig44511 Egypt department of Biology Duke UniversityDurhamNC 27708USA

Voltage-gated sodium channels are the primary target of pyrethroid insecticides.Mutations in sodium channel confer knockdown resistance(kdr)to pyrethroids in various arthropod pests.Haedoxan A(HA)is the major insecticidal component from Phryma leptostachya.It has been shown that HA alters electrical responses at the drosophila neuromuscular junction and modifies the gating properties of cockroach sodium channels expressed in Xenopus oocytes.However,whether sodium channel mutations that confer pyrethroid resistance also affect the action of HA is unknown.In this study,we conducted bioassays using HA and permethrin in two drosophila melanogaster strains:w^(1118),an insecticide-susceptible strain,and para^(tsl),a pyrethroid-resistant strain due to a I265N mutation in the sodium channel,and identified a new case of negative cross-resistance(NCr)between permethrin and HA.Both para^(tsl) larvae and adults were more resistant to permethrin,as expected.However,both para^(tsl) larvae and adults were more sensitive to HA compared to w^(1118).We confirmed that the I265N mutation reduced the sensitivity to permethrin of a drosophila sodium channel variant,dmNa_(v)22,expressed in Xenopus oocytes.Interestingly,the I265N mutation also abolished the effect of HA on sodium channels.Further characterization showed that I265 on the sodium channels is critical for the action of both pyrethroids and HA on sodium channels,pointing to an overlapping mode of action between pyrethroids and HA on the sodium channel.Overall,our results suggest an I265N-independnt mechanism(s)in para^(tsl) flies that is responsible for the NCr between permethrin and HA at the whole insect level.

关键词： botanical insecticide haedoxan A insecticidal mechanism negative crossresistance permethrin voltage-gated sodium channel

Efficient nanoparticle-based CrISPr-Cas13d induced mrNA disruption of an eye pigmentation gene in the white-backed planthopper,Sogatella furcifera

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Insect Science 2023年第6期30卷 1552-1564页

作者： Yun-Feng Ma Meng-Qi Zhang Lang-Lang Gong Xuan-Zheng Liu Gui-Jun Long Huan Guo J.Joe Hull Youssef dewer Ming He Peng He National key laboratory of Green pesticide Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationCenter for R&D of Fine Chemicals of Guizhou UniversityGuiyangChina USdA-ArS Arid Land Agricultural research Center MaricopaAZUSA Phytotoxicity research department Central Agricultural Pesticide LaboratoryAgricultural Research CenterDokkiGizaEgypt

The discovery of the clustered regularly interspaced short palindromic repeat(CrISPr)system has driven gene manipulation technology to a new era with applications reported in organisms that span the tree of life.The utility of CrISPr-mediated editing was further expanded to mrNA following identification of the rNA-targeting Cas13 family of smaller endonuclease proteins.Application of this family to insect research,however,has been more limited.In this study,the smallest Cas13 family member,Cas13d,and guide rNAs(grNAs)were complexed with a versatile nanomaterial(star polycation,SPc)to generate a proof-of-concept rNA-editing platform capable of disrupting mrNA expression of the eye pigmentation gene tryptophan 2,3-dioxygenase(SfTO)in white-backed planthoppers(WBPHs).The resulting red-eye phenotype was present in 19.76%(with SPc)and 22.99%(without SPc)of the treatment groups and was comparable to the red-eye phenotype generated following conventional rNA interference knockdown(22.22%).Furthermore,the Cas13/grNA phenotype manifested more quickly than rNA interference.Consistent with the expected Cas13d mechanism,SfTO transcript levels were significantly reduced.Taken together,the results indicate that the SPc-CrISPr-Cas13d/grNA complex negatively impacted expression of the target gene.These findings confirm the utility of this novel mrNA disruption system in insects and lay the foundation for further development of these tools in the implementation of green agricultural pest management tactics.

关键词： CrISPr-Cas13d rNA editing tryptophan 2,3-dioxygenase white-backed planthoppers

Host-guest interactions directed the morphology transformation of a charge-transfer complex of a naphthalene-tailored amphiphile/methyl viologen: From thin-films into diamond-like assemblies

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Chinese Chemical Letters 2021年第12期32卷 3998-4001页

作者： Qingtian Ji Lijun Fan Shuaishuai Liu Haojie Ye Shuzhen Xiang Peiyi Wang State key laboratory Breeding Base of Green pesticide and Agricultural Bioengineering Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationCenter for R&D of Fine Chemicals of Guizhou UniversityGuiyang 550025China

By introducing a host molecule cucurbit[8]uril(CB[8]) into a charge transfer system containing an amphiphile 1-[11-(naphthalene-2-ylmethoxy)-11-oxoundecyl]pyridinium(NP) and an electron-deficient molecule methyl viologen(MV), a novel and anisotropic ternary building block was constructed by hostguest interactions, thereby leading to the morphology transformation of the final assemblies from thinfilms(NP/MV complexes) into diamond-like structures(NP/MV/CB[8] complexes). These intriguing assemblies were firstly discovered and were similar with the shape of well-known metal organic frameworks(MOFs), but just comprised three small organic molecules without metal ions. This finding can enrich the shape of current supramolecular assemblies and thus contributing to more potential applications in material science.

关键词： Cucurbituril Amphiphile Methyl viologen Assemblies Host-guest interactions

discovery and structure-activity relationship studies of novel tetrahydro-β-carboline derivatives as apoptosis initiators for treating bacterial infections

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Journal of Integrative Agriculture 2024年第4期23卷 1259-1273页

作者： Shanshan Su Hongwu Liu Junrong Zhang Puying Qi Yue ding Ling Zhang Linli Yang Liwei Liu Xiang Zhou Song Yang National key laboratory of Green pesticide/key laboratory of Green pesticide and Agricultural Bioengineering Ministry of Education/Center for R&D of Fine ChemicalsGuizhou UniversityGuiyang 550025China

developing and excavating new agrochemicals with highly active and safe is an important tactic for protecting crop health and food safety.In this paper,to discover the new bactericide candidates,we designed,prepared a new type of1,2,3,4-tetrahydro-β-carboline(THC)derivatives and evaluated the in vitro and in vivo bioactivities against the Xanthomonas oryzae pv.oryzae(Xoo),Xanthomonas axonopodis pv.citri(Xac),and Pseudomonas syringae pv.actinidiae(Psa).The in vitro bioassay results exhibited that most title molecules possessed good activity toward the three plant pathogenic bacteria,the compound A17 showed the most active against Xoo and Xac with EC50 values of 7.27 and 4.89 mg mL^(-1)respectively,and compound A8 exhibited the best inhibitory activity against Psa with EC50value of 4.87 mg mL^(-1).Pot experiments showed that compound A17 exhibited excellent in vivo antibacterial activities to manage rice bacterial leaf blight and citrus bacterial canker,with protective efficiencies of 52.67 and 79.79%at 200 mgmL^(-1),respectively.Meanwhile,compound A8 showed good control efficiency(84.31%)against kiwifruit bacterial canker at 200 mg mL^(-1).Antibacterial mechanism suggested that these compounds could interfere with the balance of the redox system,damage the cell membrane,and induce the apoptosis of Xoo cells.Taken together,our study revealed that tetrahydro-β-carboline derivatives could be a promising candidate model for novel broadspectrum bactericides.

关键词： tetrahydro-β-carboline derivatives antibacterial activity rOS cell apoptosis

Synthesis, Antimicrobial Activity, and Molecular docking of Benzoic Hydrazide or Amide derivatives Containing a 1,2,3-Triazole Group as Potential SdH Inhibitors

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Chinese Journal of Chemistry 2021年第5期39卷 1319-1330页

作者： Yue ding Ling Zhang Song Yang Zhong Li Pei-Yi Wang State key laboratory Breeding Base of Green pesticide and Agricultural Bioengineering Key Laboratory of Green Pesticide and Agricultural BioengineeringMinistry of EducationCenter for R&D of Fine Chemicals of Guizhou UniversityGuiyongGuizhou 550025China College of Pharmacy East China University of Science&TechnologyShanghai 200237China

The present study was carried out in an attempt to synthesize a new class of antimicrobial agents containing a 1,2,3-triazole motif formed by classical copper catalyzed click chemistry.Antifungal bioassay results showed that five compounds 5a;5e,5h,5j,and 5k possessed a remarkable growth inhibitory activity against Botryosphaeria dothidea,rhizoctonia solani and Gibberella zeae with EC_(50) values within 10.0-0.306μg/mL.The in vitro efficacy was better than those of the commercial agrochemicals Azoxystrobin,Boscalid,and Fluxapyroxad.In vivo trials showed that compound 51 was effective for the control of rice sheath blight and wheat scab with the effects of 75% and 95%,respectively.Antifungal mechanism studies suggested that target compounds were potential succinate dehydrogenase inhibitors(SdHIs),which were proposed by the agreeable molecular docking study and restrained SdH activity(IC_(50)=3.95 μg/mL,51).Interestingly,compounds 5r and 5s displayed good antibacterial activity against phytopathogens.In vivo screening of 5r and 5s against rice bacterial blight afforded a superior control effect(up to 51%)than those of commercial agents Bismerthiazol and Thiodiazole copper.The current studies could support some title compounds to be the lead compounds for exploring highly bioactive antimicrobial substrates,particularly the potential SdHIs.

关键词： Hydrazide Amide 1,2,3-Triazole Molecular docking SdH inhibitory activity