Immunostimulants and autoimmunity

The review presents the recent data on the use of immunity stimulants (thymus peptides, synthetic immunomodulators, immunostimulants of bacterial origin) under conditions of experimental autoimmunity and in clinic. A brief characteristic of the immunotropic activity of the drugs is given, the mechanisms of their action on the formation of the autoimmune response and clinical effectiveness are analyzed.     

人工合成麝香酮进展

本文综述近年来采用的麝香酮合成路线、一些重要中间体的合成方法以及光学活性麝香酮合成的研究进展。     

Cannabinoids: the separation of central from peripheral effects on a structural basis.

A brief history of the therapeutic uses and legal problems of cannabis as well as the component cannabinoids is given. This is followed by a discussion of drug development from delta 1-tetrahydrocannabinol and its synthetic analogues. The controversy of whether the pharmacological effects are of central or peripheral origin is included. Then, the potentials for the development of new drugs based on the cannabinoid structure for the treatment of pain, inflammation, and related conditions are outlined. It is concluded that the central activity of cannabinoids is confirmed and that the presence of a C-5 hydroxy group confers potent peripheral activity.     

Synthetic sialic-acid-containing polyvalent antiviral inhibitors

This review gives a brief survey of synthetic inhibitors of influenza virus which have been synthesized to date. It starts with a short introduction which describes the structure and mechanism of action of influenza virus and continues with the main research directions that have been used in order to inhibit the virus. This is followed by discussion of various synthetic materials, including synthesis and antiviral properties, which that have been tested against influenza virus. The most potent inhibitory compounds proved to be polyvalent, because of their high binding affinity and steric stabilization. Finally we conclude with a brief discussion on structural characteristics, a summary, and outlook overview.     

动植物细胞培养生物反应器的研究进展

文章综合介绍了国内外细胞培养生物反应器的研究现状。在此基础上，作者提出了未来动植物细胞培养生物反应器的发展方向。     

An updated review of inhalation studies with cigarette smoke in laboratory animals

Until recently, the published literature on inhalation studies with laboratory animals and cigarette smoke consisted entirely of negative findings, as far as neoplastic disease is concerned. This paper brings readers up to date, with analyses of recent studies that do indeed appear to report success after so many years of failure. The paper consists of a brief analysis of the literature up until a couple of years ago, giving brief, representative examples of inhalation studies with the five main species of laboratory animals that have been used: rat, mouse, hamster, dog, and nonhuman primate. A brief examination of the various technologies used to expose laboratory animals is given, along with an analysis of the histopathology and related toxicology data (specifically, biomarkers of exposure) that have been reported. The paper concludes by briefly mentioning the most recent studies, where positive results have been reported.     

Gene imprinting in developmental toxicology: a possible interface between physiology and pathology

Gene imprinting is an epigenetic mechanism for accomplishing persistent change in gene expression. In this brief paper, we explore the mechanisms for imprinting genes and present data showing that the synthetic estrogen, diethylstilbestrol (DES) can developmentally imprint genes by changing the pattern of DNA methylation. We further discuss the implications of this and other findings for non-mutagenic aspects of developmental toxicology, and suggest ways to use this concept in modifying in vitro screening for developmental toxicants.     

Strong mutagenic effects of diesel engine emissions using vegetable oil as fuel

Diesel engine emissions (DEE) are classified as probably carcinogenic to humans. In recent years every effort was made to reduce DEE and their content of carcinogenic and mutagenic polycyclic aromatic compounds. Since 1995 we observed an appreciable reduction of mutagenicity of DEE driven by reformulated or newly designed fuels in several studies. Recently, the use of rapeseed oil as fuel for diesel engines is rapidly growing among German transportation businesses and agriculture due to economic reasons. We compared the mutagenic effects of DEE from two different batches of rapeseed oil (RSO) with rapeseed methyl ester (RME, biodiesel), natural gas derived synthetic fuel (gas-to-liquid, GTL), and a reference diesel fuel (DF). The test engine was a heavy-duty truck diesel running the European Stationary Cycle. Particulate matter from the exhaust was sampled onto PTFE-coated glass fibre filters and extracted with dichloromethane in a soxhlet apparatus. The gas phase constituents were sampled as condensates. The mutagenicity of the particle extracts and the condensates was tested using the Salmonella typhimurium/mammalian microsome assay with tester strains TA98 and TA100. Compared to DF the two RSO qualities significantly increased the mutagenic effects of the particle extracts by factors of 9.7 up to 59 in tester strain TA98 and of 5.4 up to 22.3 in tester strain TA100, respectively. The condensates of the RSO fuels caused an up to factor 13.5 stronger mutagenicity than the reference fuel. RME extracts had a moderate but significant higher mutagenic response in assays of TA98 with metabolic activation and TA100 without metabolic activation. GTL samples did not differ significantly from DF. In conclusion, the strong increase of mutagenicity using RSO as diesel fuel compared to the reference DF and other fuels causes deep concern on future usage of this biologic resource as a replacement of established diesel fuels.     

马蔺子素研究进展

目的对马蔺子素研究进展进行了综述。为其进一步开发利用提供参考。方法采用回顾性文献分析概括的方法。结果马蔺子素是从鸢尾科（Iridaceae）植物马蔺中提取制成的一种放射增敏剂,具有凉血止血、清热利湿等功效。结论通过分析其提取分离、化学组成、剂型种类及定量分析研究情况,为其开发利用提供科学参考。     

Netnography of Female Use of the Synthetic Growth Hormone CJC-1295: Pulses and Potions

Background. Communal online folk pharmacology fuels the drive for short cuts in attaining muscle enhancement, fat loss, and youthful skin. Objectives. The study used “netnography” to explore female use of CJC-1295, a synthetic growth hormone analogue from the perspectives contained in Internet forum activity. Methods. A systematic Internet search was conducted using variation of the term “CJC-1295”; and combined with “forum.” Ninety-six hits related to bodybuilding websites where CJC-1295 was mentioned. Following application of exclusion criteria to confine to female use and evidence of forum activity, 9 sites remained. These were searched internally for reference to CJC-1295. Twenty-three discussion threads relating to female use of CJC-1295 formed the end data set, and analyzed using the Empirical Phenomenological Psychological method. Results. Forum users appeared well versed and experienced in the poly use of performance and image drug supplementation. Choice to use CJC-1295 centered on weight loss, muscle enhancement, youthful skin, improved sleep, and injury healing. Concerns were described relating to female consequences of use given gender variations in growth hormone pulses affecting estimation of dosage, cycling, and long-term consequences. Conclusions. Public health interventions should consider female self-medicating use of synthetic growth hormone within a repertoire of product supplementation, and related adverse health consequences.     

多糖的免疫调节作用及其作用机制研究进展

多糖具有肯定的调节机体免疫功能的作用,其作用是多途径、多环节、多靶点的,如促进免疫细胞增殖与分化,分泌各种淋巴因子,调节神经－内分泌－免疫调节网络（ＮＩＭ）的平衡等。在世界药物研究趋势由化学合成药物转向天然药物的今天,人们对中药多糖类药物的研究也正如火如荼。本文对近年来多糖的免疫调节作用及其作用机制的研究进展作一概述。     

阿仑膦酸钠合成工艺研究

目的研究阿仑膦酸钠的合成工艺。方法将4-氨基丁酸和亚磷酸投入到氯苯溶液中，在90℃和95℃之间反应至溶液澄清后，将溶液温度降低，在搅拌下缓慢滴加三氯化磷，然后升温继续反应，反应结束后再加三氯化磷，继续升温反应，结束后经水解、成盐，于低温冷却结晶，滤过干燥得到阿仑膦酸钠粗品。粗品溶液经活性碳脱色，结晶得到阿仑膦酸钠精制品。结果阿仑膦酸钠总收率为70％。结论该合成路线反应步骤短、操作简单、经济合理。     

Recent developments in allene-based synthetic methods

Presented is a review of the advances in synthetic methodology that make use of the allene functional group, with emphasis on catalytic asymmetric transformations and new mechanistic insights. The review covers the period from January 2007 to May 2008 and focuses on intra- and intermolecular cycloaddition, carbocycle cycloisomerization, heterocycle synthesis, epoxidation, addition and miscellaneous transformations. A brief discussion of allenes as transition metal ligands, the use of allenes in total synthesis and potential medicinal agents that contain the allene functionality is also presented.     

迷迭香酸药理作用的研究进展

迷迭香酸是一种含多酚羟基的酸,广泛存在于多种植物中,具有多种药理作用。已广泛用于食品、化妆品、医药等方面。本文简述迷迭香酸近年来在药理作用及临床应用方面的研究进展,旨在为其开发利用提供参考。     

Fundamentals in cardiovascular imaging technologies

The aim of this paper is to introduce the prominent in vivo cardiovascular imaging modalities such as magnetic resonance imaging, nuclear imaging and ultrasound from both the physical and molecular imaging perspectives. A brief introduction to the molecular imaging principles is also reported. Special emphasis will be given to the imaging parameters of sensitivity and spatial resolution, and the trade-off between spatial resolution, image contrast and target size.     

Inhibition of farnesyl protein transferase--a review of the recent patent literature

The inhibition of farnesyl protein transferase (FPT) has been the subject of intense research over the last few years and offers a promising approach to non-cytotoxic, anticancer therapy. Several FPT inhibitors are currently in clinical trials for anticancer therapy. This paper reviews the patent applications that appeared from January to July 2001. A brief summary of the compounds in clinical evaluation is also given.     

Using molecular simulations to probe pharmaceutical materials

Evolved through the past 60 years, molecular simulations have become one of the most important analytical tools in many theoretical and applied scientific disciplines. This paper provides a brief introduction to molecular simulations as a means of addressing important scientific questions of interest to pharmaceutical scientists. The focus is on fundamental questions such as: (1) Why do simulations work? (2) How to simulate? (3) How to make the results of simulations “real?” (4) Where can simulations be applied? To demonstrate the fundamental rationale of molecular simulations, three perspectives, thermodynamics, statistical mechanics, and general statistics, are compared. The concept of stochasticity is introduced, followed by a brief account of the two major methods used in simulations, molecular dynamics and Monte Carlo simulations. A brief discussion is then given on force fields to indicate their central importance. To facilitate the discussion about possible applications to pharmaceutical systems, the characteristics of molecular simulations are first compared with those of laboratory experiments. Case studies are then introduced to demonstrate the strengths of simulations. Some frequently encountered questions also are presented and discussed.     

Synthesis and enzyme inhibitory activities of novel peptide isosteres

Design and synthesis of metabolically stable peptide analogs that can either mimic or block the bioactivity of natural peptides or enzymes is an important constituent of bioorganic and medicinal chemistry research. Isosteric replacement of a scissile peptide bond represents a viable and popular approach in the rational design of peptidomimetics. Peptidomimetics find applications as drugs, in protein engineering and so on. This is evident from the wealth of therapeutically useful peptidomimetic leads incorporating any of the peptide isosteres that are currently available. In this review, we have given a brief account of the types of peptide isosteres widely known till date. With this background, we have described some of the recent developments in synthetic approaches. This includes methods involving a common intermediate to synthesize different possible isosteres and their peptide analogs, solid phase synthesis and combinatorial approach. One such method involving stereoselective nitrile oxide cycloaddition as the key step has been studied extensively in our research laboratory. Finally, we have also discussed about some of the recent reports on the design and inhibitory activities of peptidic or non-peptidic analogs against aspartic proteases (HIV-1, renin, ACE and pepsin) and peptide analogs of an immunomodulating hexapeptide.     

The emergence and analysis of synthetic cannabinoids

In late 2008, several synthetic cannabinoids were detected in herbal smoking mixtures. Typical of these products were 'Spice Gold', 'Spice Silver' and 'Yucatan Fire', but many other products have since appeared. The analytes detected, such as JWH-018 and CP47,497 are experimental compounds, some of which were never designed for human use. Both scientific and anecdotal evidence suggest that these compounds are more potent than traditional cannabis and are being widely used. As a result, authorities around the world are now beginning to control them by either naming individual compounds or using generic legislation. This, however, is easier said than done as the synthetic cannabinoids detected are constantly changing in attempts by manufacturers to evade legislation. This paper includes background information in the style of a brief monograph, as an aid to rapidly understanding the pharmacological aspects of these compounds in the forensic context, and then presents a comprehensive set of data, obtained from analysis of purchased products by gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-tandem mass spectrometry (LC-MS/MS).