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Communications Biology · 2025 ·Vol. 8 ·期 1 ·1-13 · IF 5.1

Inhibition of transcriptional regulation of detoxification genes contributes to insecticide resistance management in Spodoptera exigua

Hu Bo,Deng Yuping,Lu Tao,Ren Miaomiao,Liu Kuitun,Rao Cong,Guo Hailiang,Su Jianya

Synthetic insecticides have been widely used for the prevention and control of disease vectors and agricultural pests. However, frequent uses of insecticides have resulted in the development of insecticide resistance in these insect pests. The resistance adversely affects the efficacy of insecticides, and seriously reduces the lifespan of insecticides. Therefore, resistance management requires new strategies to suppress insecticide resistance. Here, we confirm that CncC/Maf are the key regulators of various detoxification genes involved in insecticide resistance in Spodoptera exigua . Then, we develop a cell screening platform to identify the natural compound inhibitors of CncC/Maf and determine that sofalcone can act as a CncC/Maf inhibitor in vitro and in vivo. Bioassay results showed that sofalcone significantly enhanced the toxicity (more than 3-fold) of chlorpyrifos and lambda-cyhalothrin against S. exigua larvae. Finally, we demonstrate that sofalcone can greatly improve the susceptibility of S. exigua larvae to insecticides by inhibiting the activity of the ROS/CncC-dependent detoxifying enzymes and downregulating the expression levels of detoxification genes. CncC/Maf inhibitors can be used as broad-spectrum synergists to overcome insecticide resistance in pest populations. Altogether, our results demonstrate that reduced expression of detoxification genes resulting from suppression of transcriptional regulation of these genes contributes to controlling insecticide resistance, which provides a very novel and high-efficiency green resistance management strategy.

CAS / MDL: 959-33-1 55837-20-2
研究领域: 昆虫学 · 分子生物学 · 害虫管理
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY · 2020 · IF 5.573

Design, synthesis, and evaluation of amphiphilic sofalcone derivatives as potent Gram-positive antibacterial agents

Shuimu Lin,Yongzhi Chen,Hongxia Li,Jiayong Liu,Shouping Liu

New antimicrobial agents are urgently needed to overcome drug-resistant bacterial infections. Here we describe the design, synthesis and evaluation of a new class of amphiphilic sofalcone compounds as antimicrobial peptidomimetics . The most promising compound 14 , bearing two arginine residues , showed poor hemolytic activity , low cytotoxicity, and excellent antimicrobial activity against Gram-positive bacteria, including MRSA . Compound 14 , had good stability in various salt conditions, killed bacteria rapidly by directly disrupting bacterial cell membranes and was slow at developing bacterial resistance . Additionally, compound 14 exhibited effective in vivo efficacy in the murine model of bacterial keratitis caused by Staphylococcus aureus ATCC29213. Our studies suggested that compound 14 possessed promising potential to be used as a novel antimicrobial agent to combat drug-resistant Gram-positive bacteria.

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