Search Results (132)

Boron neutron capture therapy (BNCT) is a binary targeted radiotherapy that uses boron agents to treat refractory malignancies. This study developed a novel boronophenylalanine (BPA)-loaded liposome doped with o-carborane (CB) for BNCT. We applied response surface methodology (RSM) to identify factors affecting BPA loading and optimized encapsulation efficiency (EE) to minimize BPA loss. In in vitro experiments, these liposomes demonstrated promising characteristics for BNCT. The nanoparticle properties of CB-BPA-Lips remain stable for at least 48 h, and CB-BPA-Lips can effectively reduce the release of the agents loaded within them. Both cell viability assays and apoptosis assays have shown that CB-BPA-Lips have good biocompatibility and a lower inhibitory effect on cell viability than BPA. Cellular boron uptake peaked at 47.3642 ng B/10⁶ cells in A549 lung cancer cells and peaked at 38.8875 ng B/10⁶ cells in Bronchial Epithelium transformed with Ad12-SV40 2B (BEAS-2B) human normal bronchial epithelial cells at 24 h post-treatment, with both exceeding uptake in the BPA control group. Overall, this work presents an optimized liposomal formulation that enhances boron delivery to cancer cells and provides a potential candidate boron agent for BNCT pending in-depth in vivo studies. Full article

Metal-functionalized boron nitride nanostructures represent promising platforms for lightweight solid-state hydrogen storage. In this work, we perform a comprehensive density functional theory (DFT) investigation of pristine and metal-decorated B₄N₄ quantum dots (M = Li, Ti) to evaluate their structural stability, adsorption energetics, and near-ambient storage performance. Pristine B₄N₄ is highly stable but interacts weakly with H₂ (E_ads ≈ −0.12 eV), leading to negligible uptake under operating conditions. Li decoration moderately enhances adsorption through charge-induced polarization (E_ads ≈ −0.15 eV) but offers limited stabilization beyond the first few molecules. In contrast, Ti decoration fundamentally reshapes the interaction landscape, strengthening electrostatic, polarization, and dispersion contributions and enabling significantly stronger yet reversible H₂ binding (E_ads ≈ −0.36 eV). Sequential adsorption calculations predict maximum theoretical capacities of 14, 18, and 20 H₂ molecules for pristine, Li-, and Ti-decorated systems, respectively. Grand canonical thermodynamics show that Ti–B₄N₄ retains nearly its full loading at 30 bar and 298 K, while pristine and Li-decorated clusters store only negligible amounts. Under desorption conditions (3 bar, 373 K), Ti–B₄N₄ releases most of its stored hydrogen, yielding an exceptional reversible capacity of 15.1 wt%. Energy decomposition analysis attributes this performance to cooperative electrostatic, polarization, and dispersion enhancements. Ti–B₄N₄ emerges as a highly promising theoretical candidate, warranting future experimental validation. Full article

Radiotherapy is one of the conventional methods for the treatment of cancers. Boron neutron capture therapy (BNCT) has emerged as a promising and well-recognized modality for treating certain types of cancers. BNCT is a binary radiotherapy that largely depends on neutron beams and ¹⁰B carriers. Although an “ideal” boron carrier should fulfill multiple criteria, high tumor/normal tissue ratio (T/N > 5) and high tumor uptake of boron (>20 μg/g) are critically important. First-generation (boric acid and derivatives) and second-generation (BPA and BSH) boron carriers suffer from poor T/N and extremely high dose in clinical use (500 mg/kg and usually >30 g for each patient). Glucose transporter 1 (GLUT1) is overexpressed on the membrane surface of multiple tumors and is a potential target for third-generation boron carrier to achieve high T/N and high tumor uptake of boron. However, the boron-bearing sugar derivatives designed in the last few decades have suffered from suboptimal T/N values and significant cytotoxicity. In the present study, a total of two categories comprising 6 series (28 in total) of boron-bearing sugar derivatives were designed and synthesized and their cellular boron uptake, T/N, and cytotoxicity were evaluated. The structure–activity relationship (SAR) of these target compounds was analyzed, and one of the target compounds, B3, a phenyl C-mannoside with an o-carborane moiety, exhibited the best boron-carrying profile, which featured 10.6-fold higher boron uptake by the SCC-9 cell line and a largely improved T/N (3.3 for B3 vs. 1.4 for BPA) compared with the current clinical gold standard BPA. Therefore, the chemical structure of B3 represents a privileged candidate structure for the future design of “ideal” boron carriers for BNCT. Full article

Homeobox protein MEIS2 has been strongly implicated in colorectal cancer (CRC) progression and metastatic potential, making its targeted inhibition a promising therapeutic strategy. However, recently developed MEIS inhibitors are limited by poor aqueous solubility, instability under physiological conditions, and insufficient intracellular accumulation, which restrict their clinical applicability. To overcome these challenges, a multifunctional hybrid nanoemulsome system was developed by integrating boron–silane-doped carbon dots (CDs) with chitosan via glutaraldehyde crosslinking, followed by emulsification with oleic acid and non-ionic surfactants (Span 80 and Tween 20/80) in the presence of a MEIS inhibitor (MEISi-2). The resulting composite exhibited high structural stability, excellent biocompatibility, and a drug encapsulation efficiency of 96.2%. Fourier-transform infrared spectroscopy (FTIR) and dynamic light scattering (DLS) analyses confirmed successful hybridization and the formation of nanoemulsions with an average particle size of approximately 320 nm following drug loading. The system demonstrated controlled drug release under physiological conditions. In vitro studies using HCT116 CRC and HaCaT healthy keratinocytes revealed effective cellular uptake and selective cytotoxicity. The intrinsic fluorescence properties of CDs enabled real-time monitoring of intracellular drug delivery via DAPI-channel imaging. Overall, this hybrid nanoemulsome platform provides a stable and efficient delivery system for MEIS inhibitors and represents a promising strategy for the treatment of CRC. Furthermore, this approach may be extended to other poorly soluble amphiphilic therapeutic agents. Full article

Boron coatings were deposited by RF magnetron sputtering in an Ar atmosphere at a constant power of 80 W, varying the working pressure in the 0.6–5 Pa range. Plasma diagnostics were performed by means of a Langmuir probe to determine the electron temperature and electron density under different operating conditions. Within the investigated pressure range, the deposition rate remained nearly constant, whereas a significant decrease in coating mass density was observed with increasing pressure. The coatings display a columnar structure at all investigated pressures, with no significant differences in bulk morphology. Pressure primarily affects the surface features, leading to an increase in the density, lateral dimensions, and height of surface agglomerates with increasing pressure. Compositional analysis by EDX revealed a substantial oxygen incorporation in the films, with the lowest oxygen content (~11 at.%) measured for the coating deposited at 0.6 Pa. XPS depth profiling confirmed the presence of oxygen and evidenced the formation of boron oxide species, while the boron concentration exceeded 80 at.% in all samples. These results highlight the strong sensitivity of boron film density and oxygen uptake to sputtering pressure. Full article

Poly(amidoamine) (PAMAM) and poly-L-lysine (PLL) dendrimers have emerged as highly versatile macromolecular platforms with significant potential in biomedical applications, owing to their well-defined architecture, tunable surface chemistry, and capacity for multivalent functionalization. Their ability to carry substantial molecular payloads and to be engineered for selective interactions with biological systems has positioned them as attractive candidates for targeted drug delivery, including the transport of boron-rich compounds. Recent advances in dendrimer chemistry have enabled the incorporation of boron clusters into PAMAM and PLL structures, creating hybrid systems designed to enhance cellular uptake, improve tumor selectivity, and increase boron accumulation within malignant tissues. Given the growing interest in boron neutron capture therapy (BNCT), the integration of boron clusters into dendrimer structures represents a particularly promising direction for enhancing boron delivery to tumors. This manuscript reviews current knowledge on PAMAM and PLL dendrimers and their boron-functionalized derivatives, summarizing findings from cell culture studies, in vivo models, and clinical or preclinical investigations. Particular attention is given to both the advantageous properties of these dendrimers—such as improved delivery efficiency and biocompatibility—and their potential undesirable biological effects. As such, PAMAM and PLL dendrimers represent an important and evolving class of carriers that may significantly advance the effectiveness of boron neutron capture therapy (BNCT) in cancer treatment. Full article

BNCT (Boron Neutron Capture Therapy) is a binary radiotherapeutic modality in which high LET (Linear Energy Transfer) particles are generated from ¹⁰B(n,α)⁷Li reaction, ideally within boron-loaded tumour cells, so the therapeutic outcome depends critically on the pharmacokinetics and biodistribution of boron carriers. In this review, boron-containing agents for BNCT, with a focus on ADMET (absorption, distribution, metabolism, excretion and toxicity) and model-informed design, were examined. Low-MW (low-molecular-weight) compounds, peptide conjugates, polymeric and nanostructured platforms and cell-based vectors were surveyed and how physicochemical properties, transporter engagement and nano–bio interactions govern tumour uptake, subcellular localisation and normal tissue exposure were discussed. A shift from maximising boron content towards optimising exposure profiles using PET (Positron Emission Tomography), PBK (physiologically based pharmacokinetic) modelling and in silico ADMET tools to define irradiation windows was also discussed. Classical agents such as BPA (Boronophenylalanine) and BSH (Sodium Borocaptate) are contrasted with newer polymeric and metallacarborane-based carriers, with attention to brain penetration, endosomal escape, linker stability, biodegradation and elimination routes, as well as platform-specific toxicities. Incontestably, further progress in BNCT will highly depend on integrating imaging-derived kinetics with PBPK-informed dose planning and engineering subcellularly precise yet degradable carriers, and that ADMET-guided design and spatiotemporal coordination are central to achieving reproducible clinical benefit from BNCT’s spatial selectivity. Full article

Boron (B) is an essential but narrow-range micronutrient for citrus, with toxicity risks heightened in dry regions due to potentially high-B irrigation water and limited soil leaching. ‘Forner-Alcaide 5’ (FA5) is a promising rootstock for enhancing B-tolerance of sweet orange, but it had not been sufficiently tested before this study, specifically considering soil texture. Therefore, this greenhouse study investigated the effects on B absorption and biomass buildup of irrigating navel orange seedlings (cv. Navelina) grafted onto ‘Carrizo’ citrange (CC) and FA5 rootstocks, with 0.11, 2, or 5 mg B L⁻¹ waters and grown in clay loam or sandy loam soils. The results of this complete three-factor trial revealed that leaves are the primary sink for B (24–1300 mg kg⁻¹), indicating passive, transpiration-driven uptake and limited phloem redistribution. The presumed absence of sugar alcohols, and the weak binding affinity of B to the abundant sucrose, may account for the restricted phloem mobility of B in citrus, consistent with the mechanistic interpretation proposed in this study. FA5 rootstock showed greater B tolerance, sustaining 28% higher biomass than CC at 2 mg L⁻¹ B. Plant B uptake was found to be more related to soil soluble B than adsorbed B. Interestingly, the relationship followed a diminishing-returns pattern, thereby suggesting a balancing feedback mechanism, potentially based on B-induced stomatal closure. This analytical link between irrigation B and plant accumulation offers a framework for managing B toxicity, pending field validation. Full article

Boron neutron capture therapy (BNCT) is experiencing a global resurgence driven by advances in boron pharmacology, accelerator-based neutron sources, and molecular imaging-guided theranostics. BNCT produces high linear energy transfer particles with micrometer-range energy deposition, enabling cell-selective irradiation confined to boron-enriched tumor cells in a geometrically targeted region by the neutron beam. This mechanism offers the potential for exceptionally high therapeutic ratios, provided two core requirements are met: sufficient differential tumor uptake of ¹⁰B and a neutron beam with appropriate energy and penetration. After early clinical attempts in the mid-20th century were hindered by inadequate boron agents and reactor-based neutron beams, recent technological breakthroughs have made BNCT clinically viable. The development of hospital-compatible accelerator neutron sources, next-generation boron delivery systems (such as receptor-targeted compounds and nanoparticles), advanced theranostic approaches (such as ¹⁸F-BPA positron emission tomography and boron-sensitive magnetic resonance imaging), and AI-driven biodistribution modeling now support personalized treatment planning and patient selection. These innovations have catalyzed modern clinical implementation, exemplified by Japan’s regulatory approval of BNCT for recurrent head and neck cancer and the rapid expansion of clinical programs across Asia, Europe, and South America. Building on these foundations, BNCT has transitioned from a predominantly academic experimental modality into an increasingly commercialized and industrially supported therapeutic platform. The emergence of dedicated BNCT companies, international collaborations between accelerator manufacturers and hospitals, and pharmaceutical development pipelines for next-generation boron carriers has accelerated clinical translation. Moreover, BNCT now occupies a unique position among radiation modalities due to its hybrid nature, namely combining the biological targeting of radiopharmaceutical therapy with the external-beam controllability of radiotherapy, thereby offering new therapeutic opportunities where competitive approaches fall short. Emerging evidence suggests therapeutic promise in glioblastoma, recurrent head and neck cancers, melanoma, meningioma, lung cancer, sarcomas, and other difficult-to-treat malignancies. Looking ahead, continued innovation in compact neutron source engineering, boron nanocarriers, multimodal theranostics, microdosimetry-guided treatment planning, and combination strategies with systemic therapies such as immunotherapy will be essential for optimizing outcomes. Together, these converging developments position BNCT as a biologically targeted and potentially transformative modality in the era of precision oncology. Full article

Background: Boron neutron capture therapy (BNCT) represents a highly selective therapeutic modality for recalcitrant cancers, leveraging the nuclear reaction initiated by thermal neutron capture in boron-10 (¹⁰B) to deliver high-linear energy transfer radiation (α-particles and ⁷Li ions) directly within tumor cell boundaries. However, the widespread clinical adoption of BNCT is critically hampered by the pharmacological challenge of achieving sufficiently high, tumor-selective intracellular ¹⁰B concentrations (20–50 μg of ¹⁰B/g tissue). Conventional small-molecule boron carriers often exhibit dose-limiting non-specificity, rapid systemic clearance, and poor cellular uptake kinetics. Methods: To overcome these delivery barriers, we synthesized and characterized a novel dual-modality nanoplatform based on highly biocompatible, functionalized graphene oxide (GO). This platform was structurally optimized via covalent conjugation with high-boron content carborane clusters (dodecacarborane derivatives) for enhanced BNCT efficacy. Crucially, the nanocarrier was further decorated with plasmonic gold nanostructures (AuNPs), endowing the system with intrinsic surface-enhanced Raman scattering (SERS) properties, enabling real-time, high-resolution intracellular tracking and quantification. Results: We evaluated the synthesized GO@Carborane@Au nanoplatforms for their stability, cytotoxicity, and internalization characteristics. Cytotoxicity assays demonstrated excellent biocompatibility against the non-malignant human keratinocyte line (HaCaT) while showing selective toxicity (upon irradiation, if tested) and high cellular uptake efficiency in the aggressive human glioblastoma tumor cell line (T98G). The integrated plasmonic component allowed for the successful, non-destructive monitoring of nanoplatform delivery and accumulation within both HaCaT and T98G cells using SERS microscopy, confirming the potential for pharmacokinetic and biodistribution studies in vivo. Conclusions: This work details the successful synthesis and preliminary in vitro validation of a unique graphene oxide-based dual-modality nanoplatform designed to address the critical delivery and monitoring challenges of BNCT. By combining highly efficient carborane delivery with an integrated photonic trace marker, this system establishes a robust paradigm for next-generation theranostic agents, significantly advancing the potential for precision, image-guided BNCT for difficult-to-treat cancers like glioblastoma. Full article

Micronutrients, particularly boron (B), iron (Fe), manganese (Mn), and zinc (Zn), are pivotal for cotton (Gossypium spp.) growth, reproductive success, and fiber quality. However, their critical roles are often overlooked in fertility programs focused primarily on macronutrients. This review synthesizes recent advances in the physiological, molecular, and agronomic understanding of B, Fe, Mn, and Zn in cotton production. The overarching goal is to elucidate their impact on cotton nutrient use efficiency (NUE). Drawing from the peer-reviewed literature, we highlight how these micronutrients regulate essential processes, including photosynthesis, cell wall integrity, hormone signaling, and stress remediation. These processes directly influence root development, boll retention, and fiber quality. As a result, deficiencies in these micronutrients contribute to significant yield gaps even when macronutrients are sufficiently supplied. Key genes, including Boron Transporter 1 (BOR1), Iron-Regulated Transporter 1 (IRT1), Natural Resistance-Associated Macrophage Protein 1 (NRAMP1), Zinc-Regulated Transporter/Iron-Regulated Transporter-like Protein (ZIP), and Gossypium hirsutum Zinc/Iron-regulated transporter-like Protein 3 (GhZIP3), are crucial for mediating micronutrient uptake and homeostasis. These genes can be leveraged in breeding for high-yielding, nutrient-efficient cotton varieties. In addition to molecular hacks, advanced phenotyping technologies, such as unmanned aerial vehicles (UAVs) and single-cell RNA sequencing (scRNA-seq; a technology that measures gene expression at single-cell level, enabling the high-resolution analysis of cellular diversity and the identification of rare cell types), provide novel avenues for identifying nutrient-efficient genotypes and elucidating regulatory networks. Future research directions should include leveraging microRNAs, CRISPR-based gene editing, and precision nutrient management to enhance the use efficiency of B, Fe, Mn, and Zn. These approaches are essential for addressing environmental challenges and closing persistent yield gaps within sustainable cotton production systems. Full article

Carborane is considered a three-dimensional mimetic of phenyl rings in medicinal chemistry. BMS-202 is a potent PD-L1 inhibitor that can block the PD-L1/PD-1 interaction and restore the immune response to cancer cells. Herein, we replaced the terminal phenyl group of BMS-202 with carborane and prepared its carboranyl BMS-202 analogues. The results showed a loss of PD-L1 binding affinity due to the bulky size of carborane, suggesting that carborane cannot serve as a phenyl ring mimetic in certain cases. Docking study demonstrated that the narrow binding pocket of PD-L1 could not hold the bulky carborane, resulting in loss of its activity. Compounds 1a and 1b exhibited anti-proliferative activities on a broad scope of cancer cell lines. Further studies indicate that compound 1a can induce cell apoptosis and lead to G1 cell cycle phase arrest. The boron biodistribution study of compound 1a revealed that the brain/blood uptake ratio was 0.60 ± 0.08, exhibiting a good blood-brain penetration capability. Full article

Sugarcane productivity varies widely among genotypes, but the biochemical traits underlying these differences remain poorly characterized. In this study, six contrasting sugarcane cultivars were profiled to investigate how ionomic, hormonal, flavonoid, and photosynthetic pigment signatures are associated with yield and sucrose accumulation. Morphological traits and field performance revealed marked genotypic variation, with ZZ14 and GL1215 achieving the highest yields and sugar content, while GT59 and GT60 performed less favorably. Multivariate analyses of ionomic data showed that potassium, magnesium, and calcium were consistently enriched in high-yield cultivars, whereas sodium, boron, and manganese were negatively associated with growth traits. Hormone profiling revealed that high-yielding genotypes utilize diverse strategies: while the high-yielding GL1215 achieved superior sugar content with the lowest levels of growth-promoting hormones, the LT1790 genotype, despite having the highest levels of these hormones, showed suboptimal yield due to a costly trade-off with its hyperactive defense system. Flavonoid analysis indicated that LT1790 contained the highest levels of Quercetin, rutin, and caffeic acid, suggesting enhanced antioxidant capacity, whereas GT59 preferentially accumulated chlorogenic acid. Canonical correlation analysis confirmed that nutrient balance and metabolite composition strongly correlated with plant height, stem diameter, and sugar concentration. Together, these results suggest that high-yield sugarcane genotypes achieve a superior metabolic balance, combining efficient nutrient uptake and robust antioxidant capacity with a favorable hormone profile that promotes strong growth without triggering a costly constitutive defense system. Full article

Derivatives of natural amino acids are selectively absorbed by many types of tumour cells. This makes the use of amino acids, especially polyfunctional ones, attractive as a basis in the design of low-toxicity agents for targeted boron delivery for boron neutron capture therapy (BNCT) of tumours. We synthesized a series of new (S)-ornithine and (S)-lysine derivatives containing a 7,8-dicarba-nido-undecaborane (nido-carborane) residue attached to the amino group in the side chain or alpha position. The MTT assay demonstrated moderate cytotoxicity of the lysine and ornithine derivatives containing a nido-carborane residue in the side chain. It has been found that sodium salt of N^ε-(nido-carboran-7-yl)acetyl-(S)-lysine is capable of accumulation by MDA-MB-231 (human breast carcinoma) and SK-Mel 28 (human melanoma) cell lines, providing a boron concentration of up to 0.67 µg/10⁶ cells in in vitro experiments. This (S)-lysine derivative containing a nido-carborane residue in the side chain can be considered as a promising compound for in-depth study in vivo experiments aimed at designing an efficient boron delivery agent for BNCT. Full article

Geogenic contamination of groundwater presents a substantial threat to the enduring production and sustainability of irrigated fruit orchards, especially in arid and semi-arid regions where over 60% of horticultural irrigation depends on groundwater sources. Groundwater quality is increasingly threatened by geogenic contamination, presenting a critical global issue. Geogenic contaminants, such as fluoride and arsenic, combined with agricultural practices and inadequate wastewater treatment, pose a significant threat to groundwater. Concentrations of elements including arsenic, fluoride, boron, iron, and sodium often exceed acceptable thresholds. For instance, arsenic (As) levels up to 0.5 ppm have been reported in parts of South Asia, far exceeding the WHO guidelines limit of 0.01 mg/L. Boron concentrations above 2.0 ppm and fluoride concentrations exceeding 1.5 ppm are prevalent in impacted aquifers. Pollution consequences are far reaching, impacting agricultural ecosystems and human health as polluted water infiltrates the food chain via irrigation. These challenges are compounded by climate change and water scarcity, which further strain water sources, including those used in agriculture. Addressing groundwater contamination requires a multi-faceted approach. Strategies include developing crops that can tolerate toxicants, improving irrigation techniques, and employing advanced wastewater treatment technologies. This study solidifies current knowledge concerning the uptake processes and physiological effects of various pollutants in fruit crops. This review emphasizes the synergistic toxicity of many pollutants, identifies gaps in knowledge in species-specific tolerance, and emphasizes the dearth of comprehensive mitigating frameworks. Potential solutions, such as salt-tolerant rootstocks, gypsum amendments, and alternative irrigation timing, are examined to enhance resilient orchard systems in geogenically challenged areas. Full article