Organic and Medicinal Chemistry Division, CSIR-Indian Institute of Chemical Biology, Kolkata, India.
Department of Chemistry, National Institute of Technology Nagaland, Dimapur, India.
J Biomol Struct Dyn. 2023 Nov;41(19):9686-9694. doi: 10.1080/07391102.2022.2145370. Epub 2022 Nov 15.
Small molecules targeting G-quadruplex of oncogene promoter is considered as a promising anticancer therapeutics approach. Natural aloe compounds aloe emodin, and its glycoside derivative aloe emodin-8-glucoside and aloin have anticancer activity and also have potential DNA binding ability. These three compounds have promising binding ability towards quadruplex structures particularly G-quadruplex. Here, this study demonstrates complete biophysical study of these compounds to quadruplex structure. Aloe emodin showed highest binding stabilization with which has been proved by absorbance, fluorescence, dye displacement, ITC and SPR studies. Moreover, comparative study of these compounds with HCT 116 cells line also agreed to their anti proliferative property which may be helpful to establish these aloe compounds as potential anticancer drugs. This study comprises a complete biophysical study along with their anti proliferative property and demonstrates aloe emodin as a potent binding molecule.
小分子靶向癌基因启动子的 G-四链体被认为是一种很有前途的抗癌治疗方法。天然芦荟化合物大黄素、其糖苷衍生物大黄素-8-葡萄糖苷和芦荟苷具有抗癌活性，并且具有潜在的 DNA 结合能力。这三种化合物对四链体结构，特别是 G-四链体具有良好的结合能力。在这项研究中，我们对这些化合物与四链体结构进行了完整的生物物理研究。大黄素表现出最高的结合稳定性，这已通过吸收、荧光、染料置换、ITC 和 SPR 研究得到证实。此外，这些化合物与 HCT 116 细胞系的比较研究也证明了它们的抗增殖特性，这可能有助于将这些芦荟化合物确立为潜在的抗癌药物。本研究包括完整的生物物理研究及其抗增殖特性，并证明大黄素是一种有效的结合分子。
