Roohparvar Ramin, Huser Aurelie, Zwiers Lute-Harm, De Waard Maarten A
Laboratory of Phytopathology, Wageningen University, Wageningen, The Netherlands.
Appl Environ Microbiol. 2007 Aug;73(15):5011-9. doi: 10.1128/AEM.00285-07. Epub 2007 Jun 1.
Medical drugs known to modulate the activity of human ATP-binding cassette (ABC) transporter proteins (modulators) were tested for the ability to potentiate the activity of the azole fungicide cyproconazole against in vitro growth of Mycosphaerella graminicola and to control disease development due to this pathogen on wheat seedlings. In vitro modulation of cyproconazole activity could be demonstrated in paper disk bioassays. Some of the active modulators (amitriptyline, flavanone, and phenothiazines) increased the accumulation of cyproconazole in M. graminicola, suggesting that they reversed cyproconazole efflux. However, synergism between cyproconazole and modulators against M. graminicola on wheat seedlings could not be shown. Despite their low in vitro toxicity to M. graminicola, some modulators (amitriptyline, loperamide, and promazine) did show significant intrinsic disease control activity in preventive and curative foliar spray tests with wheat seedlings. The results suggest that these compounds have indirect disease control activity based on modulation of fungal ABC transporters essential for virulence and constitute a new class of disease control agents.
已知可调节人类ATP结合盒（ABC）转运蛋白活性的药物（调节剂），被测试其增强唑类杀菌剂环丙唑醇对小麦壳针孢体外生长的活性，以及控制该病原菌对小麦幼苗致病发展的能力。在纸片扩散生物测定中可证明环丙唑醇活性的体外调节。一些活性调节剂（阿米替林、黄烷酮和吩噻嗪）增加了环丙唑醇在小麦壳针孢中的积累，表明它们逆转了环丙唑醇的外排。然而，未显示环丙唑醇与调节剂对小麦幼苗上的小麦壳针孢有协同作用。尽管一些调节剂（阿米替林、洛哌丁胺和丙嗪）对小麦壳针孢的体外毒性较低，但在对小麦幼苗进行的预防性和治疗性叶面喷雾试验中，它们确实显示出显著的内在病害防治活性。结果表明，这些化合物基于对毒力至关重要的真菌ABC转运蛋白的调节而具有间接病害防治活性，并构成了一类新的病害防治剂。
