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Glycolipids from Sargassum filipendula, a Natural Alternative for Overcoming ABC Transporter-Mediated MDR in Cancer
Kelly Muñoz-Losada1, Kelli Monteiro Da Costa2, Tatiana Muñoz-Castiblanco1
1Grupo de Investigación en Compuestos Funcionales, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia UdeA, Calle 70 No. 52-21, Medellín, 050010, Colombia.
Abstract:
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.
Insights
Marine algae glycolipids show promise in fighting cancer drug resistance. Sargassum filipendula compounds inhibit ABC transporters, reversing multidrug resistance (MDR) and sensitizing cancer cells to chemotherapy.
Area of Science:
- Marine Biology
- Pharmacology
- Biochemistry
Background:
- Chemotherapy is a vital cancer treatment, but its effectiveness is limited by multidrug resistance (MDR).
- Multidrug resistance often arises from the overexpression of ATP-binding cassette (ABC) transporters, which actively pump chemotherapy drugs out of cancer cells.
- Glycolipids, particularly those from marine algae like Sargassum, are emerging as potential inhibitors of these ABC transporters.
Purpose of the Study:
- To isolate and characterize glycolipids from Sargassum filipendula.
- To evaluate the potential of these glycolipids in inhibiting ABC transporters and overcoming multidrug resistance in cancer.
- To assess the synergistic effect of isolated glycolipids with conventional chemotherapy drugs.
Main Methods:
- Glycolipids were extracted from Sargassum filipendula using chloroform/methanol and purified via column and thin-layer chromatography.
- Compound characterization was performed using Fourier-transform infrared spectroscopy (FTIR), Nuclear Magnetic Resonance (NMR), and Liquid Chromatography-Mass Spectrometry (LC-MS).
- Inhibition of ABC transporters and cell viability were assessed using flow cytometry and MTT assays, respectively.
Main Results:
- Ten sulfoquinovosylglycerol-type glycolipids were identified, with six being novel compounds.
- A specific glycolipid, GL-4, demonstrated significant inhibitory activity against ABCC1 and ABCB1 transporters.
- Co-administration of GL-4 with vincristine resensitized the Lucena-1 cell model to the drug, effectively reversing the multidrug resistance phenotype.
Conclusions:
- Sargassum filipendula is a rich source of bioactive glycolipids with potential anticancer applications.
- The identified glycolipids, particularly GL-4, are effective inhibitors of key ABC transporters involved in multidrug resistance.
- This study presents the first evidence of S. filipendula glycolipids overcoming acquired chemoresistance, offering a novel therapeutic strategy.
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