Natural radioactivity in some building materials in Cuba and their contribution to the indoor gamma dose rate

The natural radioactivity of some building materials commonly used in Cuba was measured by gamma spectrometry. Typical concentrations encountered so far encountered are in the ranges: 47-2511 Bq kg(-1) for (40)K; 9-71 Bq kg(-1) for (226)Ra; and 2-38 Bq kg(-1) for (232)Th. The external gamma ray absorbed doses in indoor air and the corresponding effective dose-equivalents in a typical dwelling are presented in this paper.     

<Superscript>1</Superscript>H and <Superscript>13</Superscript>C NMR characterization and stereochemical assignments of bile acids in aqueous media

The unconjugated bile acids cholic acid, deoxycholic acid, and chenodeoxycholic acid; their glycine and taurine conjugated glycocholic acid, glycodeoxycholic acid, glycochenodeoxycholic acid, taurocholic acid, taurodeoxycholic acid, and taurochenodeoxycholic acid; and a taurine conjugated ursodeoxycholic acid, tauroursodeoxycholic acid, were characterized through ¹H and ¹³C NMR in aqueous media under the physiological pH region (7.4±0.1). Assignments of ¹H and ¹³C signals of all the bile acids were made using a combination of several one- and two-dimensional, homonuclear (¹H−¹H) and heteronuclear (¹H−¹³C) correlations as well as spectral editing NMR methods. Stereochemical assignment of the five-membered ring of the bile acids is reported here for the first time. The complete characterization of various bile acids in aqueous media presented here may have implications in the study of the pathophysiology of biliary diseases through human biliary fluids using NMR spectroscopy.     

Synthesis of aromatase inhibitors and dual aromatase steroid sulfatase inhibitors by linking an arylsulfamate motif to 4-(4H-1,2,4-triazol-4-ylamino)benzonitrile: SAR, crystal structures, in vitro and in vivo activities

4-(((4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino)methyl)phenyl sulfamate (6 a) was the first dual aromatase-sulfatase inhibitor (DASI) reported. Several series of its derivatives with various linker systems between the steroid sulfatase (STS) and the aromatase inhibitory pharmacophores were synthesised and evaluated in JEG-3 cells. The X-ray crystal structures of the aromatase inhibitors, DASI precursors 42 d and 60, and DASI 43 h were determined. Nearly all derivatives show improved in vitro aromatase inhibition over 6 a but decreased STS inhibition. The best aromatase inhibitor is 42 e (IC(50)=0.26 nM) and the best DASI is 43 e (IC(50 aromatase)=0.45 nM, IC(50 STS)=1200 nM). SAR for aromatase inhibition shows that compounds containing an alkylene- and thioether-based linker system are more potent than those that are ether-, sulfone-, or sulfonamide-based, and that the length of the linker has a limited effect on aromatase inhibition beyond two methylene units. Compounds 43 d-f were studied in vivo (10 mg kg(-1), single, p.o.). The most potent DASI is 43 e, which inhibited PMSG-induced plasma estradiol levels by 92 % and liver STS activity by 98 % 3 h after dosing. These results further strengthen the concept of designing and developing DASIs for potential treatment of hormone-related cancers.     

Direct spectrophotometric analysis of Cr(VI) using a liquid waveguide capillary cell

Hexavalent chromium Cr(VI) is a notorious ground water contaminant toxic to humans and animals. Assessment of an exposure risk for aquatic receptors necessitates frequent Cr(VI) concentration data from a range of surface and groundwater locations at Cr(VI) contamination sites. In this work, we demonstrate that enhanced ultraviolet-visible (UV-vis) spectroscopy using a liquid waveguide capillary cell (LWCC) offers an easy-to-use and economical methodology for the determination of chromate anion CrO(4)(2-) in Hanford natural waters without chemical pretreatment and generation of hazardous waste. Direct determination of CrO(4)(2-) in actual surface and ground water samples with the complexities of competing ions, dissolved organics, and other potential interfering agents was achieved by measuring the chromate optical absorbance at 372 nm. For a 100 cm path length LWCC, the detection limit for chromate was found to be as low as 0.073 ppb. A quantitative relationship between the intensity of the absorbance signal and water pH allowed for the straightforward calculation of total Cr(VI) content in natural water. The described method is applicable for in-field monitoring of Cr(VI) in environmental water samples at trace levels.     

Structure-activity relationship for the first-in-class clinical steroid sulfatase inhibitor Irosustat (STX64, BN83495)

Structure–activity relationship studies were conducted on Irosustat (STX64, BN83495), the first steroid sulfatase (STS) inhibitor to enter diverse clinical trials for patients with advanced hormone‐dependent cancer. The size of its aliphatic ring was expanded; its sulfamate group was N,N‐dimethylated, relocated to another position and flanked by an adjacent methoxy group; and series of quinolin‐2(1H)‐one and quinoline derivatives of Irosustat were explored. The STS inhibitory activities of the synthesised compounds were assessed in a preparation of JEG‐3 cells. Stepwise enlargement of the aliphatic ring from 7 to 11 members increases potency, although a further increase in ring size is detrimental. The best STS inhibitors in vitro had IC₅₀ values between 0.015 and 0.025 nM . Other modifications made to Irosustat were found to either abolish or significantly weaken its activity. An azomethine adduct of Irosustat with N,N‐dimethylformamide (DMF) was isolated, and crystal structures of Irosustat and this adduct were determined. Docking studies were conducted to explore the potential interactions between compounds and the active site of STS, and suggest a sulfamoyl group transfer to formylglycine 75 during the inactivation mechanism.     

缝编机沉降片间距对缝编力的影响分析

缝编法生产非织造布的主要优势是既可采用高档原料 ,也可采用较充裕和较廉价的纤维原料 ,包括可纺和不可纺的下脚料 ,以及再生纺织原料。纤维底布采用天然纤维和化纤 ,以合纤复丝固结 ,底布耗用量不超过成品非织造布总质量的 30 %。但是缝编机的效率低 ( 0 .4～ 0 .5 ) ,影响了非织造布生产的推广 ,主要原因是固结底布的缝编线断头率高。实际产量经常仅为高速缝编机设计能力的一半 ,因而挡车工的劳动强度高 ,劳动生产率降低 ,设备停台时间长。高断头率还直接影响非织造布的质量 ,由于接头会形成疵点 (小结、漏缺等 ) ,非织造布等级下降。缝…     

Synthesis, Characterization and In vitro Antitumour Activity of Novel Organotin Derivatives of 1,2- and 1,7-Dicarba-Closo-dodecaboranes

Several organotin derivatives of 1,2- and 1,7-dicarba-closo-dodecaboranes were synthesized and characterized by ¹¹⁹Sn Mössbauer, ¹H, ¹³C and ¹¹⁹Sn NMR spectroscopy. Their antitumour activities in vitro against cancerous cell lines of human origin are reported.     

Testing applicability of black poplar (Populus nigra L.) bark to heavy metal air pollution monitoring in urban and industrial regions

A comparative study of the capabilities of black poplar-tree (Populus nigra L.) bark as a biomonitor of atmospheric heavy-metal pollution is reported. Performance indicators (concentrations and enrichment factors) of heavy metal bioaccumulation of bark were compared to the corresponding indicators of epiphytic lichens Xanthoria parietina (L.) Th. Fr. and Physcia adscendens (Fr.) H. Oliver, collected simultaneously with bark samples within the Kiev urban-industrial conurbation. The concentrations of 40 minor and trace elements in the samples were measured by a combination of epithermal and instrumental neutron activation analysis (NAA) using a 10 MW nuclear research reactor WWR-M as the neutron source. Statistical analysis of the data was carried out using non-parametric tests. It was shown that for the majority of the elements determined a good correlation exists between their concentrations in bark and in the lichen species. The accumulation capability of the bark was found to be as effective as, and in some cases better, for both types of lichens. Based on the background levels and variations of the elemental concentration in black poplar-tree bark, threshold values for the enrichment factors were established. For a number of elements (As, Au, Ce, Co, Cr, Cu, La, Mn, Mo, Ni, Sb, Sm, Ti, Th, U, V, W) an interspecies calibration was performed. An optimized pre-irradiation treatment of the bark sample was employed which efficiently separated the most informative external layer from the deeper layers of the bark and thus minimized variations of the element concentrations. Results of this study support black poplar-tree bark as an alternative to epiphytic lichens for heavy metal air pollution monitoring in urban and industrial regions, where severe environmental conditions may result in scarcity or even lack of the indicator species.