Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives
The 1,4-naphthoquinones, important members of the family of quinones are used as both crude extracts and as compound manipulated by the pharmaceutical industry. They have gained great emphasis by presenting different pharmacological properties as antibacterial, antiviral, antiprotozoal and anthelmin...
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| Format: | Article |
| Language: | English |
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Elsevier
2016-01-01
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| Series: | Toxicology Reports |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2214750016300749 |
| _version_ | 1819087036345221120 |
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| author | Valeska Santana de Sena Pereira Cláudio Bruno Silva de Oliveira Fernando Fumagalli Flávio da Silva Emery Naisandra Bezerra da Silva Valter F. de Andrade-Neto |
| author_facet | Valeska Santana de Sena Pereira Cláudio Bruno Silva de Oliveira Fernando Fumagalli Flávio da Silva Emery Naisandra Bezerra da Silva Valter F. de Andrade-Neto |
| author_sort | Valeska Santana de Sena Pereira |
| collection | DOAJ |
| description | The 1,4-naphthoquinones, important members of the family of quinones are used as both crude extracts and as compound manipulated by the pharmaceutical industry. They have gained great emphasis by presenting different pharmacological properties as antibacterial, antiviral, antiprotozoal and anthelmintic, and has antitumor activity. Our aim was to evaluate the cytotoxicity, hemolytic activity and in vivo acute toxicity of three derivatives of 2-hydroxy-1,4-naphthoquinones. The cell viability in vitro against RAW Cell Line displayed IC50 ranging of 483.5–2044.8 μM, whereas in primary culture tests using murine macrophages, IC50 were 315.8–1408.0 μM for naphthoquinones derivatives 4a and 4c respectively, besides no hemolysis was observed at the dose tested. The in vivo acute toxicity assays exhibited a significant safety margin indicated by a lack of systemic and behavioral toxicity up to 300 mg/kg, and at a dose of 1000 mg/kg the derivatives not triggering signs of toxicity although the compound 4a have promoted hepatic steatosis and hyperemia in kidney tissue. Thereby, these modifications decrease the toxicity of the tested derivatives naphthoquinones, providing a high potential for the development of news drugs. Keywords: Naphthoquinones, Cytotoxicity, Hemolytic activity, Acute toxicity |
| first_indexed | 2024-12-21T21:29:45Z |
| format | Article |
| id | doaj.art-60cec370b96940a3bfef18b080382402 |
| institution | Directory Open Access Journal |
| issn | 2214-7500 |
| language | English |
| last_indexed | 2024-12-21T21:29:45Z |
| publishDate | 2016-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Toxicology Reports |
| spelling | doaj.art-60cec370b96940a3bfef18b0803824022022-12-21T18:49:39ZengElsevierToxicology Reports2214-75002016-01-013756762Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivativesValeska Santana de Sena Pereira0Cláudio Bruno Silva de Oliveira1Fernando Fumagalli2Flávio da Silva Emery3Naisandra Bezerra da Silva4Valter F. de Andrade-Neto5Laboratory of Malaria and Toxoplasmosis Biology, Department of Microbiology and Parasitology, Federal University of Rio Grande do Norte, Natal, RN, BrazilLaboratory of Malaria and Toxoplasmosis Biology, Department of Microbiology and Parasitology, Federal University of Rio Grande do Norte, Natal, RN, BrazilDepartment of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, BrazilDepartment of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP, BrazilLaboratory of Histotecnology, Department of Morfology, Federal University of Rio Grande do Norte, Natal, RN, BrazilLaboratory of Malaria and Toxoplasmosis Biology, Department of Microbiology and Parasitology, Federal University of Rio Grande do Norte, Natal, RN, Brazil; Corresponding author.The 1,4-naphthoquinones, important members of the family of quinones are used as both crude extracts and as compound manipulated by the pharmaceutical industry. They have gained great emphasis by presenting different pharmacological properties as antibacterial, antiviral, antiprotozoal and anthelmintic, and has antitumor activity. Our aim was to evaluate the cytotoxicity, hemolytic activity and in vivo acute toxicity of three derivatives of 2-hydroxy-1,4-naphthoquinones. The cell viability in vitro against RAW Cell Line displayed IC50 ranging of 483.5–2044.8 μM, whereas in primary culture tests using murine macrophages, IC50 were 315.8–1408.0 μM for naphthoquinones derivatives 4a and 4c respectively, besides no hemolysis was observed at the dose tested. The in vivo acute toxicity assays exhibited a significant safety margin indicated by a lack of systemic and behavioral toxicity up to 300 mg/kg, and at a dose of 1000 mg/kg the derivatives not triggering signs of toxicity although the compound 4a have promoted hepatic steatosis and hyperemia in kidney tissue. Thereby, these modifications decrease the toxicity of the tested derivatives naphthoquinones, providing a high potential for the development of news drugs. Keywords: Naphthoquinones, Cytotoxicity, Hemolytic activity, Acute toxicityhttp://www.sciencedirect.com/science/article/pii/S2214750016300749 |
| spellingShingle | Valeska Santana de Sena Pereira Cláudio Bruno Silva de Oliveira Fernando Fumagalli Flávio da Silva Emery Naisandra Bezerra da Silva Valter F. de Andrade-Neto Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives Toxicology Reports |
| title | Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives |
| title_full | Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives |
| title_fullStr | Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives |
| title_full_unstemmed | Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives |
| title_short | Cytotoxicity, hemolysis and in vivo acute toxicity of 2-hydroxy-3-anilino-1,4-naphthoquinone derivatives |
| title_sort | cytotoxicity hemolysis and in vivo acute toxicity of 2 hydroxy 3 anilino 1 4 naphthoquinone derivatives |
| url | http://www.sciencedirect.com/science/article/pii/S2214750016300749 |
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