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.     

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.     

隧道式中药材干燥机

通过对我国中药材干燥现状及主要问题的分析，阐述了一种能应用于广大农村地区的隧道式中药材干燥机。着重讨论了电加热器、隧道和物料小车的设计问题，确定了合理的结构参数。性能试验表明，该机适用于各类中药材的干燥作业。     

现代超细粉碎技术在刺五加生产中的应用

阐述了现代超细粉碎技术基本原理及特点及其在刺五加生产中的应用,论述了在相同压力不同转速下和压缩空气压力以及破碎次数对粒度分布特性的影响。通过实验数据分析得出以下结论:破碎粒度随着压力的增大而减小,但当压力增大到一定值时,破碎粒度反而增大;随着转速的增大,破碎粒度变小;随着破碎次数的增加,粒度分布范围变窄,随后又变宽。     

多酸化合物的药学应用进展

介绍了多金属氧酸盐化学的发展过程,综述了多酸化合物的药学应用进展,包括其在抗艾滋病（HIV）、抗肿瘤、抗病毒等方面的研究情况.同时,展望了未来多酸药学应用研究的主要领域及亟需解决的关键问题.     

中草药生态信息管理系统的分析与设计

以Visual Studio．net为开发平台,SQL Server2000为后台数据库进行设计与开发,实现对中草药资源信息进行数据分析和监测预警。系统不但可改进传统的管理方法,而且还可提高种植专业化水平,并为中草药资源可持续发展提供决策依据。     

黄芩超微饮片的HPLC指纹图谱研究

为了研究黄芩超微饮片的指纹图谱。采用色谱柱为大连依利特公司产品HypersilBDSC18(4.6mm×200mm,5μm)。流动相为甲醇-0.1%磷酸水溶液(45:55),柱温为25℃,流速为1.0mL·min-1,检测波长为280nm,进样量为10μL。初步建立了黄芩超微饮片的HPLC指纹图谱,标定了6个共有指纹峰。研究表明,利用黄芩超微饮片HPLC指纹图谱可以较好地反映黄芩超微饮片的内在质量。     

Direct characterisation of phenolic antioxidants in infusions from four Mapuche medicinal plants by liquid chromatography with diode array detection (HPLC-DAD) and electrospray ionisation tandem mass spectrometry (HPLC-ESI-MS)

A simple, fast and direct method was developed for the qualitative analysis of phenolic constituents from infusions of Mapuche medicinal plants. Teas made of Linum chamissonis Schiede, Quinchamalium chilensis Mol., Adesmia emarginata Clos. and Escallonia illinita K. Presl. were analysed by high-performance liquid chromatography with diode array detector (HPLC-DAD) and electrospray mass spectrometry (ESI-MS). This technique allowed for the first time the tentative identification of 16 phenolic compounds in E. illinita, 27 in Q. chilensis, 10 in L. chamissonis and 19 in A. emarginata. The compounds were mainly phenolic acids, flavonoid glycosides, anthocyanins and tannins. The total phenolic and flavonoid content of the infusions was assessed as well as the free radical scavenging capacity measured by the bleaching of a solution of the 2,2-diphenyl-1-picrylhydrazyl (DPPH⁻) radical. From the four species, Q. chilensis exhibited the strongest antioxidant activity with highest total phenolic and flavonoid content.