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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY · 2022 · IF 4.966

Indoxacarb resistance-associated mutation of Liriomyza trifolii in Hainan, China

Fen Li,Xueyan Gong,Linlin Yuan,Xuelian Pan,Haifeng Jin,Rongcai Lu,Shaoying Wu

Liriomyza trifolii , which has been recently prevalent in China, harms more than 300 plant species, especially cowpea in Hainan. This pest also affects the quality and production of vegetables in winter. Indoxacarb is the first commercial oxadiazine pesticide , which is a new efficient insecticide used to control pests of Diptera, including L. trifolii . The unique mechanism of indoxacarb is that indenyl is transformed into N-demethoxycarbonyl metabolite (DCJW) in insects and acts on inactivated sodium channel; DCJW could then destroy the conduction of nerve impulses , which leads to movement disorders, feeding stoppage, paralysis, and eventually the death of pests. The field population of L. trifolii developed resistance by 769 times higher than the sensitive population in Sanya, Hainan. Results revealed the existence of a mutation (i.e., V1848I) in the sixth transmembrane segment of Domain IV of the sodium channel in the field population. The homozygous resistant genotype frequency for the V1848I mutation was 10–15% among the three field-collected populations. This paper reports for the first time the presence of the kdr mutation V1848I in resistant populations of L. trifolii to indoxacarb. The present study will contribute to the understanding of the evolution of indoxacarb resistance and contribute to the development of resistance management practices for winter vegetables in Hainan.

研究领域: 昆虫学 · 农药科学 · 农业科学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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PEST MANAGEMENT SCIENCE · 2024 ·Vol. 80 ·期 10 ·4950-4958 · IF 3.8

Point mutations in the voltage-gated sodium channel gene conferring pyrethroid resistance in China populations of the Dermanyssus gallinae

Penglong Wang,Qi Liu,Xu Wang,Tiancong Sun,Boxing Liu,Bohan Wang,Huan Li,Chuanwen Wang,Weiwei Sun,Baoliang Pan

BACKGROUND Dermanyssus gallinae , the poultry red mite (PRM), is a worldwide ectoparasite posing significant economic challenges in poultry farming. The extensive use of pyrethroids for PRM control has led to the emergence of pyrethroid resistance. The objective of this study is to detect the pyrethroid resistance and explore its associated point mutations in the voltage-gated sodium channel (VGSC) gene among PRM populations in China. RESULTS Several populations of D. gallinae , namely CJF-1, CJP-2, CJP-3, CSD-4 and CLD-5, displayed varying degrees of resistance to beta-cypermethrin compared to a susceptible field population (CBP-5). Mutations of VGSC gene in populations of PRMs associated with pyrethroid resistance were identified through sequencing its fragments IIS4–IIS5 and IIIS6. The mutations I917V, M918T/L, A924G and L925V were present in multiple populations, while no mutations were found at positions T929, I936, F1534 and F1538. CONCLUSION The present study confirmed the presence of extremely high levels of pyrethroid resistance in PRM populations in China, and for the first time detected four pyrethroid resistance mutations in the VGSC gene. Identifying pyrethroid resistance in the field population of PRM in China can be achieved through screening for VGSC gene mutations as an early detection method. Our findings underscore the importance of implementing chemical PRM control strategies based on resistance evidence, while also considering the management of acaricide resistance in the control of PRMs. © 2024 Society of Chemical Industry.

CAS / MDL: 65731-84-2
研究领域: 昆虫学 · 分子生物学 · 害虫管理
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ECONOMIC ENTOMOLOGY · 2023 · IF 2.2

Characterization and fitness cost of bifenthrin resistance in Rhopalosiphum padi (Hemiptera: Aphididae)

Liu Lang,Wang Suji,Zuo Junfeng,Zhang Xiaohe,Peng Xiong,Wang Kang,Chen Maohua

Rhopalosiphum padi is an important global wheat pest. The pyrethroid insecticide bifenthrin is widely used in the control R. padi. We explored the resistance potential, cross-resistance, adaptive costs, and resistance mechanism of R. padi to bifenthrin using a bifenthrin-resistant strain (Rp-BIF) established in laboratory. The Rp-BIF strain developed extremely high resistance against bifenthrin (1033.036-fold). Cross-resistance analyses showed that the Rp-BIF strain had an extremely high level of cross-resistance to deltamethrin (974.483-fold), moderate levels of cross-resistance to chlorfenapyr (34.051-fold), isoprocarb (27.415-fold), imidacloprid (14.819-fold), and thiamethoxam (11.228-fold), whereas negative cross-resistance was observed to chlorpyrifos (0.379-fold). The enzymatic activity results suggested that P450 played an important role in bifenthrin resistance. A super-kdr mutation (M918L) of voltage-gated sodium channel (VGSC) was found in the bifenthrin-resistant individuals. When compared with the susceptible strain (Rp-SS), the Rp-BIF strain was significantly inferior in multiple life table parameters, exhibiting a relative fitness of 0.69. Our toxicological and biochemical studies indicated that multiple mechanisms of resistance might be involved in the resistance trait. Our results provide insight into the bifenthrin resistance of R. padi and can contribute to improve management of bifenthrin-resistant R. padi in the field.

研究领域: 昆虫学 · 害虫管理 · 毒理学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Neurogastroenterology and Motility · 2017 · IF 2.457

Protein Kinase C Mediates the Corticosterone-induced Sensitization of Dorsal Root Ganglion Neurons Innervating the Rat Stomach

Meng Li,Lu Xue,Hong-Yan Zhu,Hongjun Wang,Xue Xu,Ping-An Zhang,Geping Wu,Guang-Yin Xu

Background/Aims Gastric hypersensitivity contributes to abdominal pain in patients with functional dyspepsia. Recent studies showed that hormones induced by stress are correlated with visceral hypersensitivity. However, the precise mechanisms underlying gastric hypersensitivity remain largely unknown. The aim of the present study was designed to investigate the roles of corticosterone (CORT) on excitability of dorsal root ganglion (DRG) neurons innervating the stomach. Methods DRG neurons innervating the stomach were labeled by DiI injection into the stomach wall. Patch clamp recordings were employed to examine neural excitability and voltage-gated sodium channel currents. Electromyograph technique was used to determine the responses of neck muscles to gastric distension. Results Incubation of acutely isolated DRG neurons with CORT significantly depolarized action potential threshold and enhanced the number of action potentials induced by current stimulation of the neuron. Under voltage-clamp mode, incubation of CORT enhanced voltage-gated sodium current density of the recorded neurons. Pre-incubation of GF109203X, an inhibitor of protein kinase C, blocked the CORT-induced hyperexcitability and potentiation of sodium currents. However, pre-incubation of H-89, an inhibitor of protein kinase A, did not alter the sodium current density. More importantly, intraperitoneal injection of CORT produced gastric hypersensitivity of healthy rats, which was blocked by pre-administration of GF109203X but not H-89. Conclusions Our data strongly suggest that CORT rapidly enhanced neuronal excitability and sodium channel functions, which is most likely mediated by protein kinase C but not protein kinase A signaling pathway in DRG neurons innervating the stomach, thus underlying the gastric hypersensitivity induced by CORT injection.

CAS / MDL: 133052-90-1
研究领域: 神经科学 · 药理学 · 生理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULAR PHARMACOLOGY · 2023 ·Vol. 104 ·期 4 ·133-143 · IF 3.6

Licochalcone Mediates the Pain Relief by Targeting the Voltage-Gated Sodium Channel

Qianru Zhao,Xu Zhang,Siru Long,Shaobing Wang,Hui Yu,Yongsheng Zhou,Yi Li,Lu Xue,Yan Hu,Shijin Yin

Licorice is a traditional Chinese medicine and recorded to have pain relief effects in national pharmacopoeia, but the mechanisms behind these effects have not been fully explored. Among the hundreds of compounds in licorice, licochalcone A (LCA) and licochalcone B (LCB) are two important components belonging to the chalcone family. In this study, we compared the analgesic effects of these two licochalcones and the molecular mechanisms. LCA and LCB were applied in cultured dorsal root ganglion (DRG) neurons, and the voltage-gated sodium (NaV) currents and action potentials were recorded. The electrophysiological experiments showed that LCA can inhibit NaV currents and dampen excitabilities of DRG neurons, whereas LCB did not show inhibition effect on NaV currents. Because the NaV1.7 channel can modulate Subthreshold membrane potential oscillations in DRG neuron, which can palliate neuropathic pain, HEK293T cells were transfected with NaV1.7 channel and recorded with whole-cell patch clamp. LCA can also inhibit NaV1.7 channels exogenously expressed in HEK293T cells. We further explored the analgesic effects of LCA and LCB on formalin-induced pain animal models. The animal behavior tests revealed that LCA can inhibit the pain responses during phase 1 and phase 2 of formalin test, and LCB can inhibit the pain responses during phase 2. The differences of the effects on NaV currents between LCA and LCB provide us with the basis for developing NaV channel inhibitors, and the novel findings of analgesic effects indicate that licochalcones can be developed into effective analgesic medicines.

研究领域: 药理学 · 神经科学 · 中医 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF CONTROLLED RELEASE · 2025 · IF 11.5

Ultrasound-responsive piezoelectric analgesic microspheres alleviate osteoarthritis pain

Xinhe Li,Fan Wang,Xinyu Zhang,Bo Liao,Jindong Tan,Xu He,Wang Han,Xiaoqian Ding,Zijie Wang,Anan Jiang,Chuan Liu,Liang Chen,Dingqun Bai,Xiaoyu Han

Osteoarthritis (OA) is one of the most common causes of chronic pain. However, current OA pain therapies often fail to achieve satisfactory outcomes. To effectively alleviate OA pain, ultrasound-responsive piezoelectric analgesic microspheres, constructed using ultrasound and piezoelectric nanomaterials, were developed. Barium titanate (BaTiO 3 ) piezoelectric nanoparticles modified by rabies virus glycoprotein (RVG) were loaded onto gelatin-methacrylate (GelMA) and hyaluronic acid-methacrylate (HAMA) composite hydrogel microspheres (GA/HA) obtained via microfluidic technology to construct analgesic microspheres (BaTiO 3 -RVG@GA/HA). Under ultrasound, the analgesic microspheres can generate electrical pulses. Pain signal transmission is blocked by modulating the voltage-gated sodium channel (VGSCs) Na v 1.7, thus alleviating OA pain. In vitro studies confirmed that analgesic microspheres can effectively reduce the expression of pain-related molecules. In addition, in vivo research results showed that analgesic microspheres can significantly reduce pain-related behaviors and joint pathological damage in rats, achieving improvements in OA pain and joint injury management.

CAS / MDL: 96-33-3
研究领域: 生物医学工程 · 纳米医学 · 疼痛研究 · 材料科学 · 骨科 · 神经科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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METABOLISM-CLINICAL AND EXPERIMENTAL · 2025 · IF 11.9

TGR5 attenuates DOCA-salt hypertension through regulating histone H3K4 methylation of ENaC in the kidney

Long Xu,Xinyan Wu,Luosha Long,Suchun Li,Meiying Huang,Meng Li,Pinning Feng,Moshe Levi,Wei Chen,Lei Wang,Chunling Li,Weidong Wang

Epithelial sodium channel (ENaC), located in the collecting duct principal cells of the kidney, is responsible for the reabsorption of sodium and plays a critical role in the regulation of extracellular fluid volume and consequently blood pressure. The G protein-coupled bile acid receptor (TGR5) is a membrane receptor mediating effects of bile acid and is implicated in kidney diseases. The current study aims to investigate whether TGR5 activation in the kidney regulated ENaC expression and potential mechanism. Lithocholic acid (LCA), a TGR5 agonist, markedly decreased systolic blood pressure induced by DOCA-salt in mice, which was associated with decreased ENaC expression in the kidney. DOCA-salt treatment increased renal expression of histone H3 lysine 4 trimethylation (H3K4me3) and decreased expression of lysine-specific demethylase 5A (KDM5A), a lysine demethylase, which was markedly reversed by LCA. TGR5 knockout caused further increased systolic blood pressure and ENaC expression in mice with DOCA-salt in association with increased H3K4me3 and decreased KDM5A. In immortalized mouse cortical collecting duct (mpkCCD) cells LCA markedly inhibited aldosterone-induced ENaC-mediated current. LCA treatment or TGR5 overexpression markedly inhibited ENaC and H3K4me3 protein expression in association with decreased KDM5A in mpkCCD cells treated with either aldosterone or angiotensin II. Inhibition or knockdown of KDM5A in mpkCCD cells prevented LCA-induced downregulation of ENaC expression by promoting H3K4me3 on the ENaC transcription start site. LCA upregulated KDM5A expression was likely through JNK/c-Jun signal pathway. In conclusion, LCA decreased blood pressure and ENaC protein expression in the kidney of mice with DOCA-salt, likely through activating TGR5 and upregulating KDM5A-induced H3K4me3 demethylation in ENaC promoter region.

CAS / MDL: 56-47-3
研究领域: 肾病学 · 分子生物学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2018 · IF 3.412

Semisynthesis of Matrinic Acid/Alcohol/Ester Derivatives, Their Pesticidal Activities, and Investigation of Mechanisms of Action against Tetranychus cinnabarinus

Bingchuan Zhang,Zhiqiang Sun,Min Lv,Hui Xu

To discover new natural-product-based potential pesticides, 85 matrinic acid/alcohol/ester derivatives were synthesized by structural modifications of a quinolizidine alkaloid matrine. N-(4-Methyl)benzylmatrinyl n-decylate (76) and N-(2-chloro)benzylmatrinyl n-undecylate (86) exhibited greater than seven-fold more pronounced acaricidal activity than matrine against Tetranychus cinnabarinus; N-(2-chloro)benzylmatrinyl benzoate (80) showed the most promising insecticidal activity against Mythimna separata. The carboxyl group of matrinic acids and introduction of n-decyl/n-undecylcarbonyl into matrinic alcohols were important for the acaricidal activity; introduction of alkyloxy into the carboxyl of matrinic acids and introduction of the electron-withdrawing groups on the N-benzyl of matrinic esters were necessary for the insecticidal activity. Through RT-PCR and qRT-PCR analysis, it was shown that the lactam ring of matrine was vital for action on VGSC; opening the lactam ring of matrine and the alkylcarbonyl of side-chain were two important factors for acting with α1, α2, and α4 nAChR subunits; α1, α2, α4, and β3 subunits may be the target of action of compound 86 against T. cinnabarinus.

研究领域: 化学 · 药理学 · 昆虫学 · 天然产物研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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AQUATIC TOXICOLOGY · 2019 · IF 3.794

Fenobucarb induces heart failure and cerebral hemorrhage in zebrafish

Xiao-Yu Zhu,Bo Xia,Yu-Ying Wu,Hua Yang,Chun-Qi Li,Ping Li

The potential risk and toxic mechanisms of fenobucarb (2-sec-butylphenyl methylcarbamate, BPMC) to animals and humans have not been fully elucidated. In this study, zebrafish embryos were exposed to various concentrations of BPMC from 48 hpf (hour post fertilization, hpf) to 72 hpf. We found that BPMC induced severe heart failure with bradycardia, reduced heart contractions, cardiac output and blood flow dynamics;and myocardial apoptosis. BPMC also induced cerebral hemorrhages and blood erythrocyte reduction in a dose-dependent manner. Also observed were increased ROS production and capase 9 and 3/7 activation. The mRNA levels of the ATPase-related gene ( at p2 a1l ), calcium channel-related gene ( cacna1ab ), sodium channel-related gene ( scn5Lab ), potassium channel-related gene ( kcnq1 ), the regulatory gene ( tnnc1a) for cardiac troponin C, and several apoptosis-related genes were significantly downregulated in zebrafish following BPMC exposure. These results suggest that exposure to BPMC is a possible risk factor to cardiovascular and cerebrovascular systems in animals.

CAS / MDL: 30525-89-4
研究领域: 毒理学 · 心血管研究 · 神经科学 · 发育生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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