Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms
ABSTRACT The enhancement of anti-leukemia therapy and the treatment of infections caused by multidrug-resistant pathogens are major challenges in healthcare. Although a large arsenal of drugs is available, many of these become ineffective, and as a result, the discovery of new active substances occu...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Universidade de São Paulo
2018-04-01
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| Series: | Brazilian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000400617&lng=en&tlng=en |
| _version_ | 1811271323618377728 |
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| author | Melise Silveira Nunes Litiérri Razia Garzon Roberta Filipini Rampelotto Maísa Kräulich Tizotti Rosiéli Martini Aline Locatelli Marcelo Barbosa Manfredo Hörner Rosmari Hörner |
| author_facet | Melise Silveira Nunes Litiérri Razia Garzon Roberta Filipini Rampelotto Maísa Kräulich Tizotti Rosiéli Martini Aline Locatelli Marcelo Barbosa Manfredo Hörner Rosmari Hörner |
| author_sort | Melise Silveira Nunes |
| collection | DOAJ |
| description | ABSTRACT The enhancement of anti-leukemia therapy and the treatment of infections caused by multidrug-resistant pathogens are major challenges in healthcare. Although a large arsenal of drugs is available, many of these become ineffective, and as a result, the discovery of new active substances occurs. Notably, triazenes (TZCs) have been consolidated as a promising class of compounds, characterized by significant biological activity, especially antiproliferative and antimicrobial properties. The aim of this study is the synthesis and characterization of a new triazenide complex of gold (I), as well as the in vitro assessment of its antiproliferative activity against the K562 cell line (Chronic Myeloid Leukemia), and antibacterial activity against bacterial isolates of biofilm-producing coagulase-negative staphylococci. The combination of TZC with gold metal tends to have a synergistic effect against all biofilm-producing isolates, with Minimum Inhibitory Concentration values (MIC) between 32 and 64 µg mL-1. It has also shown activity against K562 cell line, getting an IC50=4.96 µM. Imatinib mesylate (Glivec) was used as reference, with IC50=3.86 µM. To the best of our knowledge, this study represents the first report of the activity of a TZC complexed with gold ion in the oxidation state (I) against microorganisms that produce biofilm and K562 cells. |
| first_indexed | 2024-04-12T22:19:07Z |
| format | Article |
| id | doaj.art-f405ba880b864331beb8dd23c3dc46a9 |
| institution | Directory Open Access Journal |
| issn | 2175-9790 |
| language | English |
| last_indexed | 2024-04-12T22:19:07Z |
| publishDate | 2018-04-01 |
| publisher | Universidade de São Paulo |
| record_format | Article |
| series | Brazilian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-f405ba880b864331beb8dd23c3dc46a92022-12-22T03:14:27ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences2175-97902018-04-0153410.1590/s2175-97902017000400191S1984-82502017000400617Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganismsMelise Silveira NunesLitiérri Razia GarzonRoberta Filipini RampelottoMaísa Kräulich TizottiRosiéli MartiniAline LocatelliMarcelo BarbosaManfredo HörnerRosmari HörnerABSTRACT The enhancement of anti-leukemia therapy and the treatment of infections caused by multidrug-resistant pathogens are major challenges in healthcare. Although a large arsenal of drugs is available, many of these become ineffective, and as a result, the discovery of new active substances occurs. Notably, triazenes (TZCs) have been consolidated as a promising class of compounds, characterized by significant biological activity, especially antiproliferative and antimicrobial properties. The aim of this study is the synthesis and characterization of a new triazenide complex of gold (I), as well as the in vitro assessment of its antiproliferative activity against the K562 cell line (Chronic Myeloid Leukemia), and antibacterial activity against bacterial isolates of biofilm-producing coagulase-negative staphylococci. The combination of TZC with gold metal tends to have a synergistic effect against all biofilm-producing isolates, with Minimum Inhibitory Concentration values (MIC) between 32 and 64 µg mL-1. It has also shown activity against K562 cell line, getting an IC50=4.96 µM. Imatinib mesylate (Glivec) was used as reference, with IC50=3.86 µM. To the best of our knowledge, this study represents the first report of the activity of a TZC complexed with gold ion in the oxidation state (I) against microorganisms that produce biofilm and K562 cells.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000400617&lng=en&tlng=enTriazenes/synthesis/characterization/biological activityTZC/Gold ion complexedChronic myeloid leukemiaAntibacterial activity |
| spellingShingle | Melise Silveira Nunes Litiérri Razia Garzon Roberta Filipini Rampelotto Maísa Kräulich Tizotti Rosiéli Martini Aline Locatelli Marcelo Barbosa Manfredo Hörner Rosmari Hörner Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms Brazilian Journal of Pharmaceutical Sciences Triazenes/synthesis/characterization/biological activity TZC/Gold ion complexed Chronic myeloid leukemia Antibacterial activity |
| title | Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms |
| title_full | Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms |
| title_fullStr | Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms |
| title_full_unstemmed | Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms |
| title_short | Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms |
| title_sort | synthesis characterization and biological activity of a gold i triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms |
| topic | Triazenes/synthesis/characterization/biological activity TZC/Gold ion complexed Chronic myeloid leukemia Antibacterial activity |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000400617&lng=en&tlng=en |
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