Palmatine and berberine isolation artifacts

Some 8-substituted derivatives of the protoberberine alkaloids palmatine (1a) and berberine (1b) have been prepared and investigated by 1D and 2D NMR spectroscopy (H-1, C-13, N-15). Complete NMR data for the 8-hydroxy (2), 8-methoxy (3), 8-ethoxy (4), and 8-trichloromethyl (5) 7,8-dihydro derivatives of 1a and 1b, as well as X-ray data for 8-methoxydihydroberberine (3b), 8-trichloromethyldihydropalmatine (5a), and 8-trichloromethyldihydroberberine (5b), are presented. The physicochemical data for all of these compounds are reviewed and compared with previously published values.     

Thyroid abscess at an adolescent age

We report a case of thyroid abscess in a 17-year-old girl. She was presented with swelling and pain in the region of the left thyroid lobe. The diagnosis was confirmed by ultrasonography and fine needle aspiration. After incision, evacuation of the pus and antibiotic treatment manifestations of disease disappeared. Barium swallow did not prove any hypopharyngeal fistula. The girl is now without any problems for 3 years. The patient had infectious mononucleosis 2 months prior development of the thyroid abscess. We contemplate that it may had changed the immunological state that facilitated this rare inflammation.     

Osteochondrome und Exostosen bei bestrahlten Kindern

Zusammenfassung Es werden 4 eigene Beobachtungen von Exostosenbildung an den während des Wachstums bestrahlten Knochen beschrieben und ihr Auftreten in Zusammenhang mit der Strahlenwirkung gebracht; es wird auf die Notwendigkeit aufmerksam gemacht, die Benignität solcher Befunde regelmäßig zu kontrollieren.Mit 4 Textabbildungen     

Evaluation of laser fluorescence for differentiating caries dye-stainable versus caries dye-unstainable dentin in carious lesions

PURPOSE: To assess the performance of laser fluorescence (DIAGNOdent, "DD") for differentiating carious versus non-carious dentin during caries excavation using caries dye as the gold standard. METHODS: The superficial carious dentin surfaces of lesions in 25 teeth were exposed, and the surface evaluated by DD. Next, caries dye was applied and the surface was observed for dye staining. The lesion was then excavated approximately 0.5 mm with a round bur. The resulting surface was evaluated by DD, and the above sequence was repeated until three non-stained surfaces were evaluated by DD. Using "caries dye staining" as the gold standard, correct classification proportion was calculated at each DD cutpoint in the dataset. Using the optimal cutpoint, sensitivity, specificity and likelihood ratios were calculated. Non-parametric ROC analysis was performed and AUC calculated. RESULTS: With an optimal cutpoint of 11 or 12, DD was highly accurate in discriminating between dye-stainable and dye-unstainable surfaces, producing a correct classification proportion of over 98% and an AUC of 0.999 for all 176 surfaces. These results support further refinement of DD for use in caries excavation and further research relating DD to other caries excavation endpoints.     

Surgical treatment of primary hyperparathyroidism in children: report of 10 cases

Primary hyperparathyroidism in children is very rare. It is caused by overproduction of parathormone by a pathologically changed parathyroid gland. We carried out a retrospective study in 10 patients (age 10-17 years) who had surgical treatment between 1996 and 2007. The main signs of primary hyperparathyroidism were urolithiasis, nephrolithiasis, nephrocalcinosis and bone resorption, as well as non-specific signs such as fatigue, torpidness and muscle weakness. Patients were examined using sonography, MIBI-scintigraphy, CT and MRI. Calcium was measured before and after surgery; parathormone was monitored postoperatively. Surgery was curative in nine patients; reoperation was necessary in one patient because an ectopic parathyroid gland was not detected during the primary operation. Other major complications were not observed. Removal of pathologically changed parathyroid glands offers definitive and safe treatment of primary hyperparathyroidism in children. Special care should be taken if an ectopic parathyroid gland is suspected.     

The presence of P-glycoprotein in L1210 cells directly induces down-regulation of cell surface saccharide targets of concanavalin A

Overexpression of P-glycoprotein (P-gp), a plasma membrane drug transporter (ABCB1, a member of the ABC transporter family), is the most prevalent cause of multidrug resistance in cancer tissues. Lectin concanavalin A (ConA) induces massive cell death of L1210 leukemia cells (S). Cell sublines of L1210 in which P-gp overexpression was induced by selection with vincristine (R) or by stable transfection with a plasmid encoding full-length human P-gp (T) were less sensitive to ConA. Both P-gp-positive cell lines exhibited typical P-gp-mediated multidrug resistance. Resistance of R and T cells to ConA was associated with lower binding of ConA as compared to S cells when analysed by the following methods: (i) SDS PAGE and electroblotting of proteins in the crude membrane fraction followed by detection with biotinylated ConA and avidin-peroxidase, and (ii) fluorescent cytometry or confocal microscopy of the intact cells with surfaces labeled by FITC-ConA. These data indicated that the presence of P-glycoprotein in L1210 cells independently of the mode of its expression induced down-regulation of cell surface saccharide targets of ConA. Therefore, this feature may be considered as a secondary cellular response to P-glycoprotein expression.     

Biodistribution and pharmacokinetics of 125I-labeled monoclonal antibody M75 specific for carbonic anhydrase IX,an intrinsic marker of hypoxia,in nude mice xenografted with human colorectal carcinoma

Carbonic anhydrase IX (CA IX) is frequently expressed in human carcinomas and absent from the corresponding normal tissues. Strong induction by tumor hypoxia predisposes CA IX to serve as a target for cancer diagnostics and therapy. Here we evaluated targeting properties and pharmacokinetics of CA IX-specific monoclonal antibody (MAb) M75. Binding parameters of (125)I-labeled M75, including equilibrium dissociation constant, hypoxia-related binding to various cell lines and internalization, were analyzed in vitro. Biodistribution of (125)I-M75 in nude mice bearing HT-29 human colorectal carcinoma xenografts with hypoxic pattern of CA IX expression was studied by measurements of radioactivity in dissected tissues and macroautoradiography of tissue sections. Pharmacokinetics of intravenously administered (125)I-M75 was described using a 2-compartment model. Blood clearance showed a distribution phase t(1/2)(alpha) = 3.4 hr and an elimination phase t(1/2)(beta) = 55.3 hr postinjection. Despite predominant CA IX localization in less accessible perinecrotic regions, (125)I-M75 exhibited specific accumulation in xenograft, with a mean uptake of 15.3 +/- 3.6% of injected dose per gram of tumor tissue at 48 hr postadministration. Specificity of M75 localization was confirmed by low tumor uptake of control antibody. Altogether, our data demonstrate that M75 MAb is a promising tool for selective immunotargeting of hypoxic human tumors that express CA IX.     

Recurrent peripheral arterial embolism from metastatic lung choriocarcinoma--a case report

A patient with choriocarcinoma, most likely of ovarian origin, with lung metastasis is presented. The disease manifested itself by recurrent embolism into the peripheral arteries. Literature on this topic is reviewed.     

Occupational asthma follow-up — which markers are elevated in exhaled breath condensate and plasma?

Objectives

To search for optimal markers in the exhaled breath condensate (EBC), plasma and urine that would reflect the activity/severity of occupational asthma (OA) after the withdrawal from the exposure to the allergen.

Material and Methods

Markers of oxidative stress: 8-iso-prostaglandin {ie206-1} (8-isoprostane, 8-ISO), malondialdehyde (MDA), 4-hydroxy-trans-2-nonenale (HNE), cysteinyl leukotrienes (LT) and LTB₄ were determined using liquid chromatography and mass spectrometry in 43 subjects with immunological OA (49.3±11.8 years), removed from the exposure to the sensitizing agent 10.5±6.5 years ago; and in 20 healthy subjects (49.0±14.9 years). EBC was harvested both before and after the methacholine challenge test. In parallel, identical markers were collected in plasma and urine. The results were analyzed together with forced expiratory volume in one second (FEV₁), blood eosinophils, immunoglobulin E (IgE) and eosinophilic cationic protein (ECP) and statistically evaluated (Spearman rank correlation r_S, two- or one-sample t tests and alternatively Kruskal Wallis or pair Wilcoxon tests).

Results

Several parameters of lung functions were lower in the patients (FEV1% predicted, MEF25% and MEF50%, Rtot%, p < 0.001). Shorter time interval since the removal from the allergen exposure correlated with higher ECP (r_S = 0.375) and lower FEV₁%, MEF25% and MEF50% after methacholine challenge (r_S = ?0.404, ?0.425 and ?0.532, respectively). In the patients, IgE (p < 0.001) and ECP (p = 0.009) was increased compared to controls. In EBC, 8-ISO and cysteinyl LTs were elevated in the asthmatics initially and after the challenge. Initial 8-ISO in plasma correlated negatively with FEV₁ (r_S = ?0.409) and with methacholine PD₂₀ (r_S = ?0.474). 8-ISO in plasma after the challenge correlated with IgE (r_S = 0.396).

Conclusions

The improvement in OA is very slow and objective impairments persist years after removal from the exposure. Cysteinyl LTs and 8-ISO in EBC and 8-ISO in plasma might enrich the spectrum of useful objective tests for the follow-up of OA.     

Chemoprotective effect of plant phenolics against anthracycline-induced toxicity on rat cardiomyocytes. Part II. caffeic, chlorogenic and rosmarinic acids

The chemoprotective effects of caffeic (CA), chlorogenic (CHA) and rosmarinic (RA) acids were tested against the toxicity of doxorubicin (DOX) in neonatal rat cardiomyocytes and the iron-dependent DOX induced lipid peroxidation of heart membranes, mitochondria and microsomes. The protectivity of these acids was compared with dexrazoxan, used as an adjuvant during DOX chemotherapy. The cytoprotective effects were assessed by enzyme (LDH and ASAT) and troponin I leakage, secondly by intracellular ATP content. All hydroxycinnamic acids proved non-cytotoxic, and they stabilized both membranes and the energetic status of cardiomyocytes. After preincubation of cardiomyocytes with the test compounds (100, 200 microm; 1 h) the cardiomyocytes were treated with the toxic agent, DOX (100 microm; 8 h). The test compounds protected cardiomyocytes against DOX induced oxidative stress (RA > CHA > or = CA) on all monitored parameters. Substantial preservation of monolayer integrity of the cardiomyocytes by test compounds was also found microscopically. All the acids were more effective in the assays used than dexrazoxan. RA showed the most effective cytoprotectivity. All the acids significantly reduced the iron-dependent DOX induced lipid peroxidation of heart membranes, although of the test compounds, CHA was found to be the most effective (IC(50) = 8.04 +/- 0.74/6.87 +/- 0.52 micro m for microsomes/mitochondria).