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从[具体来源未明确]分离出的甲基β-紫罗糖胺二糖苷与拓扑异构酶II的结合接近度导致乳腺癌细胞系凋亡。

The binding proximity of methyl β-lilacinobioside isolated from with topoisomerase II attributes apoptosis in breast cancer cell line.

作者信息

Alallah Mohammad Ibrahim, Alhemaid Fahad, Bai Fang, Mothana Ramzi Ahmed, Elshikh Mohamed Soliman, Abul Farah Mohammad, Ali Mohammad Ajmal, Lee Joongku, Al-Anazi Khalid Mashay

机构信息

Department of Botany and Microbiology, College of Science, King Saud University, Riyadh 11451, Saudi Arabia.

Center for Theoretical Biological Physics, Rice University, Houston, TX 77005, USA.

出版信息

Saudi J Biol Sci. 2018 Dec;25(8):1826-1833. doi: 10.1016/j.sjbs.2018.02.017. Epub 2018 Feb 27.

DOI:10.1016/j.sjbs.2018.02.017
PMID:30591807
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6303161/
Abstract

The alterations in somatic genomes that controls the mechanism of cell division as a main cause of cancer, and then the drug that specifically toxic to the cancer cells further complicates the process of the development of the widely effective potential anticancer drug. The side effects of the drug as well as the radiotherapy used for the treatment of cancer is severe; therefore, the search of the natural products from the sources of wild plants having anticancer potential is become immense importance today. The ethno-medicinal survey undertaken in Al-Fayfa and Wadi-E-Damad region of southern Saudi Arabia revealed that the (Ehrenb.) N.E.Br. (family Apocynaceae) is being used for the treatment of cancer by the native inhabitants. The biological evaluation of anticancer potential of bioassay-guided fractionations of methanolic extract of whole plant of against human breast adenocarcinoma cell line (MCF-7) followed by characterization using spectroscopic methods confirmed the presence of methyl β-lilacinobioside, a novel active constituent reported for the first time from , is capable of inhibition of cell proliferation and induction of apoptosis in MCF-7 cells by regulating ROS mediated autophagy, and thus validated the folkloric claim. Based on a small-scale computational target screening, Topoisomerase II was identified as the potential binding target of methyl β-lilacinobioside.

摘要

体细胞基因组的改变控制着细胞分裂机制，这是癌症的主要成因，而对癌细胞具有特异性毒性的药物，进一步使开发广泛有效的潜在抗癌药物的过程变得复杂。用于治疗癌症的药物以及放射疗法的副作用都很严重；因此，从具有抗癌潜力的野生植物来源寻找天然产物在当今变得极为重要。在沙特阿拉伯南部的法伊法和瓦迪 - 达马德地区进行的民族药用调查显示，当地居民使用夹竹桃科的（Ehrenb.）N.E.Br.来治疗癌症。对全株甲醇提取物进行生物测定指导的分级分离，并采用光谱方法进行表征，以评估其对人乳腺癌细胞系（MCF - 7）的抗癌潜力，结果证实了首次从 中报道的新型活性成分甲基β - 紫罗碱二糖苷的存在，它能够通过调节活性氧介导的自噬来抑制MCF - 7细胞的增殖并诱导其凋亡，从而验证了民间说法。基于小规模的计算靶点筛选，拓扑异构酶II被确定为甲基β - 紫罗碱二糖苷的潜在结合靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/1c1b8798aff7/gr11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/a1fdeadf1b39/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/8e3f7faae357/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/0af4143ece2b/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/680c7f33c906/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/04e13def3ae3/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/7add07f94360/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/367937fdd7cb/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/60f64f1c51a0/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/b276d9320c98/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/eab7cba39df9/gr10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/1c1b8798aff7/gr11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/a1fdeadf1b39/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/8e3f7faae357/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/0af4143ece2b/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/680c7f33c906/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/04e13def3ae3/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/7add07f94360/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/367937fdd7cb/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/60f64f1c51a0/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/b276d9320c98/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/eab7cba39df9/gr10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a49/6303161/1c1b8798aff7/gr11.jpg

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