scholarly journals Synthesis and Characterisation of a Boron-Rich Symmetric Triazine Bearing a Hypoxia-Targeting Nitroimidazole Moiety

Symmetry ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 202
Author(s):  
Tobias Hartwig Bünning ◽  
Luigi Panza ◽  
Abdel Kareem Azab ◽  
Barbara Muz ◽  
Silvia Fallarini ◽  
...  
Keyword(s):  
Tumor Tissue ◽  
High Ratio ◽  
Neutron Capture Therapy ◽  
Boron Compounds ◽  
The Core ◽  
Boron Neutron Capture ◽  
Starting Point ◽  
Primary Fibroblasts ◽  
Normal Human ◽  
Hypoxia Markers

Boron Neutron Capture Therapy (BNCT) is a binary therapy that promises to be suitable in treating many non-curable cancers. To that, the discovery of new boron compounds able to accumulate selectively in the tumour tissue is still required. Hypoxia, a deficiency of oxygen in tumor tissue, is a great challenge in the conventional treatment of cancer, because hypoxic areas are resistant to conventional anticancer treatments. 2-Nitroimidazole derivatives are known to be hypoxia markers due to their enrichment by bioreduction in hypoxic cells. In the present work, 2-nitroimidazole was chosen as the starting point for the synthesis of a new boron-containing compound based on a 1,3,5-triazine skeleton. Two o-carborane moieties were inserted to achieve a high ratio of boron on the molecular weight, exploiting a short PEG spacer to enhance the polarity of the compound and outdistance the active part from the core. The compound showed no toxicity on normal human primary fibroblasts, while it showed noteworthy toxicity in multiple myeloma cells together with a consistent intracellular boron accumulation.

scholarly journals Gold Nanoparticles as Boron Carriers for Boron Neutron Capture Therapy: Synthesis, Radiolabelling and In vivo Evaluation

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3609 ◽  
Author(s):  
Pulagam ◽  
Gona ◽  
Gómez-Vallejo ◽  
Meijer ◽  
Zilberfain ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Mouse Model ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
The Core ◽  
Boron Neutron Capture ◽  
Biodistribution Studies ◽  
Imaging Results

Background: Boron Neutron Capture Therapy (BNCT) is a binary approach to cancer therapy that requires accumulation of boron atoms preferentially in tumour cells. This can be achieved by using nanoparticles as boron carriers and taking advantage of the enhanced permeability and retention (EPR) effect. Here, we present the preparation and characterization of size and shape-tuned gold NPs (AuNPs) stabilised with polyethylene glycol (PEG) and functionalized with the boron-rich anion cobalt bis(dicarbollide), commonly known as COSAN. The resulting NPs were radiolabelled with 124I both at the core and the shell, and were evaluated in vivo in a mouse model of human fibrosarcoma (HT1080 cells) using positron emission tomography (PET). Methods: The thiolated COSAN derivatives for subsequent attachment to the gold surface were synthesized by reaction of COSAN with tetrahydropyran (THP) followed by ring opening using potassium thioacetate (KSAc). Iodination on one of the boron atoms of the cluster was also carried out to enable subsequent radiolabelling of the boron cage. AuNPs grafted with mPEG-SH (5 Kda) and thiolated COSAN were prepared by ligand displacement. Radiolabelling was carried out both at the shell (isotopic exchange) and at the core (anionic absorption) of the NPs using 124I to enable PET imaging. Results: Stable gold nanoparticles simultaneously functionalised with PEG and COSAN (PEG-AuNPs@[4]−) with hydrodynamic diameter of 37.8 ± 0.5 nm, core diameter of 19.2 ± 1.4 nm and ξ-potential of −18.0 ± 0.7 mV were obtained. The presence of the COSAN on the surface of the NPs was confirmed by Raman Spectroscopy and UV-Vis spectrophotometry. PEG-AuNPs@[4]− could be efficiently labelled with 124I both at the core and the shell. Biodistribution studies in a xenograft mouse model of human fibrosarcoma showed major accumulation in liver, lungs and spleen, and poor accumulation in the tumour. The dual labelling approach confirmed the in vivo stability of the PEG-AuNPs@[4]−. Conclusions: PEG stabilized, COSAN-functionalised AuNPs could be synthesized, radiolabelled and evaluated in vivo using PET. The low tumour accumulation in the animal model assayed points to the need of tuning the size and geometry of the gold core for future studies.

Bahan Sasaran Sebagai Sumber Neutron yang Optimal untuk Boron Neutron Capture Therapy (BNCT)

2017 ◽  
Vol 1 ◽  
pp. 104
Author(s):  
Yan Surono ◽  
C Cari ◽  
Yohannes Sarjono
Keyword(s):  
Cancer Cells ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
Radioactive Elements ◽  
Therapeutic Technique ◽  
The Core ◽  
Boron Neutron Capture ◽  
Deadly Disease ◽  
Α Particles

<p><strong>Abstract</strong> Cancer is a deadly disease that exist on planet earth. Efforts were made to be able to kill cancer cells either by manual operation or by radiotherapy. One way to use energy radiation radioactive elements as killers of cancer cells is Boron Neutron Capture Therapy (BNCT). BNCT is a therapeutic technique that utilizes the interaction of neutron capture by the core 10B will produce α-particles and nuclei 7Li results by reaction 10B (n, α) 7Li. It therefore requires a material that will produce neutrons used in BNCT. Materials  target that will be searched in order to obtain optimal materials according to the requirements provided by the International Atomic Agency (IAEA).<em></em></p><p><em> </em></p><p><strong>Keywords </strong>: Kanker, Material, Neutron, BNCT</p><p align="center"><strong><em> </em></strong></p><p><strong>Abstrak</strong> Kanker adalah salah satu penyakit yang mematikan yang ada di planet bumi. Upaya upaya dilakukan untuk dapat membunuh sel kanker baik itu  secara operasi manual maupun dengan cara radioterapi. Salah satu cara yang memanfaatkan energi radiasi unsur unsur radioaktif sebagai pembunuh sel kanker adalah Boron Neutron Capture Therapy (BNCT). BNCT merupakan teknik terapi yang memanfaatkan interaksi tangkapan neutron oleh inti 10B yang akan menghasilkan partikel-α dan inti hasil 7Li melalui reaksi 10B(n,α) 7Li. Oleh sebab itu diperlukan material yang akan menghasilkan neutron digunakan dalam BNCT. Bahan - bahan sasaran yang akan ditelusur dalam upaya mendapatkan bahan yang optimal sesuai persyaratan yang diberikan oleh International Atomic Agency (IAEA).</p><p><em> </em></p><p><strong>Kata Kunci </strong>: Kanker, Material, Neutron, BNCT</p>

Intracellular target delivery of cell-penetrating peptide-conjugated dodecaborate for boron neutron capture therapy (BNCT)

2019 ◽  
Vol 55 (93) ◽  
pp. 13955-13958 ◽  
Author(s):  
Ikuhiko Nakase ◽  
Miku Katayama ◽  
Yoshihide Hattori ◽  
Miki Ishimura ◽  
Shunsuke Inaura ◽  
...  
Keyword(s):  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Cell Penetrating Peptides ◽  
Cell Penetrating Peptide ◽  
Neutron Capture Therapy ◽  
Boron Compounds ◽  
Target Delivery ◽  
Boron Neutron Capture ◽  
Cell Penetrating ◽  
Intracellular Target

Boron neutron capture therapy (BNCT) technology using cell-penetrating peptides (CPPs) for enhanced cellular uptake of boron compounds and their controlled localization inside cells.

Tolerance of normal human brain to boron neutron capture therapy

2004 ◽  
Vol 61 (5) ◽  
pp. 1083-1087 ◽  
Author(s):  
J.A Coderre ◽  
J.W Hopewell ◽  
J.C Turcotte ◽  
K.J Riley ◽  
P.J Binns ◽  
...  
Keyword(s):  
Human Brain ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
Normal Human Brain ◽  
Boron Neutron Capture ◽  
Normal Human
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