Abstract
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.
Highlights
Gliotoxin (GT) is a well-known secondary metabolite produced by molds of the Aspergillus, Penicillium, Gliocladium, and Trichoderma families
magnetic nanoparticles (MNPs) were synthesized in organic media by thermal decomposition and efficiently transferred temperature, 8 μM of EDC and 0.03 μM of 5(6)-TAMRA to aqueous phase by using an amphiphilic polymer (PMAO)
MNPs were synthesized in organic media by thermal decomposition and efficiently transferred to aqueous phase by using an amphiphilic polymer (PMAO)
Summary
Gliotoxin (GT) is a well-known secondary metabolite produced by molds of the Aspergillus, Penicillium, Gliocladium, and Trichoderma families. It belongs to the group of epipolithiodioxopiperazines (ETP) [1] that are mycotoxins characterized by the presence of a disulfide bridge in their structure, responsible for their biological activity [2]. Among the different members of this family, GT has been the best characterized and most extensively studied, since its discovery in 1932 [3,4,5,6]. It was initially described as an anti-microbial toxin produced by Penicillium spp. GT synthesis is carried out by Materials 2019, 12, 1092; doi:10.3390/ma12071092 www.mdpi.com/journal/materials
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