Apresentação

Four new Cu(I) complexes of the general formula [Cu-(PP)(LL)][BF 4 ], in which PP is a phosphane ligand (triphenylphosphane or 1,2-bis(diphenylphosphano)ethane (dppe)) and LL is a bioactive thiosemicarbazone ligand (4-(methyl)-1-(5nitrofurfurylidene)thiosemicarbazone) or 4-(ethyl)-1-(5nitrofurfurylidene)thiosemicarbazone) were synthesized and fully characterized by classical analytical and spectroscopic methods. The anti-trypanosome and anticancer activities were investigated in vitro on Trypanosoma cruzi and in two human cancer cell lines (ovarian OVCAR3 and prostate PC3). To test the selectivity toward parasites and cancer cells, the cytotoxicity on normal monkey kidney VERO and human dermal fibroblasts HDF cells was also evaluated. The new heteroleptic complexes were more cytotoxic on T. cruzi and chemoresistant prostate PC3 cells than the benchmark drugs nifurtimox and cisplatin. The compounds also showed a high level of cellular internalization by the OVCAR3 cells and, in particular, those containing the dppe phosphane showed activation of the cell death mechanism via apoptosis. On the other hand, the production of reactive oxygen species induced by these complexes was not evident.

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“…Parasites and cancers have many features in common [7–9] . Both can live and multiply indefinitely in mammals.…”

Section: Introductionmentioning

confidence: 99%

Copper(I)‐Thiosemicarbazone Complexes with Dual Anticancer and Antiparasitic Activity

et al. 2023

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“…The Schistosoma development process is rather slow as this trematode displays a complex life cycle that undergoes significant morphological and metabolic changes, suggesting the existence of an epigenetic control of gene expression. Interestingly, parasites and cancer cells have several properties in common, such as high metabolic and reproductive activity and the use of epigenetic processes to escape from chemotherapy and host immune surveillance [5] . Thus, the use of epi‐drugs – initially developed to treat cancer – has been considered a new promising strategy for the treatment of schistosomiasis and other parasitic diseases [6] .…”

Section: Introductionmentioning

confidence: 99%

Chemically Diverse S. mansoni HDAC8 Inhibitors Reduce Viability in Worm Larval and Adult Stages

et al. 2022

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Schistosoma mansoni HDAC8 is a reliable target to fight schistosomiasis, and several inhibitors have been reported in the literature up to now. Nevertheless, only a few displayed selectivity over the human deacetylases and some exhibited very low or no activity against parasite larvae and/or adult worms. We report here the in vitro enzyme and biological activity of a small library of HDAC inhibitors from our lab, in many cases exhibiting submicromolar/nanomolar potency against smHDAC8 and diverse degrees of selectivity over hHDAC1 and/or hHDAC6. Such compounds were tested against schistosomula, and a selection of them against the adult forms of S. mansoni, to detect their effect on viability. Some of them showed the highest viability reduction for the larval stage with IC50 values around 1 μM and/or displayed ∼40–50 % activity in adult worms at 10 μM, joined to moderate to no toxicity in human fibroblast MRC‐5 cells.

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Molecular Characterization of the Human Immunodeficiency Virus Type 1 among Children in Lima, Peru

Carrión

Laguna-Torres

Soto-Castellares

et al. 2009

AIDS Research and Human Retroviruses

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In Peru, there is a lack of information on molecular analysis in pediatric human immunodeficiency virus (HIV) infection. At present, the mother-to-child transmission rate is estimated at approximately 2-4%. The objective of this study was to assess the molecular epidemiology of HIV-1 in infected children. Children with suspected or confirmed pulmonary tuberculosis were evaluated at two public hospitals between 2002 and 2007. Whole blood samples were obtained from 90 HIV-positive children, who were confirmed to be positive by enzyme-linked immunosorbent assay and Western blot. The specimens were subjected to envelope heteroduplex mobility assay (env HMA) followed by gag and pol gene region sequence analysis. Subtype B was found in 88 (98%) of 90 children and 2 (2%) children were subtype BF recombinants. This is the first report of recombinant HIV strains in HIV-infected children in Peru. Understanding the origin, diversity, and spread of HIV strains worldwide will be necessary for the development of an effective vaccine that targets pediatric populations throughout the world.

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Apresentação

Cited by 4 publications

References 0 publications

Copper(I)‐Thiosemicarbazone Complexes with Dual Anticancer and Antiparasitic Activity

Copper(I)‐Thiosemicarbazone Complexes with Dual Anticancer and Antiparasitic Activity

Chemically Diverse S. mansoni HDAC8 Inhibitors Reduce Viability in Worm Larval and Adult Stages

Molecular Characterization of the Human Immunodeficiency Virus Type 1 among Children in Lima, Peru

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