<br>来自马尾藻的糖脂是克服 ABC 转运蛋白介导的癌症 MDR 的天然替代品,Chemistry & Biodiversity

当前位置： X-MOL 学术 › Chem. Biodivers. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

来自马尾藻的糖脂是克服 ABC 转运蛋白介导的癌症 MDR 的天然替代品
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2023-09-25 , DOI: 10.1002/cbdv.202301058
Kelly Muñoz-Losada ₁ , Kelli Monteiro Da Costa ₂ , Tatiana Muñoz-Castiblanco ₁ , Juan Camilo Mejía-Giraldo _{1,

3} , José Osvaldo Previato ₂ , Lucia Mendonça-Previato ₂ , Miguel Ángel Puertas-Mejía ₁

Affiliation

化疗是一种广泛使用的治疗癌症的策略，这种疾病每年导致数百万人死亡。然而，其功效因 ABC 转运蛋白的过度表达而降低，ABC 转运蛋白是排出化疗中使用的药物并参与多药耐药性 (MDR) 的蛋白质。糖脂已被确定为 ABC 转运蛋白的潜在抑制剂。马尾藻属藻类含有高水平的糖脂，使其成为对抗 MDR 表型的有前途的治疗替代品。通过氯仿/甲醇彻底浸渍获得马尾藻糖脂，通过柱色谱和薄层色谱纯化，然后通过 FTIR、NMR 和 LC-MS 进行表征。通过流式细胞术分析 PI 标记的细胞活力和 ABC 转运蛋白的抑制。耐药逆转的评估通过MTT测定来确定。发现10种磺基喹诺酰甘油类化合物，其中6种为首次报道。特别是，部分 4 (GL-4) 分别对 ABCC1 和 ABCB1 转运蛋白表现出强和中度的抑制活性。 GL-4 与抗肿瘤药物长春新碱联合治疗使 Lucena-1 细胞模型对药物敏感并逆转了 MDR 表型。这是首次报道从S. filipendula中分离出的糖脂能够抑制 ABC 转运蛋白，从而克服获得性耐药性。

"点击查看英文标题和摘要"

Glycolipids from Sargassum filipendula, a Natural Alternative for Overcoming ABC Transporter-Mediated MDR in Cancer

Chemotherapy is a widely used strategy to treat cancer, a disease that causes millions of deaths each year. However, its efficacy is reduced by the overexpression of ABC transporters, which are proteins that expel the drugs used in chemotherapy and involved in the multidrug resistance (MDR). Glycolipids have been identified as potential inhibitors of ABC transporters. Algae of the genus Sargassum contain high levels of glycolipids, making them a promising therapeutic alternative against the MDR phenotype. Sargassum filipendula glycolipids were obtained by exhaustive maceration with chloroform/methanol, purified by column and thin layer chromatography, and then characterized by FTIR, NMR, and LC-MS. Cell viability by PI labeling and inhibition of ABC transporters were analyzed by flow cytometry. Assessment of resistance reversal was determined by MTT assay. Ten sulfoquinovosylglycerol-type compounds were found, and six of them are reported for the first time. In particular, moiety 4 (GL-4) showed strong and moderate inhibitory activity against ABCC1 and ABCB1 transporters respectively. Treatment of GL-4 in combination with the antineoplastic drug vincristine sensitized Lucena-1 cell model to drug and reversed the MDR phenotype. This is the first report of glycolipids isolated from S. filipendula capable of inhibiting ABC transporters and thus overcoming acquired drug resistance.

更新日期：2023-09-25

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南