Schistosomicidal activity and docking of Schistosoma mansoni ATPDase 1 with licoflavone B isolated from Glycyrrhiza inflata (Fabaceae)

Carvalho, Lara Soares Aleixo de; Geraldo, Reinaldo Barros; Moraes, Josué de; Pintó, Pedro; Pinto, Priscila de Faria; Pereira, Olavo dos Santos; Filho, Ademar A. Da Silva

doi:10.1016/j.exppara.2015.09.015

Cited by 25 publications

(27 citation statements)

References 31 publications

(7 reference statements)

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“…Thus, a pattern consisting of a combination of changes in the surface morphology was detected and correlated to the death of the adult worms. These pronounced changes in the aspect of tubercles, which often appeared collapsed and disrupted, were similar to those reported in studies with other isolated natural compounds, such as piplartine, (+)-limonene epoxide, cardamonin, and licoflavone B [2, 3, 8, 21, 22]. …”

Section: Resultssupporting

confidence: 85%

“…For example, the number of intact tubercles in an area of 20 000 μ m 2 on male worms of the negative control was 43, while in the groups exposed to 12.5, 25, and 50 μ M of parthenolide it was, respectively, 12, 3, and 0,1. Similar results were obtained from the paired schistosomes exposed to some natural compounds, such as licoflavone B [8] and (+)-limonene epoxide [21]. The tegument of schistosomes is usually considered for its key role in nutrient uptake, secretory functions, and parasite protection [22], being a major target for the development of antischistosomal drugs [2, 3, 8].…”

Section: Resultssupporting

confidence: 61%

“…In this scenario, the search for bioactive plant extracts, which can be used as anthelmintic, has received considerable attention [2, 6, 8, 11]. Among medicinal plants, A. absinthium and T. parthenium have shown to be good sources for providing biologically activity compounds against parasites [13, 14, 16].…”

Section: Resultsmentioning

confidence: 99%

“…Among medicinal plants, A. absinthium and T. parthenium have shown to be good sources for providing biologically activity compounds against parasites [13, 14, 16]. Then, as part of our search for schistosomicidal molecules from Brazilian plants [2, 3, 8, 11], we performed, for the first time, the in vitro schistosomicidal assay of the crude extracts of A. absinthium (AA) and T. parthenium (TP).…”

Section: Resultsmentioning

confidence: 99%

“…All experiments were performed in triplicate and were repeated at least two times. Parasites were maintained for 48 h and monitored every 24 h using a light microscope in order to evaluate their general condition: motor activity, mortality rate, and tegumental alterations [3, 8]. …”

Section: Methodsmentioning

confidence: 99%

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Flavonoids and Sesquiterpene Lactones from Artemisia absinthium and Tanacetum parthenium against Schistosoma mansoni Worms

Almeida

Carvalho

Gazolla

et al. 2016

Evidence-Based Complementary and Alternative Medicine

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Human schistosomiasis, caused by trematode worms of the genus Schistosoma, is one of the most significant neglected tropical diseases, affecting more than 200 million individuals worldwide and praziquantel is the only available drug to treat this disease. Artemisia absinthium L. and Tanacetum parthenium L. are species popularly used as anthelmintics. We investigated the in vitro schistosomicidal activity of crude extracts of A. absinthium (AA) and T. parthenium (TP) and their isolated compounds. AA and TP, at 200 μg/mL, were active, causing 100% mortality of all adult worms. Chromatographic fractionation of AA leads to isolation of artemetin and hydroxypelenolide, while santin, apigenin, and parthenolide were isolated from TP. Artemetin, hydroxypelenolide, santin, and apigenin, at 100 μM, were inactive against adult worms. Parthenolide (12.5 to 100 μM) caused 100% mortality, tegumental alterations, and reduction of motor activity of all adult worms of S. mansoni, without affecting mammalian cells. Confocal laser scanning microscopy showed tegumental morphological alterations and changes on the numbers of tubercles of S. mansoni worms. This report provides the first evidence for the in vitro activity of parthenolide against adult worms of S. mansoni, opening the route to further schistosomicidal studies with this compound.

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Section: Resultssupporting

confidence: 85%

Section: Resultssupporting

confidence: 61%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 3 more Smart Citations

Flavonoids and Sesquiterpene Lactones from Artemisia absinthium and Tanacetum parthenium against Schistosoma mansoni Worms

Almeida

Carvalho

Gazolla

et al. 2016

Evidence-Based Complementary and Alternative Medicine

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Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

Carvalho

Silva

Souza

et al. 2021

Chemistry & Biodiversity

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Schistosomiasis, a neglected tropical disease caused by Schistosoma species, harms over 250 million people in several countries. The treatment is achieved with only one drug, praziquantel. Cardamonin, a natural chalcone with in vitro schistosomicidal activity, has not been in vivo evaluated against Schistosoma. In this work, we evaluated the in vivo schistosomicidal activities of cardamonin against Schistosoma mansoni worms and conducted enzymatic apyrase inhibition assay, as well as molecular docking analysis of cardamonin against potato apyrase, S. mansoni NTPDase 1 and S. mansoni NTPDase 2. In a mouse model of schistosomiasis, the oral treatment with cardamonin (400 mg/kg) showed efficacy against S. mansoni, decreasing the total worm load in 46.8 % and reducing in 54.5 % the number of eggs in mice. Cardamonin achieved a significant inhibition of the apyrase activity and the three‐dimensional structure of the potato apyrase, obtained by homology modeling, showed that cardamonin may interact mainly through hydrogen bonds. Molecular docking studies corroborate with the action of cardamonin in binding and inhibiting both potato apyrase and S. mansoni NTPDases.

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The Effectiveness of Ancient Mesopotamian Medical Practices: The Example of šūšu-Licorice

Scurlock

2021

Tigris and Euphrates Rivers: Their Environment From Headwaters to Mouth

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Schistosomicidal activity and docking of Schistosoma mansoni ATPDase 1 with licoflavone B isolated from Glycyrrhiza inflata (Fabaceae)

Cited by 25 publications

References 31 publications

Flavonoids and Sesquiterpene Lactones from Artemisia absinthium and Tanacetum parthenium against Schistosoma mansoni Worms

Flavonoids and Sesquiterpene Lactones from Artemisia absinthium and Tanacetum parthenium against Schistosoma mansoni Worms

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

The Effectiveness of Ancient Mesopotamian Medical Practices: The Example of šūšu-Licorice

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