School of Bioengineering and Biosciences, Lovely Professional University, Phagwara 144411, India.
Division of Forest Resources, College of Forest and Environmental Sciences, Kangwon National University, Chunchon 200701, Korea.
Molecules. 2022 Jul 19;27(14):4597. doi: 10.3390/molecules27144597.
Lung cancer remains a major public health concern among all cancer diseases due to the toxicity and side-effects of the available commercially synthesized drugs. Natural product-derived synthesized anticancer drugs are now of promising interest to fight against cancer death. Carvacrol is a major component of most essential oil-bearing plants with potential pharmacological activity, especially against various cancer cell lines. Among the other organometallic compounds, copper complexes have been reported to be effective anticancer agents against various cancer cell lines, especially lung and leukemia cancers, due to the nontoxic nature of copper in normal cells since it is an endogenic metal. In this study, we synthesized three carvacrol derivatives, i.e., carvacrol aldehyde, Schiff base, and copper-Schiff base complex, through an established synthesis protocol and characterized the synthesized product using various spectroscopic techniques. The synthesized derivatives were evaluated for in vitro cytotoxic activity against different cancer cell lines, including human lung cancer (A549) and human fibroblast (BALB-3T3). Our findings showed that the copper-Schiff base complex derived from carvacrol inhibited the proliferation and migration of the A549 cell lines in a dose-dependent manner. This activity might be due to the inhibition of cell proliferation and migration at the G/M cell-cycle phase, as well as apoptosis, possibly through the activation of the mitochondrial apoptotic pathway. To our knowledge, this is the first report on the activity of the copper-Schiff base complex of carvacrol against A549 cell lines. Our result highlights that a new synthesized copper complex from carvacrol could be a novel potential drug in the treatment of lung cancer.
由于现有商业合成药物的毒性和副作用，肺癌仍然是所有癌症疾病中的一个主要公共卫生关注点。天然产物衍生的合成抗癌药物现在成为对抗癌症死亡的有希望的关注点。香芹酚是大多数含油植物的主要成分，具有潜在的药理活性，特别是对各种癌细胞系。在其他有机金属化合物中，据报道铜配合物是对抗各种癌细胞系的有效抗癌剂，特别是肺癌和白血病，因为铜在正常细胞中是非毒性的，因为它是一种内源性金属。在这项研究中，我们通过既定的合成方案合成了三种香芹酚衍生物，即香芹酚醛、席夫碱和铜-席夫碱配合物，并使用各种光谱技术对合成产物进行了表征。合成的衍生物被评估了对不同癌细胞系的体外细胞毒性活性，包括人肺癌（A549）和人成纤维细胞（BALB-3T3）。我们的研究结果表明，香芹酚衍生的铜-席夫碱配合物以剂量依赖的方式抑制 A549 细胞系的增殖和迁移。这种活性可能是由于细胞增殖和迁移在 G/M 细胞周期阶段以及凋亡的抑制，可能是通过线粒体凋亡途径的激活。据我们所知，这是首次报道香芹酚的铜-席夫碱配合物对 A549 细胞系的活性。我们的结果表明，香芹酚的新型合成铜配合物可能是治疗肺癌的一种新型潜在药物。
