In vitro evaluation of Resveratrol as a potential pre-exposure prophylactic drug against Trypanosoma cruzi infection

Rodríguez, Matías Exequiel; Tekiel, Valeria; Campo, Vanina A.

doi:10.1016/j.ijpddr.2022.08.003

Cited by 7 publications

(6 citation statements)

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“…The data showed that only resveratrol reduced the percentage of live parasites in infected Vero cells, with an IC 50 of 50.3 µM. These results pinpoint resveratrol as a possible drug to combat trypanosomiasis, targeting the trypanosome's HDACs [36,37].…”

Section: Histone Post-translational Modifications (Hptms)mentioning

confidence: 78%

“…The data showed that only resveratrol reduced the percentage of live parasites in infected Vero cells, with an IC50 of 50.3 μM. These results pinpoint resveratrol as a possible drug to combat trypanosomiasis, targeting the trypanosome's HDACs [36,37]. Histone acetylation is usually linked to transcriptional activation, whereas low histone acetyl group content restores heterochromatin structure, contrary to gene activation.…”

Section: Histone Post-translational Modifications (Hptms)mentioning

confidence: 85%

“…Both are known for their inhibitory effect on the different HDACs, and resveratrol (Figure 2), a known class III HDAC activator. These compounds were tested in the different life cycle stages of T. cruzi [36,37]. The results indicated that both HDAC inhibitors caused histone hyperacetylation, especially of H4 and H2B.…”

Section: Histone Post-translational Modifications (Hptms)mentioning

confidence: 99%

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Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs

et al. 2023

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Protozoan parasite diseases cause significant mortality and morbidity worldwide. Factors such as climate change, extreme poverty, migration, and a lack of life opportunities lead to the propagation of diseases classified as tropical or non-endemic. Although there are several drugs to combat parasitic diseases, strains resistant to routinely used drugs have been reported. In addition, many first-line drugs have adverse effects ranging from mild to severe, including potential carcinogenic effects. Therefore, new lead compounds are needed to combat these parasites. Although little has been studied regarding the epigenetic mechanisms in lower eukaryotes, it is believed that epigenetics plays an essential role in vital aspects of the organism, from controlling the life cycle to the expression of genes involved in pathogenicity. Therefore, using epigenetic targets to combat these parasites is foreseen as an area with great potential for development. This review summarizes the main known epigenetic mechanisms and their potential as therapeutics for a group of medically important protozoal parasites. Different epigenetic mechanisms are discussed, highlighting those that can be used for drug repositioning, such as histone post-translational modifications (HPTMs). Exclusive parasite targets are also emphasized, including the base J and DNA 6 mA. These two categories have the greatest potential for developing drugs to treat or eradicate these diseases.

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Section: Histone Post-translational Modifications (Hptms)mentioning

confidence: 78%

Section: Histone Post-translational Modifications (Hptms)mentioning

confidence: 85%

Section: Histone Post-translational Modifications (Hptms)mentioning

confidence: 99%

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Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs

et al. 2023

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“…In addition, a resveratrol-mediated increase in Sirt1 led to cell death in HaCaT keratinocytes ( Lee et al, 2016 ). Moreover, RVT KDACs activation effect has been confirmed on a parasitic protozoan, T. cruzi because it suppresses T. cruzi epimastigote growth and infectivity of cell-derived trypomastigotes, as well as intracellular amastigote differentiation and/or replication by activation of KDACs III ( Campo, 2017 ; Rodriguez et al, 2022 ). Subsequently, the present study investigated RVT as an inhibitor of KATs and an activator of KDAC for the potential activity against piroplasmosis and to offer an alternative strategy to discover a promising compound against such infectious disease.…”

Section: Discussionmentioning

confidence: 98%

“…Resveratrol has anti-protozoal activity against Leishmania sp. ( Ferreira et al, 2014 ; Mousavi et al, 2022 ), Trypanosoma cruzi ( T. cruzi ) ( Campo, 2017 ; Rodriguez et al, 2022 ), Entamoeba histolytica ( Pais-Morales et al, 2016 ), and Toxoplasma gondii ( Chen et al, 2019 ; Contreras et al, 2021 ). However, the inhibitory efficacy of RVT against Babesia and Theileria was not yet evaluated.…”

Section: Introductionmentioning

confidence: 99%

Evaluating the inhibitory effect of resveratrol on the multiplication of several Babesia species and Theileria equi on in vitro cultures, and Babesia microti in mice

et al. 2023

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Introduction: Histone post-translational modification is one of the most studied factors influencing epigenetic regulation of protozoan parasite gene expression, which is mediated by histone deacetylases (KDACs) and acetyltransferases (KATs).Objective and methods: The present study investigated the role of resveratrol (RVT) as an activator of histone deacetylases in the control of various pathogenic Babesia sp. and Theileria equi in vitro, as well as B. microti infected mice in vivo using fluorescence assay. Its role in mitigating the side effects associated with the widely used antibabesial drugs diminazene aceturate (DA) and azithromycin (AZM) has also been investigated.Results: The in vitro growth of B. bovis, B. bigemina, B. divergens, B. caballi and Theileria equi (T. equi) was significantly inhibited (P < 0.05) by RVT treatments. The estimated IC50 values revealed that RVT has the greatest inhibitory effects on B. bovis growth in vitro, with an IC50 value of 29.51 ± 2.46 µM. Reverse transcription PCR assay showed that such inhibitory activity might be attributed to resveratrol’s stimulatory effect on B. bovis KDAC3 (BbKADC3) as well as its inhibitory effect on BbKATS. RVT causes a significant decrease (P < 0.05) in cardiac troponin T (cTnT) levels in heart tissue of B. microti- infected mice, thereby indicating that RVT may play a part in reducing the cardiotoxic effects of AZM. Resveratrol showed an additive effect with imidocarb dipropionate in vivo. Treatment of B. microti-infected mice with a combined 5 mg/kg RVT and 8.5 mg/kg ID resulted in an 81.55% inhibition at day 10 postinoculation (peak of parasitemia).Conclusion: Our data show that RVT is a promising antibabesial pharmacological candidate with therapeutic activities that could overcome the side effects of the currently used anti-Babesia medications.

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The role of host autophagy in intracellular protozoan parasites diseases

Silva,

Ribeiro,

Farias

et al. 2024

Archives of Biochemistry and Biophysics

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In vitro evaluation of Resveratrol as a potential pre-exposure prophylactic drug against Trypanosoma cruzi infection

Cited by 7 publications

References 68 publications

Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs

Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs

Evaluating the inhibitory effect of resveratrol on the multiplication of several Babesia species and Theileria equi on in vitro cultures, and Babesia microti in mice

The role of host autophagy in intracellular protozoan parasites diseases

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