Exploring boron applications in modern agriculture: Antifungal activities and mechanisms of phenylboronic acid derivatives

Abstract

Background The unreasonable use of chemical fungicides causes common adverse consequences that not only affect the environment, but also cause resistance and resurgence problems of plant pathogens, which are extremely harmful to human health, the economy, and the environment. Based on the rich biological activities of boron‐based compounds, 82 phenylboronic acid derivatives were selected and their antifungal activities against six agricultural plant pathogens were determined. Combined with transcriptomics tools, the mechanism of action of compound A49 (2‐chloro‐5‐trifluoromethoxybenzeneboronic acid) against Botrytis cinerea Pers (B. cinerea) was studied. Results The EC50 values of compounds A24, A25, A30, A31, A36, A41, A49 and B23 against all six fungi were under 10 μg/mL. Compound A49 displayed significant activity against B. cinerea (EC50 = 0.39 μg/mL), which was better than that of commercial fungicide boscalid (EC50 = 0.55 μg/mL). A49 not only inhibited the germination of B. cinerea spores, but also caused abnormal cell morphology, loss of cell membrane integrity, enhanced cell membrane permeability, and accumulation of intracellular reactive oxygen species. Further findings showed that A49 reduced cellular antioxidant activity, and peroxidase and catalase activities. Transcriptomic results indicated that A49 could degrade intracellular redox processes and alter the metabolism of some amino acids. Meanwhile, A49 showed obvious activity in vivo and low cytotoxicity to mammal cells. Conclusion The boron‐containing small molecule compounds had high efficiency and broad‐spectrum antifungal activities against six plant pathogens, and are expected to be candidate compounds for a new class of antifungal drugs. © 2023 Society of Chemical Industry.

Oxidative, Genotoxic and Cytotoxic Damage Potential of Novel Borenium and Borinium Compounds

“…Despite the vast body of scientific evidence, it has not been conclusively reported that B is necessary for both humans and animals. In fact, several BCCs, such as borates, boronates, and boronic acids, exhibited interesting biological activities, including antiviral [2], antibacterial [3,4], antifungal and antiparasitic [5,6], antioxidant [7,8], wound healing [9], anti-inflammatory [10,11], antimutagenic [12], anticancerogenic [13,14], radiobiological [15], and neuroprotective properties [16,17]. Interestingly it was found that people living in B-rich regions had less cancer incidence than the people living in B-poor regions [18].…”