Laboratory of Biology and Immunology of Cancer and Leishmania, Department of Morphology, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.
Graduate Program in Health Sciences, Federal University of Sergipe, Aracaju, Sergipe, Brazil.
BMC Complement Med Ther. 2023 Sep 20;23(1):333. doi: 10.1186/s12906-023-04156-9.
Lung cancer is the deadliest type of cancer in the world and the search for compounds that can treat this disease is highly important. Lawsone (2-hydroxy-1,4-naphtoquinone) is a naphthoquinone found in plants from the Lawsone genus that show a high cytotoxic effect in cancer cell lines and its derivatives show an even higher cytotoxic effect.
Sulforhodamine B was used to evaluate the cytotoxic activity of compounds on tumor cells. Clonogenic assay was used to analyze the reduction of colonies and wound healing assay to the migratory capacity of A549 cells. Apoptosis and necrosis were analyzed by flow cytometer and Giemsa staining. Hemolysis assay to determine toxicity in human erythrocytes.
Lawsone derivatives were evaluated and compound 1 (O-propargyllawsone) was the one with the highest cytotoxic effect, with IC below 2.5 µM in A549 cells. The compound was able to reduce colony formation and inhibit cell migration. Morphological changes and cytometry analysis show that the compound induces apoptosis and necrosis in A549 cells.
These results show that O-propargyllawsone show a cytotoxic effect and may induce apoptosis in A549 cells.
肺癌是世界上最致命的癌症类型,因此寻找能够治疗这种疾病的化合物非常重要。 植物中的萘醌类化合物如植物中的羟基萘醌(2-羟基-1,4-萘醌)lawsone 具有高细胞毒性作用,其衍生物的细胞毒性作用更高。
使用磺酰罗丹明 B 评估化合物对肿瘤细胞的细胞毒性活性。集落形成分析用于分析菌落减少,划痕愈合分析用于分析 A549 细胞的迁移能力。通过流式细胞仪和吉姆萨染色分析细胞凋亡和坏死。通过血红蛋白溶血试验测定人红细胞的毒性。
对 lawsone 衍生物进行了评估,化合物 1(O-炔丙基 lawsone)在 A549 细胞中具有最高的细胞毒性作用,IC 低于 2.5µM。该化合物能够减少集落形成并抑制细胞迁移。形态变化和细胞术分析表明,该化合物诱导 A549 细胞凋亡和坏死。
这些结果表明,O-炔丙基 lawsone 具有细胞毒性作用,并可能诱导 A549 细胞凋亡。