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PubMed1993

Hypolipidemic activity of boronated nucleosides and nucleotides in rodents.

Base-boronated nucleoside and phosphate-boronated nucleotides were potent hypolipidemic agents in rodents, lowering both serum cholesterol and triglyceride levels. Rat VLDL and LDL cholesterol levels were generally reduced and HDL cholesterol levels were significantly elevated after 14 days dosing at 8 mg/kg/day. Tissue cholesterol, triglyceride and phospholipid levels were reduced by selected derivatives. Increased fecal excretion of lipids did not appear to be a mechanism by which these derivatives lowered serum lipids in rodents. Rather, the agents suppressed appetite and reduced the activities of rate-limiting enzymes for de novo lipid synthesis, specifically cytoplasmic acetyl CoA synthetase, squalene synthetase, and phosphatidylate phosphohydrolase with IC50 values of approximately 10(-5) m.

Animals↗
PubMed1987

Analysis of ultratrace lithium and boron by neutron activation and mass-spectrometric measurement of 3He and 4He.

A new technique for analysis of lithium and boron at ultratrace concentrations (less than 10(-8)g g-1) is described. The method consists of mass-spectrometric assay of 3He from decay of tritium produced by thermal-neutron reaction on 6Li, and 4He produced by thermal-neutron reaction on 10B. Two neutron-irradiation facilities were used: the McMaster reactor, which is 235U-enriched and light-water moderated; and a graphite-moderated thermal column attached to the 235U-enriched, heavy-water-moderated core at the National Bureau of Standards (NBS) reactor. In the McMaster irradiations, fast neutrons (greater than 0.2 MeV) induce the reactions 14N(n, 3H)12C, 12C(n, alpha)9Be, 16O(n, alpha)13C, and 14N(n, alpha)11B. These reactions become serious sources of error in samples such as human blood which have very low concentrations of lithium and boron, and high concentrations of nitrogen, carbon and oxygen. In the NBS thermal column, fast-neutron reactions are virtually absent, and only corrections for thermal-neutron capture by deuterium, and thermal-neutron (n, alpha) reactions on oxygen, sulfur, chlorine, potassium, and calcium need to be taken into account. Results are presented for various actual samples including human blood and its components, and some standard biological reference materials, to provide a realistic base for other workers to judge the reliability of the method.

Boron↗
PubMed2004

MicroPET-based pharmacokinetic analysis of the radiolabeled boron compound [18F]FBPA-F in rats with F98 glioma.

Boron neutron capture therapy (BNCT) is one of the effective methods of radiation therapy for the treatment of tumors such as malignant glioma. Boronophenylalanine ((10)B-BPA) solution has been used as a potential boron carrier for such a treatment. The aim of this study is to investigate 4-borono-2-[(18)F]-fluoro-l-phenylalanine-fructose ([(18)F]FBPA-F) in rats injected in the brain with glioma using in vivo small animal positron emission tomography (PET) imaging (microPET). Male Fischer 344 rats with F98 glioma in the left brain were used for these studies. Dynamic PET imaging of [(18)F]FBPA-F was performed on the 13th day after tumor inoculation. Arterial blood sampling was performed to obtain an input function for tracer kinetic modeling. The accumulation ratios of [(18)F]FBPA-F for the glioma-to-normal brain approached 3. The uptake characteristics of BPA-F and [(18)F]FBPA-F were similar. The results indicate that 4h after BPA-F injection would be the optimal irradiation time for BNCT. Rate constants were estimated using a three-compartment model. This study provides useful information for the clinical application of BNCT in patients with brain tumors.

Animals↗
PubMed2004

Radiation injury of boron neutron capture therapy using mixed epithermal- and thermal neutron beams in patients with malignant glioma.

The purpose of this study was to clarify the radiation injury in acute or delayed stage after boron neutron capture therapy (BNCT) using mixed epithermal- and thermal neutron beams in patients with malignant glioma. Eighteen patients with malignant glioma underwent mixed epithermal- and thermal neutron beam and sodium borocaptate between 1998 and 2004. The radiation dose (i.e. physical dose of boron n-alpha reaction) in the protocol used between 1998 and 2000 (Protocol A, n = 8) prescribed a maximum tumor volume dose of 15 Gy. In 2001, a new dose-escalated protocol was introduced (Protocol B, n = 4); it prescribes a minimum tumor volume dose of 18 Gy or, alternatively, a minimum target volume dose of 15 Gy. Since 2002, the radiation dose was reduced to 80-90% dose of Protocol B because of acute radiation injury. A new Protocol was applied to 6 glioblastoma patients (Protocol C, n = 6). The average values of the maximum vascular dose of brain surface in Protocol A, B and C were 11.4+/-4.2 Gy, 15.7+/-1.2 and 13.9+/-3.6 Gy, respectively. Acute radiation injury such as a generalized convulsion within 1 week after BNCT was recognized in three patients of Protocol B. Delayed radiation injury such as a neurological deterioration appeared 3-6 months after BNCT, and it was recognized in 1 patient in Protocol A, 5 patients in Protocol B. According to acute radiation injury, the maximum vascular dose was 15.8+/-1.3 Gy in positive and was 12.6+/-4.3 Gy in negative. There was no significant difference between them. According to the delayed radiation injury, the maximum vascular dose was 13.8+/-3.8 Gy in positive and was 13.6+/-4.9 Gy in negative. There was no significant difference between them. The dose escalation is limited because most patients in Protocol B suffered from acute radiation injury. We conclude that the maximum vascular dose does not exceed over 12 Gy to avoid the delayed radiation injury, especially, it should be limited under 10 Gy in the case that tumor exists in speech center.

Adult↗
PubMed2006

Solution behavior of a sugar-based carborane for boron neutron capture therapy: a nuclear magnetic resonance investigation.

The physico-chemical properties of beta-lactosyl-closo-orthocarborane in water solution were investigated by multinuclear NMR, (13)C NMR relaxation, and ab-initio calculations. This molecule represents a potentially selective boron carrier in Boron Neutron Cancer Therapy (BNCT) and exhibits amphiphilic characteristics. Its structural and dynamic features were studied comparing NMR data acquired in both aggregating and non-aggregating conditions. Aggregates are characterized by rapid exchange with the bulk and by high sensitivity to temperature conditions. An unusually stable intra-molecular CH...O hydrogen bond was found to persist in water solution both for the free molecules and after aggregate formation. At the same time, inter-molecular specific CH()O interactions do not seem effective in the aggregate formation process, which appears to take place only on non-specific hydrophobic basis.

Boranes↗
PubMed2006

Effect of farmyard manure application on boron adsorption-desorption characteristics of some soils.

Boron (B) availability to crop plants depends on soil properties as well as management practices like liming, fertilization and use of organic manures. To assess the effect of farmyard manure (FYM) application on availability of added B, adsorption-desorption of B was investigated in five different soils receiving varying doses of FYM (0, 5 and 10 g FYM kg(-1) soil). Two surfaces Freundlich model was found best to account for B adsorption-desorption data of all soils. Application of FYM increased B adsorption capacities pertaining to low (K1) and high (K2) concentration ranges in all soils, except Soil C (Alfisol) having a pH of 9.8, in which the higher rate of FYM decreased the value of K2. Application of FYM did not change B desorption capacities of soils corresponding to low B concentration range (K(1)(1)) significantly, however, it increased B desorption capacity pertaining to high B concentration (K(1)(2)) in all soils, except Soils C (Alfisol) and E (Entisol) having pH of 9.8 and 5.1, respectively. Application of FYM increased the desorption slope factor applicable to low concentration range (1/n(1)(1)) in Soil A (Inceptisol), but decreased it in Soil E (Entisol). The 1/n(1)(2) (desorption slope factor applicable to high concentration range) decreased with FYM application in all soils except Soil E (Entisol), where it was increased. Boron desorption index (slope(ads)/slope(des)) decreased with FYM application in low B concentration range, but increased in high concentration range for all soils except soil E (Entisol, pH 5.1), in which a reverse trend was observed. Application of FYM increased the retention of added B in soils and may help reducing the leaching losses.

Adsorption↗
PubMed2006

Electrochemical oxidation of benzene on boron-doped diamond electrodes.

This work presents an electrochemical investigation of the benzene oxidation process in aqueous solution on boron-doped diamond (BDD) electrodes. Additionally, in order to determine the main products generated during the oxidation process, electrolysis and high performance liquid chromatography experiments were carried out. The complete degradation of this compound was performed aiming to a further application in waste water treatment. The cyclic voltammetry studies indicate that benzene is irreversibly oxidized in acid medium (H2SO4 0.5 M) on the BDD electrode surface at 2.0 V versus Ag/AgCl in a diffusion controlled process. During the cycling, other products are generated, and a pair of peaks was observed that can be associated with the oxi-reduction of anyone of the following species: hydroquinone, benzoquinone, resorcinol or catechol. The electrolysis experiments were carried out at 2.4 and 2.5 V on the BDD electrode surface in a solution containing 1x10(-2) M of benzene (below the saturation concentration in aqueous solution), for 3 and 5 h, respectively. The main products measured were: hydroquinone, resorcinol, p-benzoquinone, catechol and phenol. The complete electrochemical benzene degradation was performed in the electrolysis experiments using a rotating BDD disc electrode (2.5 V for 5 h) and the main products detected were all measured at concentrations lower than 10(-5) M in this condition. The boron-doped diamond electrode had proved to be a valuable tool for the electrochemical degradation of the benzene, a very stable chemical compound.

Benzene↗
PubMed2006

Boron neutron capture therapy using mixed epithermal and thermal neutron beams in patients with malignant glioma-correlation between radiation dose and radiation injury and clinical outcome.

PURPOSE: To clarify the correlation between the radiation dose and clinical outcome of sodium borocaptate-based intraoperative boron neutron capture therapy in patients with malignant glioma. METHODS AND MATERIALS: The first protocol (P1998, n = 8) prescribed a maximal gross tumor volume (GTV) dose of 15 Gy. In 2001, a dose-escalated protocol was introduced (P2001, n = 11), which prescribed a maximal vascular volume dose of 15 Gy or, alternatively, a clinical target volume (CTV) dose of 18 Gy. RESULTS: The GTV and CTV doses in P2001 were 1.1-1.3 times greater than those in P1998. The maximal vascular volume dose of those with acute radiation injury was 15.8 Gy. The mean GTV and CTV dose in long-term survivors with glioblastoma was 26.4 and 16.5 Gy, respectively. A statistically significant correlation between the GTV dose and median survival time was found. In the 11 glioblastoma patients in P2001, the median survival time was 19.5 months and 1- and 2-year survival rate was 60.6% and 37.9%, respectively. CONCLUSION: Dose escalation contributed to the improvement in clinical outcome. To avoid radiation injury, the maximal vascular volume dose should be <12 Gy. For long-term survival in patients with glioblastoma after boron neutron capture therapy, the optimal mean dose of the GTV and CTV was 26 and 16 Gy, respectively.

Adolescent↗
PubMed2006

Buildup of gold nanoparticle multilayer thin films based on the covalent-bonding interaction between boronic acids and polyols.

A novel method for the fabrication of gold nanoparticle multilayer films based on the covalent-bonding interaction between boronic acid and polyols, poly(vinyl alcohol) (PVA), was developed. The multilayer buildup was monitored by UV-vis absorbance spectroscopy, which showed a linear increase of the film absorbance with the number of adsorbed Au layers and indicated the stepwise and uniform assembling process. The atomic force microscopy (AFM) image showed that a compact gold multilayer thin film was successfully assembled. The residual boronic acid group on the surface of thin film could incorporate glycosylated-protein horseradish peroxidase (HRP), and good catalytic activity for H2O2 could be observed.

Boronic Acids↗
PubMed2004

Dose response of the AIA rabbit stifle joint to boron neutron capture synovectomy.

This study assessed the treatment with boron neutron capture synovectomy of synovitis in the antigen-induced arthritis (AIA) model. A boron compound, potassium dodecahydrododeca-borate (K(2)B(12)H(12)), was injected into stifle joints of 24 AIA and 12 normal rabbits and activated by neutron bombardment of the joint to achieve doses from 800 to 81,000 RBE-cGy. Synovial ablation in the AIA joint was accomplished at doses of 6,000 to 7,000 RBE-cGy with no adverse effects to skin or extracapsular tissues.

Animals↗
PubMed2004

The influence of dietary boron supplementation on egg quality and serum calcium, inorganic phosphorus, magnesium levels and alkaline phosphatase activity in laying hens.

This study was performed to investigate the influence of dietary boron (B) supplementation on egg production, interior and exterior egg quality and serum parameters related to egg formation in laying hens. Two hundred and twenty four, 18 week old, Hyline Brown 98 strain hens were assigned to 7 groups with 4 replicates. After 10 days of adaptation the hens were fed for 8 weeks on diets supplemented with 0, 5, 10, 50, 100, 200 and 400 mg/kg (diet) B (H(3)BO(3)). Live weight, feed consumption and egg production were reduced in the 400 mg/kg B supplemented group. Increases were determined in serum Ca, inorganic P and Mg levels and serum ALP activity was not influenced by supplemental B. Boron changed the interior and exterior quality of eggs. In particular, high level of B supplementation reduced live weight, feed consumption and egg production and changed some blood metabolites.

Alkaline Phosphatase↗
PubMed2006

Crystal structure of the boronic acid-based proteasome inhibitor bortezomib in complex with the yeast 20S proteasome.

The dipeptide boronic acid bortezomib, also termed VELCADE, is a proteasome inhibitor now in use for the treatment of multiple myeloma, and its use for the treatment of other malignancies is being explored. We determined the crystal structure of the yeast 20S proteasome in complex with bortezomib to establish the specificity and binding mode of bortezomib to the proteasome's different catalytically active sites. This structure should enable the rational design of new boronic acid derivatives with improved affinities and specificities for individual active subunits.

Animals↗
PubMed2004

Boron isotope fractionation in groundwaters as an indicator of past permafrost conditions in the fractured crystalline bedrock of the fennoscandian shield.

The Fennoscandian Shield has been subjected to several glaciations over the past million years, the last of which (Weichselian Ice Age) ended only at about 10Ka. Here we used boron isotopes and B contents to (a) establish the degree of water-rock interaction (WRI) and (b) clarify freezing processes within groundwaters from the Aspo site in Sweden and from various sites in Finland. The high delta(11)B values recorded by all groundwaters (up to 51.9 per thousand) including diluted, boron-poor, inland groundwaters suggest selective uptake of (10)B into ice related to freezing processes under permafrost conditions. According to co-existing ice and residual brines in a Canadian frozen mine, this fractionation process, enhanced by Rayleigh fractionation, can generate a natural field of isotopic variation around 60 per thousand and provides a new application of B isotope that makes possible to easily characterise groundwaters that underwent past permafrost conditions.

Boron↗
PubMed2001

Separation of mistletoe lectins based on the degree of glycosylation using boronate affinity chromatography.

A mixture of two mistletoe lectins (MLs) has been separated according to the degree of glycosylation using boronate affinity chromatography. The mistletoe lectins, mistletoe lectin I (MLI) and mistletoe lectin III (MLIII) with degrees of glycosylation of 6.1 and 3.8%, respectively, were used in the investigation. MLI exhibited a higher retention time than MLIII due to its higher degree of glycosylation. Separation was confirmed by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The developed method may lead to new applications for the boronate affinity technique, as well as provide an alternative separation method for MLs.

Boronic Acids↗
PubMed2003

Linear alkylbenzene sulfonate and boron monitoring in four catchments in the UK contribution to GREAT-ER #11.

A comprehensive monitoring programme was carried out in the Aire, Calder, Went and Rother catchments in the UK. A total of 804 effluent samples from 36 sewage treatment works (STWs) and 1100 water samples from 54 river sampling sites were analysed. Concentrations of linear alkylbenzene sulfonate (LAS), boron and other water quality determinands in STW effluent and river waters over a 2-year period (August 1996-August 1998) are reported. The data illustrate the temporal and spatial variations in concentrations of LAS and boron in river waters and effluents. Concentrations of LAS in effluents reflect the biological treatment employed and the influence of tertiary treatment is clearly demonstrated.

Alkanesulfonic Acids↗
PubMed1997

An assessment of heavy metals and boron contamination in workplace atmospheres from ceramic factories.

The occupational exposure in workplace atmospheres of ceramic factories to some metals (Ba, Cd, Co, Cr, Cu, Ni, Zn) and boron has been studied. During 1994 samples were collected at several ceramic factories from the Comunitat Valenciana (Spain) in a random fashion to avoid correlation problems regarding data analysis; factories were sampled to provide a representative cross-section. Powdered samples were treated with concentrated nitric acid according to the National Institute for Occupational Safety and Health (NIOSH) digestion procedure for the analysis of metals in air samples. Heavy metals were analyzed by AAS and boron by UV/Visible spectrophotometry using the Azomethine-H method. Concentrations found for Cd, Cr, Cu, Ni and Zn were considered very low in the environment of this industrial sector. However, Co, Ba and B were detected in several samples with concentrations above the threshold limit value (TLV), referred to airborne concentrations of substances in workplace atmospheres. Principal component analysis (PCA) has also been carried out in order to classify the workplaces studied and their potential hazard to the workers.

Air Pollutants, Occupational↗
PubMed1982

Unaffected blood boron levels in newborn infants treated with a boric acid ointment.

No rise in the boron content of the plasma of 22 newborn infants was demonstrated following repeated daily application of a water-emulsifying ointment containing the equivalent of 3% boric acid to the napkin region. The mean plasma-boron concentration fell over 5 days from a pretreatment value of 0.49 to 0.29 mg/litre, the corresponding values in ten untreated neonates being 0.62 and 0.21 mg/litre, respectively. No statistically significant differences were found. The results confirm the safety of such ointments for application to the skin, a conclusion predicted by theoretical estimates of the maximum possible boric acid absorption following application of the ointment.

Boric Acids↗
PubMed1999

The combined effect of boronophenylalanine and borocaptate in boron neutron capture therapy for SCCVII tumors in mice.

PURPOSE: To increase the effect of boron neutron capture therapy (BNCT) on tumors in vivo, the combined effects of para-boronophenylalanine (BPA) and borocaptate sodium (BSH) were investigated. METHODS AND MATERIALS: 10B-enriched BPA and BSH were administered to C3H/He mice bearing SCCVII tumors by intragastric and intravenous injections, respectively. The colony formation and tumor control assays were employed for investigating antitumor effects of BNCT. The extent of homogeneity of tumor cell killing effect was examined by the distribution of frequencies of binuclear cells (BNC) producing a certain number of micronuclei (0,1,2,--,> or =5) to total number of BNC and by the comparison between surviving cell fraction (SF) in colony formation assay and the normal nuclear division fraction (NNDF) at first mitosis following BNCT. RESULTS: The relationships between SF and radiation dose in Gy (D) at around 10 ppm of 10B in tumors were as follow: -InSF = -0.101 + 0.648 Gy(-1) x D, 0.0606+0.435 Gy(-1) x D, and -0.0155 + 0.342 Gy(-1) x D for BPA, BPA + BSH, and BSH, respectively. In tumor control assay, BPA was also more effective than BSH, but the difference of effectiveness significantly decreased: 1.9 times more effective in colony assay vs. 1.2 times in tumor control assay. The most effective treatment to achieve tumor cure was BNCT using BPA + BSH, and it was 1.9 times more effective than BSH-BNCT. In BSH-BNCT, NNDF decreased exponentially with radiation dose and was equal to SF. However, NNDF following BPA-BNCT showed a biphasic decrease with radiation dose, and SF was much lower than NNDF. In the combination of BPA and BSH, the discrepancy between NNDF and SF decreased in comparison with BPA-BNCT. The distribution of frequency of BNC with a certain number of micronuclei to total BNC was very close to Poisson distribution in BSH-BNCT tumors; however, it deviated from the Poisson in BPA-BNCT tumors. In combination with BPA and BSH, the distribution showed an intermediate pattern. These findings indicate that BSH distributes homogeneously with a heterogeneous distribution of BPA in tumors, and the heterogeneous effect of BPA-BNCT was improved by the combination of two boron compounds. CONCLUSION: The heterogeneous cell killing effect of BPA-BNCT was improved by the combination of BSH, and increased tumor control rates. Therefore, this combination may improve clinical outcome of BNCT although the effects on normal tissues have to be examined before clinical application.

Animals↗