文献类型：期刊文献

英文题名：Formononetin derivatives containing benzyl piperidine: A brand new, highly efficient inhibitor targeting Xanthomonas spp

作者：Zhang, Miaohe Feng, Shuang Song, Junrong Ruan, Xianghui Xue, Wei

第一作者：Zhang, Miaohe;张妙鹤

通信作者：Ruan, XH[1];Xue, W[1]

机构：[1]Guizhou Univ, State Key Lab Green Pesticide, Key Lab Green Pesticide & Agr Bioengn, Minist Educ,Ctr R&D Fine Chem, Guiyang 550025, Peoples R China;[2]Guizhou Inst Technol, Sch Chem Engn, Guiyang 550025, Peoples R China;[3]Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China;[4]Nat Prod Res Ctr Guizhou Prov, Guiyang 550014, Peoples R China

第一机构：Guizhou Univ, State Key Lab Green Pesticide, Key Lab Green Pesticide & Agr Bioengn, Minist Educ,Ctr R&D Fine Chem, Guiyang 550025, Peoples R China

通信机构：corresponding author), Guizhou Univ, State Key Lab Green Pesticide, Key Lab Green Pesticide & Agr Bioengn, Minist Educ,Ctr R&D Fine Chem, Guiyang 550025, Peoples R China.

年份：2025

卷号：73

起止页码：133-146

外文期刊名：JOURNAL OF ADVANCED RESEARCH

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001519098700005)】；

基金：Authors gratefully acknowledge the Science Foundation of Guizhou Province (No. ZK2024008) , the Key Research and Development Program of Hainan Province (No. ZDYF2024XDNY202) , the academic new seedling cultivation and exploration and innovation project of Guizhou Institute of Technology (No. GZLGXM-20) , the Young Science and Technology Talents Development Program of Education Department of Guizhou Province (No. KY2022346) .

语种：英文

外文关键词：Formononetin derivatives; Antibacterial activities; Virulence factors; Defense enzymes activities; Proteomics; Metabolomics

摘要：Introduction: Plant bacterial diseases take an incalculable toll on global food security. The indiscriminate use of chemical synthetic pesticide not only facilitates pathogen resistance of pathogenic bacteria, but also poses a major threat to human health and environmental protection. Therefore, it is of great economic value and scientific significance to develop a new antibacterial drug with environmental friendliness and unique mechanism of action. Objectives: To design and synthesize formononetin derivatives based on natural products, evaluate their in vitro and in vivo antibacterial activities and elucidate the mechanisms involved. Methods: The synthesis was carried out by classical active group splicing method. The antibacterial activities were evaluated using turbidimetry and pot experiments. The antibacterial mechanism was further investigated using scanning electron microscopy (SEM), virulence factors, defense enzymes activities, proteomics and metabolomics. Results: 40 formononetin derivatives containing benzyl piperidine were designed and synthesized. The antibacterial results demonstrated that H32 exhibited the most potent inhibitory effect against Xanthomonas oryzae pv. Oryzae (Xoo) with the EC50 of 0.07 lg/mL, while H6 displayed the highest inhibitory activity against Xanthomonas axonopodis pv. Citri (Xac) with the EC50 of 0.24 lg/mL. Furthermore, the control efficacy of H32 against rice bacterial leaf blight (BLB) and H6 against citrus canker (CC) was validated through pot experiments. SEM, virulence factors and host enzyme activities assay indicated that H32 could not only reduce the virulence of Xoo, but also activate the activities of defense enzymes and improve the disease resistance of host plants. The proteomics and metabolomics analysis demonstrated that H32 could inhibit the synthesis of branched-chain amino acids, make Xoo cells in a starvation state, inhibit its proliferation, weaken its virulence and reduce its colonization and infection of host cells. Conclusion: Formononetin derivatives containing benzyl piperidine could be used as potentially effective inhibitors against Xanthomonas spp. (c) 2024 The Authors. Published by Elsevier B.V. on behalf of Cairo University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).