咪唑
抗真菌
抗真菌药
化学
药理学
组合化学
有机化学
微生物学
生物
作者
Madhu Tippannanavar,Ankita Verma,Rajesh Kumar,Robin Gogoi,Aditi Kundu,Neeraj Patanjali
标识
DOI:10.1021/acs.jafc.9b06387
摘要
In spite of modern crop protection measures, the overall crop losses due to pests and pathogens are huge. Rhizoctonia solani, Macrophomina phaseolina, Sclerotium rolfsii, and Fusarium oxysporum are one of the most devastating soil-borne fungi and cause numerous plant diseases. Therefore, the present study aimed to systematically design and develop new nanofungicides based on imidazole drugs, clotrimazole, econazole nitrate, and miconazole nitrate, for effective and efficient management of plant diseases. The assessment of these antifungal medicines for their fungicide likeness using Hao's rule and their enzyme inhibitory potential by molecular docking was helpful in ensuring their utility as antifungal agents in managing phytopathogenic fungi. Nanotechnological strategies were used to develop nanoformulations of test compounds in poly(ethylene glycol) 300 for further augmenting their bioactivity. Transmission electron microscopy studies confirmed the nanosize of the prepared products. Analysis of their in vitro and in vivo antifungal properties revealed their usefulness in controlling the test fungi, R. solani, M. phaseolina, S. rolfsii, and F. oxysporum. Excellent in vitro antifungal activities were displayed by the clotrimazole nanoformulation with a median effective dose (ED50) of 1.18 μg/mL against R. solani, the econazole nitrate nanoformulation with an ED50 of 5.25 μg/mL against S. rolfsii, and the miconazole nitrate nanoformulation with an ED50 of 1.49 and 1.82 μg/mL against M. phaseolina and F. oxysporum. Furthermore, in vivo studies against test fungi demonstrated the antifungal potency of all the nanoformulations with disease incidences ranging from 11.11 to 27.38% in plants treated with nanoformulations of test chemicals as compared to the inoculated control (39.68-72.38%).
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