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

从 Caralluma retrospiciens 中分离得到的甲基 β-紫丁香二糖苷与拓扑异构酶 II 的结合邻近性导致乳腺癌细胞系发生凋亡。

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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 Caralluma retrospiciens (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 C. retrospiciens 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 C. retrospiciens, 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.

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