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[Side effects of dermatologic local therapy].

After application of dermatics systemic as well as topical side effects are to be expected, the latter also by usage of remedies and cosmetics. Even though life-threatening or lethal complications caused by potent substances like mercury compounds, phenols, salicylic acid, boric acid and others seldom have been observed, it is necessary to prevent them completely. Most frequent are allergic contact eczemas, but occasionally also toxic irritations of the skin can be registered. The side effects discussed, especially those caused by steroids and antibiotics, demand strong criteria for indication, scientific mode of administration and intensification of the topical efforts for standardization of dermatological treatment.

Administration, Topical↗

Sensitivity of ornithophillic fungi to some drugs.

The occurrence of ornithophillic fungi and related dermatophytes was evaluated from the poultry farm soil samples. Two test species of Microsporum were tested by 'Spore germination' and 'Disc diffusion method' against the two well known antifungal antibiotics i.e. griseofulvin and mycostatin (polyene antibiotic). The data showed cent percent inhibition of fungal spore germination and increased zone of inhibition at higher doses. The antimicrobial drugs including acetyl salicylic acid, benzoic acid and boric acid were also assessed at different doses against the test organisms. Acetyl salicylic acid and boric acid were found to be toxic at higher doses, while these pathogens seems to be somewhat resistant for benzoic acid. It is suggested that the effective doses of these drugs should also be tried for allergic effects on birds and other animals before commercial use.

Animals↗

Laboratory evaluation of boric acid-sugar solutions as baits for management of German cockroach infestations.

Boric acid dust has a long history as an insecticide in urban pest management, and it has been shown to be an effective alternative to conventional neurotoxic insecticides. However, dust formulations require specialized equipment and are difficult to apply, whereas gel and paste formulations contain large amounts of boric acid and tend to be less efficacious than other insecticide baits. The purpose of this study was to evaluate the effectiveness of borate solutions as baits against the German cockroach. Several borate-sugar combinations were evaluated in choice and no-choice assays in the laboratory. Mortality was recorded for 15 d and expressed as lethal time90, the time taken to kill 90% of the cockroaches. Results showed that boric acid was more effective than sodium tetraborate or disodium octaborate tetrahydrate and that aqueous solutions containing mixtures of 0.5-2% boric acid and any of several inexpensive sugars, including fructose, glucose, maltose, and sucrose as a phagostimulant, at molar concentrations of 0.05-1.0, can provide rapid and effective kill of German cockroaches, Blattella germanica (L.).

Animals↗

[Bremen nose ointment--a new boric acid-free nasal ointment].

Drug treatment containing boric acid, has not been permitted with the exception of ophthalmological preparations, since 1.6.1981. Attention is brought to possible complications during treatment with the well-known boric acid containing Wittmaack'sche Nasensalbe. In preparing a new unguent for the nose we took Chlorhexidindiacetat as an antiseptic. The antibacterial and toxicological features of Chlorhexidindiacetat are mentioned. Different therapeutical possibilities of this new nose unguent are listed.

Animals↗

Boric acid-phenolic relationships within the Pinus echinata-Pisolithus tinctorius ectomycorrhizal association.

At germination, container-grown shortleaf pine seedlings were inoculated with Pisolithus tinctorius (Pers.) Coker & Couch or left uninoculated, and both groups were fertilized semiweekly with a modified Hoagland's solution supplemented with 0 or 0.4 mM boric acid. After 12, 16 and 24 weeks, seedling root tissue was analyzed for ectomycorrhizal colonization, phenolic concentration and phenoloxidase activity. In addition, phenoloxidase activity was assayed in P. tinctorius that had been cultured in a liquid medium containing boric acid. Inoculation with P. tinctorius increased the root phenolic concentration of 16- and 24-week-old seedlings, and increased root phenoloxidase activity in 12-, 16- and 24-week-old seedlings. Fertilization with boric acid reduced the phenolic concentration of P. tinctorius ectomycorrhizae after 24 weeks. Although boric acid fertilization did not affect the phenoloxidase activity of 12-, 16- and 24-week-old inoculated roots, or that of 16- and 24-week-old uninoculated roots, it increased the phenoloxidase activity of P. tinctorius grown in vitro and 12-week-old uninoculated roots. We conclude that boric acid fertilization influences the phenolic relations of the shortleaf pine-P. tinctorius ectomycorrhizal association, possibly through a boric acid-induced increase in phenoloxidase activity.

Journal Article↗

[The determination of anions of very weak acids by incompletely suppressed conductometric detection].

A novel method, incompletely suppressed conductometric detection, has been developed for the determination of anions of very weak acids. The principle of the method is discussed. The advantages of the method over the suppressed and nonsupressed methods for the determination of anions of very weak acids are also discussed theoretically. Results showed that the detection limits of the method for arsenous acid and boric acid were lower than those of nonsuppressed conductometric method. Being compared with suppressed conductometric method, the sensitivity was improved greatly. For 250 mg/L boric acid, 261- and 1002-fold increases in peak height and peak area were obtained, respectively. Within the linear range of the detection, the linear correlation coefficients of the peak areas of two weak acids were 0.9991 and 0.9985, respectively.

Anions↗

Cellular changes in boric acid-treated DU-145 prostate cancer cells.

Epidemiological, animal, and cell culture studies have identified boron as a chemopreventative agent in prostate cancer. The present objective was to identify boron-induced changes in the DU-145 human prostate cancer cell line. We show that prolonged exposure to pharmacologically-relevant levels of boric acid, the naturally occurring form of boron circulating in human plasma, induces the following morphological changes in cells: increases in granularity and intracellular vesicle content, enhanced cell spreading and decreased cell volume. Documented increases in beta-galactosidase activity suggest that boric acid induces conversion to a senescent-like cellular phenotype. Boric acid also causes a dose-dependent reduction in cyclins A-E, as well as MAPK proteins, suggesting their contribution to proliferative inhibition. Furthermore, treated cells display reduced adhesion, migration and invasion potential, along with F-actin changes indicative of reduced metastatic potential. Finally, the observation of media acidosis in treated cells correlated with an accumulation of lysosome-associated membrane protein type 2 (LAMP-2)-negative acidic compartments. The challenge of future studies will be to identify the underlying mechanism responsible for the observed cellular responses to this natural blood constituent.

Boric Acids↗

Unidimensional thin-layer chromatography of phospholipids on boric acid-impregnated plates.

A unidimensional thin-layer chromatography system for the separation of phospholipids has been developed. The method employs precoated plates impregnated with boric acid and is capable of resolving eight phospholipid standards, including phosphatidylinositol, phosphatidylserine, and phosphatidylglycerol. Liver, kidney, and platelet phospholipids of the rat were resolved into six major classes using this method. Each was judged to be pure by two-dimensional thin-layer chromatography. The use of boric acid thin-layer chromatography for the separation of phospholipids should find wide application.

Animals↗

[Treatment of trophic ulcers of lower extremities by use of boric acid-hydrocortisone mixture].

Cryostabilized boric-hydrocortisone aquaeous mixture was used in combined treatment of varicose trophic ulcers complicated by eczema and dermatitis in 70 patients. The gauze bandages, moistened by this mixture were used locality in preoperation period. In carrying out cutaneous plastic operation a free graft was preliminarily kept in the mixture for 5-7 min. During postoperation days the bandages were applied daily up to complete healing of the cutaneous flap, only upper layers of the bandage being changed. After the patient was discharged from the hospital the courses of boric-hydrocortisone applications were repeated 3-4 times for the first year. Bacterio-cytolodical examinations were carried out. The effectiveness of the use of the mixture was determined manifested by reduction of the duration of preoperative preparation and by improvement of longterm results.

Administration, Topical↗

11B magnetic resonance imaging and MAS spectroscopy of trimethylborate-treated radiata pine wood.

Boron-11 nuclear magnetic resonance imaging and spectroscopy have been used to characterise the nature and distribution of boron compounds after preservative treatment of radiata pine wood with trimethylborate (TMB). One day after treatment, 11B magnetic resonance imaging microscopy showed significant differences in the morphological distribution of boron species, with there apparently being no treatment penetration of the latewood. 11B MAS NMR spectroscopy of freshly preservative-treated radiata pine wood, which had been separated into latewood and earlywood, showed the only boron species present in the latewood to be boric acid while in the earlywood both TMB and boric acid were initially present. Due to quadrupolar broadening and a short T2 value, the boric acid signal relaxed too quickly to be observable and this caused the apparent lack of 11B in the image when only boric acid was present. TMB undergoes hydrolysis to form boric acid and in radiata pine latewood, this hydrolysis reaction is rapid.

Borates↗

Systemic reactions to topically applied drugs.

Topical drugs can be absorbed percutaneously in sufficient amounts to cause untoward systemic effects. Generally speaking, infants and young children appears to be more vulnerable than adults. It has been shown that the prolonged and extensive use of topical corticosteroids can induce iatrogenic hypercorticism and that they may also impair the patients ability to cope with stress. Furthermore, the relatively limited use, areawise and timewise, of agents such as phenol, resorcinol, salicylic acid, hexachlorophene, boric acid, mercurials, and podophyllin may suffice to elicit dire systemic reactions.

Administration, Topical↗

The preservation of urine samples for determination of renal stone risk factors.

A preservation technique for urine specimens before determination of stone risk factors was evaluated. The purpose of these experiments was to prove the effectiveness of the preservatives used to prevent changes in the concentrations of those constituents measured. Measured concentrations in fresh specimens were compared with those in the same specimens after storage with the preservatives. Refrigeration at 4 degrees C up to five days was appropriate in a laboratory setting, as no significant changes in urinary concentrations occurred. Refrigeration, however, did not offer a convenient method for shipping. Chemical preservation was found to be an effective alternative to refrigeration. Thymol prevented changes in concentration of pH, citrate, uric acid, sulfate, sodium, potassium, and cyclic AMP, while a mixture of hydrochloric (HCl) acid and boric acid prevented changes in calcium, magnesium, phosphorus, oxalate, ammonium, and creatinine. Thus, the addition of thymol or HCl/boric acid to urine specimens will prevent significant changes in the concentrations of stone risk factors.

Boric Acids↗

Defects in cervical vertebrae in boric acid-exposed rat embryos are associated with anterior shifts of hox gene expression domains.

BACKGROUND: Previously, we showed that prenatal exposure to boric acid (BA), an industrial agent with large production, causes alterations of the axial skeleton in rat embryos, reminiscent of homeotic transformations. Indeed, Sprague-Dawley rats exposed in utero to BA on gestation day 9 (GD 9) had only six, rather than the normal seven, cervical vertebrae. This finding, observed in 91% of GD 21 fetuses, suggests posterior transformations of vertebrae. The present study attempts to determine if these skeletal alterations could be explained by modifications of the hox code, involved in the establishment of positional information along the craniocaudal axis of the embryo. METHODS: Pregnant rats were treated by gavage with BA (500 mg/kg, twice) on GD 9. Embryos were collected on GD 11 or GD 13.5 and processed for in situ hybridization. Several hox genes were selected according to the position of their cranial limit of expression in the cervical and thoracic region. RESULTS: At GD 13.5, we detected a cranial shift of the anterior limit of expression of hoxc6 and hoxa6. We observed no difference between control and treated embryos in the location of the cranial limit of expression of the other genes: hoxd4, hoxa4, hoxc5, and hoxa5. CONCLUSIONS: Our results demonstrate that following in utero exposure to BA on GD 9, a disturbance of the expression of hox genes involved inthe specification of most anterior vertebrae is observed at GD 13.5. Based on their expression domain and on their implication in the definition of the cervicothoracic vertebral boundary, it is likely that the anteriorization of hoxc6 and hoxa6 reported here is correlated to the morphological phenotype observed in BA-exposed fetuses at GD 21.

Animals↗

Separation of the high-ceiling diuretic Torasemide and its metabolites by capillary zone electrophoresis with diode-array detection.

A capillary zone electrophoretic method was developed for the separation of the high-ceiling loop diuretic Torasemide and three of its metabolites (M1, M3 and M5) using an experimental design approach. Two different experimental designs were employed to optimize the developed method: (i) a fractional factorial design examining six factors at two levels (2(6-2)) and (ii) a central composite design examining two factors at two levels (2(2)+2x2+p). The factors studied were: pH, buffer concentration, proportion of boric acid in the mixed boric acid:potassium dihydrogen phosphate background electrolyte, temperature, applied voltage and percentage of organic modifier. Resolution between peaks was established as response. Separation of the four studied compounds was achieved in less than 8 min, using an electrolyte of 20 mM boric acid:potassium dihydrogen phosphate (75:25 v/v) with 15% MeOH adjusted to pH 9.7 with KOH, at a potential of 28 kV. Detection wavelength and temperature were 206 nm and 35 degrees C, respectively.

Diuretics↗

Reversible inhibitors of penicillinases.

Reversible competitive inhibitors of a penicillinase, beta-lactamase 1 from Bacillus cereus, were studied. These represent the first inhibitors of a penicillinase that lack the beta-lactam ring. The products of the enzymic reaction, namely penicilloic acids, are inhibitors; their decarboxylation products, the penilloic acids, are also inhibitors, and have somewhat lower Ki values. Inhibitors have been prepared from benzylpenicillin, phenoxymethyl-penicillin, methicillin (2,6-dimethoxybenzamidopenicillanic acid) and 3-hydroxy-4-nitrobenzamidopenicillanic acid. Decarboxylation of the penicilloic acids from benzyl-penicillin, or from phenoxymethylpenicillin, leads to epimerization (at C-5) of the penilloic acid. Nuclear-magnetic resonance spectroscopy at a frequency of 270 MHz can distinguish the epimers. Other competitive inhibitors studied were boric acid, benzene boronic acid and m-aminobenzeneboronic acid. Boric acid itself was the best inhibitor of beta-lactamase I so far found.

Bacillus cereus↗

Boron supplementation inhibits the growth and local expression of IGF-1 in human prostate adenocarcinoma (LNCaP) tumors in nude mice.

Prostate-specific antigen (PSA) is a serine protease and one of the most abundant proteins secreted by the human prostate epithelium. PSA is used as a well-established marker of prostate cancer. The involvement of PSA in several early events leading to the development of malignant prostate tumors has made it a target for prevention and intervention. It is thought that PSA cleaves insulin-like growth factor binding protein-3 (IGFBP-3), providing increased local levels of IGF-1, leading to tumor growth. Separately, there are data that suggest an enzymatic regulatory role for dietary boron, which is a serine protease inhibitor. In this study we have addressed the use of boric acid as a PSA inhibitor in an animal study. We have previously reported that low concentrations (6 ug/mL) of boric acid can partially inhibit the proteolytic activity of purified PSA towards a synthetic fluorogenic substrate. Also, by Western blot we have followed the degradation of fibronectin by enzymatically active PSA and have found significant inhibition in the presence of boric acid. We proposed that dietary supplementation with boric acid would inhibit PSA and reduce the development and proliferation of prostate carcinomas in an animal model. We tested this hypothesis using nude mice implanted subcutaneously with LNCaP cells in Matrigel. Two groups (10 animals/group) were dosed with boric acid solutions (1.7, 9.0 mgB/kg/day) by gavage. Control group received only water. Tumor sizes were measured weekly for 8 weeks. Serum PSA and IGF-1 levels were determined at terminal sacrifice. The size of tumors was decreased in mice exposed to the low and high dose of boric acid by 38% and 25%, respectively. Serum PSA levels decreased by 88.6% and 86.4%, respectively, as compared to the control group. There were morphological differences between the tumors in control and boron-dosed animals, including a significantly lower incidence of mitotic figures in the boron-supplemented groups. Circulating IGF-1 levels were not different among groups, though expression of IGF-1 in the tumors was markedly reduced by boron treatment, which we have shown by immunohistochemistry. These data indicate that low-level dietary boron supplementation reduced tumor size and content of a tumor trophic factor, IGF-1. This promising model is being evaluated in further studies.

Adenocarcinoma↗

Effects of moisture on the toxicity of inorganic and organic insecticidal dust formulations to German cockroaches (Blattodea: Blattellidae).

Toxicity of boric acid (40-99% [AI]), silica gel, eugenol, and deltamethrin dust formulations to adult male German cockroaches, Blattella germanica (L.), was evaluated at five different relative humidities ranging from 0 to 100% and in the presence of 0 to 1 ml of water. Victor boric acid dust was generally the most toxic boric acid formulation at all relative humidities, despite having the lowest percentage (40%) of boric acid; however, this was the only formulation to have sucrose and other edible ingredients. There was no consistent effect of relative humidity on dust toxicity; LT50 values of Roach Prufe (98% boric acid), Victor, and Drione (silica gel and synergized pyrethrins) increased significantly linearly with relative humidity, whereas other formulations were unaffected. The LT50 values of all boric acid-based dust formulations declined exponentially when wetted with increasing volumes of water. Water did not affect the toxicity of deltamethrin and eugenol dusts, but it caused a linear decline in toxicity of silica gel (Dri-Die). The toxicity of a formulation containing silica gel and synergized pyrethrins (Drione) increased exponentially with increasing amounts of water. Moisture in the form of relative humidity does not strongly affect the toxicity of most insecticidal dust formulations. Presence of water, however, increases the toxicity of boric acid dusts and Drione. Toxicity of the hydrophobic deltamethrin (DeltaDust) and eugenol (EcoPCO D) dusts were unaffected by water.

Animals↗