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At least 343 records · Page 19Linked to original sources
PubMed2003

Calenzanane sesquiterpenes from the red seaweed Laurencia microcladia from the Bay of Calenzana, Elba Island: acid-catalyzed stereospecific conversion of calenzanol into indene- and guaiazulene-type sesquiterpenes.

It is shown here that calenzanane sesquiterpenes (1 and 6) can be isolated from organic extracts from the red seaweed Laurencia microcladia Kützing from the Bay of Calenzana, Elba Island, provided contact with acidic media is minimized. Such contact induces rearrangements of 1 in dry solvents to indene-type 5 and the blue-colored guaiazulenium-type ion 17, via spectrometrically (NMR) characterized indene-type transient intermediates 10, 14, and 12. Addition of NEt(3) to the reaction mixture at appropriate stages allowed the isolation of 12 (and 8 on workup on SiO(2)), and guaiazulene (18). Prolonged contact with silica gel led to complete degradation of 1, giving calenzanane-type epimeric enones 20 a/20 b as well as indene-type epimeric carbinols 22 a/22 b and fulvene 7. The latter was also formed during silica-gel flash chromatography of the algal extracts. A unifying mechanistic view of these branching and cascade transformations may have both heuristic value, suggesting possible artefact origin of azulenoids, and synthetic applications.

Azulenes↗
PubMed2001

Absolute stereochemistry of guaianolides, of matricin and its epimers, of yarrow proazulenes, and of chamazulene carboxylic acid.

Known determinations of the absolute configuration of guaianolides were collected and found to be few. The absolute configurations of guaianolides rest on the assumption that 7-H always has alpha-orientation. For matricin, only the relative configuration was determined. On the basis of a detailed study of the NMR spectra of matricin and its epimers, and of synthetic, NMR, and CD studies with its decomposition product, chamazulene carboxylic acid, we were able to reconfirm the accepted 3S,3aR,4S,9R,9aS,9bS configuration of matricin.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1998

Azulenyl nitrone spin traps protect against MPTP neurotoxicity.

Azulenyl nitrones are a unique class of free radical spin-trapping compounds. We administered both a water-soluble and a lipid-soluble azulenyl nitrone to mice prior to administration of MPTP. Both compounds produced significant neuroprotection against depletions of dopamine and its metabolites measured 1 week after MPTP administration. There were no effects on MPP+ levels. These findings provide further evidence that free radical scavengers can produce significant neuroprotection against MPTP neurotoxicity.

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine↗
PubMed1996

Therapeutic effect of egualen sodium (KT1-32), a new antiulcer agent, on chronic gastritis induced by sodium taurocholate in rats.

We investigated the therapeutic effects of egualen sodium (KT1-32), a new antiulcer agent, on chronic erosive and atrophic gastritis induced by 5 months' administration of sodium taurocholate (TCA; 5 mM) in rats. The chronic gastritis was manifested by mucosal surface injuries (erosions), reduced mucosal thickness, reduction of the number of parietal cells, infiltration of inflammatory cells, and proliferation of collagenous fiber. Egualen sodium, (10-100 mg/kg, t.i.d.) administered orally to the rats for 2 weeks after the withdrawal of TCA, dose-dependently and significantly decreased the total length of erosions. The indicators of atrophic gastritis, i.e., reduced mucosal thickness and reduction in the number of parietal cells, were improved dose-dependently by the administration of this agent. Egualen sodium also reduced the inflammatory cell infiltration and the proliferation of collagenous fiber in the gastric mucosa in a dose-dependent manner. The reduced staining of neutral gastric mucus was improved by a high dose (100 mg/kg) of egualen sodium. The therapeutic effects of egualen sodium on experimental gastritis were superior to those of sofalcone and sodium guaiazulene 3-sulfonate. These results suggest that egualen sodium may be a promising agent for the treatment of erosive and atrophic gastritis.

Administration, Oral↗
PubMedDate not supplied

Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid.

The aim of this study was to determine the bioavailability of a novel oxazolidinone, DRF-6196, in mice and rats following intravenous (i.v) and oral dosing and to compare the pharmacokinetics with those obtained following linezolid dosing. Blood samples were drawn at predetermined intervals up to 24 h post-dose after either DRF-6196 or linezolid administration. The concentrations of DRF-6196 and linezolid in various plasma samples were determined by a HPLC method. Following oral administration maximum concentrations of DRF-6196 were achieved within 0.5 h irrespective of the species. While the doses increased in the ratio of 1 : 3 : 10, mean Cmax and AUC(0-infinity) values in mice for DRF-6196 increased in the ratio of 1 : 3.87 : 8.53 and 1 : 2.51 : 9.24, respectively. Both the Cmax and AUC(0-infinity) values increased almost proportional to the dose administered in mice. Following i.v administration, the concentration of DRF-6196 declined in a bi-exponential fashion with terminal elimination half-life of 1.5 h irrespective of the species. The systemic clearance and volume of distribution of DRF-6196 in mice were 1.14 L/h/kg and 0.66 L/kg, respectively after i.v administration, while the respective values in rats were 0.61 L/h/kg and 0.41L/kg, respectively. Elimination half-life ranged between 0.8-1.5 h. Absolute oral bioavailability of DRF-6196 was found to be 80-96% across the test dose range. Although plasma levels of DRF-6196 were lesser compared to linezolid in the initial hours, it may not have any consequences on the clinical effectiveness of the molecule.

Acetamides↗
PubMed2002

Intraindividual comparison of two different skin care conceptions in patients undergoing radiotherapy of the head-and-neck region. Creme or powder?

OBJECTIVES: This study evaluated for the first time in intraindividual comparison the conception of care with creme or powder. Acute skin reactions on the left and right side of the neck during symmetrically performed radiotherapy and subjective impairment were assessed. PATIENTS AND METHODS: Twelve patients receiving radiotherapy of the head-and-neck region up to 50, 60, 66 and 72 Gy, respectively, were asked to treat one side of the neck with creme, the contralateral side with powder after random assignment. Objective and subjective assessment and photodocumentation were performed at therapy onset and weekly during therapy. The photodocumentation provides an impressive course of acute skin reactions under these care concepts. RESULTS: Altogether we saw no relevant difference in favor of care with creme or powder according to objective as well as subjective assessment criteria (Figure 2 and 3). In this intraindividual comparison the results are independent from interindividual different sensitivity to radiotherapy, total dose or fractionation. Therefore the small patient number is a minor limitation for evidence. Our results are in accordance to trials comparing other care concepts. CONCLUSIONS: A relevant effect concerning onset and degree of acute skin reactions or differences in symptom relief could not be demonstrated. Both conceptions are to be regarded equal in terms of subjective symptom relief and in extent of acute skin reactions. The lack of differences may be explained by the fact that the underlying pathophysiological processes cannot be influenced by topical agents.

Adult↗
PubMed2003

Moist skin care can diminish acute radiation-induced skin toxicity.

BACKGROUND: Radiation treatment may induce acute skin reactions. There are several methods of managing them. Validity of these methods, however, is not sufficiently studied. We therefore investigated, whether moist skin care with 3% urea lotion will reduce acute radiation skin toxicity. PATIENTS AND METHODS: 88 patients with carcinomas of the head and neck undergoing radiotherapy with curative intent (mean total dose 60 Gy, range: 50-74 Gy) were evaluated weekly for acute skin reactions according to the RTOG-CTC score. In 63 patients, moist skin care with 3% urea lotion was performed. The control group consisted of 25 patients receiving conventional dry skin care. The incidence of grade I, II, and III reactions and the radiation dose at occurrence of a particular reaction were determined and statistically analyzed using the log-rank test. The dose-time relations of individual skin reactions are described. RESULTS: At some point of time during radiotherapy, all patients suffered from acute skin reactions grade I, > 90% from grade II reactions. 50% of patients receiving moist skin care experienced grade I reactions at 26 Gy as compared to 22 Gy in control patients (p = 0.03). Grade II reactions occurred at 51 Gy versus 34 Gy (p = 0.006). Further, 22% of the patients treated with moist skin care suffered from acute skin toxicity grade III as compared to 56% of the controls (p = 0.0007). CONCLUSION: Moist skin care with 3% urea lotion delays the occurrence and reduces the grade of acute skin reactions in percutaneously irradiated patients with head and neck tumors.

Amifostine↗
PubMed1991

Management of oral mucositis during local radiation and systemic chemotherapy: a study of 98 patients.

Oral mucositis is among the complications of head and neck irradiation and systemic chemotherapy. To determine whether or not mucositis could be prevented or reduced in intensity by using Kamillosan Liquidum as an oral rinse, 98 patients were placed on study protocols. Twenty patients who were treated with radiation therapy and 46 patients who received systemic chemotherapy participated in prophylactic oral care with Kamillosan oral rinse. Thirty-two patients were treated therapeutically after mucositis had developed. Sixteen patients receiving chemotherapy were treated therapeutically and prophylactically with Kamillosan oral rinse during repeated cycles of chemotherapy. Only one of the 20 patients who had had radiation therapy developed grade 3 mucositis in the final week of treatment. Thirty-six of the 46 patients undergoing chemotherapy did not develop clinically noticeable mucositis. It appears that resolution of mucositis is accelerated by Kamillosan rinse. Prophylactic oral care appeared to modify the oral environment favorably and maintain tissue integrity.

Adult↗
PubMed2004

A facile synthesis of 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, a selective 15-lipoxygenase inhibitor.

A facile method to synthesize 1-ethoxy-4-cyano-5-ethoxycarbonyl-3H-azuleno[1,2-c]pyran-3-one, in yield of 92%, which showed selective inhibition effect on 15-lipoxygenase(soybean source) at IC(50)=24.2+/-2.7 microM while no inhibition effect was observed at greater than 300 microM on 5-lipoxygenase, lipid peroxidase, phospholipase A(2), protein kinase C, and cyclooxygenase.

Animals↗
PubMed2005

Preparative isolation and purification of rupestonic acid from the Chinese medicinal plant Artemisia rupestris L. by high-speed counter-current chromatography.

Rupestonic acid was purified for the first time by high-speed counter-current chromatography from a dichloromethane extract of the traditional Chinese medicinal plant Artemisia rupestris L. The separation was performed in two steps with a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (6:4:3.5:6.5, v/v) with 0.5% acetic acid in stationary-phase. From 200 mg of the crude extract, 27.9 mg of rupestonic acid was obtained at over 98% purity as determined by HPLC analysis, and its chemical structure was confirmed by MS, 1H and 13C nuclear magnetic resonance.

Artemisia↗
PubMed2006

Comprehensive two-dimensional gas chromatography coupled to time-of-flight mass spectrometry in the identification of organic compounds in atmospheric aerosols from coniferous forest.

Comprehensive two-dimensional gas chromatography coupled to time-of-flight mass spectrometry (GC x GC-TOF-MS) was applied in the identification of organic compounds in atmospheric aerosols from coniferous forest. The samples were collected at Hyytiälä, Finland, as part of the QUEST campaign, in Spring 2003. Manual and automated search procedures were compared in the identification. An automated procedure is preferable when a large number of data files need to be processed; but manual search was more accurate with the present samples, where the number of compounds was large and most of the compounds of interest were present at trace level. Altogether, about 50 compounds were identified on the basis of mass spectra and linear retention indices. The identified compounds included oxidised monoterpenes, acyclic alkanes, alkenes, ketones and aldehydes, as well as a few alcohols, acids, and aromatic compounds.

Aerosols↗
PubMed2006

Determination of chamazulene carboxylic acid in serum by high-performance liquid chromatography. Development and validation.

A new, simple and sensitive high-performance liquid chromatographic (HPLC) method was developed for the determination of chamazulene carboxylic acid (CCA) in serum. The technique is based on a single liquid-liquid extraction of the substance using ibuprofen as internal standard (I.S.). The separation was achieved on a C(18) reversed-phase column using acetonitrile/water (4:6, pH 3) as mobile phase. The effluent was monitored at 221 and 286 nm. The calibration curves were linear over the concentration range of 0.1-30 microg/ml. The intra- and inter-day RSDs were in all cases less than 15 and 11%, respectively. The limit of quantitation was 0.1 microg/ml. The assay was developed and validated to be applied in a pharmacokinetic study in healthy volunteers.

Azulenes↗