<i>In Vitro</i> and <i>in Vivo</i> Antischistosomal Activities of Chalcones

Pereira, Vinícius R. D.; Alves, Ismael J.; Silveira, Lígia S. da; Geraldo, Reinaldo Barros; Pinto, Priscila de Faria; Teixeira, F. S.; Salvadori, M. C.; Silva, Marcos P.; Alves, Lara A.; Capriles, Priscila V. S. Z.; Almeida, Ayla das Chagas; Coimbra, Elaine Soares; Pintó, Pedro; Couri, Mara R.C.; Moraes, Josué de; Filho, Ademar A. Da Silva

doi:10.1002/cbdv.201800398

Cited by 21 publications

(11 citation statements)

References 39 publications

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“…Similar results were found for epiisopilosine, an alkaloid found in jaborandi ( Pilocarpus microphyllus ), which demonstrated reduction in the total number of worms when evaluated orally at a single dose of 400 mg/kg [21] . Also, some synthetic chalcones showed a reduction of about 32 % in the total number of worms after oral treatment with a single dose of 400 mg/kg [10] . However, according to literature, [22] considering the effectivity of an antischistosomal compound in vivo , only the active drugs that show worm burden reduction >80 % can be further characterized on mice bearing juvenile worms in the drug‐screening process.…”

Section: Resultssupporting

confidence: 76%

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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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Section: Resultssupporting

confidence: 76%

“…Additionally, the concerns over the emerging PZQ‐resistance development [6] have renewed interest in the search for new antischistosomal agents, particularly from natural sources [1,7,8] . Among natural compounds, chalcones have been shown promising antischistosomal activities [1,5,9,10] …”

Section: Introductionmentioning

confidence: 99%

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

Carvalho

Silva

Souza

et al. 2021

Chemistry & Biodiversity

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“…An in vivo study with 2 ′ -Hydroxyflavanone showed that this flavonoid reduced the lesion size and L. amazonensis load in a murine model of cutaneous leishmaniasis [117]. Pereira et al stated the in vivo schistosomicidal activities of oral treatment with chalcones against Schistosoma mansoni worms, and the results showed that in mice there occurred a total worm reduction [118].…”

Section: Potential Of Dimeric Flavonoids As Antimicrobials: Form Lab ...mentioning

confidence: 99%

Antimicrobial Activity of Dimeric Flavonoids

Lopes,

Campos,

Medeiros

et al. 2024

Compounds

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Distributed throughout the environment are various microorganisms such as bacteria, fungi, parasites, and viruses. Although many are part of the human microbiome, many are pathogenic and cause infections ranging from mild to severe. In recent years, the identification of multidrug-resistant microorganisms has become a serious public health problem. The resulting infections call into question the therapeutic capacity of health systems and lead to approximately 70,000 deaths annually worldwide. The progressive resistance to antibiotics and antifungals has been a major challenge for the medical and pharmaceutical community, requiring the search for new compounds with antimicrobial properties. Several studies have demonstrated the potential of natural and synthesized flavonoids, especially the dimers of these molecules. In this review are presented many examples of dimeric flavonoids that have demonstrated antimicrobial activity against viruses, like influenza and Human Immunodeficiency Virus (HIV), protozoal infections, such as Leishmaniasis and Malaria, fungal infections by Candida albicans and Cryptococcus neoformans, and bacterial infections caused, for example, by Staphylococcus aureus and Escherichia coli. In the pursuit to find potential safe agents for therapy in microbial infections, natural dimeric flavonoids are an option not only for the antimicrobial activity, but also for the low toxicity usually associated with these compounds when compared to classic antimicrobials.

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“…The schistosomicidal effect of two synthetic chalcones ( E -4’-hydroxychalcone and E -2’-hydroxy-4-methoxychalcone) was studied by Pereira et al. (2018) .…”

Section: Development Of E-ntpdases Inhibitorsmentioning

confidence: 99%

E-NTPDases: Possible Roles on Host-Parasite Interactions and Therapeutic Opportunities

Paes-Vieira

Gomes-Vieira

Meyer‐Fernandes

2021

Front. Cell. Infect. Microbiol.

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Belonging to the GDA1/CD39 protein superfamily, nucleoside triphosphate diphosphohydrolases (NTPDases) catalyze the hydrolysis of ATP and ADP to the monophosphate form (AMP) and inorganic phosphate (Pi). Several NTPDase isoforms have been described in different cells, from pathogenic organisms to animals and plants. Biochemical characterization of nucleotidases/NTPDases has revealed the existence of isoforms with different specificities regarding divalent cations (such as calcium and magnesium) and substrates. In mammals, NTPDases have been implicated in the regulation of thrombosis and inflammation. In parasites, such as Trichomonas vaginalis, Trypanosoma spp., Leishmania spp., Schistosoma spp. and Toxoplasma gondii, NTPDases were found on the surface of the cell, and important processes like growth, infectivity, and virulence seem to depend on their activity. For instance, experimental evidence has indicated that parasite NTPDases can regulate the levels of ATP and Adenosine (Ado) of the host cell, leading to the modulation of the host immune response. In this work, we provide a comprehensive review showing the involvement of the nucleotidases/NTPDases in parasites infectivity and virulence, and how inhibition of NTPDases contributes to parasite clearance and the development of new antiparasitic drugs.

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In Vitro and in Vivo Antischistosomal Activities of Chalcones

Cited by 21 publications

References 39 publications

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

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

Antimicrobial Activity of Dimeric Flavonoids

E-NTPDases: Possible Roles on Host-Parasite Interactions and Therapeutic Opportunities

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