McKee Mary L, Zheng Limian, O'Sullivan Elaine C, Kehoe Roberta A, Doyle Prestwich Barbara M, Mackrill John J, McCarthy Florence O
School of Chemistry and Analytical and Biological Chemistry Research Facility, University College Cork, Western Road, Cork T12 K8AF, Ireland.
Department of Physiology, School of Medicine, University College Cork, Western Road, Cork T12 K8AF, Ireland.
Pathogens. 2020 Jul 10;9(7):558. doi: 10.3390/pathogens9070558.
The pathogen is responsible for worldwide catastrophic crop damage and discovery of new inhibitors of this organism is of paramount agricultural and industrial importance. Current strategies for crop treatment are inadequate with limitations of efficacy and market alternatives. Ellipticines have recently been reported to have fungicidal properties and have been assessed against growth with promising results. We hereby report a probe of the ellipticine framework to investigate the alkyl subunit and screen a set ellipticines and derivatives to identify new lead compounds to act against . A series of ellipticinium salt derivatives have been identified with exceptional growth inhibitory activity and apparent lack of toxicity towards a human cell-line surpassing the effect of known and marketed fungicides. This report identifies the potential of this natural product derivative as a novel fungicide.
该病原体导致了全球范围内灾难性的作物损害，发现针对这种生物体的新抑制剂具有至关重要的农业和工业意义。当前的作物处理策略存在不足，在功效和市场替代品方面都有局限性。最近有报道称椭圆玫瑰树碱具有杀菌特性，并已针对其生长进行评估，结果很有前景。我们在此报告对椭圆玫瑰树碱骨架进行的一项探索，以研究烷基亚基，并筛选一组椭圆玫瑰树碱及其衍生物，以鉴定针对该病原体的新先导化合物。已鉴定出一系列椭圆玫瑰树碱盐衍生物，它们具有卓越的生长抑制活性，且对人类细胞系明显无毒性，其效果超过了已知的市售杀菌剂。本报告确定了这种天然产物衍生物作为新型杀菌剂的潜力。
