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PubMed2000

Inhibition of HIV-1 protease by a boron-modified polypeptide.

Six boronated tetrapeptides with the carboxy moiety of phenylalanine replaced by dihydroxyboron were synthesized, and their activities against human immunodeficiency virus 1 (HIV-1) protease subsequently investigated. The sequences of these peptides were derived from HIV-1 protease substrates, which included the C-terminal part of the scissile bond (Phe-Pro) within the gag-pol polyprotein. Enzymatic studies showed that these compounds were competitive inhibitors of HIV-1 protease with K(i) values ranging from 5 to 18 microM when experiments were performed at high enzyme concentrations (above 5 x 10(-8) M); however, at low protease concentrations inhibition was due in part to an increase of the association constants of the protease subunits. Ac-Thr-Leu-Asn-PheB inhibited HIV-1 protease with a K(i) of 5 microM, whereas the non-boronated parental compound was inactive at concentrations up to 400 microM, which indicates the significance of boronation in enzyme inhibition. The boronated tetrapeptides were inhibitory to an HIV-1 protease variant that is resistant to several HIV-1 protease inhibitors. Finally, fluorescence analysis showed that the interactions between the boronated peptide Ac-Thr-Leu-Asn-PheB and HIV-1 protease resulted in a rapid decrease of fluorescence emission at 360 nm, which suggests the formation of a compound/enzyme complex. Boronated peptides may provide useful reagents for studying protease biochemistry and yield valuable information toward the development of protease dimerization inhibitors.

Boron Compounds↗
PubMed2002

Measured variation in boron loads reaching European sewage treatment works.

Per capita boron loads reaching 48 sewage treatment works (STWs) in The Netherlands, Germany, Italy, and the UK have been determined from monitoring data. These have been compared with the per capita input predicted from boron in detergents, as determined from detergent product sales data. The resulting distribution of the ratios of measured boron to boron predicted from consumer usage has a 90th percentile of less than 1.5. Boron has previously been shown to be a good marker for substances contained in detergent products, as it cannot be biodegraded and is not substantially adsorbed in the sewer, and there is little or no removal during sewage treatment processes. The monitoring information on the distribution of boron loads found at the different STWs should thus be indicative of the distribution of other substances released to the environment by detergent products, as specified by the relevant industrial category (IC 5-personal/domestic) in the Technical Guidance Documents. Variation in detergent product consumption figures from 18 European countries is also low, with the country with the highest per capita detergent consumption having only 1.3 times the European average detergent use. Thus the present practice of determining a "reasonable worst case" by multiplying the average per capita consumption by a factor of four to account for geographic differences in distribution, is considered to be inappropriate. This should be replaced by a factor of less than two, which combines within country and between country variations to provide a reasonable worst case approximation of the load reaching the sewage treatment facility.

Boron↗
PubMed1988

Nitrogen-15 NMR spectroscopy of the catalytic-triad histidine of a serine protease in peptide boronic acid inhibitor complexes.

15N NMR spectroscopy was used to examine the active-site histidyl residue of alpha-lytic protease in peptide boronic acid inhibitor complexes. Two distinct types of complexes were observed: (1) Boronic acids that are analogues of substrates form complexes in which the active-site imidazole ring is protonated and both imidazole N-H protons are strongly hydrogen bonded. With the better inhibitors of the class this arrangement is stable over the pH range 4.0-10.5. The results are consistent with a putative tetrahedral intermediate like complex involving a negatively charged, tetrahedral boron atom covalently bonded to O gamma of the active-site serine. (2) Boronic acids that are not substrate analogues form complexes in which N epsilon 2 of the active-site histidine is covalently bonded to the boron atom of the inhibitor. The proton bound to N delta 1 of the histidine in these histidine-boronate adducts remains strongly hydrogen bonded, presumably to the active-site aspartate. Benzeneboronic acid, which falls in this category, forms an adduct with histidine. In both types of complexes the N-H protons of His-57 exchange unusually slowly as evidenced by the room temperature visibility of the low-field 1H resonances and the 15N-H spin couplings. These results, coupled with the kinetic data of the preceding paper [Kettner, C. A., Bone, R., Agard, D. A., & Bachovchin, W. W. (1988) Biochemistry (preceding paper in this issue)], indicate that occupancy of the specificity subsites may be required to fully form the transition-state binding site. The significance of these findings for understanding inhibitor binding and the catalytic mechanism of serine proteases is discussed.

Binding Sites↗
PubMed2005

Boron isotopes in the Seine River, France: a probe of anthropogenic contamination.

Boron concentrations and isotopic compositions have been measured in the dissolved load of the Seine Basin rivers, France. Hydrology and chemistry of the Seine River and its tributaries are strongly influenced by human activities, as the anthropogenic pressure on the Seine catchment is one of the highest in Europe. The samples were collected between 1994 and 1996 during various stages of flow, complemented by a time-series of the Seine River in Paris for 1 yr. In particular, the decennial flood event of winter 1994 was sampled. Boron appears to be conservative in rivers and not influenced by adsorption onto suspended matter and/or consumption by microorganisms. Despite the complexity of the Seine River system, dissolved boron and its isotopes are found to be suitable tracers of contamination. The total dissolved boron of the Seine River at Paris is explained by the contribution from three distinct components: Urban effluents constitute 65% of the boron discharge measured in the Seine River whereas agriculture-affected waters contribute less than 10% with a more marked influence during high water discharges. Rainwater contribution is important (25% mean), reaching 30% of dissolved boron during high flood events.

Animals↗
PubMed2005

Aromaticity of planar boron clusters confirmed.

Low-energy boron clusters are characterized by two-dimensional geometry. Aromaticity of these planar boron clusters was established in terms of topological resonance energy (TRE). All planar boron clusters were found to be highly aromatic with large positive TREs even if they have 4n pi-electrons. Aromaticity must therefore be the origin of unusual planar or quasi-planar geometry. Thus, the aromaticity concept is as useful in boron chemistry as it is in general organic chemistry. It is evident that the Hückel 4n + 2 rule of aromaticity should not be applied to such polycyclic pi-systems. Some of the boron clusters are in the triplet electronic state to attain higher aromaticity. Multivalency and electron deficiency of boron atoms are responsible for lowering the energies of low-lying pi molecular orbitals and then for enhancing aromaticity. For polycyclic pi-systems, paratropicity does not always indicate antiaromaticity.

Boron↗
PubMed2003

Investigation into the relationship between major and minor element contents and particle size and leachability of boron in fly ash from coal fuel thermal power plants.

A basic investigation of boron in discharged fly ash by coal fuel thermal power plants in several worldwide locations was carried out. Eight kinds of fly ash sample were prepared from eight coal fuel thermal power plants. Two of the fly ash samples were used to examine the relationship between the concentration of boron in fly ash and the particle size. When the particle size of fly ash is smaller, there is a possibility that it will be released into the air and spread over a wide area in the environment. However, it has become apparent that fly ash of smaller particle size has a higher concentration of boron and a higher enrichment factor. In other fly ash samples, the boron contents were examined and leaching tests were carried out. There is acidic fly ash as well as alkaline fly ash that contains larger amounts of acidic or basic salts. On alkaline fly ash, when the concentration of boron bound to Fe-Mn oxide is low; it has become apparent that leaching boron is increased in a solution with lower pH of approximately 4 which is nearly the pH of acid rain.

Air Pollutants↗
PubMed2001

High concentrations of fluoride and boron in drinking water wells in the Muenster region--results of a preliminary investigation.

In 1998, two cases of severe dental fluorosis in schoolchildren occurred in the Muenster region. These cases took place in one household, where fluoridated toothpaste, fluoridated salt, and fluoride tablets were consumed. Furthermore, the family used drinking water from its private well only. Analyses of the well water ordered by local health officials revealed very high amounts of fluoride, boron, and other electrolytes. This unusual combination of high amounts of fluoride and boron could also be found in the water of a great number of other private wells that are the only source for drinking water in this rural region of the Muensterland. Anthropogenic sources could be excluded. Because of this, the results of the water samples were collated to the specific geological situation in this area. In the Muenster region there are marl layers of the chalk era covered with quarternary sediments. The quarternary sediments are up to 10 to 20 metres thick and they usually conduct the groundwater. The marl contains high concentrations of fluoride and boron. In some places the groundwater has contact with these layers. To check the amount of fluoride and boron in the groundwater, indicator values were sought, which can give a hint of high contents of these trace elements. In this study the conductivity and acidity were identified as possible indicators of a high amount of fluoride and boron in the drinking water in this specific region. To work economically and efficiently, the drinking water should be checked for fluoride and boron on a regular basis only when these values are extraordinarily high. In the case of high concentrations, especially of fluoride, in the drinking water the persons concerned should be informed about their potential health risk, giving them the opportunity to optimise the total daily intake of fluoride.

Boron↗
PubMed1988

Peptide boronic acids, substrate analogs, inhibit chymase, and histamine release from rat mast cells.

Peptide boronic acids, such as methoxysuccinyl-Ala-Ala-Pro-(L)boro-Phe-OH, its pinacol ester, and t-butyloxycarbonyl-Phe-Pro-(L)boro-Phe-pinacol, inhibited the activity of chymase from connective tissue mast cells approximately 40- to 80-fold more than atypical chymase from mucosal mast cells, and did not inhibit trypsin. Only peptide boronic acids containing "L" forms of boronic acids were inhibitory. The Ki values of these peptide boronic acids for chymase were in the 60-170 nM concentration range, like those of the natural inhibitors tested, but all the natural inhibitors tested except Eglin C and chymostatin inhibited both chymase and trypsin. Thus these peptide boronic acids should be useful for selective inhibition of chymase with less inhibitory activity for atypical chymase and without inhibition of trypsin. These peptide boronic acids markedly inhibited histamine release induced by anti-rat immunoglobulin E, suggesting that chymase in connective tissue mast cells plays some role in the process of histamine release. These peptides are assumed to be therapeutically useful for treatment of allergic inflammations catalyzed by chymase.

Animals↗
PubMed2001

The effect of pregnancy on renal clearance of boron in rats given boric acid orally.

Boric acid (H(3)BO(3)) has been shown to cause developmental abnormalities in the offspring of pregnant rats. Comparative data on the renal clearance of boron (B) in rats and humans, both pregnant and nonpregnant, exposed to boric acid (BA) would reduce uncertainty in interspecies extrapolation from rats to humans. The purpose of this study was to evaluate the effect of pregnancy on the plasma half-life and renal clearance of boron in Sprague-Dawley rats given a single oral dose of boric acid. For the half-life study, nonpregnant and pregnant (gestation day 16) rats were given a single dose of 30 mg/kg of boric acid by gavage, and plasma samples were collected at 2-3 h intervals. The plasma half-life of boron was determined to be 2.9 +/- 0.2 and 3.2 +/- 0.3 h in nonpregnant and pregnant rats, respectively. In the clearance study, nonpregnant and pregnant (GD 16) rats were given a single gavage dose of 0.3, 3, or 30 mg/kg of boric acid. Boron clearance was slightly higher in pregnant rats (3.3 +/- 0.6, 3.2 +/- 0.5, and 3.4 +/- 0.5 ml/min/kg, respectively) compared to nonpregnant rats (3.1 +/- 0.8, 3.0 +/- 0.6, and 3.2 +/- 0.5 ml/min/kg, respectively), but the difference was not statistically significant and not dose-related. Boron clearance was less than creatinine clearance, suggesting tubular reabsorption in both groups. In conclusion, pregnancy did not appear to significantly alter the renal clearance or the plasma half-life of boron in Sprague-Dawley rats under the conditions of this study.

Administration, Oral↗
PubMed1999

Boron neutron capture therapy of brain tumors: an emerging therapeutic modality.

Boron neutron capture therapy (BNCT) is based on the nuclear reaction that occurs when boron-10, a stable isotope, is irradiated with low-energy thermal neutrons to yield alpha particles and recoiling lithium-7 nuclei. For BNCT to be successful, a large number of 10B atoms must be localized on or preferably within neoplastic cells, and a sufficient number of thermal neutrons must be absorbed by the 10B atoms to sustain a lethal 10B (n, alpha) lithium-7 reaction. There is a growing interest in using BNCT in combination with surgery to treat patients with high-grade gliomas and possibly metastatic brain tumors. The present review covers the biological and radiobiological considerations on which BNCT is based, boron-containing low- and high-molecular weight delivery agents, neutron sources, clinical studies, and future areas of research. Two boron compounds currently are being used clinically, sodium borocaptate and boronophenylalanine, and a number of new delivery agents are under investigation, including boronated porphyrins, nucleosides, amino acids, polyamines, monoclonal and bispecific antibodies, liposomes, and epidermal growth factor. These are discussed, as is optimization of their delivery. Nuclear reactors currently are the only source of neutrons for BNCT, and the fission reaction within the core produces a mixture of lower energy thermal and epithermal neutrons, fast or high-energy neutrons, and gamma-rays. Although thermal neutron beams have been used clinically in Japan to treat patients with brain tumors and cutaneous melanomas, epithermal neutron beams now are being used in the United States and Europe because of their superior tissue-penetrating properties. Currently, there are clinical trials in progress in the United States, Europe, and Japan using a combination of debulking surgery and then BNCT to treat patients with glioblastomas. The American and European studies are Phase I trials using boronophenylalanine and sodium borocaptate, respectively, as capture agents, and the Japanese trial is a Phase II study. Boron compound and neutron dose escalation studies are planned, and these could lead to Phase II and possibly to randomized Phase III clinical trials that should provide data regarding therapeutic efficacy.

Boron Neutron Capture Therapy↗
PubMedDate not supplied

Determination of the concentration of complex boronated compounds in biological tissues by inductively coupled plasma atomic emission spectrometry.

The application of inductively coupled plasma atomic emission spectrometry (ICP-AES) to the determination of the concentration of complex boron-containing compounds in biological tissue samples is described. Tissue digestion is achieved with perchloric acid and hydrogen peroxide in 1 hr at 75 degrees C. The ICP-AES method gave a linear response for elemental boron concentration in the range 0.05 to 100 ppm and does not require the reduction of the boron to a simple species, such as boric acid. Complete recovery of boron in complex boron cluster compounds was obtained. The procedure has been applied to the determination of the boron content in compounds synthesised for neutron capture therapy and is suitable for use in biodistribution studies of such compounds.

Animals↗
PubMed1993

The effect of boron supplementation on lean body mass, plasma testosterone levels, and strength in male bodybuilders.

The effect of boron supplementation was investigated in 19 male bodybuilders ages 20-27 years. Ten were given a 2.5-mg boron supplement while 9 were given a placebo every day for 7 weeks. Plasma total and free testosterone, plasma boron, lean body mass, and strength measurements were determined on Days 1 and 49 of the study. Plasma boron values were significantly (p < 0.05) different as the experimental group increased from (+/- SD) 20.1 +/- 7.7 ppb pretest to 32.6 +/- 27.6 ppb posttest, while the control group mean decreased from 15.1 +/- 14.4 ppb pretest to 6.3 +/- 5.5 ppb posttest. Analysis of variance indicated no significant effect of boron supplementation on any of the dependent variables. Both groups demonstrated significant increases in total testosterone, lean body mass, 1-RM squat, and 1-RM bench press. The findings suggest that 7 weeks of bodybuilding can increase total testosterone, lean body mass, and strength in lesser trained bodybuilders, and that boron supplementation had no effect on these measures.

Adult↗
PubMed2000

Chronic boron or copper deficiency induces limb teratogenesis in Xenopus.

Sets of adult male and female Xenopus laevis were administered a boron-deficient (-B) diet under low-boron culture conditions, a boron-supplemented (+B) diet under ambient boron culture conditions, a copper-deficient (-Cu) diet under low-copper culture conditions, or a copper-supplemented (+Cu) diet under ambient copper culture conditions, for 120 d. Adults from each group were' subsequently bred, and the progeny were cultured and bred. Results from these studies indicated that although pronounced effects on adult reproduction and early embryo-larval development were noted in the -B F1 generation, no effects on limb development were observed. No significant effects on reproduction, early embryogenesis, or limb development were noted in the +B group, irrespective of generation. Highly specific forelimb and hindlimb defects, including axial flexures resulting in crossed limbs and reduction deficits, were observed in -B F2 larvae, but not in the +B F2 larvae. As was noted in the boron-deficiency studies, significant effects on reproduction and early embryo development were observed in the -Cu F1 generation, but not in the +Cu F, generation. Unlike the effects associated with boron deficiency, maldevelopment of the hindlimbs (32 responders, n = 40) was found in the F1 generation.

Animals↗
PubMed2004

Transmembrane partitioning of boron and other elements in RAW 264.7 and HL60 cell cultures.

The trace element boron is essential for all higher plants and is beneficial or has been established as essential for several animal models of human nutrition. To help identify the biomolecules that require boron for function in humans, we determined whether intracellular boron is retained against a concentration gradient. Cells (Abelson leukemia virus BALB murine monocyte-macrophage RAW 264.7 [RAW] and HL60) and supplemented media (Dulbecco's modified essential media [+ 10% fetal calf serum] and Iscove's modified Dulbecco's medium [+ 5% fetal calf serum], respectively) were analyzed for mineral concentrations after culture and subculture. Special corrections were made for trapped extracellular media in cell pellets and endocytosed media. For RAW cells, the partitioning coefficients (PC; intracellular/extracellular ratios) were, in rank order, as follows: Mn, 110; Fe, 67; P, 65; Zn, 32; K, 15; Cu, 7.1; Mg, 4.3; B, 1.7; Ca, 0.4; Na, 0.3. For HL60 cells, the partitioning coefficients were, in rank order, as follows: Mn, 212; Zn, 211; P, 123; K, 21; Fe, 16; Mg, 11; B, 1.7; Ca, 0.8; Na, 0.3. Trapped extracellular media was estimated to be 6.7 +/- 0.8%; trapped extracellular and endocytosed media together was 24.8 +/- 0.3% of the mass within the isolated cell pellets. The partitioning coefficients indicate a positive gradient for intracellular accumulation of boron, zinc, phosphorus, manganese, magnesium, potassium, iron, and copper in RAW264.7 and HL60 cells. Specifically, the data indicate the existence of a selective boron-binding molecular species within the cell or the existence of a boron-specific membrane transporter.

Animals↗
PubMed2000

Boron neutron capture therapy for malignant gliomas.

Boron neutron capture therapy (BNCT) represents a promising modality for a relatively selective radiation dose delivery to the tumour tissue. Boron-10 nuclei capture slow 'thermal' neutrons preferentially and, upon capture, promptly undergo 10B(n,alpha)7Li reaction. The ionization tracks of energetic and heavy lithium and helium ions resulting from this reaction are only about one cell diameter in length (approximately 14 microm). Because of their high linear energy transfer (LET) these ions have a high relative biological effectiveness (RBE) for controlling tumour growth. The key to effective BNCT of tumours, such as glioblastoma multiforme (GBM), is the preferential accumulation of boron-10 in the tumour, including the infiltrating GBM cells, as compared with that in the vital structures of the normal brain. Provided that a sufficiently high tumour boron-10 concentration (approximately 10(9) boron-10 atoms/cell) and an adequate thermal neutron fluence (approximately 10(12) neutrons/cm2) are achieved, it is the ratio of the boron-10 concentration in tumour cells to that in the normal brain cells that will largely determine the therapeutic gain of BNCT.

Boron Neutron Capture Therapy↗
PubMed2000

The influence of lipophilicity on binding of boronated DNA-intercalating compounds in human glioma spheroids.

Five boronated DNA-intercalating compounds [5-ortho-carboranyl phenanthridinium (5-o-CP), 5-para-carboranyl phenanthridinium (5-p-CP), 6-para-carboranyl phenanthridinium, water-soluble boronated phenanthridinium and water-soluble boronated acridine (WSA1)], primarily developed for boron neutron capture therapy (BNCT), were analysed regarding their binding in cultured human malignant glioma spheroids. Comparisons were made with the corresponding DNA intercalators ethidium bromide and acridine orange. Octanol/phosphate buffered saline-water coefficients were determined for all compounds, and it was found that the most lipophilic (5-o-CP and 5-p-CP) were most toxic and accumulated high amounts of boron in monolayer cells. These compounds bound primarily in the outermost part of spheroids with poor penetration into the inner region, even after 2 days of continuous exposure. On the other hand, the most hydrophilic compound (WSA1) showed lower toxicity and lower boron accumulation in monolayer cells, and rapid binding in the inner region of spheroids. A reasonable explanation for this observation is that the lipophilic compounds interact mainly with lipophilic parts of the cells, like cellular membranes, and therefore rapidly binds to cells, preventing penetration and binding to cells in the deeper region of the spheroids. The possibility of using these compounds for BNCT are discussed.

Acridines↗
PubMed2004

Dietary boron intake and prostate cancer risk.

Boron affects human steroid hormone levels. Circulating testosterone and estradiol levels have been proposed to modify prostate cancer risk. However, the association between dietary boron intake and the risk of prostate cancer has not been evaluated by any epidemiological study. We explored the association between dietary boron intake and the risk of prostate cancer in the USA. Our analysis was based on data from the third National Health and Nutrition Examination Survey (NHANES III). Cross-sectional case-control study design was employed by comparing boron intake of 95 prostate cancer cases with that of 8,720 male controls. After controlling for age, race, education, smoking, body mass index, dietary caloric intake, and alcohol consumption, increased dietary boron intake was associated with a decreased risk of prostate cancer with a dose-response pattern. The adjusted odds ratio was 0.46 (95% confidence interval: 0.21-0.98) for the highest quartile of boron intake comparing to the lowest quartile (P for trend = 0.0525). The observed association should be interpreted with caution because of the small case sample size and the nature of the cross-sectional study design, but deserve further investigation.

Adolescent↗
PubMedDate not supplied

Boron affects energy metabolism in the streptozotocin-injected, vitamin D3-deprived rat.

Dietary boron, in amounts usually found in human diets comprised mainly of fruits and vegetables, apparently affects both mineral and energy metabolism. Therefore, the effects of boron on a model system with a perturbed metabolic insulin-vitamin D3 axis was examined. Weanling male rats were fed a ground corn-high protein casein-corn oil-based diet (0.06 micrograms B/g and no supplemental vitamin D3) supplemented with B (as orthoboric acid) at 0 or 2.4 mg/kg. After 55 days, all rats were equilibrated in individual metabolic cages. After another 6 days, one half of the rats in both dietary groups were injected intraperitoneally with streptozotocin (STZ). All rats were killed 3 days after STZ treatment. STZ affected many aspects of energy metabolism. In the non-STZ rats, supplemental dietary boron substantially depressed plasma insulin, plasma pyruvate concentrations, and creatine kinase activity and increased plasma thyroxine (T4) concentrations. The finding that boron did not affect growth, but did affect several indices of energy metabolism in the non-STZ animals suggests that boron functions as a regulator of energy metabolism in the rat. A decrease in plasma aspartate transaminase activity (an indicator of enhanced cell membrane integrity) in the non-STZ rats suggests that boron exerts a protective influence over normal liver metabolism.

Animals↗