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柳叶红千层树皮提取物的抗增殖、诱导凋亡和抗氧化潜力:一项体外和计算机模拟研究。

Anti-proliferative, apoptosis inducing, and antioxidant potential of Callistemon lanceolatus bark extracts: an in vitro and in silico study.

作者信息

Kumar Ramesh, Kushwaha Prem Prakash, Singh Atul Kumar, Kumar Shashank, Pandey Abhay Kumar

机构信息

Department of Biochemistry, University of Allahabad, Allahabad (Prayagraj), 211002, Uttar Pradesh, India.

Department of Biochemistry, Central University of Punjab, Bathinda, 151401, Punjab, India.

出版信息

Med Oncol. 2023 May 8;40(6):169. doi: 10.1007/s12032-023-02035-4.

Abstract

The present study reports anticancer and antioxidant activities of Callistemon lanceolatus bark extracts. Anticancer activity was studied against MDA-MB-231 cells. Antioxidant assessment of the chloroform and methanol extracts showed considerable free radical scavenging, metal ion chelating, and reducing power potential. Chloroform extract exhibited potent inhibition of cancer cell proliferation in MTT assay (IC 9.6 μg/ml) and promoted programmed cell death. Reactive oxygen species (ROS) generation, mitochondria membrane potential (MMP) disruption ability, and nuclear morphology changes were studied using H-DCFDA, JC-1, and Hoechst dyes, respectively, using confocal microscopy. Apoptotic cells exhibited fragmented nuclei, increased ROS generation, and altered MMP in dose- and time-dependent manner. Chloroform extract upregulated the BAX-1 and CASP3 mRNA expression coupled with downregulation of BCL-2 gene. Further, in silico docking of phytochemicals present in C. lanceolatus with anti-apoptotic Bcl-2 protein endorsed apoptosis by its inhibition and thus corroborated the experimental findings. Obatoclax, a known inhibitor of Bcl-2 was used as a reference compounds.

摘要

本研究报告了柳叶红千层树皮提取物的抗癌和抗氧化活性。针对MDA-MB-231细胞研究了其抗癌活性。对氯仿提取物和甲醇提取物的抗氧化评估显示出相当可观的自由基清除、金属离子螯合和还原能力。氯仿提取物在MTT试验中对癌细胞增殖表现出强效抑制作用(IC 9.6 μg/ml),并促进程序性细胞死亡。分别使用H-DCFDA、JC-1和Hoechst染料,通过共聚焦显微镜研究了活性氧(ROS)生成、线粒体膜电位(MMP)破坏能力和核形态变化。凋亡细胞呈现细胞核碎片化、ROS生成增加以及MMP以剂量和时间依赖性方式改变。氯仿提取物上调BAX-1和CASP3 mRNA表达,同时下调BCL-2基因。此外,柳叶红千层中存在的植物化学物质与抗凋亡Bcl-2蛋白的计算机模拟对接通过其抑制作用证实了细胞凋亡,从而证实了实验结果。已知的Bcl-2抑制剂Obatoclax用作参考化合物。

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