Efficacy of carvacryl acetate in vitro and following oral administration to mice harboring either prepatent or patent Schistosoma mansoni infections

Silva, Bianca C.; Mengarda, Ana C.; Rodrigues, Vinícius C.; Cajas, Rayssa A.; Carnaúba, Paulo U.; Espírito-Santo, Maria Cristina Carvalho do; Bezerra-Filho, Carlos S. M.; Sousa, Damião Pergentino de; Moraes, Josué de

doi:10.1007/s00436-021-07333-2

Cited by 4 publications

(3 citation statements)

References 42 publications

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“…Based on the results obtained, tetrahydrofuran lignans, mainly verrucosin, have a potent schistosomicidal activity, and these compounds are more effective against schistosomes than other plant-derived products. For example, the following in vitro effective concentrations against S. mansoni adult worms were observed in the literature: 30 µM with neolignan licarin A 25 , 52 µM with monoterpene 3,7-dimethylloctanol 32 , 56.8 µM with monoterpene carvacrol 33 , 42.16 µM with carvacryl acetate, a derivative of carvacrol 34 , 85 µM with sesquiterpene nerolidol 35 , 50 µM with sesquiterpene cnicin 36 , 26.1 µM with diterpene ent -kaur-16-en-19-oic acid 24 , 50 µM with licochalcone A 37 , 50 µM 2-oxopopulifolic acid methyl ester, and 2-oxopopulifolic acid 38 , and 25 µM with chalcone cardamonin 39 .…”

Section: Resultsmentioning

confidence: 99%

Neolignans isolated from Saururus cernuus L. (Saururaceae) exhibit efficacy against Schistosoma mansoni

Brito

Wilairatana

Roquini

et al. 2022

Sci Rep

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Schistosomiasis, a parasitic disease caused by the blood fluke of the genus Schistosoma, affects over 230 million people, especially in developing countries. Despite the significant economic and public health consequences, only one drug is currently available for treatment of schistosomiasis, praziquantel. Thus, there is an urgent demand for new anthelmintic agents. Based on our continuous studies involving the chemical prospection of floristic biodiversity aiming to discover new bioactive compounds, this work reports the in vitro antiparasitic activity against Schistosoma mansoni adult worms of neolignans threo-austrobailignan-6 and verrucosin, both isolated from Saururus cernuus L. (Saururaceae). These neolignans showed a significant in vitro schistosomicidal activity, with EC50 values of 12.6–28.1 µM. Further analysis revealed a pronounced reduction in the number of S. mansoni eggs. Scanning electron microscopy analysis revealed morphological alterations when schistosomes were exposed to either threo-austrobailignan-6 or verrucosin. These relevant antischistosomal properties were accompanied by low cytotoxicity potential against the animal (Vero) and human (HaCaT) cell lines, resulting in a high selectivity index. Considering the promising chemical and biological properties of threo-austrobailignan-6 and verrucosin, this research should be of interest to those in the area of neglected diseases and in particular antischistosomal drug discovery.

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Section: Resultsmentioning

confidence: 99%

Neolignans isolated from Saururus cernuus L. (Saururaceae) exhibit efficacy against Schistosoma mansoni

Brito

Wilairatana

Roquini

et al. 2022

Sci Rep

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“…However, under intraperitoneal administration, both free licochalcone A and L-SLNs significantly decreased worm burden and intestinal egg load [62] Carvacryl acetate Oral 100, 200, or 400 mg/kg/day Carvacryl acetate (400 mg/kg) showed moderate efficacy against S. mansoni, with slightly reduced worm burden (32-40%). Egg production was markedly reduced (70-80%) [63] Cardamonin Oral 400 mg/kg/day Oral treatment with cardamonin (400 mg/kg) demonstrated efficacy against S. mansoni, with decreased total worm load in 46.8% of mice and a 54.5% reduction in egg numbers [64] Asiaticoside Oral 400 mg/kg/day A single oral dose (400 mg/kg) of asiaticoside presented significant in vivo antischistosomal efficacy, markedly decreasing total worm and egg burden [65] Plumbagin Intraperitoneal 20 mg/kg/day Mice treated with plumbagin (20 mg/kg) showed reductions of 64.28% and 59.88% in male and female worms, respectively. Plumbagin treatment also alleviated schistosome-induced hepatosplenomegaly and reduced hepatic granuloma and liver collagen content [66] Juglone Intraperitoneal 2 mg/Kg/day Treatment with the compound reduced male and female worms by 63.1% and 52.1%, respectively.…”

Section: In Vivo Studiesmentioning

confidence: 99%

“…The oral administration of different natural compounds at doses ranging between 1.5 and 400 mg/kg demonstrated variable worm and egg burden reduction (31.8 to 100%) in infected mice [44,53,54,60,63,64]. In addition, Carvalho et al [65] demonstrated the effective antischistosomal activity of asiaticoside (400 mg/kg) against Schistosoma spp.…”

Section: Initial Work Bymentioning

confidence: 99%

Therapeutic Potential of Natural Products in the Treatment of Schistosomiasis

Azevedo,

Meira,

da Silva

et al. 2023

Molecules

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It is estimated that 250 million people worldwide are affected by schistosomiasis. Disease transmission is related to the poor sanitation and hygiene habits that affect residents of impoverished regions in tropical and subtropical countries. The main species responsible for causing disease in humans are Schistosoma Mansoni, S. japonicum, and S. haematobium, each with different geographic distributions. Praziquantel is the drug predominantly used to treat this disease, which offers low effectiveness against immature and juvenile parasite forms. In addition, reports of drug resistance prompt the development of novel therapeutic approaches. Natural products represent an important source of new compounds, especially those obtained from plant sources. This review compiles data from several in vitro and in vivo studies evaluating various compounds and essential oils derived from plants with cercaricidal and molluscicidal activities against both juvenile and adult forms of the parasite. Finally, this review provides an important discussion on recent advances in molecular and computational tools deemed fundamental for more rapid and effective screening of new compounds, allowing for the optimization of time and resources.

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Toward anthelmintic drug candidates for toxocariasis: Challenges and recent developments

Mengarda

Silva

et al. 2023

European Journal of Medicinal Chemistry

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Efficacy of carvacryl acetate in vitro and following oral administration to mice harboring either prepatent or patent Schistosoma mansoni infections

Cited by 4 publications

References 42 publications

Neolignans isolated from Saururus cernuus L. (Saururaceae) exhibit efficacy against Schistosoma mansoni

Neolignans isolated from Saururus cernuus L. (Saururaceae) exhibit efficacy against Schistosoma mansoni

Therapeutic Potential of Natural Products in the Treatment of Schistosomiasis

Toward anthelmintic drug candidates for toxocariasis: Challenges and recent developments

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