桦木醇及其衍生物对选定结直肠癌细胞系活力及其抗氧化系统的影响。
The Influence of Betulin and Its Derivatives on Selected Colorectal Cancer Cell Lines' Viability and Their Antioxidant Systems.
发表日期：2024 Aug 17
作者：
Marcel Madej, Celina Kruszniewska-Rajs, Magdalena Kimsa-Dudek, Agnieszka Synowiec-Wojtarowicz, Elwira Chrobak, Ewa Bębenek, Stanisław Boryczka, Stanisław Głuszek, Jolanta Adamska, Sebastian Kubica, Jarosław Matykiewicz, Joanna Magdalena Gola
来源：
Epigenetics & Chromatin
摘要：
氧化应激被认为是结直肠癌（CRC）发生的主要原因之一。根据疾病的阶段，可以观察到主要抗氧化酶，即超氧化物歧化酶（SOD）、过氧化氢酶（CAT）和谷胱甘肽过氧化物酶（GPx）的不同活性。由于结直肠癌的治疗方法有限，目前正在寻找针对氧化应激相关途径的具有潜在抗肿瘤活性的新物质，其中天然来源的物质（包括桦木醇）处于领先地位。对桦木醇分子进行化学修饰，以获得具有改善的药代动力学特性和更高的生物活性的新衍生物。本研究的目的是评估桦木醇及其新衍生物对结直肠癌细胞系活力和主要抗氧化系统的影响。研究表明，桦木醇及其衍生物EB5在蛋白质和mRNA水平上都不同程度地影响抗氧化酶活性。 SW1116 细胞系对测试化合物的抵抗力比 RKO 更强，这可能是由于这些细胞系的遗传和表观遗传特征存在差异。
Oxidative stress is considered one of the main reasons for the development of colorectal cancer (CRC). Depending on the stage of the disease, variable activity of the main antioxidant enzymes, i.e., superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx), is observed. Due to limited treatment methods for CRC, new substances with potential antitumor activity targeting pathways related to oxidative stress are currently being sought, with substances of natural origin, including betulin, leading the way. The betulin molecule is chemically modified to obtain new derivatives with improved pharmacokinetic properties and higher biological activity. The aim of this study was to evaluate the effects of betulin and its new derivatives on viability and major antioxidant systems in colorectal cancer cell lines. The study showed that betulin and its derivative EB5 affect the antioxidant enzyme activity to varying degrees at both the protein and mRNA levels. The SW1116 cell line is more resistant to the tested compounds than RKO, which may be due to differences in the genetic and epigenetic profiles of these lines.