Cardamonin Presents <i>in Vivo</i> Activity against <i>Schistosoma mansoni</i> and Inhibits Potato Apyrase

Carvalho, Lara Soares Aleixo de; Silva, Lívia Mara; Souza, Vinícius Carius de; Silva, Marcos Paulo Nascimento da; Capriles, Priscila V. S. Z.; Pinto, Priscila de Faria; Moraes, Josué de; Filho, Ademar Alves da Silva

doi:10.1002/cbdv.202100604

Cited by 7 publications

(13 citation statements)

References 48 publications

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“…Many natural products have demonstrated anti-schistosomiasis activity [10,[50][51][52]. The aurone scaffold is another source of antimalarial compounds [53,54] that has been investigated for anti-schistosomiasis potential [55,56].…”

Section: Other Antimalarialsmentioning

confidence: 99%

“…The latter of those, perhexiline maleate (62), is an anti-angina drug whose efficacy against schistosomiasis had been studied previously [86,87]. Starting from those three hits, pharmacophore Leads resulting from a large high-throughput screening experiment (51)(52)(53)(54)(55)(56)(57)(58)(59).…”

Section: Figurementioning

confidence: 99%

“…Figure 9.Leads resulting from a large high-throughput screening experiment(51)(52)(53)(54)(55)(56)(57)(58)(59).…”

mentioning

confidence: 99%

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Recent Advances in Anti-Schistosomiasis Drug Discovery

Marker¹,

Debbert²

2022

Parasitic Helminths and Zoonoses - From Basic to Applied Research

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Schistosomiasis, a parasitic disease caused by infection by helminths of the Schistosoma genus, affects over 200 million people, primarily in the developing world. Treatment of this disease largely relies on one drug, praziquantel. Although this drug is cheap, safe, and effective, the looming prospect of drug resistance makes the development of a pipeline of anti-schistosomiasis drugs a priority. Many new drug leads have arisen from screening existing sets of compounds such as the Open Access Boxes developed by the Medicines for Malaria Venture (MMV) in collaboration with the Drugs for Neglected Diseases Initiative (DNDI). Other leads have been found through work focused on druggable targets such as kinases, histone deacetylases, proteases, and others. This chapter will discuss recent work concerning the discovery and development of novel anti-schistosomiasis drug leads from many sources.

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Section: Other Antimalarialsmentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

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Recent Advances in Anti-Schistosomiasis Drug Discovery

Marker¹,

Debbert²

2022

Parasitic Helminths and Zoonoses - From Basic to Applied Research

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“…Additionally, previous studies have showed that the SmNTPDases isoforms have immune cross-reactivity with the potato ( Solanum tuberosum ) apyrase [ 9 , 10 , 11 ], sharing high homology and similarity in their active sites [ 9 , 10 , 11 , 12 ]. Regarding this, some natural compounds, such as cardamonin, have promoted the inhibition of both SmNTPDases and potato apyrase, also showing in vivo antischistosomal effects against S. mansoni [ 13 , 14 , 15 ]. Since its obtainment with high purity is easy, it has been proposed that potato apyrase may be used in the initial screening for selecting potential antischistosomal compounds with affinity for SmNTPDases in complex samples, such as plant extracts [ 13 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

“…Regarding this, some natural compounds, such as cardamonin, have promoted the inhibition of both SmNTPDases and potato apyrase, also showing in vivo antischistosomal effects against S. mansoni [ 13 , 14 , 15 ]. Since its obtainment with high purity is easy, it has been proposed that potato apyrase may be used in the initial screening for selecting potential antischistosomal compounds with affinity for SmNTPDases in complex samples, such as plant extracts [ 13 , 15 ]. In this regard, in a preliminary assessment of some plant extracts against potato apyrase, the hydroalcoholic extract of Centella erecta (L.f.) Fern.…”

Section: Introductionmentioning

confidence: 99%

Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity

et al. 2022

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Schistosomiasis, caused by parasites of the genus Schistosoma, is a neglected disease with high global prevalence, affecting more than 240 million people in several countries. Praziquantel (PZQ) is the only drug currently available for the treatment. S. mansoni NTPDases (known as SmNTPDases, ATP diphosphohydrolases or ecto-apyrases) are potential drug targets for the discovery of new antischistosomal drugs. In this study, we screen NTPDases inhibitors from Centella erecta (Apiaceae) using an ultrafiltration combined UHPLC-QTOF-MS method and potato apyrase, identifying asiaticoside as one of the apyrase-binding compounds. After isolation of asiaticoside from C. erecta extract, we assessed its in vivo antischistosomal activities against Schistosoma mansoni worms and its in vitro enzymatic apyrase inhibition. Also, molecular docking analysis of asiaticoside against potato apyrase, S. mansoni NTPDases 1 and 2 were performed. Asiaticoside showed a significant in vitro apyrase inhibition and molecular docking studies corroborate with its possible actions in potato apyrase and S. mansoni NTPDases. In mice harboring a patent S. mansoni infection, a single oral dose of asiaticoside (400 mg/kg. p.o.) showed significantly in vivo antischistosomal efficacy, markedly decreasing the total worm load and egg burden, giving support for further exploration of apyrase inhibitors as antischistosomal agents.

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Oral Administration of Kaempferol Isolated from Baccharis Mattogrosensis Enables In Vivo Activity Against Schistosoma Mansoni

Albuquerque,

Luz,

Rodrigues

et al. 2024

Chemistry & Biodiversity

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Baccharis mattogrosensis is a species from Asteraceae which has been used in Brazilian folk medicine to treatment of several illnesses, including those caused by parasites. In the present work, the MeOH extract of aerial parts of B. mattogrosensis was subjected to chromatographic fractionation to afford three flavonoids: apigenin (1), quercetin (2), and kaempferol (3) as well as a mixture three chlorogenic acids: 3,4‐O‐dicaffeoylquinic (4), 3,5‐O‐dicaffeoylquinic (5), and 4,5‐O‐dicaffeoylquinic (6) acids. When tested in vitro, kaempferol (3) exhibited activity against Schistosoma mansoni with EC50 = 81.86 μM, whereas compounds 1, 2, 4 – 6 showed to be inactives. Considering this result, the effects of kaempferol (3) against S. mansoni infection using in vivo assay was tested at first time. Using a single oral dose (400 mg/kg) of kaempferol (3) to S. mansoni‐infected mice reduced the worm burden by 25.5%. Similarly, the number of eggs, which are responsible for a variety of pathologies and transmission of schistosomiasis, was decreased by 28.8% in treated mice. Collectively, although kaempferol (3) is partially active when administered orally in a mouse model of schistosomiasis, our results suggest that this compound could be, in future studies, administered in different forms, such as nanoformulation.

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

Cited by 7 publications

References 48 publications

Recent Advances in Anti-Schistosomiasis Drug Discovery

Recent Advances in Anti-Schistosomiasis Drug Discovery

Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity

Oral Administration of Kaempferol Isolated from Baccharis Mattogrosensis Enables In Vivo Activity Against Schistosoma Mansoni

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