利用磁性纳米颗粒实现生物活性真菌代谢产物Gliotoxin的细胞内递送

Comas Laura, Polo Esther, Domingo M Pilar, Hernández Yulán, Arias Maykel, Esteban Patricia, Martínez-Lostao Luis, Pardo Julián, Martínez de la Fuente Jesús, Gálvez Eva M

Instituto de Carboquímica (ICB-CSIC), 50018 Zaragoza, Spain.

Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CiQUS), Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

Materials (Basel). 2019 Apr 2;12(7):1092. doi: 10.3390/ma12071092.

Gliotoxin (GT), a secondary metabolite produced by Aspergillus molds, has been proposed as a potential anti-tumor agent. Here we have developed a nanoparticle approach to enhance delivery of GT in tumor cells and establish a basis for its potential use as therapeutical drug. GT bound to magnetic nanoparticles (MNPs) retained a high anti-tumor activity, correlating with efficient intracellular delivery, which was increased in the presence of glucose. Our results show that the attachment of GT to MNPs by covalent bonding enhances intracellular GT delivery without affecting its biological activity. This finding represents the first step to use this potent anti-tumor agent in the treatment of cancer.

Gliotoxin (GT)，一种由曲霉菌产生的次生代谢产物，已被提议作为一种潜在的抗肿瘤药物。在此，我们开发了一种纳米颗粒方法，以增强GT在肿瘤细胞中的递送，并为其作为治疗药物的潜在用途奠定基础。与磁性纳米颗粒（MNPs）结合的GT保留了高抗肿瘤活性，这与有效的细胞内递送相关，在葡萄糖存在的情况下递送效率会提高。我们的结果表明，通过共价键将GT附着到MNPs上可增强细胞内GT递送，而不影响其生物活性。这一发现代表了在癌症治疗中使用这种强效抗肿瘤药物的第一步。