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Schistosomiasis control using piplartine against Biomphalaria glabrata at different developmental stages.

Rapado LN, Pinheiro Ade S, Lopes PO, Fokoue HH, Scotti MT, Marques JV, Ohlweiler FP, Borrely SI, Pereira CA, Kato MJ, Nakano E, Yamaguchi LF - PLoS Negl Trop Dis (2013)

Bottom Line: These results indicated that the high molluscicidal activity displayed by root extracts (LC50 20.28 µg/ml) was due to the presence of piplartine, a well-known biologically-active amide.The toxicity to these organisms was less compared with the toxicity of niclosamide, a commercial molluscicide.Thus, piplartine is a potential candidate for a natural molluscicide that has been extracted from a tropical plant species and showed less toxic to environment.

View Article: PubMed Central - PubMed

Affiliation: Laboratório de Parasitologia, Instituto Butantan, São Paulo, Brazil.

ABSTRACT

Background: Schistosomiasis is one of the most significant diseases in tropical countries and affects almost 200 million people worldwide. The application of molluscicides to eliminate the parasite's intermediate host, Biomphalaria glabrata, from infected water supplies is one strategy currently being used to control the disease. Previous studies have shown a potent molluscicidal activity of crude extracts from Piper species, with extracts from Piper tuberculatum being among the most active.

Methods and findings: The molluscicidal activity of P. tuberculatum was monitored on methanolic extracts from different organs (roots, leaves, fruit and stems). The compounds responsible for the molluscicidal activity were identified using (1)H NMR and ESIMS data and multivariate analyses, including principal component analysis and partial least squares. These results indicated that the high molluscicidal activity displayed by root extracts (LC50 20.28 µg/ml) was due to the presence of piplartine, a well-known biologically-active amide. Piplartine was isolated from P. tuberculatum root extracts, and the molluscicidal activity of this compound on adults and embryos of B. glabrata was determined. The compound displayed potent activity against all developmental stages of B. glabrata. Next, the environmental toxicity of piplartine was evaluated using the microcrustacean Daphnia similis (LC50 7.32 µg/ml) and the fish Danio rerio (1.69 µg/ml). The toxicity to these organisms was less compared with the toxicity of niclosamide, a commercial molluscicide.

Conclusions: The development of a new, natural molluscicide is highly desirable, particularly because the commercially available molluscicide niclosamide is highly toxic to some organisms in the environment (LC50 0.25 µg/ml to D. similis and 0.12 µg/ml to D. rerio). Thus, piplartine is a potential candidate for a natural molluscicide that has been extracted from a tropical plant species and showed less toxic to environment.

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Related in: MedlinePlus

Calculated (squares) and predicted (circles) PLS data.These data were generated from ESIMS data, versus measured and autoscaled LC50 values of P. tuberculatum extracts for B. glabrata.
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pntd-0002251-g001: Calculated (squares) and predicted (circles) PLS data.These data were generated from ESIMS data, versus measured and autoscaled LC50 values of P. tuberculatum extracts for B. glabrata.

Mentions: The PLS results from the ESIMS data generated significant coefficients of determination and values of internal prediction (0.98 and 0.83, respectively); however, only four samples were analyzed in this study. Figure 1 shows the experimental LC50 values and the predictions of the model. From the scores and correlation loadings plot in Figure S5, it was determined that quasi-molecular ions with m/z ratios of 221, 222, 340 and 341 (highly represented in root extracts) inversely correlate with their LC50 values, which indicate that these quasi-molecular ions are the major contributors to root extract activity.


Schistosomiasis control using piplartine against Biomphalaria glabrata at different developmental stages.

Rapado LN, Pinheiro Ade S, Lopes PO, Fokoue HH, Scotti MT, Marques JV, Ohlweiler FP, Borrely SI, Pereira CA, Kato MJ, Nakano E, Yamaguchi LF - PLoS Negl Trop Dis (2013)

Calculated (squares) and predicted (circles) PLS data.These data were generated from ESIMS data, versus measured and autoscaled LC50 values of P. tuberculatum extracts for B. glabrata.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3675008&req=5

pntd-0002251-g001: Calculated (squares) and predicted (circles) PLS data.These data were generated from ESIMS data, versus measured and autoscaled LC50 values of P. tuberculatum extracts for B. glabrata.
Mentions: The PLS results from the ESIMS data generated significant coefficients of determination and values of internal prediction (0.98 and 0.83, respectively); however, only four samples were analyzed in this study. Figure 1 shows the experimental LC50 values and the predictions of the model. From the scores and correlation loadings plot in Figure S5, it was determined that quasi-molecular ions with m/z ratios of 221, 222, 340 and 341 (highly represented in root extracts) inversely correlate with their LC50 values, which indicate that these quasi-molecular ions are the major contributors to root extract activity.

Bottom Line: These results indicated that the high molluscicidal activity displayed by root extracts (LC50 20.28 µg/ml) was due to the presence of piplartine, a well-known biologically-active amide.The toxicity to these organisms was less compared with the toxicity of niclosamide, a commercial molluscicide.Thus, piplartine is a potential candidate for a natural molluscicide that has been extracted from a tropical plant species and showed less toxic to environment.

View Article: PubMed Central - PubMed

Affiliation: Laboratório de Parasitologia, Instituto Butantan, São Paulo, Brazil.

ABSTRACT

Background: Schistosomiasis is one of the most significant diseases in tropical countries and affects almost 200 million people worldwide. The application of molluscicides to eliminate the parasite's intermediate host, Biomphalaria glabrata, from infected water supplies is one strategy currently being used to control the disease. Previous studies have shown a potent molluscicidal activity of crude extracts from Piper species, with extracts from Piper tuberculatum being among the most active.

Methods and findings: The molluscicidal activity of P. tuberculatum was monitored on methanolic extracts from different organs (roots, leaves, fruit and stems). The compounds responsible for the molluscicidal activity were identified using (1)H NMR and ESIMS data and multivariate analyses, including principal component analysis and partial least squares. These results indicated that the high molluscicidal activity displayed by root extracts (LC50 20.28 µg/ml) was due to the presence of piplartine, a well-known biologically-active amide. Piplartine was isolated from P. tuberculatum root extracts, and the molluscicidal activity of this compound on adults and embryos of B. glabrata was determined. The compound displayed potent activity against all developmental stages of B. glabrata. Next, the environmental toxicity of piplartine was evaluated using the microcrustacean Daphnia similis (LC50 7.32 µg/ml) and the fish Danio rerio (1.69 µg/ml). The toxicity to these organisms was less compared with the toxicity of niclosamide, a commercial molluscicide.

Conclusions: The development of a new, natural molluscicide is highly desirable, particularly because the commercially available molluscicide niclosamide is highly toxic to some organisms in the environment (LC50 0.25 µg/ml to D. similis and 0.12 µg/ml to D. rerio). Thus, piplartine is a potential candidate for a natural molluscicide that has been extracted from a tropical plant species and showed less toxic to environment.

Show MeSH
Related in: MedlinePlus