Development of biosafety pyrazole-5-sulfonamide derivatives for sustainable control of peanut stem rot

IF 9.2

Advanced Agrochem Pub Date : 2026-06-01 Epub Date: 2025-08-23 DOI:10.1016/j.aac.2025.08.002

Xiang Cheng , Fanglei Wang , Shumeng Wang , Yiyang Shao , Yuting Hu , Dandan Wang , Guogen Yang , Xianhai Lv , Qiang Bian , Xihao Chang

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Abstract

Sclerotium rolfsii threatens global peanut production with 15–80 % yield losses. Fungicide resistance to SDHIs (e.g., thifluzamide) and triazoles demands novel antifungal agents. Nineteen pyrazole-5-sulfonamide derivatives (E1 - E19) were synthesized and these antifungal activities were evaluated via in vitro EC₅₀, in vivo greenhouse assays, and mechanistic studies (scanning electron microscopy (SEM), transmission electron microscopy (TEM), reactive oxygen species (ROS), membrane integrity, and transcriptomics). These results showed that compound E10 exhibited superior in vitro anti-S. rolfsii activity (EC₅₀ = 0.53 mg/L) rivaling thifluzamide (EC₅₀ = 0.58 mg/L), and in vivo trials demonstrated E10 (200 mg/L) conferred 78.93 % protective and 75.65 % curative efficacy against peanut stem rot, comparable to thifluzamide (84.46 %/81.33 %). E10 suppressed sclerotia production and germination, disrupted hyphal ultrastructure, and induced membrane damage via ROS burst. Transcriptomics revealed E10-triggered dysregulation of oxidative phosphorylation and fatty acid degradation pathways, linking ROS-mediated lipid peroxidation to fungal death. In addition, low phytotoxicity on peanut seedlings at 200 mg/L of E10 with germination rates >85 % and no morphological abnormalities, and E10 showed low ecotoxicity (Eisenia fetida LC₅₀ > 200 mg/kg). Compound E10 demonstrated promise as a low ecological risk fungicide against S. rolfsii warranting further study.

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生物安全吡唑-5-磺胺衍生物对花生茎腐病的可持续防治

rolfsii菌核菌对全球花生生产造成15-80%的产量损失。对sdis（如硫氟唑胺）和三唑的杀菌剂耐药性需要新的抗真菌剂。合成了19种吡唑-5-磺酰胺衍生物（E1 - E19），并通过体外EC 50、体内温室实验和机制研究（扫描电镜（SEM）、透射电镜（TEM）、活性氧（ROS）、膜完整性和转录组学）对其抗真菌活性进行了评价。结果表明，化合物E10对花生茎腐病的体外抗S. rolfsii活性（EC 50 = 0.53 mg/L）优于硫氟唑胺（EC 50 = 0.58 mg/L），体内试验表明，E10 （200 mg/L）对花生茎腐病的保护效果为78.93%，治疗效果为75.65%，与硫氟唑胺（84.46%/81.33%）相当。E10抑制菌核产生和萌发，破坏菌丝超微结构，并通过ROS爆发诱导膜损伤。转录组学揭示了E10触发的氧化磷酸化和脂肪酸降解途径失调，将ros介导的脂质过氧化与真菌死亡联系起来。此外，E10在200 mg/L浓度下对花生幼苗具有较低的植物毒性，发芽率b> 85%，无形态异常，E10表现出较低的生态毒性（Eisenia fetida LC 50 > 200 mg/kg）。化合物E10作为一种具有较低生态风险的杀菌剂，值得进一步研究。•新型吡唑-5-磺酰胺E10 （EC 50 = 0.53 mg/L）可与氟唑胺对抗S. rolfsii。•E10对温室花生茎腐病防治效果好，200 mg/L时防治效果为78.93%（保护性），75.65%（治疗性）。•双重机制：E10破坏膜完整性并诱导ros介导的细胞凋亡。•E10抑制菌核的产生和萌发，以及黑色素的生物合成。•低生态毒性（蚯蚓LC 50 bb0 200 mg/kg），无植物毒性。

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来源期刊

Advanced Agrochem

CiteScore

3.50

自引率

0.00%

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