In vitro activity of N-phenyl-1,10-phenanthroline-2-amines against tachyzoites and bradyzoites of Toxoplasma gondii

Martins‐Duarte, Erica S.; Portes, Juliana de Araujo; Silva, Ramon Borges da; Pires, Hugo Silva; Garden, Simon J.; Souza, Wanderley de

doi:10.1016/j.bmc.2021.116467

Cited by 5 publications

(6 citation statements)

References 56 publications

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“…TEM sample preparation was done according to previously published protocols ( 47 ). In short, intracellular parasites were fixed in 2.5% glutaraldehyde–0.1 M sodium phosphate buffer for 2 h at room temperature.…”

Section: Methodsmentioning

confidence: 99%

Separate To Operate: the Centriole-Free Inner Core of the Centrosome Regulates the Assembly of the Intranuclear Spindle in Toxoplasma gondii

Tomasina

González

Martins‐Duarte

et al. 2022

mBio

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Section: Methodsmentioning

confidence: 99%

Separate To Operate: the Centriole-Free Inner Core of the Centrosome Regulates the Assembly of the Intranuclear Spindle in Toxoplasma gondii

Tomasina

González

Martins‐Duarte

et al. 2022

mBio

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“…After 2 h of incubation, the absorbance of the samples was detected at 490 nm using the Versamax ELISA plate reader (Molecular Devices) and cytotoxicity was calculated as the percentage of viable cells in relation to control cells. The cytotoxic concentration of 50% (CC 50 ) for the host cells was determined, and the selective index (SI) was calculated as the ratio of CC 50 /EC 50 [ 22 ].…”

Section: Methodsmentioning

confidence: 99%

In Vitro Activity of Essential Oils from Piper Species (Piperaceae) against Tachyzoites of Toxoplasma gondii

Filho

Cunha²,

Stanton³

et al. 2023

Metabolites

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Toxoplasmosis is a tropical and neglected disease caused by the parasitic protozoa Toxplasma gondii. Conventional treatment with sulfadiazine and pyrimethamine plus folinic acid, has some drawbacks, such as inefficacy in the chronic phase, toxic side effects, and potential cases of resistance have been observed. In this study, the activity of essential oils (EOs) from three Piper species and their main constituents, including α-Pinene (Piper lindbergii and P. cernuum), β-Pinene (P. cernuum), and dillapiole (P. aduncum), were evaluated against tachyzoites of T. gondii. α-Pinene was more active [(IC50 0.3265 (0.2958 to 0.3604) μg/mL)] against tachyzoites than P. lindbergii EO [0.8387 (0.6492 to 1.084) μg/mL]. Both α-Pinene and P. lindbergii EO exhibited low cytotoxicity against NHDF cells, with CC50 41.37 (37.64 to 45.09) µg/mL and 83.80 (75.42 to 91.34) µg/mL, respectively, suggesting they could be of potential use against toxoplasmosis.

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“…The cytotoxic effect of the most active compounds was evaluated through MTS assay as previously described [ 12 , 30 ]. For that, 96-well tissue plates containing NHDF cells were treated with different concentrations of compounds up to 10 µM for seven days.…”

Section: Methodsmentioning

confidence: 99%

“…The flasks were washed and fresh RPMI was added for another two hours. After this, the compounds were added and infected cells were treated for 48 h. The sample fixation and processing for microscopy were performed as previously described [ 12 ]. The thin sections of the material were observed in a Fei TecNai G2 120 kV Spirit Electron Microscope at UFMG Microscopy Center.…”

Section: Methodsmentioning

confidence: 99%

“…The development of new drugs and treatments that are economically viable, safe, and effective for the treatment of parasitic diseases is one of the main current challenges. Although there are discussions in the academic sphere, we can frame toxoplasmosis in neglected parasitic infections, since there is no interest in the production of new therapeutic compounds by the pharmaceutical industry, due to the low expected financial return [ 12 ]. In this context, the repositioning of existing compounds and drugs is a promising strategy for the availability of new treatments [ 13 , 14 ].…”

Section: Introductionmentioning

confidence: 99%

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Medicines for Malaria Venture Pandemic Box In Vitro Screening Identifies Compounds Highly Active against the Tachyzoite Stage of Toxoplasma gondii

dos Santos,

Oliveira Costa,

Vaz

et al. 2023

TropicalMed

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Toxoplasmosis is a disease that causes high mortality in immunocompromised individuals, such as AIDS patients, and sequelae in congenitally infected newborns. Despite its great medical importance, there are few treatments available and these are associated with adverse events and resistance. In this work, after screening the drugs present in the Medicines for Malaria Venture Pandemic Box, we found new hits with anti-Toxoplasma gondii activity. Through our analysis, we selected twenty-three drugs or drug-like compounds that inhibited the proliferation of T. gondii tachyzoites in vitro by more than 50% at a concentration of 1 µM after seven days of treatment. Nineteen of these compounds have never been reported active before against T. gondii. Inhibitory curves showed that most of these drugs were able to inhibit parasite replication with IC50 values on the nanomolar scale. To better understand the unprecedented effect of seven compounds against T. gondii tachyzoites, an ultrastructural analysis was carried out using transmission electron microscopy. Treatment with 0.25 µM verdinexor, 3 nM MMV1580844, and 0.25 µM MMV019724 induced extensive vacuolization, complete ultrastructural disorganization, and lytic effects in the parasite, respectively, and all of them showed alterations in the division process. Treatment with 1 µM Eberconazole, 0.5 µM MMV1593541, 1 µM MMV642550, 1 µM RWJ-67657, and 1 µM URMC-099-C also caused extensive vacuolization in the parasite. The activity of these drugs against intracellular tachyzoites supports the idea that the drugs selected in the Pandemic Box could be potential future drugs for the treatment of acute toxoplasmosis.

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In vitro activity of N-phenyl-1,10-phenanthroline-2-amines against tachyzoites and bradyzoites of Toxoplasma gondii

Cited by 5 publications

References 56 publications

Separate To Operate: the Centriole-Free Inner Core of the Centrosome Regulates the Assembly of the Intranuclear Spindle in Toxoplasma gondii

Separate To Operate: the Centriole-Free Inner Core of the Centrosome Regulates the Assembly of the Intranuclear Spindle in Toxoplasma gondii

In Vitro Activity of Essential Oils from Piper Species (Piperaceae) against Tachyzoites of Toxoplasma gondii

Medicines for Malaria Venture Pandemic Box In Vitro Screening Identifies Compounds Highly Active against the Tachyzoite Stage of Toxoplasma gondii

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