Center for Advanced Studies of the Biodiversity, Guamá Science and Technology Park, Federal University of Pará, Belém 66075-750, PA, Brazil.
Campus Tomé Açu, Federal Rural University of the Amazon, Tomé Açu 68680-000, PA, Brazil.
Molecules. 2024 Mar 21;29(6):1395. doi: 10.3390/molecules29061395.
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.
依贝是紫葳科植物。从这种树中提取的化合物中,拉帕醇值得注意,因为其结构修饰可以产生具有抗癌特性的β-拉帕醇。这项工作的目的是在体外细胞水平上检验这一假设,并评估其使用的潜在安全性。进行了以下测试:MTT 细胞活力测定、凋亡指数测定、彗星试验和微核试验。结果表明,β-拉帕醇对所有测试的细胞系均具有高细胞毒性:ACP02(胃腺癌细胞)、MCF7(乳腺癌细胞)、HCT116(结肠癌细胞)和 HEPG2(肝癌细胞)。关于遗传毒性,细胞暴露于亚致死剂量的β-拉帕醇会引起 DNA 损伤(通过彗星试验评估)和核异常,如核质桥和核芽(通过微核试验评估)。除了 ACP02 细胞在 MTT 试验中对该化合物的细胞毒性相对具有抗性外,所有测试的细胞系对β-拉帕醇的反应相似。我们的结果表明,尽管β-拉帕醇对癌细胞系显示出抗增殖活性,但它也会对这些细胞造成有害影响,这表明在治疗癌症时应谨慎使用β-拉帕醇。