New functionalized mercaptoundecahydrododecaborate derivatives for potential application in boron neutron capture therapy: Synthesis, characterization and dynamic visualization in cells

Genady, Afaf R.; Ioppolo, Joseph A.; Azaam, Mohamed M.; El‐Zaria, Mohamed E.

doi:10.1016/j.ejmech.2015.02.033

Cited by 21 publications

(18 citation statements)

References 44 publications

(77 reference statements)

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“…This behavior is required for a drug to reach to its target. Various studies were carried out to show the solubility of such compounds in a hydrophobic environment [50,51], thus Genady et al [52] have recently demonstrated that a fluorescent dye can penetrate and accumulate in the cellular membrane of mammalian cells.…”

Section: Boron Cluster Implication For Drug Designmentioning

confidence: 99%

Boron Chemistry for Medical Applications

2020

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Boron compounds now have many applications in a number of fields, including Medicinal Chemistry. Although the uses of boron compounds in pharmacological science have been recognized several decades ago, surprisingly few are found in pharmaceutical drugs. The boron-containing compounds epitomize a new class for medicinal chemists to use in their drug designs. Carboranes are a class of organometallic compounds containing carbon (C), boron (B), and hydrogen (H) and are the most widely studied boron compounds in medicinal chemistry. Additionally, other boron-based compounds are of great interest, such as dodecaborate anions, metallacarboranes and metallaboranes. The boron neutron capture therapy (BNCT) has been utilized for cancer treatment from last decade, where chemotherapy and radiation have their own shortcomings. However, the improvement in the already existing (BPA and/or BSH) localized delivery agents or new tumor-targeted compounds are required before realizing the full clinical potential of BNCT. The work outlined in this short review addresses the advancements in boron containing compounds. Here, we have focused on the possible clinical implications of the new and improved boron-based biologically active compounds for BNCT that are reported to have in vivo and/or in vitro efficacy.

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Section: Boron Cluster Implication For Drug Designmentioning

confidence: 99%

Boron Chemistry for Medical Applications

2020

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“…As a result, higher boron concentration resulted in higher prompt gamma ray image reproducibility. Because a new boronate compound is being developed to increase the boron uptake ratio in the target volume, the reliability and usefulness of prompt gamma ray images can be gradually increased [ 12 , 13 ]. Thus, the clinically applicable boron concentration range can also be increased.…”

Section: Resultsmentioning

confidence: 99%

Quantitative analysis of prompt gamma ray imaging during proton boron fusion therapy according to boron concentration

Shin

Kim

et al. 2017

Oncotarget

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The purpose of this study is to evaluate the prompt gamma ray imaging technique according to the clinical boron concentration range during proton boron fusion therapy (PBFT). To acquire a prompt gamma ray image from 32 projections, we simulated four head single photon emission computed tomography and a proton beam nozzle using a Monte Carlo simulation. We used modified ordered subset expectation maximization reconstruction algorithm with a graphic processing unit for fast image acquisition. Boron concentration was set as 20 to 100 μg at intervals of 20 μg. For quantitative analysis of the prompt gamma ray image, we acquired an image profile drawn through two boron uptake regions (BURs) and calculated the contrast value, signal-to-noise ratio (SNR), and difference between the physical target volume and volume of the prompt gamma ray image. The relative counts of prompt gamma rays were noticeably increased with increasing boron concentration. Although the intensities on the image profiles showed a similar tendency according to the boron concentration, the SNR and contrast value were improved with increasing boron concentration. This study suggests that a tumor monitoring technique using prompt gamma ray detection can be clinically applicable even if the boron concentration is relatively low.

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“…Iquchi Y et al created a BSH fused with a short arginine peptide-labeled positron emission tomography (PET) probe, and the imaging results showed a high uptake in the tumor area [15]. Genady AR and his colleagues compounded a series of mono- and dicarboxyalkyl BSH derivatives, and found that BSH-conjugated triazole 15 induced a significant increase in the level of boron accumulation in HeLa cells [16]. …”

Section: Discussionmentioning

confidence: 99%

Targeting glioma stem cells enhances anti-tumor effect of boron neutron capture therapy

Sun

Huang

et al. 2016

Oncotarget

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The uptake of (10)boron by tumor cells plays an important role for cell damage in boron neutron capture therapy (BNCT). CD133 is frequently expressed in the membrane of glioma stem cells (GSCs), resistant to radiotherapy and chemotherapy, and represents a potential therapeutic target. To increase (10)boron uptake in GSCs, we created a polyamido amine dendrimer, conjugated CD133 monoclonal antibodies, encapsulating mercaptoundecahydrododecaborate (BSH) in void spaces, and monitored the uptake of the bioconjugate nanoparticles by GSCs in vitro and in vivo. Fluorescence microscopy showed the specific uptake of the bioconjugate nanoparticles by CD133-positive GSCs. Treatment with the biconjugate nanoparticles resulted in a significant lethal effect after neutron radiation due to efficient and CD133-independent cellular targeting and uptake in CD133-expressing GSCs. A significantly longer survival occurred in combination with the biconjugate nanoparticles and BSH compared with BSH alone in human intracranial GBM models employing CD133-positive GSCs xenografts. Our data demonstrated that this bioconjugate nanoparticle targets human CD133-positive GSCs and is a potential boron agent in BNCT.

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New functionalized mercaptoundecahydrododecaborate derivatives for potential application in boron neutron capture therapy: Synthesis, characterization and dynamic visualization in cells

Cited by 21 publications

References 44 publications

Boron Chemistry for Medical Applications

Boron Chemistry for Medical Applications

Quantitative analysis of prompt gamma ray imaging during proton boron fusion therapy according to boron concentration

Targeting glioma stem cells enhances anti-tumor effect of boron neutron capture therapy

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