New iminodibenzyl derivatives with anti-leishmanial activity

Arndt, Anderson; Liria, Cleber Wanderlei; Yokoyama-Yasunaka, Jenicer K.U.; Miranda, Maria Terêsa Machini de; Uliana, Sílvia Reni Bortolin; Espósito, Breno Pannia

doi:10.1016/j.jinorgbio.2017.04.004

Cited by 6 publications

(4 citation statements)

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“…The development of metal complexes aimed at treating neglected diseases offers opportunities for pharmaceutical products because of their specific and unique physicochemical properties (Ong, Roy, Andrews, & Gasser, 2019), variety of coordination numbers, different oxidation states (Selvaganapathy & Raman, 2016) and the possibility of using a multi-target molecule approach for increasing drug efficiency (Arndt et al, 2017).…”

Section: Introductionmentioning

confidence: 99%

“…It is present as a structural and catalytic cofactor of several enzymes (Puig & Thiele, 2020) and in several studies, such as that by Gandin et al (2014), it has been shown that copper(I) complexes are capable of inhibiting the growth of tumor cells in vitro and in vivo. Arndt et al (2017) and Portas, Miguel, Yokoyama-Yasunaka, Uliana, and Espósito, (2012) demonstrated that different Cu(II) complexes have antileishmanial activity in vitro against L. (L.) amazonensis promastigotes.…”

Section: Introductionmentioning

confidence: 99%

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In vitro evaluation of antileishmanial activity of copper (I) complexes

et al. 2021

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In the research for the development of new drugs for the therapy of American tegumentary leishmaniasis, copper has been studied for its antileishmania activity. This study aims to report the activity of three copper(I) complexes on parasites of the species L. amazonensis and L. guyanensis. The metal complexes were tested according to in vitro antileishmanial assays, against promastigote and amastigote forms of the most prevalent species in the state of Amazonas, Brazil. Cytotoxicity of the complexes was evaluated in murine macrophage-like cell line (MJ774). The results of the in vitro assays indicated that, among the copper complexes tested, the homoleptic phosphine complex [Cu(thp)4][PF6](thp=tris-hydroxymethylphosphine) presented promising activity against the evolutionary forms of L. amazonensis, and obtained a IC50 of 26.45 and 24.61 µM in a period of 48 and 72 h, respectively. The results for copper complex at concentration 160 µM in amastigote forms showed a decrease in the infection index (32% of infected cells) and, in the cytotoxicity assay with MJ774, 52.43% of cell viability was observed. The results showed that the complex [Cu(thp)4][PF6] presented significant biological activity, indicating a need for future in vivo studies.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

In vitro evaluation of antileishmanial activity of copper (I) complexes

et al. 2021

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“…Various chemical structures were reported with TR inhibitor activity and leishmaniacidal activity to the literature: Ag(0) nanoparticles encapsulated by ferritin molecules [89], Cu(II) diketonates [90], oxabicyclo[3.3.1]nonanones [73], azole-based compounds -e. pyrrole [91], β-carboline-quinazolinone hybrid [92], phenothiazine and phenoxazine derived chloroacetamides [93], selenocyanates and diselenide compounds [94,95], iminodibenzyl derivatives with ethylenediamine, ethanolamine and diethylenetriamine and their copper(II) complexes [96], diaryl sulfide derivatives [97], ammonium trichloro [1,2-ethanediolato-O,O′]-tellurat [98], all-hydrocarbon stapled peptides [99] chalcone derivatives [100], thiophene derivatives [101], imidazole-phenyl-thiazole compounds [102], isothiocyanate derivatives [103], (phenylthio)pyrimidin-4-amine derivatives [104], ferrocenylquinoline derivatives [105], triazole-phenyl-thiazoles derivatives [106], fluorene derivatives [107], adamantan derivatives, and their gold complexes [108] and natural products [109,110] (Figure 6).…”

Section: Trypanothione Reductase (Tr Tryr Trypanothione-disulfide Red...mentioning

confidence: 99%

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

Istanbullu¹,

Bayraktar²

2022

Leishmaniasis - General Aspects of a Stigmatized Disease

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The leishmaniases are a group of diseases caused by protozoan parasites—Leishmania sp. Leishmaniasis is classified among the 20 neglected diseases by WHO. Although the disease has been known for more than 120 years, the number of drugs used for the treatment is still limited to 5–6. The first-line drugs against leishmaniasis are pentavalent antimonials, which were introduced to the treatment 70 years ago—despite all their side effects. Molecular targets are becoming increasingly important for efficacy and selectivity in postgenomic drug research studies. In this chapter, we have discussed potential therapeutic targets of antileishmanial drug discovery such as pteridine reductase (PTR1), trypanothione reductase (TR), N-myristoyltransferase (NMT), trypanothione synthetase (TryS), IU-nucleoside hydrolase, and topoisomerases, enzymes and their inhibitors reported in the literature.

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“…Several studies have investigated the activity of copper complexes in different oxidation states, and Cu(II) complexes have shown promising results in vitro against Leishmania spp. (Maffei et al 2009;Portas et al 2012;Arndt et al 2017;Méndez-Arriaga et al 2018).…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo activity of a hypotoxic copper(I) complex against dermotropic Leishmania species

et al. 2021

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Cutaneous leishmaniasis is a disease caused by protozoa of the genus Leishmania and, currently, the treatment of first choice is meglumine antimoniate. However, due to its limited effectiveness and high toxicity, it is necessary to seek new active principles for leishmaniasis treatment. Metal complexes are gaining importance due to their effectiveness and low toxicity. In this context, the present study aimed to evaluate the in vitro and in vivo antileishmanial activity of the hypotoxic copper(I) complex [HB(pz)3]Cu(PCN). Four dermotropic species of Leishmania were tested with the metal complex and its effectiveness was determined through parasitic viability and infectivity rate, and cytotoxicity was determined using a redox dye (resazurin). For the in vivo tests, hamsters were infected and the lesions treated with a formulated ointment containing the complex, the effectiveness of which was assessed by measuring the diameter of the inoculum/snout location and determining the parasitic load. The results demonstrated moderate toxicity in murine macrophages and human monocytes and better efficacy in Leishmania (V.) braziliensis when compared to the other species tested, with a 50% reduction in the viability of promastigote and amastigote forms (in vitro). General data from daily topical treatment for up to 30 days showed low efficacy for reducing lesions, and no clinical and parasitological cure was observed in the experimental animals. Thus, the [HB(pz)3]Cu(PCN) complex proved to be promising in in vitro studies against L. (V.) braziliensis, and should be further tested in new formulations and new experimental treatment schemes.

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New iminodibenzyl derivatives with anti-leishmanial activity

Cited by 6 publications

References 36 publications

In vitro evaluation of antileishmanial activity of copper (I) complexes

In vitro evaluation of antileishmanial activity of copper (I) complexes

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

In vitro and in vivo activity of a hypotoxic copper(I) complex against dermotropic Leishmania species

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