Background:

Fluensulfone is identified as a new nematicide for chemical control of plant parasitic nematodes.

Plant parasitic nematodes can infest crops and present a threat to food security. Currently available chemical controls such as methyl bromide, organophosphates as well as carbamates have an unacceptable toxicity level to non-target organisms and are being withdrawn.

In vitro: Previous study showed that the model genetic organism Caenorhabditis elegans was susceptible to the treatment of fluensulfone. While the required dose was higher than that which had nematicidal activity against Meloidogyne spp. In addition, the profile of effects on motility, egg-hatching and survival was similar to that reported for plant parasitic nematodes.C. elegans therefore provided a tractable paradigm to analyze the effects of fluensulfone on nematode behaviour. Moreover, it was also found that fluensulfone had pleiotropic actions and inhibited development, egg-laying, egg-hatching, feeding and locomotion [1].

In vivo: In mice, but not in rats, fluensulfone at high doses has shown an increased incidence of lung adenomas. Moreover, fluensulfone was not genotoxic. In addition, the administration of fluensulfone to mice resulted in an early increase in Clara cell proliferation [2].

Clinical trial: Up to now, fluensulfone is still in the preclinical development stage.

参考文献:
[1] Kearn J,Ludlow E,Dillon J,O'Connor V,Holden-Dye L.  Fluensulfone is a nematicide with a mode of action distinct from anticholinesterases and macrocyclic lactones. Pestic Biochem Physiol.2014 Feb;109:44-57.
[2] Strupp C,Banas DA,Cohen SM,Gordon EB,Jaeger M,Weber K.  Relationship of metabolism and cell proliferation to the mode of action of fluensulfone-induced mouse lung tumors: analysis of their human relevance using the IPCS framework. Toxicol Sci.2012 Jul;128(1):284-94.