Key Laboratory of Crop Integrated Pest Management in South China, Ministry of Agriculture, South China Agricultural University, Guangzhou 510642, China.
Int J Mol Sci. 2018 Dec 14;19(12):4044. doi: 10.3390/ijms19124044.
Rice sheath blight, caused by , is a globally important rice disease and the increasing resistance of this pathogen highlights the need for new active compounds against rice sheath blight. In this study, natural -carboline alkaloids were optimized to obtain a series of 1,2,4,9-tetrahydro-3-thia-9-aza-fluorene derivatives and evaluated for their fungicidal activity and mode of action against . Of these compounds, exhibited significant in vitro fungicidal activity against , with an EC value of 2.35 μg/mL, and was more active than validamycin A. In vivo bioassay also demonstrated that displayed superior protective and curative activities as compared to validamycin A. Mechanistically, not only induced the loss of mitochondrial membrane potential and accumulation of reactive oxygen species, but also interfered with DNA synthesis. Therefore, compound displayed pronounced in vitro and in vivo fungicidal activity against and could be used as a potential candidate for the control of rice sheath blight.
稻纹枯病由引起，是一种全球性重要的水稻病害，该病原菌的抗药性不断增强，凸显了开发防治稻纹枯病新活性化合物的必要性。在本研究中，对天然 - 咔啉生物碱进行了优化，得到了一系列 1,2,4,9-四氢-3-硫-9-氮杂-芴衍生物，并评估了它们对的杀菌活性和作用模式。在这些化合物中，表现出对的显著体外杀菌活性，EC 值为 2.35 μg/mL，活性优于井冈霉素 A。体内生物测定也表明，与井冈霉素 A 相比，表现出更好的保护和治疗活性。在机制上，化合物不仅诱导了线粒体膜电位的丧失和活性氧的积累，还干扰了 DNA 的合成。因此，化合物对表现出明显的体外和体内杀菌活性，可作为防治稻纹枯病的潜在候选药物。
