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

Filho, Adalberto Alves Pereira; Cunha, Mariana M.; Stanton, Mariana A.; Yamaguchi, Lydia F.; Kato, Massuo Jorge; Martins‐Duarte, Erica S.

doi:10.3390/metabo13010095

Cited by 4 publications

(4 citation statements)

References 33 publications

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“…For the preliminary evaluation of the 400 compounds contained in the Pandemic Box, 6-well plates were seeded with neonatal Normal Human Dermal Fibroblast cells (NHDF; Lonza, kindly donated by Dr. Sheila Nardelli, Fiocruz Paraná, Brazil) in RPMI 1640 medium supplemented with 2% Fetal Bovine Serum (Gibco), Penicillin/Streptomycin, Amphotericin B (Life Technologies, Eugene, OR, USA), and 2 mM glutamine (complete medium). After NHDF reached confluency, each well was replaced with fresh medium containing one compound at a concentration of 1 µM, and then infected with 1000 newly egressed tachyzoites from RH strain [ 29 ]. Screening at 1 μM is recommended by MMV.…”

Section: Methodsmentioning

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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Section: Methodsmentioning

confidence: 99%

“…Screening at 1 μM is recommended by MMV. As a control, infected cells were incubated with complete medium and 0.01% DMSO [ 29 ]. The plates were then kept in an incubator at 37 °C in a humid atmosphere with 5% CO 2 for seven days.…”

Section: Methodsmentioning

confidence: 99%

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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“…Both compounds displayed considerable toxicity against E. granulosus protoscoleces, with LC 50 values of 16.14 μM and 31.23 μM, respectively (Tabari et al., 2019). Additionally, compound 27 shows antiprotozoal and nematocidal activity (Bailén et al., 2022; Lima et al., 2021; Pacheco et al., 2022; Pereira Filho et al., 2023 ) . The compounds isofuranodiene ( 29 ) and beta‐myrcene ( 30 ) have been found to possess moderate activity against E. granulosus protoscoleces.…”

Section: Anti‐echinococcal Activity Of Terpenesmentioning

confidence: 99%

Could natural terpenes be an alternative for the treatment of neglected tropical diseases?

Soto‐Sánchez

2024

Chem Biol Drug Des

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Existing chemotherapy for neglected tropical diseases (NTDs) can often be toxic and ineffective, highlighting the necessity for new treatments. Terpenes are secondary metabolites with pharmacological potential. This aim of this mini‐review is to explore the most promising natural terpenes with anti‐leishmanicidal, anti‐schistosomicidal, and anti‐echinococcal activity, their mechanisms of action, and their efficacy as combination therapy. The study identified a tetracyclic diterpenoid, a sesquiterpene lactone, and a triterpene with the highest biological activity against leishmaniasis. Additionally, a triterpenoid and a tetraterpene showed potent activity against schistosomiasis and echinococcosis, respectively. Compounds have antiparasitic effects by inducing cell death, inhibiting cell stress‐related proteins, degrading extracellular matrix, and modulating immune and inflammatory responses. The employment of combination therapy and terpene nanotransporters appears to enhance the antiparasitic activity of these compounds. Although identifying specific molecular targets is necessary, the use of terpenes in combination therapy presents a safe and highly promising approach for the rational development of more potent and selective antiparasitic drugs.

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“…Studies have indicated that the essential oils from different plants exhibit low cytotoxicity and better inhibition of the proliferation of T. gondii [10,11]. Screening antiparasitic drugs from natural products from medicinal plants is an important procedure during new drug research and development [12].…”

Section: Introductionmentioning

confidence: 99%

In Vitro Evaluation Reveals Effect and Mechanism of Artemether against Toxoplasma gondii

Duan

Pan

et al. 2023

Metabolites

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Due to the limited effectiveness of existing drugs for the treatment of toxoplasmosis, there is a dire need for the discovery of new therapeutic options. Artemether is an important drug for malaria and several studies have indicated that it also exhibits anti-T. gondii activity. However, its specific effect and mechanisms are still not clear. To elucidate its specific role and potential mechanism, we first evaluated its cytotoxicity and anti-Toxoplasma effect on human foreskin fibroblast cells, and then analyzed its inhibitory activity during T. gondii invasion and intracellular proliferation. Finally, we examined its effect on mitochondrial membrane potential and reactive oxygen species (ROS) in T. gondii. The CC50 value of artemether was found to be 866.4 μM, and IC50 was 9.035 μM. It exhibited anti-T. gondii activity and inhibited the growth of T. gondii in a dose-dependent manner. We also found that the inhibition occurred primarily in intracellular proliferation, achieved by reducing the mitochondrial membrane integrity of T. gondii and stimulating ROS production. These findings suggest that the mechanism of artemether against T. gondii is related to a change in the mitochondrial membrane and the increase in ROS production, which may provide a theoretical basis for optimizing artemether derivatives and further improving their anti-Toxoplasma efficacy.

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

Cited by 4 publications

References 33 publications

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

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

Could natural terpenes be an alternative for the treatment of neglected tropical diseases?

In Vitro Evaluation Reveals Effect and Mechanism of Artemether against Toxoplasma gondii

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