Department of Pesticide Science, Plant Protection College, Shenyang Agricultural University, Shenyang 110866, China.
Molecules. 2022 Jan 29;27(3):936. doi: 10.3390/molecules27030936.
SYAUP-CN-26 (1, 2-((3-bromophenethyl)amino)--(4-chloro-2-trifluoromethylphenyl) cyclohexane-1-sulfonamide) is a novel sulfonamide compound with excellent activity against . The present study sought to explore the mutant of resistant to SYAUP-CN-26 using SYAUP-CN-26 plates. Moreover, the cell membrane functions of , histidine kinase activity, relative conductivity, triglyceride, and cell membrane structure were determined, and the target gene histidine kinase Bos1 (AF396827.2) of procymidone was amplified and sequenced. The results showed that compared to the sensitive strain, the cell membrane permeability, triglyceride, and histidine kinase activity of the resistant strain showed significant changes. The relative conductivity of the sensitive strain increased by 6.95% and 9.61%, while the relative conductivity of the resistant strain increased by 0.23% and 1.76% with 26.785 µg/mL (EC) and 79.754 µg/mL (MIC) of SYAUP-CN-26 treatment. The triglyceride inhibition rate of the resistant strain was 23.49% and 37.80%, which was 0.23% and 1.76% higher than the sensitive strain. Compared to the sensitive strain, the histidine kinase activity of the resistant strain was increased by 23.07% and 35.61%, respectively. SYAUP-CN-26 significantly damaged the cell membrane structure of the sensitive strain. The sequencing of the Bos1 gene of the sensitive and resistant strains indicated that SYAUP-CN-26 resistance was associated with a single point mutation (P348L) in the Bos1 gene. Therefore, it was inferred that the mutant of resistant to SYAUP-CN-26 might be regulated by the Bos1 gene. This study will provide a theoretical basis for further research and development of sulfonamide compounds for and new agents for the prevention and control of resistant .
SYAUP-CN-26（1，2-（（3-溴苯乙基）氨基）-（4-氯-2-三氟甲基苯基）环己烷-1-磺酰胺）是一种新型磺酰胺化合物，对具有优异的活性。本研究旨在使用 SYAUP-CN-26 平板探索对 SYAUP-CN-26 产生抗性的突变体。此外，还测定了 细胞膜功能、组氨酸激酶活性、相对电导率、甘油三酯和细胞膜结构，并扩增和测序了丙环唑的靶基因组氨酸激酶 Bos1（AF396827.2）。结果表明，与敏感菌株相比，抗性菌株的细胞膜通透性、甘油三酯和组氨酸激酶活性均发生显著变化。26.785µg/mL（EC）和 79.754µg/mL（MIC）SYAUP-CN-26 处理后，敏感菌株的相对电导率分别增加了 6.95%和 9.61%，而抗性菌株的相对电导率分别增加了 0.23%和 1.76%。抗性菌株的甘油三酯抑制率分别为 23.49%和 37.80%，比敏感菌株高 0.23%和 1.76%。与敏感菌株相比，抗性菌株的组氨酸激酶活性分别增加了 23.07%和 35.61%。SYAUP-CN-26 显著破坏了敏感菌株的细胞膜结构。敏感和抗性菌株 Bos1 基因的测序表明，SYAUP-CN-26 抗性与 Bos1 基因的单点突变（P348L）有关。因此，推断对 SYAUP-CN-26 产生抗性的 突变体可能受 Bos1 基因调控。本研究为进一步研究和开发磺酰胺化合物防治 和新的抗性药剂提供了理论依据。
