Durch Wasserstoffperoxid ausgelöste Ringverengung von Aminohydroxy-hexahydrobenzoxazolcarbonsäureamid zu Amino-cyclopentanspirooxazolinon

A Ring Contraction Induced by Hydrogenperoxide 2-Amino-7a-carbamoyl-3a-hydroxy-3a,4,5,6,7,7a-hexahydro-benzoxazole ( 1 ) and hydrogenperoxide rearrange to 2′-amino-cyclopentanespiro-5′-oxazolin-4′-one ( 5 ). 5 and aniline hydrochloride form the phenylaminoderivative 6 , 5 and 2,5-dichlorophenylhydrazine hydrochloride form the 2,5-dichlorophenylhydrazinederivative 7 . 5 and hydrochloric acid afford cyclopentanespiro-5′-oxazolidin-2′,4′-dione ( 8 ). Hydrolysis of 5 or 8 furnish 1-hydroxy-cyclopentane-carboxylic acid ( 9 ).     

Personalized Nutrition as a Key Contributor to Improving Radiation Response in Breast Cancer

Understanding metabolic and immune regulation inherent to patient populations is key to improving the radiation response for our patients. To date, radiation therapy regimens are prescribed based on tumor type and stage. Patient populations who are noted to have a poor response to radiation such as those of African American descent, those who have obesity or metabolic syndrome, or senior adult oncology patients, should be considered for concurrent therapies with radiation that will improve response. Here, we explore these populations of breast cancer patients, who frequently display radiation resistance and increased mortality rates, and identify the molecular underpinnings that are, in part, responsible for the radiation response and that result in an immune-suppressive tumor microenvironment. The resulting immune phenotype is discussed to understand how antitumor immunity could be improved. Correcting nutrient deficiencies observed in these populations should be considered as a means to improve the therapeutic index of radiation therapy.     

Eilatin Ru(II) complexes display anti-HIV activity and enantiomeric diversity in the binding of RNA

Eilatin-containing octahedral ruthenium complexes inhibit HIV-1 replication in CD4+ HeLa cells and in human peripheral blood monocytes with IC(50) values of approximately 1 microM. Similar metal complexes that lack eilatin display 15-100-fold lower anti-HIV activities. [Ru(bpy)(2)"pre-eilatin"](2+), a complex that contains a nonplanar analogue of eilatin, shows significantly lower nucleic acid binding and lower anti-HIV activity than eilatin complexes. This result indicates that the extended planar surface presented by eilatin is important for both activities. Rev peptide and ethidium bromide displacement assays are used to probe the nucleic acid affinity and specificity of Lambda- and Delta-[Ru(bpy)(2)eilatin](2+). Two HIV-1 RNA sites are compared and a significant binding preference for the Rev response element over the transactivation response region is found. Simple DNA duplexes show a consistent selectivity for Lambda-[Ru(bpy)(2)eilatin](2+) compared to Delta-[Ru(bpy)(2)eilatin](2+), while RNAs show more diverse enantiomeric selectivities.     

Verbal and nonverbal short-term memory impairment in untreated Parkinson's disease.

Extended previous research (J. A. Cooper et al, 1991) and examined whether the impairment in verbal and nonverbal short-term memory (STM) documented in chronically treated patients with Parkinson's disease (PD) is attributable to the pathology of the disease or to antiparkinsonian drug therapy. Verbal recall by a group of 58 never-treated PD patients was virtually perfect when the retention intervals were distractor free but was impaired, as compared with a matched group of 34 healthy control Ss, following distractor-filled intervals. Nonverbal recall by the PD group showed significant forgetting after distractor-free but not distractor-filled intervals. Recall was not related to depressive symptoms, motor disability, or distractor task performance. Thus, STM impairment in PD occurs for both verbal and nonverbal material and arises directly from the disease pathology rather than from antiparkinsonian medication. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Far-infrared-solar imaging from a balloon-borne platform

Far-infrared solar imaging with a balloonborne 60 cm-diameter Cassegrain telescope is described and related to previous solar observations in the millimeter range, the ir, vis and uv spectral regions. Solar images have been taken at 50 μm, 80 μm and 200 μm and represented as brightness temperature maps. The spectral windows observed correspond to the transition zone chromosphere-phocosphere of the solar atmosphere with a characteristic temperature minimum. Temperature enhancements of a few 100 K over the temperature of the quiet sun are reported for active solar regions, e.g. plages and sunspot regions. Far-infrared images provide less spatial resolution but more reliable temperature assignements than corresponding white-light, Ca II K and H_α pictures.     

Anaerobic biodegradability of carboxymethyloxysuccinate,a detergent builder

Controlled amounts of C-14 labeled trisodium car-boxymethyloxysuccinate, an experimental detergent builder, were added to a laboratory anaerobic digester system. The daily dosages were increased incrementally from 4 to 20 ppm, dosages being held at each level for 24 days. Biodegradation commenced after 6 days, and once complete acclimation occurred, removals were rapid and complete at all dosage levels, yielding CO₂ and CH₄ as virtually the only end-products of decomposition. After 96 days of application, total removal was in excess of 95%. Further, this com-pound did not interfere with the normal digestion processes or display any inhibitory effects on the bacterial population.     

Response Surface Methodology as an Approach to Optimization of an Oral Solution

Response surface methodology was used to optimize the cloud point and turbidity of a nonionic surfactant solution that had been used to solubilize a very slightly water soluble drug. A formulation suitable for oral administration with turbidity less than four parts per million and cloud point greater than 60°C was desired. A first-order experiment, specifically, a 2⁴ factorial with four center points, was designed to investigate the effect of four formulation components that had been identified as the most likely to affect turbidity and cloud point. When lack-of-fit tests for the first order linear model indicated that a second-order model would provide a better approximation to the response surface in the experimental region, a central composite design with six center points was run in order to fit second-order linear models. Within the experimental region of the second-order design, a simple first-order linear model with the concentration of one component was adequate to describe the cloud point response function; turbidity was fitted with a three component second-order response equation. Experimental runs were performed to confirm the optimum combination of components predicted by the fitted response functions. Response surface methodology provided an efficient approach to development of a nonionic surfactant solution with turbidity less than 4 ppm and cloud point greater than 60°C while maintaining the concentration of formulation ingredients within ranges suitable for oral administration     

Adult marijuana users seeking treatment.

In an effort to study the efficacy of attracting and intervening with adult marijuana users, 290 men and 92 women were screened for participation in a treatment-outcome study focused on marijuana cessation. The well-educated, self-referred sample reported using marijuana on 79 of the past 90 days before testing. Indices of the severity of marijuana abuse and general psychopathology were in the clinical range for a majority of Ss. Ss who did not report evidence of alcohol or other drug abuse (n?=?144) reported less severe consequences of marijuana use and experienced less general psychological distress than Ss who also reported lifetime (n?=?165) or current abuse (n?=?73) of other substances in addition to marijuana. The findings indicate the need for clinical research targeting adults who are dependent on marijuana. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Working and strategic memory deficits in schizophrenia.

Working memory and its contribution to performance on strategic memory tests in schizophrenia were studied. Patients (n?=?18) and control participants (n?=?15), all men, received tests of immediate memory (forward digit span), working memory (listening, computation, and backward digit span), and long-term strategic (free recall, temporal order, and self-ordered pointing) and nonstrategic (recognition) memory. Schizophrenia patients performed worse on all tests. Education, verbal intelligence, and immediate memory capacity did not account for deficits in working memory in schizophrenia patients. Reduced working memory capacity accounted for group differences in strategic memory but not in recognition memory. Working memory impairment may be central to the profile of impaired cognitive performance in schizophrenia and is consistent with hypothesized frontal lobe dysfunction associated with this disease. Additional medial-temporal dysfunction may account for the recognition memory deficit. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Scintillation properties of CsBa2Br5:Eu

In this study, the scintillation properties of Eu²⁺ activated CsBa₂Br₅ are reported. It is an analog of Eu²⁺ doped CsBa₂I₅ scintillator that exhibits excellent scintillation properties. Microcrystalline powder samples of this compound were synthesized by reaction in the molten state of cesium bromide, barium bromide and europium bromide. The concentration of an Eu was varied from 0% to 10%. The luminescence was studied under UV and X-ray excitation. The light output is strongly Eu²⁺ concentration dependent, reaching an estimated maximum of about 92,000 photons/MeV at 2% Eu under X-ray excitation. About 50% of the scintillation light decays in less than 1 μs. CsBa₂Br₅:Eu²⁺ exhibits a complex concentration dependent emission centered around 435 nm.