Design, Synthesis, and Cercaricidal Activity of Novel High‐efficient, Low‐toxic Self‐spreading <scp>PEG</scp>‐<i>N</i>‐salicylanilide Derivatives Against Cercariae Larvae of <i>Schistosome Japonicum</i> Floating on the Water Surface

Guo, Wei; Zheng, Lvyin; Wu, Ren-Miao; Fan, Xiaolin

doi:10.1111/cbdd.12439

Cited by 5 publications

(4 citation statements)

References 17 publications

(19 reference statements)

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“…Six species of the genus Schistosoma including S. japonicum , S. mansoni , S. haematobium , S. mekongi , S. malayensis , and S. intercalatum can cause disease in people (Gryseels et al 2006 ). The life cycle of the parasite is complex with an intermediate host ( Oncomelania snails), definitive host (humans and mammals), and seven lifecycle stages involving the adult worm, egg, miracidium, mother sporocyst, daughter sporocyst, cercariae, and schistosomulum (Colley et al 2014 ; Guo et al 2008 , 2015 ). It is a great challenge to control schistosomiasis in undeveloped regions because of financial burden and environmental pressures.…”

Section: Introductionmentioning

confidence: 99%

Molluscicides against the snail-intermediate host of Schistosoma: a review

et al. 2021

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Schistosomiasis, a neglected tropical disease (NTD), is one of the most prevalent parasitoses in the World. Certain freshwater snail species are the intermediate host in the life cycle of schistosome species. Controlling snails employing molluscicides is an effective, quick, and convenient intervention strategy to prevent the spread of Schistosoma species in endemic regions. Advances have been made in developing both synthetic molluscicides and molluscicides derived from plants. However, at present, the development of molluscicides is not adapted to the actual demand for snails and schistosoma controlling. We undertake a systematic review of exploitation and application of synthetic molluscicides and molluscicides derived from plants to combat intermediate host snails. The detailed molluscicidal activity, structure–activity relationship, structural feature, and possible mechanism of some molluscicides are also highlighted, which may afford an important reference for the design of new, more effective molluscicides with low environmental impact and realize the aim of controlling schistosome at transmission stages. Supplementary Information The online version contains supplementary material available at 10.1007/s00436-021-07288-4.

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Section: Introductionmentioning

confidence: 99%

Molluscicides against the snail-intermediate host of Schistosoma: a review

et al. 2021

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“…It exhibited strong to moderate cytotoxicity on several human cell lines (12,13). In the last 2 decades, most of the modifications of niclosamide have focused on improving its solubility by altering formulations (e.g., as wettable powder, suspension concentrate, and polymeric controlled-release formulations) (14)(15)(16)(17) or by linking it with surfactants (e.g., polyethylene glycols [PEGs]) (18)(19)(20)(21). To the best of our knowledge, little effort has been made to reduce its toxicity through structure modification.…”

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confidence: 99%

Synthesis, Bioactivity Evaluation, and Toxicity Assessment of Novel Salicylanilide Ester Derivatives as Cercaricides against Schistosoma japonicum and Molluscicides against Oncomelania hupensis

Wang

Qin

Zhu

et al. 2016

Antimicrob Agents Chemother

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A series of novel salicylanilide ester derivatives were synthesized, characterized, and evaluated for cercaricidal potential against Schistosoma japonicum and molluscicidal potential against Oncomelania hupensis. Four derivatives exhibited remarkable cercaricidal activity superior to that of niclosamide. Among them, the most active compound, 4-chloro-2-((2-methoxy-4-nitrophenyl)carbamoyl)phenyl 4-methoxybenzoate (compound 4c), showed a marked minimum effective cercaricidal concentration as low as 0.43 M and significant molluscicidal activity, with a 50% lethal concentration (LC 50 ) of 0.206 g/m 2 . Particularly, compound 4c displayed 88-fold decreased fish toxicity on Danio rerio and 44-fold reduced cytotoxicity on human kidney HEK293 cells in comparison with the toxicity of niclosamide. The results indicated that 4c could serve as a promising drug candidate, with environmental safety properties, against Schistosoma japonicum at transmission stages. The preliminary molecular mechanism of target compounds in Schistosoma japonicum cercariae was also investigated. Salicylanilide ester derivatives exhibited an inhibitory effect on nitric oxide synthase (NOS) but no effect on lactate dehydrogenase (LDH) and acetylcholinesterase (AChE), and a strong and significant correlation between NOS inhibitory efficacy and cercaricidal activity was observed. In addition, 4c could downregulate the expression of NOS in a dose-dependent manner. These results suggested that NOS was probably one of the drug targets of salicylanilide esters. S chistosomiasis japonica, caused by infection withSchistosoma japonicum, is recognized as a considerable economic and public health concern in Asia, including China, Indonesia, and the Philippines (1-3). According to estimates, over 58 million people are infected (4). Schistosome infection occurs through contact with water contaminated by cercariae, the free-living stage of the parasite shed from intermediate host Oncomelania snails (5). Although praziquantel is available for treatment, there is the fact that it cannot prevent individuals from reinfection. Repeated and intense exposure to cercariae could lead to an ineffective response of early-stage chronic cases in routine control programs, which would increase the risk of infections progressing to an advanced stage. A successful control program of the disease should be constructed as an integrated control scheme including cercaricidal methods, snail control programs, and chemotherapy.Niclosamide has a long track record as a successful molluscicide against Oncomelania snails (6, 7). Moreover, it is effective for cercaria control both under laboratory conditions and in field experiments (8-10). However, niclosamide has relatively poor solubility in water and is a well-known environmentally hazardous chemical. It has been proved highly toxic to 18 species of fish (11). It exhibited strong to moderate cytotoxicity on several human cell lines (12, 13). In the last 2 decades, most of the modifications of niclosamide have focused on improving its so...

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“…Schistosoma cercariae are (a non-feeding infective stage) penetrate and reproduce within a host of the class Mammalia [20]. Among the species of Schistosoma which may infect humans, the most harmful are Schistosoma mansoni , Schistosoma japonicum and Schistosoma haematobium , which together comprise over 95% of human infections [25].…”

Section: Introductionmentioning

confidence: 99%

Comparative study of excretory–secretory proteins released by Schistosoma mansoni-resistant, susceptible and naïve Biomphalaria glabrata

et al. 2019

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Background Schistosomiasis is a harmful neglected tropical disease caused by infection with Schistosoma spp., such as Schistosoma mansoni. Schistosoma must transition within a molluscan host to survive. Chemical analyses of schistosome-molluscan interactions indicate that host identification involves chemosensation, including naïve host preference. Proteomic technique advances enable sophisticated comparative analyses between infected and naïve snail host proteins. This study aimed to compare resistant, susceptible and naïve Biomphalaria glabrata snail-conditioned water (SCW) to identify potential attractants and deterrents. Methods Behavioural bioassays were performed on S. mansoni miracidia to compare the effects of susceptible, F1 resistant and naïve B. glabrata SCW. The F1 resistant and susceptible B. glabrata SCW excretory–secretory proteins (ESPs) were fractionated using SDS-PAGE, identified with LC-MS/MS and compared to naïve snail ESPs. Protein-protein interaction (PPI) analyses based on published studies (including experiments, co-expression, text-mining and gene fusion) identified S. mansoni and B. glabrata protein interaction. Data are available via ProteomeXchange with identifier PXD015129. Results A total of 291, 410 and 597 ESPs were detected in the susceptible, F1 resistant and naïve SCW, respectively. Less overlap in ESPs was identified between susceptible and naïve snails than F1 resistant and naïve snails. F1 resistant B. glabrata ESPs were predominately associated with anti-pathogen activity and detoxification, such as leukocyte elastase and peroxiredoxin. Susceptible B. glabrata several proteins correlated with immunity and anti-inflammation, such as glutathione S-transferase and zinc metalloproteinase, and S. mansoni sporocyst presence. PPI analyses found that uncharacterised S. mansoni protein Smp_142140.1 potentially interacts with numerous B. glabrata proteins. Conclusions This study identified ESPs released by F1 resistant, susceptible and naïve B. glabrata to explain S. mansoni miracidia interplay. Susceptible B. glabrata ESPs shed light on potential S. mansoni miracidia deterrents. Further targeted research on specific ESPs identified in this study could help inhibit B. glabrata and S. mansoni interactions and stop human schistosomiasis.

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Design, Synthesis, and Cercaricidal Activity of Novel High‐efficient, Low‐toxic Self‐spreading PEG‐N‐salicylanilide Derivatives Against Cercariae Larvae of Schistosome Japonicum Floating on the Water Surface

Cited by 5 publications

References 17 publications

Molluscicides against the snail-intermediate host of Schistosoma: a review

Molluscicides against the snail-intermediate host of Schistosoma: a review

Synthesis, Bioactivity Evaluation, and Toxicity Assessment of Novel Salicylanilide Ester Derivatives as Cercaricides against Schistosoma japonicum and Molluscicides against Oncomelania hupensis

Comparative study of excretory–secretory proteins released by Schistosoma mansoni-resistant, susceptible and naïve Biomphalaria glabrata

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