Abstract
Based on the molluscicidal activity of ginkgolic acids (GAs) isolated from Ginkgo biloba L and synthetic GA analogues, a series of long chain, substituted at 4 and 5 position, salicylic acid derivatives, including the Z/E isomers and their saturated derivatives, were prepared. Their molluscicidal activities against the host snail Oncomelania hupensis were evaluated. The acute fish toxicity against the wild-type zebrafish of saturated derivatives was tested. The results and analysis of the structural-activity relationship revealed that the E-isomers and their saturated derivatives were better molluscicidal agents than their respective Z-isomers. Molluscicidal activities were increased with the growing of the alkyl chain lengths. Acute fish toxicity test indicated that the synthesized salicylic acid derivatives were much safer than niclosamide in field use. Key words: Hydrocarbyl substituted salicylic acid derivatives, synthesis, molluscicidal activity, Oncomelania hupensis, schistosomiasis, acute fish toxicity, zebrafish.
Highlights
Schistosomiasis is one of the most prevalent of the tropical infectious diseases with more than 200 million people infected globally and close to 800 million at risk (Steinmann et al, 2006)
The niclosamide is the only commercially available molluscicide recommended by the World Health
We study the molluscicidal effects of a series of Z/E isomers of Ginkgolic acids (GAs) analogues with different chain lengths (5 to 13 carbon atoms) and phenyl rings and find that the E-isomers are better molluscicidal agents than their respective Z-isomers and molluscicidal activity is found to decrease regularly with the shortening of the alkyl chain lengths (Zhang et al, 2011)
Summary
Schistosomiasis is one of the most prevalent of the tropical infectious diseases with more than 200 million people infected globally and close to 800 million at risk (Steinmann et al, 2006). In China, zoonotic schistosomiasis, caused by Schistosoma japonicum, is a chronic debilitating disease in the south, with 325,824 infected in 2010 (Lei et al, 2011) and 65 million people at risk of infection (Zhou et al, 2005; McManus et al, 2010). The snail, Oncomelania hupensis, is the main agent responsible for the transmission of this disease. Snail control can be a powerful intervention tool as it essentially removes the intermediate host from the parasite’s life cycle, breaking transmission (Fong, 2013). China is facing a new challenge because schistosomiasis has reemerged in some regions due to an addition in habitats suitable for the snails, including increased flood areas and large water resource development projects (Yuan et al, 2005).
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