Note of Caution for the Aqueous Behaviour of Metal-Based Drug Candidates

Poor aqueous solubility is one of the recurrent drawbacks of many compounds in medicinal chemistry. To overcome this limitation, the dilution of drug candidates from stock solutions of an organic solvent is common practice. However, the precise characterisation of these compounds in aqueous solutions is often neglected, leading to some uncertainties regarding the nature of the actual active species. In this communication, we demonstrate that two ruthenium complexes previously reported by our group for their chemotherapeutic potential against cancer, namely [Ru(DIP)₂(sq)](PF₆) and [Ru(DIP)₂(3-methoxysq)](PF₆), where DIP is 4,7-diphenyl-1,10-phenanthroline, sq=semiquinonate and 3-methoxysq=3-methoxysemiquinonate, form colloids in water-DMSO (1 % v/v) mixtures that are invisible to the naked eyes. [Ru(DIP)₂(3-methoxysq)](PF₆) was found to form a highly stable and monodispersed colloid with nanoaggregates of ∼25 nm. In contrast, [Ru(DIP)₂(sq)](PF₆) was found to form large reticulates of mostly spherical aggregates which size was found to increase over time. The difference in size and shape distribution of drug candidates is of tremendous significance as the study of their biological activity might be severely affected. Overall, we strongly believe that these observations should be taken into account by the scientific community working on the development of metal-based drugs with poor water solubility.     

关于新疆热电厂职业危害分析与讨论

对比不同热电厂企业工人接触职业危害因素情况,分析原因,为在建或已建热电厂提供职业危害因素预防措施,降低企业由于设计、施工或管理方面原因造成后期运行过程中职业危害接触超标情况的发生。根据我室历年对新疆地区热电厂职业危害因素检测结果与评价报告的比较,找出不同热电厂职业病危害因素的共性及异性,分析不同设备、工艺及管理方式不同所造成职业危害因素检测结果的差异及原因。建议优化厂区工艺及土建设计;优化设备选型及原料选择运用现代化的管理手段,加强职业卫生管理体系宣贯的有效运作。     

N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains

Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC₅₀ value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity.     

A new monitoring system for piping systems in fossil fired power plants

A CEC-funded project has been performed to tackle the problem of producing an advanced Life Monitoring System (LMS) which would calculate the creep and fatigue damage experienced by high temperature pipework components. Four areas were identified where existing Life Monitoring System technology could be improved:

1. 1. the inclusion of creep relaxation

2. 2. the inclusion of external loads on components

3. 3. a more accurate method of calculating thermal stresses due to temperature transients

4. 4. the inclusion of high cycle fatigue terms.

The creep relaxation problem was solved using stress reduction factors in an analytical in-elastic stress calculation. The stress reduction factors were produced for a number of common geometries and materials by means of non-linear finite element analysis. External loads were catered for by producing influence coefficients from in-elastic analysis of the particular piping system and using them to calculate bending moments at critical positions on the pipework from load and displacement measurements made at the convenient points at the pipework. The thermal stress problem was solved by producing a completely new solution based on Green's Function and Fast Fourier transforms. This allowed the thermal stress in a complex component to be calculated from simple non-intrusive thermocouple measurements made on the outside of the component. The high-cycle fatigue problem was dealt with precalculating the fatigue damage associated with standard transients and adding this damage to cumulative total when a transient occurred.

The site testing provided good practical experience and showed up problems which would not otherwise have been detected.     

An adaptive tracking problem for a family of retarded time-delay plants

Most of the existing switching control techniques are developed specifically for finite-dimensional linear time-invariant (LTI) systems. In many practical applications, however, it is essential to take time delay into consideration in the modelling as the control system can be highly sensitive to delay. In this paper, a multi-model switching control algorithm is proposed for retarded time-delay systems. It is assumed that the plant is represented by a family of known multi-input multi-output, observable, LTI models with multiple delays in the states, and that corresponding to each model in the known family, there exists a high-performance finite-dimensional LTI controller. In addition, it is supposed that a bound on the magnitude of the external inputs and disturbances is available. It is then shown that the proposed switching controller can stabilize the uncertain system, and that under some mild conditions, output tracking can be achieved in the given problem setting. Copyright © 2007 John Wiley & Sons, Ltd.     

Mapping nonnative plants using hyperspectral imagery

Nonnative plant species are causing enormous ecological and environmental impacts from local to global scale. Remote sensing images have had mixed success in providing spatial information on land cover characteristics to land managers that increase effective management of invasions into native habitats. However, there has been limited evaluation of the use of hyperspectral data and processing techniques for mapping specific invasive species based on their spectral characteristics. This research evaluated three different methods of processing hyperspectral imagery: minimum noise fraction (MNF), continuum removal, and band ratio indices for mapping iceplant (Carpobrotus edulis) and jubata grass (Cortaderia jubata) in California's coastal habitat. Validation with field sampling data showed high mapping accuracies for all methods for identifying presence or absence of iceplant (97%), with the MNF procedure producing the highest accuracy (55%) when the classes were divided into four different densities of iceplant.     

油库油料计量操作中存在的问题及其解决办法

介绍了油库油料计量中，在油品高度、油品温度和油品密度测量中存在的问题及应遵循的操作规范和注意事项。     

水浴法加温液氧泵

1　故障现象一次 ,我们用KL -1 5型制氧制氮车开机制氮 ,给一只容积为 40升、最高工作压力为1 4 7MPa的气瓶灌充氮气 ,当气瓶充气压力升高到一定值时不再上升。反复开泵 ,压力基本不变。液氧泵停止时 ,出口压力无明显下降。经分析判断导致气瓶压力升高到一定值时不再上升的原因是由于液氧泵被冻结所致。2　排除方法首先关闭液氧泵。拧开制冷机氢气放气阀 ,使压力下降到 1 0MPa。开大放气阀 ,使二级压力保持在 0 3 5MPa左右。调整正流空气调节阀 ,调节好中部温度。关闭液氮进液氧泵阀和气氮出液氧泵阀。戴棉布手套 ,拆开液氮进口接头、…     

浅议如何用绿色植物防治矿区环境污染

绿色植物能吸收CO2 ,释放O2 ,清除有毒污染物 ,阻滞灰尘 ,杀灭细菌等致病微生物 ;在矿区环境污染治理时 ,应切实加强矿区绿化工作 ,扩大植被覆盖率 ,保持矿区生态平衡 ,促进矿区的可持续发展。