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体外甲醇提取物对 叶的抗癌活性,特别关注人乳腺癌细胞系。

In Vitro Anticancer Activity of Methanolic Extract of Leaves with Special Emphasis on Human Breast Cancer Cell Line.

机构信息

Department of Pharmacology & Toxicology, National Institute of Pharmaceutical Education and Research, 168, Maniktala Main Road, Kolkata 700054, India.

Department of Natural Products, National Institute of Pharmaceutical Education and Research, 168, Maniktala Main Road, Kolkata 700054, India.

出版信息

Molecules. 2022 Nov 25;27(23):8222. doi: 10.3390/molecules27238222.

Abstract

Natural products are being targeted as alternative anticancer agents due to their non-toxic and safe nature. The present study was conducted to explore the in vitro anticancer potential of leaf extract. The methanolic leaf extract was prepared, and the phytochemicals and antioxidant potential were determined by LCMS analysis and DPPH radical scavenging assay, respectively. A docking study performed with five major alkaloidal phytoconstituents showed that they had a good binding affinity towards the active site of NF-κB. Cell viability assay was carried out in five different cell lines, and the extract exhibited the highest cytotoxicity in MCF-7, a breast cancer cell line. Extract-treated cells showed a significant increase in nitric oxide and reactive oxygen species production. Cell cycle analysis showed an arrest in cell growth at the Sub-G0 phase. The extract successfully inhibited cell migration and colony formation and altered mitochondrial membrane potential. The activities of superoxide dismutase and glutathione were also found to decrease in a dose-dependent manner. The percentage of apoptotic cells was found to increase in a dose-dependent manner in MCF-7 cells. The expressions of caspase-3, Bax, and cleaved-PARP were increased in extract-treated cells. An increase in the expression of NF-κB was found in the cytoplasm in extract-treated cells. leaf extract showed a potential anticancer effect in MCF-7 cells.

摘要

天然产物因其无毒、安全的特性而被作为抗癌药物的替代品。本研究旨在探索叶提取物的体外抗癌潜力。通过 LCMS 分析和 DPPH 自由基清除测定法,分别对叶的甲醇提取物进行了植物化学成分和抗氧化能力的检测。对 5 种主要生物碱类植物成分进行的对接研究表明,它们与 NF-κB 的活性位点具有良好的结合亲和力。在 5 种不同的细胞系中进行了细胞活力测定,结果表明该提取物在 MCF-7(乳腺癌细胞系)中表现出最高的细胞毒性。提取物处理的细胞显示出一氧化氮和活性氧物质产生的显著增加。细胞周期分析显示细胞生长在 Sub-G0 期停滞。该提取物成功抑制了细胞迁移和集落形成,并改变了线粒体膜电位。超氧化物歧化酶和谷胱甘肽的活性也被发现呈剂量依赖性降低。在 MCF-7 细胞中,凋亡细胞的比例呈剂量依赖性增加。提取物处理的细胞中 caspase-3、Bax 和 cleaved-PARP 的表达增加。提取物处理的细胞中细胞质中 NF-κB 的表达增加。叶提取物在 MCF-7 细胞中表现出潜在的抗癌作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5fc8/9737760/0aa4ecbc3bef/molecules-27-08222-g001.jpg

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