Loading...
Please wait, while we are loading the content...
Similar Documents
Homocystamide Conjugates of Human Serum Albumin as a Platform to Prepare Bimodal Multidrug Delivery Systems for Boron Neutron Capture Therapy
| Content Provider | MDPI |
|---|---|
| Author | Popova, Tatyana Dymova, Maya A. Koroleva, Ludmila S. Zakharova, Olga D. Lisitskiy, Vladimir A. Raskolupova, Valeria I. Sycheva, Tatiana Taskaev, Sergei Silnikov, Vladimir N. Godovikova, Tatyana S. |
| Copyright Year | 2021 |
| Description | Boron neutron capture therapy is a unique form of adjuvant cancer therapy for various malignancies including malignant gliomas. The conjugation of boron compounds and human serum albumin (HSA)—a carrier protein with a long plasma half-life—is expected to extend systemic circulation of the boron compounds and increase their accumulation in human glioma cells. We report on the synthesis of fluorophore-labeled homocystamide conjugates of human serum albumin and their use in thiol-‘click’ chemistry to prepare novel multimodal boronated albumin-based theranostic agents, which could be accumulated in tumor cells. The novelty of this work involves the development of the synthesis methodology of albumin conjugates for the imaging-guided boron neutron capture therapy combination. Herein, we suggest using thenoyltrifluoroacetone as a part of an anticancer theranostic construct: approximately 5.4 molecules of thenoyltrifluoroacetone were bound to each albumin. Along with its beneficial properties as a chemotherapeutic agent, thenoyltrifluoroacetone is a promising magnetic resonance imaging agent. The conjugation of bimodal HSA with undecahydro-closo-dodecaborate only slightly reduced human glioma cell line viability in the absence of irradiation (~30 μM of boronated albumin) but allowed for neutron capture and decreased tumor cell survival under epithermal neutron flux. The simultaneous presence of undecahydro-closo-dodecaborate and labeled amino acid residues (fluorophore dye and fluorine atoms) in the obtained HSA conjugate makes it a promising candidate for the combination imaging-guided boron neutron capture therapy. |
| Starting Page | 6537 |
| e-ISSN | 14203049 |
| DOI | 10.3390/molecules26216537 |
| Journal | Molecules |
| Issue Number | 21 |
| Volume Number | 26 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-10-29 |
| Access Restriction | Open |
| Subject Keyword | Molecules Oncology Boron Neutron Capture Therapy Boron Delivery Agents Thenoyltrifluoroacetone Boronated Albumin Theranostic Conjugate in Vitro Efficacy Evaluation Irradiated By Epithermal Neutron Flux Colony Forming Assay |
| Content Type | Text |
| Resource Type | Article |
