Department of Biochemistry and Molecular Biology, Medical University of Lublin, 20-093 Lublin, Poland.
Department of Pharmacognosy with Medicinal Plants Garden, Medical University of Lublin, 20-093 Lublin, Poland.
Molecules. 2023 Oct 31;28(21):7366. doi: 10.3390/molecules28217366.
Emodin-8--glucoside (E-8--G) is a glycosylated derivative of emodin that exhibits numerous biological activities, including immunomodulatory, anti-inflammatory, antioxidant, hepatoprotective, or anticancer activities. However, there are no reports on the activity of E-8--G against cancers of the nervous system. Therefore, the aim of the study was to investigate the antiproliferative and cytotoxic effect of E-8--G in the SK-N-AS neuroblastoma, T98G human glioblastoma, and C6 mouse glioblastoma cancer cells. As a source of E-8--G the methanolic extract from the aerial parts of Houtt. (Polygonaceae) was used. Thanks to the application of centrifugal partition chromatography (CPC) operated in the descending mode using a mixture of petroleum ether:ethyl acetate:methanol:water (4:5:4:5 ///) and a subsequent purification with preparative HPLC, E-8--G was obtained in high purity in a sufficient quantity for the bioactivity tests. Assessment of the cancer cell viability and proliferation were performed with the MTT (3-(bromide 4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium), CTG (CellTiter-Glo) and BrdU (5-bromo-2'-deoxyuridine) assays, respectively. E-8--G inhibits the viability and proliferation of SK-N-AS neuroblastoma, T98G human glioblastoma multiforme, and C6 mouse glioblastoma cells dose-dependently. E-8--G seems to be a promising natural antitumor compound in the therapy of nervous system tumors.
大黄素-8--葡萄糖苷(E-8--G)是大黄素的一种糖基化衍生物,具有多种生物活性,包括免疫调节、抗炎、抗氧化、保肝或抗癌活性。然而,目前尚无关于 E-8--G 对神经系统癌症活性的报道。因此,本研究旨在研究 E-8--G 对 SK-N-AS 神经母细胞瘤、T98G 人胶质母细胞瘤和 C6 小鼠胶质母细胞瘤癌细胞的增殖和细胞毒性作用。E-8--G 的来源是使用 Houtt.(Polygonaceae)地上部分的甲醇提取物。由于采用了在下降模式下操作的离心分配色谱(CPC),使用石油醚:乙酸乙酯:甲醇:水(4:5:4:5///)的混合物,并随后通过制备型 HPLC 进行纯化,以足够的量获得了高纯度的 E-8--G 用于生物活性测试。使用 MTT(3-(溴-4,5-二甲基噻唑-2-基)-2,5-二苯基四唑)、CTG(CellTiter-Glo)和 BrdU(5-溴-2'-脱氧尿苷)测定法分别评估癌细胞活力和增殖。E-8--G 剂量依赖性地抑制 SK-N-AS 神经母细胞瘤、T98G 人胶质母细胞瘤和 C6 小鼠胶质母细胞瘤细胞的活力和增殖。E-8--G 似乎是治疗神经系统肿瘤的有前途的天然抗肿瘤化合物。