Antiparasitic properties of 4-nerolidylcatechol from Pothomorphe umbellata (L.) Miq. (Piperaceae) in vitro and in mice models with either prepatent or patent Schistosoma mansoni infections

Costa, Danilo de Souza; Leal, Carla Monteiro; Cajas, Rayssa A.; Gazolla, Matheus Coutinho; Silva, Lívia Mara; Carvalho, Lara Soares Aleixo de; Lemes, Bruna L.; Moura, Renato Oliveira de; Almeida, Juliana; Moraes, Josué de; Filho, Ademar A. Da Silva

doi:10.1016/j.jep.2023.116607

Cited by 4 publications

(1 citation statement)

References 42 publications

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“…[57] The toxicity assay was conducted using a previously established method. [58] In summary, L4 stage worms were transferred to 96-well plates, with approximately 25 worms per well. Each well contained a mixture of 60 % M9 buffer, 10 μg/mL cholesterol, and 40 % brain heart infusion (BHI) medium.…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

In Situ Preparation of Dehydrodieugenol‐Loaded Silver Nanoparticles and their Antischistosomal Activity

Oliveira,

Camilo,

Soares

et al. 2024

Chemistry & Biodiversity

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Schistosomiasis is a major neglected disease that imposes a substantial worldwide health burden, affecting approximately 250 million people globally. As praziquantel is the only available drug to treat schistosomiasis, there is a critical need to identify new anthelmintic compounds, particularly from natural sources. To enhance the activity of different natural products, one potential avenue involves its combination with silver nanoparticles (AgNP). Based on this approach, a one‐step green method for the in situ preparation of dehydrodieugenol (DHDG) by oxidation coupling reaction using silver and natural eugenol is presented. AgNP formation was confirmed by UV‐Vis spectroscopy due to the appearance of the surface plasmon resonance (SPR) band at 430 nm which is characteristic of silver nanoparticles. The nanoparticles were spherical with sizes in the range of 40 to 50 nm. Bioassays demonstrated that the silver nanoparticles loaded with DHDG exhibited significant anthelmintic activity against Schistosoma mansoni adult worms without toxicity to mammalian cells and an in vivo animal model (Caenorhabditis elegans), contributing to the development of new prototypes based on natural products for the treatment of schistosomiasis.

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Section: Cytotoxicity Assaymentioning

confidence: 99%

In Situ Preparation of Dehydrodieugenol‐Loaded Silver Nanoparticles and their Antischistosomal Activity

Oliveira,

Camilo,

Soares

et al. 2024

Chemistry & Biodiversity

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In vivo antischistosomal efficacy of Porcelia ponderosa γ-lactones

Souza,

Totini,

Cajás

et al. 2024

Phytomedicine

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Targeting the Schistosoma mansoni nutritional mechanisms to design new antischistosomal compounds

Pavani,

Cirino,

Teixeira

et al. 2023

Sci Rep

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The chemical classes of semicarbazones, thiosemicarbazones, and hydrazones are present in various compounds, each demonstrating diverse biological activities. Extensive studies have revealed their potential as schistosomicidal agents. Thiosemicarbazones, in particular, have shown inhibitory effects on Schistosoma mansoni's cathepsin B1 enzyme (SmCB1), which plays a crucial role in hemoglobin degradation within the worm's gut and its nutrition processes. Consequently, SmCB1 has emerged as a promising target for novel schistosomiasis therapies. Moreover, chloroquinoline exhibits characteristics in its aromatic structure that hold promise for developing SmCB1 inhibitors, along with its interaction with hemoglobin's heme group, potentially synergizing against the parasite's gut. In this context, we report the synthesis of 22 hybrid analogs combining hydrazones and quinolines, evaluated against S. mansoni. Five of these hybrids demonstrated schistosomicidal activity in vitro, with GPQF-8Q10 being the most effective, causing worm mortality within 24 h at a concentration of 25 µM. GPQF-8Q8 proved to be the most promising in vivo, significantly reducing egg presence in feces (by 52.8%) and immature eggs in intestines (by 45.8%). These compounds exhibited low cytotoxicity in Vero cells and an in in vivo animal model (Caenorhabditis elegans), indicating a favorable selectivity index. This suggests their potential for the development of new schistosomiasis therapies. Further studies are needed to uncover specific target mechanisms, but these findings offer a promising starting point.

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Antiparasitic properties of 4-nerolidylcatechol from Pothomorphe umbellata (L.) Miq. (Piperaceae) in vitro and in mice models with either prepatent or patent Schistosoma mansoni infections

Cited by 4 publications

References 42 publications

In Situ Preparation of Dehydrodieugenol‐Loaded Silver Nanoparticles and their Antischistosomal Activity

In Situ Preparation of Dehydrodieugenol‐Loaded Silver Nanoparticles and their Antischistosomal Activity

In vivo antischistosomal efficacy of Porcelia ponderosa γ-lactones

Targeting the Schistosoma mansoni nutritional mechanisms to design new antischistosomal compounds

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