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1.
Pestic Biochem Physiol ; 202: 105958, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38879340

ABSTRACT

The wheat aphid Sitobion miscanthi is a dominant and destructive pest in agricultural production. Insecticides are the main substances used for effective control of wheat aphids. However, their extensive application has caused severe resistance of wheat aphids to some insecticides; therefore, exploring resistance mechanisms is essential for wheat aphid management. In the present study, CYP6CY2, a new P450 gene, was isolated and overexpressed in the imidacloprid-resistant strain (SM-R) compared to the imidacloprid-susceptible strain (SM-S). The increased sensitivity of S. miscanthi to imidacloprid after knockdown of CYP6CY2 indicates that it could be associated with imidacloprid resistance. Subsequently, the posttranscriptional regulation of CYP6CY2 in the 3' UTR by miR-3037 was confirmed, and CYP6CY2 participated in imidacloprid resistance. This finding is critical for determining the role of P450 in relation to the resistance of S. miscanthi to imidacloprid. It is of great significance to understand this regulatory mechanism of P450 expression in the resistance of S. miscanthi to neonicotinoids.


Subject(s)
Aphids , Cytochrome P-450 Enzyme System , Insecticide Resistance , Insecticides , MicroRNAs , Neonicotinoids , Nitro Compounds , Neonicotinoids/pharmacology , Nitro Compounds/pharmacology , Animals , Insecticides/pharmacology , Insecticide Resistance/genetics , Aphids/genetics , Aphids/drug effects , MicroRNAs/genetics , MicroRNAs/metabolism , Cytochrome P-450 Enzyme System/genetics , Cytochrome P-450 Enzyme System/metabolism , Insect Proteins/genetics , Insect Proteins/metabolism , Imidazoles/pharmacology
2.
Nat Commun ; 15(1): 4813, 2024 Jun 06.
Article in English | MEDLINE | ID: mdl-38844461

ABSTRACT

Porcine Reproductive and Respiratory Syndrome Virus (PRRSV) poses a major threat to the global swine industry, yet effective prevention and control measures remain elusive. This study unveils Nitazoxanide (NTZ) as a potent inhibitor of PRRSV both in vitro and in vivo. Through High-Throughput Screening techniques, 16 potential anti-PRRSV compounds are identified from a library comprising FDA-approved and pharmacopeial drugs. We show that NTZ displays strong efficacy in reducing PRRSV proliferation and transmission in a swine model, alleviating viremia and lung damage. Additionally, Tizoxanide (TIZ), the primary metabolite of NTZ, has been identified as a facilitator of NMRAL1 dimerization. This finding potentially sheds light on the underlying mechanism contributing to TIZ's role in augmenting the sensitivity of the IFN-ß pathway. These results indicate the promising potential of NTZ as a repurposed therapeutic agent for Porcine Reproductive and Respiratory Syndrome (PRRS). Additionally, they provide valuable insights into the antiviral mechanisms underlying NTZ's effectiveness.


Subject(s)
Antiviral Agents , High-Throughput Screening Assays , Nitro Compounds , Porcine Reproductive and Respiratory Syndrome , Porcine respiratory and reproductive syndrome virus , Thiazoles , Animals , Porcine respiratory and reproductive syndrome virus/drug effects , Nitro Compounds/pharmacology , Swine , Antiviral Agents/pharmacology , High-Throughput Screening Assays/methods , Porcine Reproductive and Respiratory Syndrome/drug therapy , Porcine Reproductive and Respiratory Syndrome/virology , Thiazoles/pharmacology , Virus Replication/drug effects , Cell Line , Viremia/drug therapy , Viremia/virology
3.
Pestic Biochem Physiol ; 202: 105973, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38879316

ABSTRACT

Using a high-efficiency insecticide in combination with fungicides that have different mechanisms of action is a conventional method in the current management of brown planthopper (BPH) resistance. In this study, we investigate the separate and combined effects of the low-toxicity fungicide validamycin and the non-cross-resistant insecticide imidacloprid on the fitness and symbiosis of BPH. These research results indicate that when the proportion of active ingredients in validamycin is combined with imidacloprid at a ratio of 1:30, the toxicity ratio and co-toxicity coefficient are 1.34 and 691.73, respectively, suggesting that the combination has a synergistic effect on the control of BPH. The number of yeast-like symbiotic (YLS) and dominant symbiotic (Noda) in the imidacloprid + validamycin groups were significantly lower than the other three treatment groups (validamycin, imidacloprid, and water). The results of the study on population fitness show that the lifespan of the BPH population in validamycin, imidacloprid, and imidacloprid + validamycin was shortened. Notably, the BPH populations in the imidacloprid + validamycin groups were significantly lower than other groups in terms of average generation cycle, intrinsic growth rate, net reproduction rate, finite rate of increase, and fitness. The Real-time quantitative PCR showed that validamycin and imidacloprid + validamycin can significantly inhibit the expression of the farnesyl diphosphate farnesyl transferase gene (EC2.5.1.21) and uricase gene (EC1.7.3.3), with imidacloprid + validamycin demonstrating the most pronounced inhibitory effect. Our research results can provide insights and approaches for delaying resistance and integrated management of BPH.


Subject(s)
Hemiptera , Insecticides , Neonicotinoids , Nitro Compounds , Symbiosis , Animals , Hemiptera/drug effects , Neonicotinoids/pharmacology , Nitro Compounds/pharmacology , Insecticides/pharmacology , Inositol/analogs & derivatives , Inositol/pharmacology , Imidazoles/pharmacology , Fungicides, Industrial/pharmacology
4.
Pestic Biochem Physiol ; 202: 105935, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38879327

ABSTRACT

Imidacloprid (IMI) is a contaminant widespread in surface water, causing serious intestinal damage in the common carp. Melatonin (MT), an endogenous indoleamine hormone, plays a crucial role in mitigating pesticide-induced toxicity. Our previous research has demonstrated that MT effectively reduces the production of intestinal microbial-derived signal peptidoglycan (PGN) induced by IMI, thereby alleviating intestinal tight junction injuries in the common carp. In this study, we performed a transcriptomic analysis to explore the effect of MT on the IMI exposure-induced gut damage of the common carp. The results elucidated that the ferroptosis, mitogen-activated protein kinases (MAPKs), and nucleotide oligomerization domain (NOD)-like signaling pathways were significantly associated with IMI exposure and MT treatment. Meanwhile, the exposure to IMI resulted in the formation of pyroptotic bodies and distinct morphological features of ferroptosis, both mitigated with the addition of MT. Immunofluorescence double staining demonstrated that MT abolished the elevated expression of NOD-like receptor thermal protein domain associated protein 3 (NLRP3) and Gasdermin D (GSDMD) induced by IMI, as well as reduced expression of ferritin heavy chains (FTH) and glutathione peroxidase 4 (GPX4) in gut tissues. Subsequently, we found that the exposure to IMI or PGN enhanced the expression of toll-like receptors (TLR) 2 (a direct recognition receptor of PGN) triggering the P38MAPK signaling pathway, thereby aggravating the process of pyroptosis and ferroptosis of cell models. The addition of MT or SB203580 (a P38MAPK inhibitor) significantly reduced pyroptotic cells, and also decreased iron accumulation. Consequently, these results indicate that MT alleviates IMI-induced pyroptosis and ferroptosis in the gut of the common carp through the PGN/TLR2/P38MAPK pathway.


Subject(s)
Carps , Ferroptosis , Melatonin , Neonicotinoids , Nitro Compounds , Peptidoglycan , Pyroptosis , Animals , Carps/metabolism , Ferroptosis/drug effects , Melatonin/pharmacology , Pyroptosis/drug effects , Neonicotinoids/pharmacology , Neonicotinoids/toxicity , Peptidoglycan/pharmacology , Nitro Compounds/toxicity , Nitro Compounds/pharmacology , Insecticides/toxicity , Intestines/drug effects
5.
J Agric Food Chem ; 72(25): 14141-14151, 2024 Jun 26.
Article in English | MEDLINE | ID: mdl-38864686

ABSTRACT

The cotton aphid, Aphis gossypii, is a polyphagous pest that stunts host plant growth via direct feeding or transmitting plant virus. Due to the long-term application of insecticides, A. gossypii has developed different levels of resistance to numerous insecticides. We found that five field populations had evolved multiple resistances to neonicotinoids. To explore the resistance mechanism mediated by uridine diphosphate glycosyltransferases (UGTs), two upregulated UGT genes in these five strains, UGT350C3 and UGT344L7, were selected for functional analysis of their roles in neonicotinoid detoxification. Transgenic Drosophila bioassay results indicated that compared with the control lines, the UGT350C3 and UGT344L7 overexpression lines were more tolerant to thiamethoxam, imidacloprid, and dinotefuran. Knockdown of UGT350C3 and UGT344L7 significantly increased A. gossypii sensitivity to thiamethoxam, imidacloprid, and dinotefuran. Molecular docking analysis demonstrated that these neonicotinoids could bind to the active pockets of UGT350C3 and UGT344L7. This study provides functional evidence of neonicotinoid detoxification mediated by UGTs and will facilitate further work to identify strategies for preventing the development of neonicotinoid resistance in insects.


Subject(s)
Aphids , Glycosyltransferases , Insecticide Resistance , Insecticides , Neonicotinoids , Nitro Compounds , Animals , Aphids/genetics , Aphids/enzymology , Aphids/drug effects , Neonicotinoids/pharmacology , Neonicotinoids/metabolism , Neonicotinoids/chemistry , Insecticides/pharmacology , Insecticides/chemistry , Insecticides/metabolism , Insecticide Resistance/genetics , Glycosyltransferases/genetics , Glycosyltransferases/metabolism , Glycosyltransferases/chemistry , Nitro Compounds/pharmacology , Nitro Compounds/metabolism , Molecular Docking Simulation , Insect Proteins/genetics , Insect Proteins/metabolism , Insect Proteins/chemistry , Thiamethoxam , Drosophila/genetics , Drosophila/enzymology , Drosophila/drug effects , Drosophila/metabolism , Guanidines
6.
Eur J Med Chem ; 274: 116559, 2024 Aug 05.
Article in English | MEDLINE | ID: mdl-38850856

ABSTRACT

Tuberculosis remains the second deadliest infectious disease in humans and a public health threat due to the emergence of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains. Therefore, it is urgent to identify new anti-tuberculosis treatments and novel therapeutic targets to prevent the emergence of resistance. In recent years, the study of anti-tuberculosis properties of nitroaromatic compounds has led to the identification of two novel biological targets, the deazaflavin (F420)-dependent nitroreductase Ddn and the decaprenylphosphoryl-ß-d-ribose 2'-epimerase DprE1. This review aims to show why Ddn and DprE1 are promising therapeutic targets and highlight nitroaromatic compounds interest in developing new anti-tuberculosis treatments active against MDR-TB and XDR-TB. Despite renewed interest in the development of new anti-tuberculosis nitroaromatic compounds, pharmaceutical companies often exclude nitro-containing molecules from their drug discovery programs because of their toxic and mutagenic potential. This exclusion results in missed opportunities to identify new nitroaromatic compounds and promising therapeutic targets.


Subject(s)
Antitubercular Agents , Mycobacterium tuberculosis , Nitroreductases , Antitubercular Agents/pharmacology , Antitubercular Agents/chemistry , Humans , Mycobacterium tuberculosis/drug effects , Nitroreductases/metabolism , Bacterial Proteins/antagonists & inhibitors , Bacterial Proteins/metabolism , Nitro Compounds/chemistry , Nitro Compounds/pharmacology , Molecular Structure , Microbial Sensitivity Tests , Drug Development , Alcohol Oxidoreductases
7.
Chem Biol Interact ; 398: 111086, 2024 Aug 01.
Article in English | MEDLINE | ID: mdl-38825054

ABSTRACT

Oleic acid (OA) is a monounsaturated compound with many health-benefitting properties such as obesity prevention, increased insulin sensitivity, antihypertensive and immune-boosting properties, etc. The aim of this study was to analyze the effect of oleic acid (OA) and some anticancer drugs against oxidative damage induced by nitropropionic acid (NPA) in rat brain. Six groups of Wistar rats were treated as follows: Group 1, (control); group 2, OA; group 3, NPA + OA; group 4, cyclophosphamide (CPP) + OA; group 5, daunorubicin (DRB) + OA; and group 6, dexrazoxane (DXZ) + OA. All compounds were administered intraperitoneally route, every 24 h for 5 days. Their brains were extracted to measure lipoperoxidation (TBARS), H2O2, Ca+2, Mg+2 ATPase activity, glutathione (GSH) and dopamine. Glucose, hemoglobin and triglycerides were measured in blood. In cortex GSH increased in all groups, except in group 2, the group 4 showed the highest increase of this biomarker. TBARS decrease, and dopamine increase in all regions of groups 4, 5 and 6. H2O2 increased only in cerebellum/medulla oblongata of group 5 and 6. ATPase expression decreased in striatum of group 4. Glucose increased in group 6, and hemoglobin increased in groups 4 and 5. These results suggest that the increase of dopamine and the antioxidant effect of oleic acid administration during treatment with oncologic agents could result in less brain injury.


Subject(s)
Antineoplastic Agents , Brain , Glutathione , Oleic Acid , Oxidative Stress , Rats, Wistar , Animals , Oxidative Stress/drug effects , Oleic Acid/pharmacology , Brain/drug effects , Brain/metabolism , Rats , Male , Glutathione/metabolism , Antineoplastic Agents/pharmacology , Hydrogen Peroxide/metabolism , Nitro Compounds/pharmacology , Dopamine/metabolism , Propionates/pharmacology , Cyclophosphamide , Lipid Peroxidation/drug effects , Daunorubicin/pharmacology , Thiobarbituric Acid Reactive Substances/metabolism , Adenosine Triphosphatases/metabolism , Antioxidants/pharmacology
8.
Int J Mol Sci ; 25(12)2024 Jun 13.
Article in English | MEDLINE | ID: mdl-38928242

ABSTRACT

Drug resistance in infectious diseases developed by bacteria and fungi is an important issue since it is necessary to further develop novel compounds with biological activity that counteract this problem. In addition, new pharmaceutical compounds with lower secondary effects to treat cancer are needed. Coordination compounds appear to be accessible and promising alternatives aiming to overcome these problems. In this review, we summarize the recent literature on coordination compounds based on nitrobenzoic acid (NBA) as a ligand, its derivatives, and other nitro-containing ligands, which are widely employed owing to their versatility. Additionally, an analysis of crystallographic data is presented, unraveling the coordination preferences and the most effective crystallization methods to grow crystals of good quality. This underscores the significance of elucidating crystalline structures and utilizing computational calculations to deepen the comprehension of the electronic properties of coordination complexes.


Subject(s)
Coordination Complexes , Ligands , Coordination Complexes/chemistry , Coordination Complexes/pharmacology , Nitrobenzoates/chemistry , Nitrobenzoates/pharmacology , Humans , Crystallography, X-Ray/methods , Nitro Compounds/chemistry , Nitro Compounds/pharmacology
9.
Redox Biol ; 74: 103202, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38865901

ABSTRACT

Stimulator of Interferon Genes (STING) is essential for the inflammatory response to cytosolic DNA. Despite that aberrant activation of STING is linked to an increasing number of inflammatory diseases, the development of inhibitors has been challenging, with no compounds in the pipeline beyond the preclinical stage. We previously identified endogenous nitrated fatty acids as novel reversible STING inhibitors. With the aim of improving the specificity and efficacy of these compounds, we developed and tested a library of nitroalkene-based compounds for in vitro and in vivo STING inhibition. The structure-activity relationship study revealed a robustly improved electrophilicity and reduced degrees of freedom of nitroalkenes by conjugation with an aromatic moiety. The lead compounds CP-36 and CP-45, featuring a ß-nitrostyrene moiety, potently inhibited STING activity in vitro and relieved STING-dependent inflammation in vivo. This validates the potential for nitroalkene compounds as drug candidates for STING modulation to treat STING-driven inflammatory diseases, providing new robust leads for preclinical development.


Subject(s)
Alkenes , Inflammation , Membrane Proteins , Nitro Compounds , Membrane Proteins/antagonists & inhibitors , Membrane Proteins/metabolism , Animals , Inflammation/drug therapy , Humans , Mice , Alkenes/chemistry , Alkenes/pharmacology , Nitro Compounds/chemistry , Nitro Compounds/pharmacology , Structure-Activity Relationship
10.
PLoS One ; 19(6): e0290858, 2024.
Article in English | MEDLINE | ID: mdl-38833488

ABSTRACT

The tarnished plant bug, (TPB) Lygus lineolaris Palisot de Beauvois (Hemiptera: Miridae) is a key pest of cotton in the midsouth region and some areas of the eastern United States. Its control methods have been solely based on chemical insecticides which has contributed to insecticidal resistance and shortened residual periods for control of this insect pest. This study was conducted over a two-year period and examined the efficacy and residual effect of four commercial insecticides including lambda-cyhalothrin (pyrethroid), acephate (organophosphate), imidacloprid (neonicotinoid), and sulfoxaflor (sulfoxamine). The effectiveness and residual effects of these insecticides were determined by application on cotton field plots on four different dates during each season using three different concentrations (high: highest labeled commercial dose (CD), medium: 1/10 of the CD, low: 1/100 of the CD) on field cotton plots. Four groups of cotton leaves were randomly pulled from each treated plot and control 0-, 2-, 4-, 7-, and 9-days post treatment (DPT) and exposed to a lab colony of TPB adults. One extra leaf sample/ plot/ spray /DPT interval (0-2-4-7-9-11) during 2016 was randomly collected from the high concentration plots and sent to Mississippi State Chemical Laboratory for residual analysis. Mortality of TPB adults was greatest for those placed on leaves sprayed with the organophosphate insecticide with mortalities (%) of 81.7±23.4 and 63.3±28.8 (SE) 1-day after exposure (DAE) on leaves 0-DPT with the high concentration for 2016 and 2017, respectively, reaching 94.5±9.5 and 95.4±7.6 6-DAE each year. Mortality to all insecticides continued until 9 and 4-DPT for high and medium concentrations, respectively. However, organophosphate (39.4±28.6) and pyrethroid (24.4±9.9) exhibited higher mortality than sulfoxamine (10.6±6.6) and the neonicotinoid (4.0±1.5) 7-DAE on 9-DPT leaves with the high concentration. Based on our results using the current assay procedure, TPB adults were significantly more susceptible to contact than systemic insecticides and due to its residual effect, organophosphate could kill over 80% of the TPB population 7-DPT.


Subject(s)
Gossypium , Insecticides , Neonicotinoids , Nitriles , Nitro Compounds , Phosphoramides , Pyrethrins , Insecticides/pharmacology , Gossypium/parasitology , Animals , Pyrethrins/pharmacology , Neonicotinoids/pharmacology , Mississippi , Nitriles/pharmacology , Nitro Compounds/pharmacology , Insect Control/methods , Heteroptera/drug effects , Imidazoles/pharmacology , Hemiptera/drug effects , Organothiophosphorus Compounds , Pyridines , Sulfur Compounds
11.
J Agric Food Chem ; 72(23): 12967-12974, 2024 Jun 12.
Article in English | MEDLINE | ID: mdl-38814790

ABSTRACT

Structure-activity relationships of diazinoyl nicotinic insecticides (diazinoyl isomers and 5- or 6-substituted pyrazin-2-oyl analogues) are considered in terms of affinity to the insect nicotinic acetylcholine receptor (nAChR) and insecticidal activity against the imidacloprid-resistant brown planthopper. Among the test compounds, 3-(6-chloropyridin-3-ylmethyl)-2-(pyrazinoyl)iminothiazoline shows the highest potency in nAChR affinity and insecticidal activity. Aplysia californica acetylcholine binding protein (AChBP) mutants (Y55W + Q57R and Y55W + Q57T) are utilized to compare molecular recognition of nicotinic insecticides with diverse pharmacophores. N-nitro- or N-cyanoimine imidacloprid or acetamiprid, respectively, exhibits a high affinity to these AChBP mutants at a similar potency level. Intriguingly, the pyrazin-2-oyl analogue has a higher affinity to AChBP Y55W + Q57R than that to Y55W + Q57T, thereby indicating that pyrazine nitrogen atoms contact Arg57 guanidinium and Trp55 indole NH. Furthermore, nicotine prefers AChBP Y55W + Q57T over Y55W + Q57R, conceivably suggesting that the protonated nicotine is repulsed by Arg57 guanidinium, consistent with its inferior potency to insect nAChR.


Subject(s)
Hemiptera , Insect Proteins , Insecticides , Neonicotinoids , Receptors, Nicotinic , Animals , Insecticides/chemistry , Insecticides/pharmacology , Receptors, Nicotinic/metabolism , Receptors, Nicotinic/chemistry , Receptors, Nicotinic/genetics , Hemiptera/chemistry , Hemiptera/genetics , Hemiptera/drug effects , Hemiptera/metabolism , Structure-Activity Relationship , Insect Proteins/metabolism , Insect Proteins/genetics , Insect Proteins/chemistry , Neonicotinoids/chemistry , Neonicotinoids/pharmacology , Neonicotinoids/metabolism , Nitro Compounds/chemistry , Nitro Compounds/pharmacology , Nitro Compounds/metabolism , Aplysia/chemistry , Aplysia/metabolism , Aplysia/genetics , Nicotine/chemistry , Nicotine/metabolism , Nicotine/analogs & derivatives , Nicotine/pharmacology
12.
J Agric Food Chem ; 72(22): 12469-12477, 2024 Jun 05.
Article in English | MEDLINE | ID: mdl-38771932

ABSTRACT

Photopharmacology can be implemented in a way of regulating drug activities by light-controlling the molecular configuations. Three photochromic ligands (PCLs) that bind on one or two sites of GABARs and nAChRs were reported here. These multiphoton PCLs, including FIP-AB-FIP, IMI-AB-FIP, and IMI-AB-IMI, are constructed with an azobenzene (AB) bridge that covalently connects two fipronil (FIP) and imidacloprid (IMI) molecules. Interestingly, the three PCLs as well as FIP and IMI showed great insecticidal activities against Aedes albopictus larvae and Aphis craccivora. IMI-AB-FIP in both trans/cis isomers can be reversibly interconverted depending on light, accompanied by insecticidal activity decrease or increase by 1.5-2.3 folds. In addition, IMI-AB-FIP displayed synergistic effects against A. craccivora (LC50, IMI-AB-FIP = 14.84-22.10 µM, LC50, IMI-AB-IMI = 210.52-266.63 µM, LC50, and FIP-AB-FIP = 36.25-51.04 µM), mainly resulting from a conceivable reason for simultaneous targeting on both GABARs and nAChRs. Furthermore, modulations of wiggler-swimming behaviors and cockroach neuron function were conducted and the results indirectly demonstrated the ligand-receptor interactions. In other words, real-time regulations of receptors and insect behaviors can be spatiotemporally achieved by our two-photon PCLs using light.


Subject(s)
Aedes , Azo Compounds , Insecticides , Neonicotinoids , Nitro Compounds , Pyrazoles , Animals , Nitro Compounds/chemistry , Nitro Compounds/pharmacology , Insecticides/chemistry , Insecticides/pharmacology , Azo Compounds/chemistry , Azo Compounds/pharmacology , Neonicotinoids/chemistry , Neonicotinoids/pharmacology , Pyrazoles/chemistry , Pyrazoles/pharmacology , Aedes/drug effects , Larva/drug effects , Larva/growth & development , Insect Proteins/chemistry , Insect Proteins/metabolism , Behavior, Animal/drug effects , Light , Receptors, Nicotinic/chemistry , Receptors, Nicotinic/metabolism , Receptors, GABA/metabolism , Receptors, GABA/chemistry
13.
Arch Insect Biochem Physiol ; 116(1): e22115, 2024 May.
Article in English | MEDLINE | ID: mdl-38770623

ABSTRACT

Zeugodacus cucurbitae (Coquillett) is an important fruit and vegetable pest, especially in high-temperature seasons. In our previous research, we developed a temperature-sensitive sustained-release attractant for Z. cucurbitae, that not only can control the release rate of cuelure according to the temperature change, but also shows an excellent trapping effect on Z. cucurbitae. To further enhance the killing effect of the temperature-sensitive attractant on Z. cucurbitae, this study proposed using it in combination with an insecticide to prepare a temperature-sensitive insecticide for Z. cucurbitae. Based on the controlled release technology of pesticides, a temperature-sensitive Z. cucurbitae insecticide was developed by using PNIPAM gel as a temperature-sensitive switch to carry both cuelure and insecticide at the same time. In addition, the lethal effect of different pesticides on Z. cucurbitae were tested by indoor toxicity test, and the best pesticide combination was screened out. The temperature-sensitive insecticide prepared in this study not only had excellent thermal response and controlled release ability, but also enhanced its toxicological effects on Z. cucurbitae because it contained insecticides. Among them, combining thiamethoxam and clothianidin with the temperature-sensitive attractants was the most effective, and their lethality reached more than 97% against Z. cucurbitae. This study is not only of great practical significance for the monitoring and controlling Z. cucurbitae, but also provides theoretical basis and reference value for the combination of temperature-sensitive attractant and insecticide.


Subject(s)
Insecticides , Neonicotinoids , Temperature , Insecticides/pharmacology , Animals , Neonicotinoids/pharmacology , Nitro Compounds/pharmacology , Insect Control/methods , Weevils/drug effects , Thiazoles/pharmacology
14.
J Agric Food Chem ; 72(19): 10805-10813, 2024 May 15.
Article in English | MEDLINE | ID: mdl-38712504

ABSTRACT

Aryl hydrocarbon receptor (AhR) and aryl hydrocarbon receptor nuclear translocator (ARNT) mediate the responses of adaptive metabolism to various xenobiotics. Here, we found that BoAhR and BoARNT are highly expressed in the midgut of Bradysia odoriphaga larvae. The expression of BoAhR and BoARNT was significantly increased after exposure to imidacloprid and phoxim. The knockdown of BoAhR and BoARNT significantly decreased the expression of CYP6SX1 and CYP3828A1 as well as P450 enzyme activity and caused a significant increase in the sensitivity of larvae to imidacloprid and phoxim. Exposure to ß-naphthoflavone (BNF) significantly increased the expression of BoAhR, BoARNT, CYP6SX1, and CYP3828A1 as well as P450 activity and decreased larval sensitivity to imidacloprid and phoxim. Furthermore, CYP6SX1 and CYP3828A1 were significantly induced by imidacloprid and phoxim, and the silencing of these two genes significantly reduced larval tolerance to imidacloprid and phoxim. Taken together, the BoAhR/BoARNT pathway plays key roles in larval tolerance to imidacloprid and phoxim by regulating the expression of CYP6SX1 and CYP3828A1.


Subject(s)
Insect Proteins , Insecticides , Larva , Neonicotinoids , Nitro Compounds , Receptors, Aryl Hydrocarbon , Animals , Insecticides/pharmacology , Larva/metabolism , Larva/genetics , Larva/growth & development , Larva/drug effects , Nitro Compounds/pharmacology , Nitro Compounds/metabolism , Neonicotinoids/pharmacology , Neonicotinoids/metabolism , Insect Proteins/metabolism , Insect Proteins/genetics , Receptors, Aryl Hydrocarbon/metabolism , Receptors, Aryl Hydrocarbon/genetics , Diptera/metabolism , Diptera/genetics , Diptera/drug effects , Diptera/growth & development , Aryl Hydrocarbon Receptor Nuclear Translocator/metabolism , Aryl Hydrocarbon Receptor Nuclear Translocator/genetics , Cytochrome P-450 Enzyme System/metabolism , Cytochrome P-450 Enzyme System/genetics , Inactivation, Metabolic , Transcription Factors/genetics , Transcription Factors/metabolism
15.
Pestic Biochem Physiol ; 201: 105863, 2024 May.
Article in English | MEDLINE | ID: mdl-38685216

ABSTRACT

The whitefly Bemisia tabaci poses a significant threat to various crops and ornamental plants and causes severe damage to the agricultural industry. Over the past few decades, B. tabaci has developed resistance to several pesticides, including imidacloprid. Therefore, elucidating the mechanism that leads to insecticide detoxification is very important for controlling B. tabaci and managing whitefly resistance to neonicotinoid insecticides. Among insect detoxification enzymes, glutathione S-transferase (GST) is an important phase II detoxification enzyme that helps detoxify exogenous toxic substances. In this study, we cloned the BtGSTz1 gene and observed that its expression level was greater in imidacloprid-resistant populations than sensitive populations of B. tabaci. By silencing BtGSTz1 via RNA interference, we found a significant increase in the mortality of imidacloprid-resistant B. tabaci. Additionally, prokaryotic expression and in vitro metabolism studies revealed that the recombinant BtGSTz1 protein could metabolize 36.36% of the total imidacloprid, providing direct evidence that BtGSTz1 plays a crucial role in the detoxification of imidacloprid. Overall, our study elucidated the role of GSTs in physiological activities related to insecticide resistance, which helps clarify the resistance mechanisms conferred by GSTs and provides useful insights for sustainable integrated pest management.


Subject(s)
Glutathione Transferase , Hemiptera , Insecticide Resistance , Insecticides , Neonicotinoids , Nitro Compounds , Hemiptera/drug effects , Hemiptera/genetics , Hemiptera/metabolism , Animals , Neonicotinoids/pharmacology , Neonicotinoids/metabolism , Nitro Compounds/pharmacology , Nitro Compounds/metabolism , Glutathione Transferase/metabolism , Glutathione Transferase/genetics , Insecticides/pharmacology , Insecticides/metabolism , Insecticide Resistance/genetics , Insect Proteins/metabolism , Insect Proteins/genetics , RNA Interference , Imidazoles/pharmacology , Imidazoles/metabolism
16.
Chem Biol Interact ; 395: 111013, 2024 May 25.
Article in English | MEDLINE | ID: mdl-38663798

ABSTRACT

Ulcerative colitis is a chronic disease with colonic mucosa injury. Nitazoxanide is an antiprotozoal drug in clinic. Nitazoxanide and its metabolite tizoxanide have been demonstrated to activate AMPK and inhibit inflammation, therefore, the aim of the present study is to investigate the effect of nitazoxanide on dextran sulfate sodium (DSS)-induced colitis and the underlying mechanism. Oral administration of nitazoxanide ameliorated the symptoms of mice with DSS-induced colitis, as evidenced by improving the increased disease activity index (DAI), the decreased body weight, and the shortened colon length. Oral administration of nitazoxanide ameliorated DSS-induced intestinal barrier dysfunction and reduced IL-6 and IL-17 expression in colon tissues. Mechanistically, nitazoxanide and its metabolite tizoxanide treatment activated AMPK and inhibited JAK2/STAT3 signals. Nitazoxanide and tizoxanide treatment increased caudal type homeobox 2 (CDX2) expression, increased alkaline phosphatase (ALP) activity and promoted tight junctions in Caco-2 cells. Nitazoxanide and tizoxanide treatment restored the decreased zonula occludens-1(ZO-1) and occludin protein levels induced by LPS or IL-6 in Caco-2 cells. On the other hand, nitazoxanide and tizoxanide regulated macrophage bias toward M2 polarization, as evidenced by the increased arginase-1expression in bone marrow-derived macrophages (BMDM). Nitazoxanide and tizoxanide reduced the increased IL-6, iNOS and CCL2 pro-inflammatory gene expressions and inhibited JAK2/STAT3 activation in BMDM induced by LPS. In conclusion, nitazoxanide protects against DSS-induced ulcerative colitis in mice through improving intestinal barrier and inhibiting inflammation and the underlying mechanism involves AMPK activation and JAK2/STAT3 inhibition.


Subject(s)
Colitis, Ulcerative , Dextran Sulfate , Intestinal Mucosa , Nitro Compounds , STAT3 Transcription Factor , Thiazoles , Animals , Thiazoles/pharmacology , Thiazoles/therapeutic use , Colitis, Ulcerative/chemically induced , Colitis, Ulcerative/drug therapy , Colitis, Ulcerative/pathology , Colitis, Ulcerative/metabolism , Nitro Compounds/pharmacology , Mice , Humans , Caco-2 Cells , Intestinal Mucosa/drug effects , Intestinal Mucosa/metabolism , Intestinal Mucosa/pathology , Dextran Sulfate/toxicity , STAT3 Transcription Factor/metabolism , Male , Janus Kinase 2/metabolism , AMP-Activated Protein Kinases/metabolism , Inflammation/drug therapy , Colon/drug effects , Colon/pathology , Colon/metabolism , Mice, Inbred C57BL , Signal Transduction/drug effects , Nitric Oxide Synthase Type II/metabolism , Interleukin-6/metabolism , Disease Models, Animal
17.
Vet Parasitol ; 328: 110178, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38569277

ABSTRACT

The control of the sheep blowfly relies on the use of insecticides. There have been several reports of in vitro and in vivo resistance to the most widely-used flystrike control chemical, dicyclanil. A recent report also described in vitro resistance to imidacloprid in a strain collected from a single property over three consecutive seasons that also showed resistance to dicyclanil. The present study aimed to use in vitro assays to examine five field-collected blowfly strains to determine if this co-occurrence of resistance to dicyclanil and imidacloprid was present more widely in field strains and to also measure resistance patterns to the other currently-used flystrike control chemicals. Each of the strains showed significant levels of resistance to both dicyclanil and imidacloprid: resistance factors at the IC50 of 9.1-23.8 for dicyclanil, and 8.7-14.1 for imidacloprid. Resistance factors at the IC95 ranged from 16.5 to 53.7, and 14.6-24.3 for dicyclanil and imidacloprid, respectively. Resistance factors were up to 8.5 for cyromazine at the IC95. Resistance to dicyclanil and imidacloprid was suppressed by co-treatment with the cytochrome P450 inhibitor, aminobenzotriazole, implicating this enzyme system in the observed resistances. We discuss the implications of the co-occurrence of resistance to dicyclanil and imidacloprid on insecticide rotation strategies for blowfly control. We also discuss the roles of insecticide resistance, environmental factors (e.g. rainfall), operational factors (e.g. insecticide application technique) and other animal health issues (e.g. scouring / diarrhoea) that together will impact on the likelihood of flystrike occurring at an earlier time point than expected after insecticide application.


Subject(s)
Diptera , Insecticide Resistance , Insecticides , Neonicotinoids , Nitro Compounds , Animals , Insecticides/pharmacology , Neonicotinoids/pharmacology , Nitro Compounds/pharmacology , Diptera/drug effects , Sheep , Sheep Diseases/parasitology , Juvenile Hormones , Triazines
18.
Viruses ; 16(2)2024 02 12.
Article in English | MEDLINE | ID: mdl-38400057

ABSTRACT

Canine parvovirus (CPV) is a single-stranded DNA virus that can cause typical hemorrhagic enteritis, and it is one of the common canine lethal viruses. In previous studies, we screened the Food and Drug Administration (FDA)'s drug library and identified nitazoxanide (NTZ), which has anti-CPV capabilities. To investigate the potential antiviral mechanisms, we first reconfirmed the inhibitory effect of NTZ on the CPV by inoculating with different doses and treating for different lengths of time. Then, the differences in the transcription levels between the 0.1%-DMSO-treated virus group and the NTZ-treated virus group were detected using RNA-seq, and a total of 758 differential expression genes (DEGs) were finally identified. Further Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses of the DEGs revealed that these genes are involved in a variety of biological processes and/or signaling pathways, such as cell cycle, mitosis and cell proliferation and differentiation. A protein-protein interaction (PPI) analysis further identified hub genes associated with cell cycle and division among the DEGs. In addition, the expression levels of some of the enriched genes were detected, which were consistent with the high-throughput sequencing results. Moreover, when the cell cycle was regulated with cell cycle checkpoint kinase 1 (Chk1) inhibitor MK-8776 or Prexasertib HCl, both inhibitors inhibited the CPV. In summary, the transcriptome differential analysis results presented in this paper lay the foundation for further research on the molecular mechanism and potential targets of NTZ anti-CPV.


Subject(s)
Parvoviridae Infections , Parvovirus, Canine , Animals , Dogs , Gene Expression Profiling/methods , Nitro Compounds/pharmacology , Thiazoles/pharmacology , Parvovirus, Canine/genetics , Computational Biology/methods , Transcriptome
19.
Pest Manag Sci ; 80(7): 3451-3458, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38415819

ABSTRACT

BACKGROUND: Mating is an essential factor that governs the size of insect populations that reproduce sexually. The extensive application of insecticides has both lethal and sublethal effects on the physiology and mating behavior of insect natural enemies. The predatory bug Cyrtorhinus lividipennis is a natural enemy of planthopper and leafhopper populations in the rice ecosystem. Unfortunately, the effects of insecticides on the mating behavior of C. lividipennis are not well-understood. RESULTS: The mating behavior of C. livdipennis consisted of mounting, antennal touch and mating attempts, genital insertion, adjustment of posture, and separation of the mating pair. Approximately 82.5% of the C. lividipennis mating pairs displayed their first mating at 12-36 h postemergence. Mating activity occurred throughout a 24-h period, with peak activity at 12:00-14:00 h, and the mean duration of mating was 48.75 min. Sublethal exposure to imidacloprid increased mating latency. Compared with the controls, the duration of courtship, pre-mating and adjusting posture for males treated with imidacloprid were prolonged. The duration of mating for females treated with imidacloprid was prolonged relative to untreated controls. The fecundity and daily spawning capacity of females treated with imidacloprid were higher than the untreated controls. CONCLUSION: Our results provide insight into the mating process of C. lividipennis. Imidacloprid prolonged the duration of mating, which may explain the enhanced reproductive output in C. lividipennis females treated with imidacloprid. These findings will be useful in both rearing C. lividipennis and deploying this natural enemy in rice fields. © 2024 Society of Chemical Industry.


Subject(s)
Insecticides , Neonicotinoids , Nitro Compounds , Sexual Behavior, Animal , Animals , Sexual Behavior, Animal/drug effects , Female , Male , Nitro Compounds/pharmacology , Insecticides/pharmacology , Heteroptera/drug effects , Heteroptera/physiology
20.
Pest Manag Sci ; 80(6): 3000-3009, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38312101

ABSTRACT

BACKGROUND: To improve integrated pest management (IPM) performance it is essential to assess pesticide side effects on host plants, insect pests, and natural enemies. The green peach aphid (Myzus persicae Sulzer) is a major insect pest that attacks various crops. Aphidius gifuensis is an essential natural enemy of M. persicae that has been applied effectively in controlling M. persicae. Thiamethoxam is a neonicotinoid pesticide widely used against insect pests. RESULTS: The current study showed the effect of thiamethoxam against Solanum tuberosum, M. persicae, and A. gefiuensis and the physiological and molecular response of the plants, aphids, and parasitoids after thiamethoxam application. Thiamethoxam affected the physical parameters of S. tuberosum and generated a variety of sublethal effects on M. persicae and A. gefiuensis, including nymph development time, adult longevity, and fertility. Our results showed that different thiamethoxam concentrations [0.1, 0.5, and 0.9 µm active ingredient (a.i.)/L] on different time durations (2, 6, and 10 days) increased the antioxidant enzyme activities SOD, POD, and CAT of S. tuberosum, M. persicae, and A. gefiuensis significantly compared with the control. Our results also showed that different thiamethoxam concentrations (0.1, 0.5, and 0.9 µm a.i./L) on different time durations (2, 6, and 10 days) increased the expression of superoxide dismutase (SOD), peroxidase (POD), catalase (CAT), acetylcholinesterase (AChE), carboxylesterase (CarE) and glutathione-S-transferase (GST) genes of S. tuberosum, M. persicae, and A. gefiuensis compared with the control. CONCLUSION: Our findings reveal that using thiamethoxam at suitable concentrations and time durations for host plants and natural enemies may enhance natural control through the conservation of natural enemies by overcoming any fitness disadvantages. © 2024 Society of Chemical Industry.


Subject(s)
Aphids , Insecticides , Neonicotinoids , Solanum tuberosum , Thiamethoxam , Thiazoles , Animals , Aphids/drug effects , Aphids/genetics , Solanum tuberosum/parasitology , Insecticides/pharmacology , Neonicotinoids/pharmacology , Thiazoles/pharmacology , Wasps/drug effects , Wasps/physiology , Oxazines/pharmacology , Nitro Compounds/pharmacology , Nymph/drug effects , Nymph/growth & development , Nymph/parasitology
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