<i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies
Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we repo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-09-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/18/5535 |
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| author | Oscar A. Lenis-Rojas Sandra Cordeiro Marta Horta-Meireles Jhonathan Angel Araujo Fernández Sabela Fernández Vila Juan Andrés Rubiolo Pablo Cabezas-Sainz Laura Sanchez Alexandra R. Fernandes Beatriz Royo |
| author_facet | Oscar A. Lenis-Rojas Sandra Cordeiro Marta Horta-Meireles Jhonathan Angel Araujo Fernández Sabela Fernández Vila Juan Andrés Rubiolo Pablo Cabezas-Sainz Laura Sanchez Alexandra R. Fernandes Beatriz Royo |
| author_sort | Oscar A. Lenis-Rojas |
| collection | DOAJ |
| description | Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing <i>n</i>-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex <b>Fe1</b> displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC<sub>50</sub> values in the low micromolar range. The antiproliferative effect of <b>Fe1</b> was even higher than cisplatin. Interestingly, <b>Fe1</b> showed low in vivo toxicity, and in vivo analyses of <b>Fe1</b> and <b>Fe2</b> compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo. |
| first_indexed | 2024-03-10T07:24:11Z |
| format | Article |
| id | doaj.art-719b6affd54745608726e7a8ff19619b |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T07:24:11Z |
| publishDate | 2021-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-719b6affd54745608726e7a8ff19619b2023-11-22T14:24:35ZengMDPI AGMolecules1420-30492021-09-012618553510.3390/molecules26185535<i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological StudiesOscar A. Lenis-Rojas0Sandra Cordeiro1Marta Horta-Meireles2Jhonathan Angel Araujo Fernández3Sabela Fernández Vila4Juan Andrés Rubiolo5Pablo Cabezas-Sainz6Laura Sanchez7Alexandra R. Fernandes8Beatriz Royo9ITQB NOVA, Instituto de Tecnologia Química e Biológica António Xavier, Av. da República, 2780-157 Oeiras, PortugalUCIBIO, Departamento Ciências da Vida, NOVA School of Science and Technology, NOVA University, Campus de Caparica, 2829-516 Caparica, PortugalITQB NOVA, Instituto de Tecnologia Química e Biológica António Xavier, Av. da República, 2780-157 Oeiras, PortugalDepartamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, SpainDepartamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, SpainDepartamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, SpainDepartamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, SpainDepartamento de Zoología Genética y Antropología Física, Facultad de Veterinaria, Universidad de Santiago de Compostela, Campus de Lugo, 27002 Lugo, SpainUCIBIO, Departamento Ciências da Vida, NOVA School of Science and Technology, NOVA University, Campus de Caparica, 2829-516 Caparica, PortugalITQB NOVA, Instituto de Tecnologia Química e Biológica António Xavier, Av. da República, 2780-157 Oeiras, PortugalCisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing <i>n</i>-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex <b>Fe1</b> displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC<sub>50</sub> values in the low micromolar range. The antiproliferative effect of <b>Fe1</b> was even higher than cisplatin. Interestingly, <b>Fe1</b> showed low in vivo toxicity, and in vivo analyses of <b>Fe1</b> and <b>Fe2</b> compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.https://www.mdpi.com/1420-3049/26/18/5535<i>N</i>-heterocyclic carbeneiron(II)–NHC complexesanticancer activityzebrafish |
| spellingShingle | Oscar A. Lenis-Rojas Sandra Cordeiro Marta Horta-Meireles Jhonathan Angel Araujo Fernández Sabela Fernández Vila Juan Andrés Rubiolo Pablo Cabezas-Sainz Laura Sanchez Alexandra R. Fernandes Beatriz Royo <i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies Molecules <i>N</i>-heterocyclic carbene iron(II)–NHC complexes anticancer activity zebrafish |
| title | <i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies |
| title_full | <i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies |
| title_fullStr | <i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies |
| title_full_unstemmed | <i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies |
| title_short | <i>N</i>-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies |
| title_sort | i n i heterocyclic carbene iron complexes as anticancer agents in vitro and in vivo biological studies |
| topic | <i>N</i>-heterocyclic carbene iron(II)–NHC complexes anticancer activity zebrafish |
| url | https://www.mdpi.com/1420-3049/26/18/5535 |
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