Anticancer Potential and Safety Profile of β-Lapachone In Vitro
Ipê is a plant of the Bignoniaceae family. Among the compounds extracted from this tree, lapachol is notable because its structural modification allows the production of β-lapachone, which has anticancer properties. The objective of this work was to test this hypothesis at a cellular level in vitro...
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MDPI AG
2024-03-01
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| Online Access: | https://www.mdpi.com/1420-3049/29/6/1395 |
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| author | Karina Motta Melo Lima Luana França Calandrini de Azevedo Jorge Dores Rissino Valdicley Vieira Vale Erica Vanessa Souza Costa Maria Fani Dolabela Cleusa Yoshiko Nagamachi Julio Cesar Pieczarka |
| author_facet | Karina Motta Melo Lima Luana França Calandrini de Azevedo Jorge Dores Rissino Valdicley Vieira Vale Erica Vanessa Souza Costa Maria Fani Dolabela Cleusa Yoshiko Nagamachi Julio Cesar Pieczarka |
| author_sort | Karina Motta Melo Lima |
| collection | DOAJ |
| description | Ipê is a plant of the Bignoniaceae family. Among the compounds extracted from this tree, lapachol is notable because its structural modification allows the production of β-lapachone, which has anticancer properties. The objective of this work was to test this hypothesis at a cellular level in vitro and assess its potential safety for use. The following tests were performed: MTT cell viability assay, apoptotic index determination, comet assay, and micronucleus test. The results showed that β-lapachone had a high cytotoxic capacity for all cell lines tested: ACP02 (gastric adenocarcinoma cells), MCF7 (breast carcinoma cells), HCT116 (colon cancer cells) and HEPG2 (hepatocellular carcinoma cells). Regarding genotoxicity, the exposure of cells to sublethal doses of β-lapachone induced DNA damage (assessed by the comet assay) and nuclear abnormalities, such as nucleoplasmic bridges and nuclear buds (assessed by the micronucleus test). All tested cell lines responded similarly to β-lapachone, except for ACP02 cells, which were relatively resistant to the cytotoxic effects of the compound in the MTT test. Our results collectively indicate that although β-lapachone showed antiproliferative activity against cancer cell lines, it also caused harmful effects in these cells, suggesting that the use of β-lapachone in treating cancer should be carried out with caution. |
| first_indexed | 2024-04-24T17:58:25Z |
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| id | doaj.art-867fba0984fd4bbcae5e5a83e7c68539 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-04-24T17:58:25Z |
| publishDate | 2024-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-867fba0984fd4bbcae5e5a83e7c685392024-03-27T13:57:16ZengMDPI AGMolecules1420-30492024-03-01296139510.3390/molecules29061395Anticancer Potential and Safety Profile of β-Lapachone In VitroKarina Motta Melo Lima0Luana França Calandrini de Azevedo1Jorge Dores Rissino2Valdicley Vieira Vale3Erica Vanessa Souza Costa4Maria Fani Dolabela5Cleusa Yoshiko Nagamachi6Julio Cesar Pieczarka7Center for Advanced Studies of the Biodiversity, Guamá Science and Technology Park, Federal University of Pará, Belém 66075-750, PA, BrazilCenter for Advanced Studies of the Biodiversity, Guamá Science and Technology Park, Federal University of Pará, Belém 66075-750, PA, BrazilCenter for Advanced Studies of the Biodiversity, Guamá Science and Technology Park, Federal University of Pará, Belém 66075-750, PA, BrazilPostgraduate Program in Pharmaceutical Innovation, Federal University of Pará, Belém 66075-110, PA, BrazilPostgraduate Program in Pharmaceutical Innovation, Federal University of Pará, Belém 66075-110, PA, BrazilPostgraduate Program in Pharmaceutical Innovation, Federal University of Pará, Belém 66075-110, PA, BrazilCenter for Advanced Studies of the Biodiversity, Guamá Science and Technology Park, Federal University of Pará, Belém 66075-750, PA, BrazilCenter for Advanced Studies of the Biodiversity, Guamá Science and Technology Park, Federal University of Pará, Belém 66075-750, PA, BrazilIpê is a plant of the Bignoniaceae family. Among the compounds extracted from this tree, lapachol is notable because its structural modification allows the production of β-lapachone, which has anticancer properties. The objective of this work was to test this hypothesis at a cellular level in vitro and assess its potential safety for use. The following tests were performed: MTT cell viability assay, apoptotic index determination, comet assay, and micronucleus test. The results showed that β-lapachone had a high cytotoxic capacity for all cell lines tested: ACP02 (gastric adenocarcinoma cells), MCF7 (breast carcinoma cells), HCT116 (colon cancer cells) and HEPG2 (hepatocellular carcinoma cells). Regarding genotoxicity, the exposure of cells to sublethal doses of β-lapachone induced DNA damage (assessed by the comet assay) and nuclear abnormalities, such as nucleoplasmic bridges and nuclear buds (assessed by the micronucleus test). All tested cell lines responded similarly to β-lapachone, except for ACP02 cells, which were relatively resistant to the cytotoxic effects of the compound in the MTT test. Our results collectively indicate that although β-lapachone showed antiproliferative activity against cancer cell lines, it also caused harmful effects in these cells, suggesting that the use of β-lapachone in treating cancer should be carried out with caution.https://www.mdpi.com/1420-3049/29/6/1395Ipêantiproliferative activitygenotoxicitymutagenicityapoptosis |
| spellingShingle | Karina Motta Melo Lima Luana França Calandrini de Azevedo Jorge Dores Rissino Valdicley Vieira Vale Erica Vanessa Souza Costa Maria Fani Dolabela Cleusa Yoshiko Nagamachi Julio Cesar Pieczarka Anticancer Potential and Safety Profile of β-Lapachone In Vitro Molecules Ipê antiproliferative activity genotoxicity mutagenicity apoptosis |
| title | Anticancer Potential and Safety Profile of β-Lapachone In Vitro |
| title_full | Anticancer Potential and Safety Profile of β-Lapachone In Vitro |
| title_fullStr | Anticancer Potential and Safety Profile of β-Lapachone In Vitro |
| title_full_unstemmed | Anticancer Potential and Safety Profile of β-Lapachone In Vitro |
| title_short | Anticancer Potential and Safety Profile of β-Lapachone In Vitro |
| title_sort | anticancer potential and safety profile of β lapachone in vitro |
| topic | Ipê antiproliferative activity genotoxicity mutagenicity apoptosis |
| url | https://www.mdpi.com/1420-3049/29/6/1395 |
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