Synthesis and bioactivity of some new 1-tolyl-3-aryl-4-methylimidazole-2-thiones

Three series of new 1-(isomeric methyl)benzoyl-3-arylthioureas (1–3a–i) were prepared from 2-, 3-, and 4-methylbenzoyl chlorides via isothiocyanate formation followed by treatment with various substituted anilines. The base-catalyzed condensation of thioureas (1–3a–i) with acetone was carried out in the presence of bromine to afford the corresponding 1-(isomeric methyl) benzoyl-3-aryl-4-methyl-imidazole-2-thiones (4–6a–i) in good yield. Thioureas and the corresponding thiones were characterized by spectroscopic data and elemental analyses. The mass fragmentation pattern of thiones is also discussed. The thiones were evaluated for antibacterial, antifungal, and insecticidal activities and exhibit significant antibacterial activity and slight but not significant antifungal and insecticidal properties.     

阿魏酸衍生物及其生物活性

阿魏酸具有抗血小板聚集、抗氧化、抗自由基、抗菌消炎、抗肿瘤、抗突变、增强免疫功能等多方面的生物活性。研究人员现已设计并合成了阿魏酸盐类修饰物及酯类、醚类、酰胺类等衍生物,并通过药效筛选发现了一些生物活性强于阿魏酸的化合物。综述阿魏酸结构改造与修饰及阿魏酸衍生物的生物活性方面的研究进展。     

Phytochemistry and bioactivities of sesquiterpenoids from the Artemisia species

The genus Artemisia is one of the largest and most widely distributed genera of the family Compositae. One type of the mainly active metabolites found in the Artemisia plants is sesquiterpenoids with extensive biological activities, including anti-inflammatory, immunomodulatory, anti-tumour, antimalarial, antinociceptive, antimicrobial and other activities. In this review, wecomprehensively summarized the progressconcerning the phytochemistry and biological activities of sesquiterpenoids obtained from the Artemisiaspecies from 2010 to July 2016. Furthermore,several future research perspectives and development of sesquiterpenoids as potential therapeutic agents were discussed as well.     

A review of therapeutic potential of Saussurea lappa-An endangered plant from Himalaya

There are 300 known Saussurea species. Among them, Saussurea lappa (S. lappa) is a representative perennial herb, globally distributed across Himalaya region. S. lappa has been traditionally used in medicines without obvious adverse effects. Despite significant progress in phytochemical and biological analyses of S. lappa over the past few years, inclusive and critical reviews of this plant are anachronistic or quite limited in scope. The present review aims to summarize up-to-date information on the active constituents, pharmacology, traditional uses, trade and challenges in conservation and sustainable use of S. lappa from the literature. In addition to botanical studies and records of the traditional use of S. lappa in over 43 diseases, scientific studies investigating the latent medicinal uses of this species and its constituent phytochemicals for a range of disorders are presented and discussed. The structure, bioactivity, and likely mechanisms of action of S. lappa and its phytochemicals are highlighted. Although some progress has been made, further scrupulous efforts are required to investigate the individual compounds isolated from S. lappa to validate and understand its traditional uses and develop clinical applications. The present review offers preliminary information and gives direction for further basic and clinical research into this plant.     

Diterpenoids of macromycetes

This review surveys the chemical and biological literature dealing with the isolation, structure elucidation and bioactivity of diterpenoids from the fruiting bodies of macromycetes, concentrating on work that has appeared in the literature up to December 2007. In addition, this paper examines the research of diterpenoids produced by macromycetes grown in mycelial culture and the culture conditions for the fermentation of macromycetes. (© 2009 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)     

紫堇属植物中异喹啉类生物碱的化学结构和生物活性的研究进展

目的综述紫堇属中异喹啉类生物碱的化学成分和生物活性的研究进展。方法阅读国内外文献数据库中近年来关于紫堇属植物的文献,从化学结构和生物活性方面对文献进行整理和综述。结果紫堇属植物含有丰富的异喹啉类生物碱,按照结构类型可分为9类:原小檗碱类、原阿片碱类、苯酞异喹啉类、苯菲啶类、苄基异喹啉类、阿朴菲类、枯拉灵类、螺苄异喹啉类、其他类。紫堇属植物中的生物碱具有清热解毒、消炎止痛等功效,还具有免疫、抗菌、抗炎等生物活性。结论本文对紫堇属植物中含有的异喹啉类生物碱的化学结构和生物活性进行了整理,为紫堇属植物的深入研究和临床应用提供理论依据。     

缬草挥发油的化学成分及药理活性研究进展

目的概述缬草挥发油的化学成分及药理活性。方法通过文献检索调查缬草挥发油。结果缬草挥发油含龙脑及其乙酸甲酯等成分,具有镇静催眠等作用。结论缬草挥发油是一类重要化学成分,具有多方面的生物活性。     

不同培养基对人牙周膜细胞生物学行为的影响

目的：研究α—MEM、DMEM—LG、RPMI1640三种培养基对人牙周膜细胞（human periodontal ligament cells，hPDLcs）生物学行为的影响，为体外培养人牙周膜细胞寻找合适的培养基。方法：采用改良组织块培养法，分别用α-MEM、DMEM—LG、RPMI1640三种培养基对hPDLcs进行体外培养，比较三组细胞在游出成功率、增殖及矿化等方面的差异。结果：α-MEM促进hPDLcs增殖作用最强。α—MEM组培养的细胞表达的碱性磷酸酶（alkaline phosphatase，ALP）含量最高，与其它两组间有显著差异。DMEM—LG组矿化结节形成个数最多且体积大。结论：α-MEM促进hPDLcs增殖，DMEM—LG促进hPDLcs分化。应根据实验要求选择合适培养基。     

中药拳参生物活性研究进展

拳参为传统的中草药之一,其主要有效成分为黄酮、蒽醌、鞣质等化合物,具有传统的清热、消肿、镇静的功效。对拳参的生物活性的研究进展进行概述。     

Bioactivities of polyphenolics from the roots of <Emphasis Type="Italic">Bauhinia racemosa</Emphasis>

Absctract  Various extracts of Bauhinia racemosa Lamk. (roots) and the isolated polyphenolics, viz. 1,7,8,12b-tetrahydro-2,2,4-trimethyl-10-methoxy-2H-benzo [6,7] cyclohepta[1,2,3-de][1]benzopyran-5,9-diol (racemosol) (1), 1,7,8,12b-tetrahydro-2,2,4-trimethyl-2H-benzo[6,7]cyclohepta[1,2,3-de][1]benzopyran-5,10,11-triol (2), and 1,7,8,12b-tetrahydro-2,2,4-trimethyl-2H-benzo[6,7] cyclohepta [1,2,3-de][1]benzopyran-5,9,10-triol (de-O-methyl racemosol) (3) were screened for antibacterial, antifungal, and antiviral activities. The isolated compounds exhibited profound antibacterial and antifungal activities while methanol extract exhibited potential efficacy against Herpes simplex virus.