Caboni Pierluigi, Tronci Laura, Liori Barbara, Tocco Graziella, Sasanelli Nicola, Diana Andrea
Department of Life and Environmental Sciences, University of Cagliari, via Ospedale 72, 09124 Cagliari, Italy.
Department of Life and Environmental Sciences, University of Cagliari, via Ospedale 72, 09124 Cagliari, Italy.
Pestic Biochem Physiol. 2014 Jun;112:33-9. doi: 10.1016/j.pestbp.2014.05.002. Epub 2014 May 23.
Carbonyl groups are known to form covalent adducts with endogenous proteins, but so far, their nematicidal mechanism of action of has been overlooked. The nematicidal activity of ten lactones was tested in vitro against the root knot nematodes Meloidogyne incognita and Meloidogynearenaria. In particular, the saturated lactones α-methylene-γ-butyrolactone or tulipaline A (1) and γ-butyrolactone (3) were active against M. incognita with an EC50/48h of 19.3±10.0 and 40.0±16.2mg/L respectively. Moreover the α, β-unsaturated lactone 5,6-dihydro-2H-pyran-2-one (2) exhibited the strongest nematicidal activity against the two species with EC50/48h 14.5±5.3 and 21.2±9.7mg/L respectively. Here we propose that the toxic effects of lactones and aldehydes on M.incognita and M. arenaria might be a consequence of their vacuolar-type H(+)-ATPase (V-ATPase) inhibition activity; in fact α-methylene-γ-butyrolactone (1) and salicylaldehyde (12) produced an increased pH in lysosomal-like organelles on HeLa human cell line and this alteration was most likely related to a V-ATPase impairment.
已知羰基会与内源性蛋白质形成共价加合物，但迄今为止，它们的杀线虫作用机制一直被忽视。测试了十种内酯对根结线虫南方根结线虫和花生根结线虫的体外杀线虫活性。特别是，饱和内酯α-亚甲基-γ-丁内酯或郁金香素A（1）和γ-丁内酯（3）对南方根结线虫有活性，48小时的半数有效浓度（EC50）分别为19.3±10.0和40.0±16.2mg/L。此外，α，β-不饱和内酯5,6-二氢-2H-吡喃-2-酮（2）对这两个物种表现出最强的杀线虫活性，48小时的EC50分别为14.5±5.3和21.2±9.7mg/L。在此我们提出，内酯和醛对南方根结线虫和花生根结线虫的毒性作用可能是它们抑制液泡型H(+)-ATP酶（V-ATP酶）活性的结果；事实上，α-亚甲基-γ-丁内酯（1）和水杨醛（12）使HeLa人细胞系中溶酶体样细胞器的pH值升高，这种变化很可能与V-ATP酶受损有关。
