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In Vitro Nematicidal Activity of Aryl Hydrazones and Comparative GC-MS Metabolomics Analysis

机译:芳基Hy的体外杀线虫活性和比较GC-MS代谢组学分析

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A series of aryl hydrazones were synthesized and in vitro assayed for their activity on the root-knot nematode Meloidogyne incognita. The phenylhydrazones of thiophene-2-carboxyaldehyde 5, 3-methyl-2-thiophenecarboxyaldehyde, 6, and salicylaldehyde, 2, were the most potent with EC50/48h values of 16.6 +/- 2.2, 23.2 +/- 2.7, and 24.3 +/- 1.4 mg/L, respectively. A GC-MS metabolomics analysis, after in vitro nematode treatment with hydrazone 6 at 100 mg/L for 12 h, revealed elevated levels of fatty acids such as lauric acid, stearic acid, 2-octenoic acid, and palmitic acid. Whereas control samples showed the highest levels of monoacylglycerols such as monostearin and 2-monostearin, surprisingly, 2 h after treatment with hydrazone 6, nematodes excreted 3 times the levels of ammonia eliminated in the same conditions by controls. Thus, phenylhydrazones may represent a good scaffold in the discovery and synthesis of new nematicidal compounds, and a metabolomics approach may be helpful in understanding their mechanisms of toxicity and mode of action.
机译:合成了一系列芳基,并体外分析了它们对根结线虫Meloidogyne incognita的活性。噻吩-2-羧醛5、3-甲基-2-噻吩羧醛6和水杨醛2的苯hydr最有效,EC50 / 48h值为16.6 +/- 2.2、23.2 +/- 2.7和24.3 +分别为1.4 mg / L。在用100 mg / L的,6进行体外线虫处理12 h后,GC-MS代谢组学分析显示,脂肪酸水平升高,如月桂酸,硬脂酸,2-辛烯酸和棕榈酸。对照样品显示出单酰基甘油(例如单硬脂精和2-单硬脂精)的最高含量,令人惊讶的是,在用6,6处理2小时后,线虫的排泄量是对照中在相同条件下消除的氨水平的3倍。因此,苯hydr在新的杀线虫化合物的发现和合成中可能是一个很好的支架,而代谢组学方法可能有助于理解它们的毒性机制和作用方式。

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