scholarly journals Synthesis, Molecular Docking, and In Vitro Boron Neutron Capture Therapy Assay of Carboranyl Sinomenine

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4697
Author(s):  
Jianghong Cai ◽  
Narayan S. Hosmane ◽  
Masao Takagaki ◽  
Yinghuai Zhu
Keyword(s):  
Rheumatoid Arthritis ◽  
Molecular Docking ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Dimethyl Formamide ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture ◽  
Elemental Analyses ◽  
Slow Neutrons

In comparison with pristine sinomenine and carborane precursors, the calculations of molecular docking with matrix metalloproteinases (MMPs) and methylcarboranyl-n-butyl sinomenine showed improved interactions. Accordingly, methylcarboranyl-n-butyl sinomenine shows a high potential in the treatment of rheumatoid arthritis (RA) in the presence of slow neutrons. The reaction of potassium salt of sinomenie, which is generated from the deprotonation of sinomenine (1) using potassium carbonate in a solvent of N,N-dimethyl formamide, with 4-methylcarboranyl-n-butyl iodide, (2) forms methylcarboranyl-n-butyl sinomenine (3) in 54.3% yield as a new product. This new compound was characterized by 1H, 13C, and 11B NMR spectroscopy, FT-IR spectroscopy, and elemental analyses to confirm its molecular composition. In addition to molecular docking interactions with MMPs, the in vitro killing effects of 3, along with its toxicity measurements, exhibited its potential to be the new drug delivery agent for boron neutron capture synovectomy (BNCS) and boron neutron capture therapy (BNCT) for the treatment of rheumatoid arthritis (RA) and cancers in the presence of slow neutrons, respectively.

Towards improved boron neutron capture therapy agents: evaluation of in vitro cellular uptake of a glutamine-functionalized carborane

2009 ◽  
Vol 14 (6) ◽  
pp. 883-890 ◽  
Author(s):  
Antonella Crivello ◽  
Carlo Nervi ◽  
Roberto Gobetto ◽  
Simonetta Geninatti Crich ◽  
Iboya Szabo ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture

scholarly journals Quality Management System Program of in Vitro/in Vivo Test Facility of Boron Neutron Capture Therapy at Kartini Research Reactor

2016 ◽  
Vol 1 (2) ◽  
pp. 108
Author(s):  
Widarto Widarto ◽  
Isman Mulyadi Tri Atmoko ◽  
Gede Sutresna Wijaya
Keyword(s):  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Research Reactor ◽  
Test Facility ◽  
Neutron Capture Therapy ◽  
In Vivo Test ◽  
Boron Neutron Capture ◽  
System Program

The quality manajement system program of in vitro / in vivo test facility of  Boron Neutron Capture Therapy (BNCT) methode as quality assurance requirement for utilization of radial pearcing beamport of Kartini research have been done.  Identification and management of technical specification and parameters meassurement of to the radial piercing beamport have been determined for preparing in vitro / in vivo test facility. The parameters are epithermal neutron flux is  9,8243E+05  n cm<sup>-2</sup> s<sup>-1</sup>and  thermal neutron flux is 3,0691E+06 n cm<sup>-2</sup> s<sup>-1</sup>, radiation shielding of parafin,  dimension and size  of piercing radial and instrumentatin and control system for automatic transfer of in vitro / in vivo samplels have been documented. Management system of the documents for fullfil  basic guidance to perform working job of in vitro / in vivo at the piercing radial beamport of Kartini Research Reactor in order purpose utilization of the reactor  for safety worker of the radiation area, society  and invironment beeing safely

scholarly journals Cyclic-RGDyC functionalized liposomes for dual-targeting of tumor vasculature and cancer cells in glioblastoma: An in vitro boron neutron capture therapy study

Oncotarget ◽  
2017 ◽  
Vol 8 (22) ◽  
pp. 36614-36627 ◽  
Author(s):  
Weirong Kang ◽  
Darren Svirskis ◽  
Vijayalekshmi Sarojini ◽  
Ailsa L. McGregor ◽  
Joseph Bevitt ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Tumor Vasculature ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture ◽  
Dual Targeting

Functionalized mesoporous silica nanoparticles for innovative boron-neutron capture therapy of resistant cancers

2018 ◽  
Author(s):  
Guillaume Vares ◽  
Vincent Jallet ◽  
Yoshitaka Matsumoto ◽  
Cedric Rentier ◽  
Kentaro Takayama ◽  
...  
Keyword(s):  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Mesoporous Silica Nanoparticles ◽  
Alpha Particles ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture

AbstractTreatment resistance, relapse and metastasis remain critical issues in some challenging cancers, such as chondrosarcomas. Boron-neutron Capture Therapy (BNCT) is a targeted radiation therapy modality that relies on the ability of boron atoms to capture low energy neutrons, yielding high linear energy transfer alpha particles. We have developed an innovative boron-delivery system for BNCT, composed of multifunctional fluorescent mesoporous silica nanoparticles (B-MSNs), grafted with an activatable cell penetrating peptide (ACPP) for improved penetration in tumors and with Gadolinium for magnetic resonance imaging (MRI)in vivo. Chondrosarcoma cells were exposedin vitroto an epithermal neutron beam after B-MSNs administration. BNCT beam exposure successfully induced DNA damage and cell death, including in radio-resistant ALDH+ cancer stem cells (CSCs), suggesting that BNCT using this system might be a suitable treatment modality for chondrosarcoma or other hard-to-treat cancers.

scholarly journals Boron neutron capture therapy in cancer: past, present and future

2007 ◽  
Vol 51 (5) ◽  
pp. 852-856 ◽  
Author(s):  
Mario A. Pisarev ◽  
Maria Alejandra Dagrosa ◽  
Guilermo J. Juvenal
Keyword(s):  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Alpha Particles ◽  
Neutron Capture Therapy ◽  
Selective Uptake ◽  
Complete Control ◽  
Boron Neutron Capture ◽  
A Cell ◽  
Undifferentiated Thyroid Cancer

Undifferentiated thyroid cancer (UTC) is a very aggressive tumor with no effective treatment, since it lacks iodine uptake and does not respond to radio or chemotherapy. The prognosis of these patients is bad, due to the rapid growth of the tumor and the early development of metastasis. Boron neutron capture therapy (BNCT) is based on the selective uptake of certain boron non-radioactive compounds by a tumor, and the subsequent irradiation of the area with an appropriate neutron beam. 10B is then activated to 11B, which will immediately decay releasing alpha particles and 7Li, of high linear energy transfer (LET) and limited reach. Clinical trials are being performed in patients with glioblastoma multiforme and melanoma. We have explored its possible application to UTC. Our results demonstrated that a cell line of human UTC has a selective uptake of borophenylalanine (BPA) both in vitro and after transplantation to nude mice. Treatment of mice by BNCT led to a complete control of growth and cure of 100% of the animals. Moreover dogs with spontaneous UTC also have a selective uptake of BPA. At the present we are studying the biodistribution of BPA in patients with UTC before its application in humans.

Carboranyl-porphyrazines and derivatives for boron neutron capture therapy: From synthesis to in vitro tests

2013 ◽  
Vol 257 (15-16) ◽  
pp. 2213-2231 ◽  
Author(s):  
Daniela Pietrangeli ◽  
Angela Rosa ◽  
Sandra Ristori ◽  
Anna Salvati ◽  
Saverio Altieri ◽  
...  
Keyword(s):  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
In Vitro Tests ◽  
Neutron Capture Therapy ◽  
Boron Neutron Capture

scholarly journals Aza-BODIPY: A New Vector for Enhanced Theranostic Boron Neutron Capture Therapy Applications

Cells ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1953
Author(s):  
Ghadir Kalot ◽  
Amélie Godard ◽  
Benoît Busser ◽  
Jacques Pliquett ◽  
Mans Broekgaarden ◽  
...  
Keyword(s):  
Boron Neutron Capture Therapy ◽  
Neutron Capture ◽  
Ex Vivo ◽  
Chorioallantoic Membrane ◽  
Water Soluble ◽  
Neutron Capture Therapy ◽  
Breakdown Spectroscopy ◽  
Boron Neutron Capture ◽  
Tumor Area ◽  
Slow Neutrons

Boron neutron capture therapy (BNCT) is a radiotherapeutic modality based on the nuclear capture of slow neutrons by stable 10B atoms followed by charged particle emission that inducing extensive damage on a very localized level (<10 μm). To be efficient, a sufficient amount of 10B should accumulate in the tumor area while being almost cleared from the normal surroundings. A water-soluble aza-boron-dipyrromethene dyes (BODIPY) fluorophore was reported to strongly accumulate in the tumor area with high and BNCT compatible Tumor/Healthy Tissue ratios. The clinically used 10B-BSH (sodium borocaptate) was coupled to the water-soluble aza-BODIPY platform for enhanced 10B-BSH tumor vectorization. We demonstrated a strong uptake of the compound in tumor cells and determined its biodistribution in mice-bearing tumors. A model of chorioallantoic membrane-bearing glioblastoma xenograft was developed to evidence the BNCT potential of such compound, by subjecting it to slow neutrons. We demonstrated the tumor accumulation of the compound in real-time using optical imaging and ex vivo using elemental imaging based on laser-induced breakdown spectroscopy. The tumor growth was significantly reduced as compared to BNCT with 10B-BSH. Altogether, the fluorescent aza-BODIPY/10B-BSH compound is able to vectorize and image the 10B-BSH in the tumor area, increasing its theranostic potential for efficient approach of BNCT.

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