Antiparasitic activity of nerolidol in a mouse model of schistosomiasis

Silva, Marcos P.; Oliveira, Rosimeire Nunes de; Mengarda, Ana C.; Roquini, Daniel B.; Allegretti, Silmara Marques; Salvadori, M. C.; Teixeira, F. S.; Sousa, Damião Pergentino de; Pintó, Pedro; Filho, Ademar A. Da Silva; Moraes, Josué de

doi:10.1016/j.ijantimicag.2017.06.005

Cited by 59 publications

(45 citation statements)

References 38 publications

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“…This finding could be attributed to a high reduction in the worm burden as a result of treatment with spironolactone and/or inhibition of oviposition by adult helminths. A significant reduction in eggs collected from the intestine (oogram) or feces has been described with other antischistosomal compounds (21)(22)(23). In addition, the pathology normally associated with the deposition of schistosome eggs in the spleen and liver was clearly ameliorated, mainly when spironolactone was administered for 5 days.…”

Section: Discussionmentioning

confidence: 94%

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In Vitro and In Vivo Studies of Spironolactone as an Antischistosomal Drug Capable of Clinical Repurposing

Guerra

Silva

et al. 2019

Antimicrob Agents Chemother

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Schistosomiasis is a parasitic flatworm disease that infects over 200 million people worldwide, especially in poor communities. Treatment and control of the disease rely on just one drug, praziquantel. Since funding for drug development for poverty-associated diseases is very limited, drug repurposing is a promising strategy. In this study, from a screening of 13 marketed diuretics, we identified that spironolactone, a potassium-sparing diuretic, had potent antischistosomal effects on Schistosoma mansoni in vitro and in vivo in a murine model of schistosomiasis. In vitro, spironolactone at low concentrations (<10 µM) is able to alter worm motor activity and the morphology of adult schistosomes, leading to parasitic death. In vivo, oral treatment with spironolactone at a single dose (400 mg/kg) or daily for five consecutive days (100 mg/kg/day) in mice harboring either patent or prepatent infections significantly reduced worm burden, egg production, and hepato- and splenomegaly (P < 0.05 to P < 0.001). Taken together, with the safety profile of spironolactone, supported by its potential to affect schistosomes, these results indicate that spironolactone could be a potential treatment for schistosomiasis and make it promising for repurposing.

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Section: Discussionmentioning

confidence: 94%

“…For maintenance of parasite life cycle, mice were infected with S. mansoni (BH strain) by subcutaneous injection of ϳ120 cercariae. Cercariae were harvested from infected intermediate host snails Biomphalaria glabrata by exposure to light for 3 h according to standard procedures from our laboratory (21,29).…”

Section: Methodsmentioning

confidence: 99%

In Vitro and In Vivo Studies of Spironolactone as an Antischistosomal Drug Capable of Clinical Repurposing

Guerra

Silva

et al. 2019

Antimicrob Agents Chemother

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“…Thus, the essential oil extracted from the Tunisian plant, and more precisely from its flowers, is very rich in (E)-nerolidol, since it is present at 40% of the total volatile constituents (Table 2). (E)-nerolidol is an odorant compound prized by the perfume industry (18) but some studies have shown that it may have anti-parasitic (19), anti-malarial (20), anti-mite (21) and cytotoxic (22) properties. A recent study has even highlighted the effect of RT*: Retention time, RI: Retention index determined on a HP5-MS fused silica column relative to a series of n-alkanes (C8-C26), tr: trace, percentage lower than 0.1% (E)-nerolidol and caryophyllene oxide (23) on some cancer cells.…”

Section: Component Identificationmentioning

confidence: 99%

Chemical composition, antibacterial and antioxidant activities of essential oils from flowers, leaves and aerial parts of Tunisian Dittrichia Viscosa

Gharred

Dbeibia

Falconieri

et al. 2019

Journal of Essential Oil Research

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The objective of this work was to determine the chemical composition, the antioxidant and antibacterial activities of the essential oils (EOs) extracted by hydrodistillation from different organs of the D. viscosa: flowers, leaves and aerial parts. The main compounds identified by GC/MS are oxygenated sesquiterpenes. Among these compounds, (E)-nerolidol (40.7%) is the most abundant constituent of flowers' essential oil while caryophyllene oxide (9.9%), isolongifolan-7-α-ol (10.3%) and α-eudesmol (9.1%) are the major constituents of the leaves' essential oil. The presence of these compounds in the aerial parts' essential oil is solely due to those of the flowers and leaves that constitute these aerial parts. The volatile extracts showed antioxidant effects with IC 50 values ranging between 9.25 and 9.75 mg.mL −1. On the other hand, EOs showed antibacterial effects on both Gram-positive and Gram-negative bacteria. The highest activity was obtained with flowers' essential oil against Enterococcus faecalis and Escherichia coli.

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“…Two weeks after oral treatment, mice were euthanized, and the surviving schistosomes located at the mesenteric veins and the liver were counted and sexed, as described previously. [35,36] The assessment of therapeutic efficacy was also based on the technique of quantitative and qualitative oograms, using a fragment of the intestine (10 mm), [16,17] as well as the Kato-Katz method for quantitative feces examination. [37] In the oogram pattern, eggs were scored as immature, mature, or dead.…”

Section: In Vivo Schistosomicidal Assaysmentioning

confidence: 99%

In Vitro and in Vivo Antischistosomal Activities of Chalcones

Pereira

Alves

Silveira

et al. 2018

Chemistry & Biodiversity

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In this study, we evaluated the in vitro and in vivo schistosomicidal activities of chalcones against Schistosoma mansoni worms. In vitro assays revealed that chalcones 1 and 3 were the most active compounds, without affecting significantly mammalian cells. Confocal laser scanning microscopy and scanning electron microscopy studies revealed reduction on the numbers of tubercles and morphological alterations in the tegument of S. mansoni worms after in vitro incubation with chalcones 1 and 3. In a mouse model of schistosomiasis, the oral treatment (400 mg/kg) with chalcone 1 or 3 significantly caused a total worm burden reduction in mice. Chalcone 1 showed significant inhibition of the S. mansoni ATP diphosphohydrolase activity, which was corroborated by molecular docking studies. The results suggested that chalcones could be explored as lead compounds with antischistosomal properties.

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Antiparasitic activity of nerolidol in a mouse model of schistosomiasis

Cited by 59 publications

References 38 publications

In Vitro and In Vivo Studies of Spironolactone as an Antischistosomal Drug Capable of Clinical Repurposing

In Vitro and In Vivo Studies of Spironolactone as an Antischistosomal Drug Capable of Clinical Repurposing

Chemical composition, antibacterial and antioxidant activities of essential oils from flowers, leaves and aerial parts of Tunisian Dittrichia Viscosa

In Vitro and in Vivo Antischistosomal Activities of Chalcones

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