Yangyang Gao1,2, Lifei He1,2, Jiamei Zhu1,2, Jiagao Cheng3, Beixing Li1,2, Feng Liu1,2, Wei Mu1,2. 1. Shandong Provincial Key Laboratory for Biology of Vegetable Diseases and Insect Pests, Shandong Agricultural University, Tai'an, P.R. China. 2. College of Plant Protection, Shandong Agricultural University, Tai'an, P.R. China. 3. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai, China.
Abstract
BACKGROUND: A new generation of succinate dehydrogenase inhibitors (SDHIs) with high efficiency and broad-spectrum antifungal activity has been frequently used in crop production. Sclerotinia stem rot is a major disease of various plants and crops caused by Sclerotinia sclerotiorum. Although benzovindiflupyr and isopyrazam reportedly have high activity against S. sclerotiorum, little is known about the bioactivity of different SDHIs classes against S. sclerotiorum or the mechanism of their differential antifungal activity. RESULTS: The in vitro tests revealed that the pyrazole-4-carboxamides of SDHIs (benzovindiflupyr, isopyrazam, fluxapyroxad, pydiflumetofen) had the highest activity against S. sclerotiorum followed by pyridine carboxamides (boscalid), pyridinyl-ethyl benzamides (fluopyram) and thiazole carboxamides (thifluzamide), and of these thifluzamide showed poor antifungal activity with EC50 values greater than 6.01 mg L-1 . The pyrazole-4-carboxamides of SDHIs showed satisfactory protective and curative activity against Sclerotinia stem rot. After treatment with the pyrazole-4-carboxamides of SDHIs, mitochondrial function in S. sclerotiorum decreased significantly. The enzyme activity assays revealed a lower affinity between thifluzamide and the Sc-Sdh complex than was observed for the other six fungicides, with IC50 values ranging from 0.0036 to 1.2088 μmol L-1 . Additionally, the docking positions of fungicides were similar, yet binding energies were different in the docking study with the Sdh complex. The correspondingly weaker hydrogen bonds may be responsible for the poor activity of thifluzamide against S. sclerotiorum. CONCLUSION: Understanding different binding features of various SDHIs classes with the Sc-Sdh complex might be beneficial for the design and development of highly effective broad-spectrum fungicides to ensure high yield and quality in crops by reducing fungicide use.
BACKGROUND: A new generation of succinate dehydrogenase inhibitors (SDHIs) with high efficiency and broad-spectrum antifungal activity has been frequently used in crop production. Sclerotinia stem rot is a major disease of various plants and crops caused by Sclerotinia sclerotiorum. Although benzovindiflupyr and isopyrazam reportedly have high activity against S. sclerotiorum, little is known about the bioactivity of different SDHIs classes against S. sclerotiorum or the mechanism of their differential antifungal activity. RESULTS: The in vitro tests revealed that the pyrazole-4-carboxamides of SDHIs (benzovindiflupyr, isopyrazam, fluxapyroxad, pydiflumetofen) had the highest activity against S. sclerotiorum followed by pyridine carboxamides (boscalid), pyridinyl-ethyl benzamides (fluopyram) and thiazole carboxamides (thifluzamide), and of these thifluzamide showed poor antifungal activity with EC50 values greater than 6.01 mg L-1 . The pyrazole-4-carboxamides of SDHIs showed satisfactory protective and curative activity against Sclerotinia stem rot. After treatment with the pyrazole-4-carboxamides of SDHIs, mitochondrial function in S. sclerotiorum decreased significantly. The enzyme activity assays revealed a lower affinity between thifluzamide and the Sc-Sdh complex than was observed for the other six fungicides, with IC50 values ranging from 0.0036 to 1.2088 μmol L-1 . Additionally, the docking positions of fungicides were similar, yet binding energies were different in the docking study with the Sdh complex. The correspondingly weaker hydrogen bonds may be responsible for the poor activity of thifluzamide against S. sclerotiorum. CONCLUSION: Understanding different binding features of various SDHIs classes with the Sc-Sdh complex might be beneficial for the design and development of highly effective broad-spectrum fungicides to ensure high yield and quality in crops by reducing fungicide use.
Authors: Celeste de Jesus Pereira Franco; Oberdan Oliveira Ferreira; Jorddy Neves Cruz; Everton Luiz Pompeu Varela; Ângelo Antônio Barbosa de Moraes; Lidiane Diniz do Nascimento; Márcia Moraes Cascaes; Antônio Pedro da Silva Souza Filho; Rafael Rodrigues Lima; Sandro Percário; Mozaniel Santana de Oliveira; Eloisa Helena de Aguiar Andrade Journal: Molecules Date: 2022-07-22 Impact factor: 4.927