In Vitro Trypanocidal Activity of Tetraethylthiuram Disulfide and Sodium Diethylamine-N-Carbodithioate on Trypanosoma cruzi

Lane, Joshua E.; Ribeiro‐Rodrigues, Rodrigo; Suarez, Cristina C.; Bogitsh, Burton J.; Jones, Mark M.; Singh, P. K.; Carter, Clint E.

doi:10.4269/ajtmh.1996.55.263

Cited by 37 publications

(26 citation statements)

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“…Several Fe 3+ chelating agents showed activity against epimastigotes, that could be decrease in the presence of iron (Jones et al 1993, Singh et al 1997, and tetraethyl derivative of aminothiol was active against trypomastigotes (Deharo et al 2000). The metal chelator sodium diethylamine-N-carbodithioate showed, in relation to Bz a similar activity against epimastigotes and intracellular amastigotes but lower activity against trypomastigotes (Lane et al 1996). Another chelator, 1,10-phenanthroline inhibited epimastigote proliferation and led to electron-dense deposits in the kinetoplast, mitochondrion, and endoplasmic reticulum, identified as containing predominantly calcium and suggesting to the authors the involvement of disruption of calcium homeostasis in the trypanocidal activity (Lane et al 1998).…”

Section: Synthetic Drugsmentioning

confidence: 98%

A Critical Review on Chagas Disease Chemotherapy

Coura¹,

Castro

2002

Mem. Inst. Oswaldo Cruz

839

444

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Section: Synthetic Drugsmentioning

confidence: 98%

A Critical Review on Chagas Disease Chemotherapy

Coura¹,

Castro

2002

Mem. Inst. Oswaldo Cruz

839

444

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“…Disulfiram has been given to humans to eradicate a number of protozoan parasites, including Giardia lamblia (Nash and Rice, 1998), Plasmodium falciparum (Scheibel et al, 1979), and Trypanosoma cruzi (Lane et al, 1996) for decades. Its toxicity to humans is relatively low, with few significant Fig.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Invasion and Angiogenesis by Zinc-Chelating Agent Disulfiram

Shian¹,

Kao²,

Wu³

et al. 2003

Mol Pharmacol

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Cell invasion and angiogenesis are crucial processes in cancer metastasis that require extracellular matrix (ECM) degradation. Proteolytic degradation of the ECM components is a central event of invasion and angiogenesis processes. During these processes, matrix metalloproteinases (MMPs) seem to be primarily responsible for much of the ECM degradation. Disulfiram is frequently used in the treatment of alcoholism and has been reported to possess antiretroviral activity and can eject intrinsic zinc out of human immunodeficiency virus (HIV) nucleocapsid protein. In this report, we show that disulfiram inhibited invasion and angiogenesis in both tumor and endothelial cells at nontoxic concentrations. The 3 H-labeled type IV collagen degradation assay suggested that disulfiram has type IV collagenase inhibitory activity, and this inhibition was responsible for blocking invasion and angiogenesis through cell-mediated and noncell-mediated pathways. However, the mechanisms underlying cell-mediated signal pathways are not fully characterized. Our data demonstrate that the non-cell-mediated pathway is dominant. Thus, disulfiram could directly interact with MMP-2 and MMP-9 and inhibit their proteolytic activity through a zincchelating mechanism. Addition of zinc could reverse the inhibition of invasiveness and collagenase inhibition through disulfiram treatment. This finding implies that MMP-2 and MMP-9 may be the inhibitory targets for a potential disulfiram treatment. These observations raise the possibility clinical therapeutic applications for disulfiram used as a potential inhibitor of metastatic cell invasion and angiogenesis.

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“…The trypomastigotes viability was based on the cellular conversion of the soluble tetrazolium salt MTT into the insoluble formazan by mitochondrial enzymes. The formazan extraction was carried out with 10% (v/v) SDS for 18 h at 24 o C (Lane et al, 1996) in a spectrophotometer Multiskan MS (Uniscience) microplate reader.…”

Section: Trypanocidal Activitymentioning

confidence: 99%

Chemical constituents of the volatile oil from leaves of Annona coriacea and in vitro antiprotozoal activity

Siqueira

Oliani

Sartoratto³

et al. 2011

Rev. bras. farmacogn.

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Abstract:The essential oil of the leaves from Annona coriacea Mart., Annonaceae, was extracted by hydrodistillation in a Clevenger apparatus and analyzed by GC/MS and GC/FID. The oil yield was 0.05% m/m. Sixty compounds were identified, in a complex mixture of sesquiterpenes (76.7%), monoterpenes (20.0%) and other constituents (3.3%). Bicyclogermacrene was its major compound (39.8%) followed by other sesquiterpenes. Most of the monoterpenes were in low concentration (<1%). Only β-pinene and pseudolimonene presented the highest level of 1.6%. The volatile oil presented anti-leishmanial and trypanocidal activity against promastigotes of four species of Leishmania and trypomastigotes of Trypanosoma cruzi, showing to be more active against Leishmania (L.) chagasi (IC50 39.93 µg/mL) (95% CI 28.00-56.95 µg/mL).

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In Vitro Trypanocidal Activity of Tetraethylthiuram Disulfide and Sodium Diethylamine-N-Carbodithioate on Trypanosoma cruzi

Cited by 37 publications

References 0 publications

A Critical Review on Chagas Disease Chemotherapy

A Critical Review on Chagas Disease Chemotherapy

Inhibition of Invasion and Angiogenesis by Zinc-Chelating Agent Disulfiram

Chemical constituents of the volatile oil from leaves of Annona coriacea and in vitro antiprotozoal activity

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