菊科倍半萜二聚体的研究进展

倍半萜二聚体是菊科植物中存在的一类结构复杂的天然化学成分,近些年来其日渐成为天然药物化学领域研究的热点。本论文根据倍半萜二聚体连接的方式不同,把其分为环化,酯键,碳-碳单键等聚合方式形成的倍半萜二聚体。药理研究表明,该类化学成分在抗炎,抗肿瘤,神经保护等方面具有显著活性。通对2011～2018年143个倍半萜二聚体化学结构和药理活性综述,为该类成分的研究和开发提供参考。     

1,3-二炔类天然产物的合成及生物活性研究进展

多炔类化合物是广泛存在于自然界的一类天然产物,由于其独特的结构和药理活性,近年来引起了国内外化学家和生物学家的广泛关注。目前多炔类天然产物的研究多集中于1,3-二炔类化合物,该类天然产物具有多样性的结构和生物活性如抗癌、神经毒性、抗炎活性、免疫抑制活性等,但相关进展综述迄今尚未见报道。本文系统的综述了近年国内外对1,3-二炔类天然产物的合成及药理活性研究进展,以期为1,3-二炔类天然产物的开发和利用提供思路和方法。     

百合皂苷类化学成分提取及药理活性研究进展

百合属植物化学成分多样,近年来成为天然产物化学研究的重点。文中着重对百合中重要化学成分百合皂苷的提取方法、化学成分及药理活性进行综述,为百合皂苷的开发利用提供参考。     

碳苷黄酮及其药理活性研究进展

随着天然产物化学的不断发展,越来越多具有生物学功能和药理活性的植物碳苷黄酮得到了分离、纯化和鉴定。本文综述了近些年来从水果、蔬菜和药物植物中分离鉴定的碳苷黄酮及其清除自由基、抗氧化、抗辐射等广谱药理活性,以期为碳苷黄酮的研究和开发提供信息和指导。     

11-脱氧18α-和18β-甘草次酸类抗癌复合物的制备和结构表征

为寻找新型肝靶向抗癌前药,将具有肝靶向特征的天然分子甘草次酸的半合成衍生物与抗癌药环磷酰胺的活性代谢物氮芥磷酰二氯偶联制成11-脱氧甘草次酸类两个目标化合物和7个中间体。化合物的化学结构用常规光谱分析法进行鉴定,对合成工艺、理化性质和光谱特征进行系统描述。本研究对甘草次酸类新型肝靶向抗癌前药的药理活性筛选奠定基础。     

仪花属植物化学成分及药理活性研究进展

豆科仪花属植物,主要分布于我国南部。该属植物主要含有间苯三酚类、黄酮类、二苯乙烯类、三萜类等化学成分,具有抗氧化、扩张血管、抗心律失常和镇痛等多种药理活性,民间主要用于治疗跌打损伤、骨折和外伤出血。本文较系统的综述了近十年国内外对仪花属植物的化学成分及药理活性的研究进展,以期为仪花属植物的开发利用提供一定的科学依据。     

甘草属植物中三萜化合物的研究进展（综述）

本文综述了甘草属植物中三萜化合物近年来的药理活性研究,化学结构和结构鉴定中的波谱特征。     

油茶化学成分及其抗菌抗炎活性的研究进展

油茶(Camellia oleifera Abel.)是我国特有的木本油料作物,具有较高的食用和药用价值,油茶所含化学成分包括三萜类、酚类和甾醇类等,三萜类和酚类化合物为油茶最主要的化学成分。药理研究表明,油茶籽提取物(茶油)以及部分三萜类(茶皂苷)和酚类化合物具有良好的抗菌抗炎活性。本文对油茶化学成分和抗菌抗炎活性进行系统性的总结,以期为油茶资源的合理开发提供一定的理论依据。     

异甾体生物碱类化合物及药理活性研究进展

异甾体生物碱类结构多变,药理活性多样,主要分布于百合科贝母属和藜芦属植物中。近十五年内共报道了80个新发现的异甾体生物碱类成分,药理活性涉及抗炎、镇痛、降压、平喘、抗血栓、胆碱酯酶抑制、抗病毒和抗肿瘤等作用。本文综述了2006至2020年间该类化合物的植物来源、化学结构及药理活性,并对该类化合物的未来研究探索进行了讨论与展望。     

Pachysandra型生物碱的化学结构及活性筛选

本文简要报道黄杨科凳果族植物中Ｐａｃｈｓａｎｄｒａ型生物碱的化学结构研究概况及药理活性筛选的初步结果。药理活性筛选结果表明,筛选的化合物大多具有抗癌（Ｐ３８８和Ｌ１２１０）活性,部分化合物显示较高活性的抗溃疡作用。     

Natural source,bioactivity and synthesis of 3-Arylcoumarin derivatives

3-arylcoumarins with different pharmacological properties widely exist in a variety of natural plants. The extensive research on 3-arylcoumarins was attributed to its therapeutic and relatively easy isolation. Therefore, 3-arylcoumarins can be recognised as useful structures for the design of novel compounds with potential pharmacological interest, particularly in the fields of anti-inflammatory, anti-cancer, antioxidant, Monoamine oxidase (MAO) enzyme inhibition, etc. The current review highlights the biological activities, design, and chemical synthetic methods of 3-arylcoumarins derivatives as well as their important natural product sources.     

Microalgae as sources of pharmaceuticals and other biologically active compounds

In the last decade the screening of microalgae, especially the cyanobacteria (blue-green algae), for antibiotics and pharmacologically active compounds has received ever increasing interest. A large number of antibiotic compounds, many with novel structures, have been isolated and characterised. Similarly many cyanobacteria have been shown to produce antiviral and antineoplastic compounds. A range of pharmacological activities have also been observed with extracts of microalgae, however the active principles are as yet unknown in most cases. Several of the bioactive compounds may find application in human or veterinary medicine or in agriculture. Others should find application as research tools or as structural models for the development of new drugs. The microalgae are particularly attractive as natural sources of bioactive molecules since these algae have the potential to produce these compounds in culture which enables the production of structurally complex molecules which are difficult or impossible to produce by chemical synthesis.     

Marine pharmacology in 2007–8: Marine compounds with antibacterial,anticoagulant, antifungal,anti-inflammatory,antimalarial, antiprotozoal,antituberculosis, and antiviral activities; affecting the immune and nervous system,and other miscellaneous mechanisms of action

The peer-reviewed marine pharmacology literature in 2007–8 is covered in this review, which follows a similar format to the previous 1998–2006 reviews of this series. The preclinical pharmacology of structurally characterized marine compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, anticoagulant, antifungal, antimalarial, antiprotozoal, antituberculosis and antiviral activities were reported for 74 marine natural products. Additionally, 59 marine compounds were reported to affect the cardiovascular, immune and nervous systems as well as to possess anti-inflammatory effects. Finally, 65 marine metabolites were shown to bind to a variety of receptors and miscellaneous molecular targets, and thus upon further completion of mechanism of action studies, will contribute to several pharmacological classes. Marine pharmacology research during 2007–8 remained a global enterprise, with researchers from 26 countries, and the United States, contributing to the preclinical pharmacology of 197 marine compounds which are part of the preclinical marine pharmaceuticals pipeline. Sustained preclinical research with marine natural products demonstrating novel pharmacological activities, will probably result in the expansion of the current marine pharmaceutical clinical pipeline, which currently consists of 13 marine natural products, analogs or derivatives targeting a limited number of disease categories.     

甾体皂苷生物转化研究进展

甾体皂苷是中药中一类较为复杂的糖苷类化合物,具有多方面的药理活性。生物转化是利用各种酶系或微生物对天然活性化合物进行生物合成与结构修饰。利用生物转化技术可以对甾体皂苷类化合物完成化学法难以进行的结构改造和修饰,从而获得具有更高药用价值的目标化合物。本文对近几年利用微生物和酶法转化对甾体皂苷结构修饰的研究进展进行了综述,并分析了甾体皂苷生物转化研究中存在的问题,展望了其研究的前景。     

Genotoxicity and Cytotoxicity Evaluation of the Neolignan Analogue 2-(4-Nitrophenoxy)-1Phenylethanone and its Protective Effect Against DNA Damage

Neolignans are secondary metabolites found in various groups of Angiosperms. They belong to a class of natural compounds with great diversity of chemical structures and pharmacological activities. These compounds are formed by linking two phenylpropanoid units. Several compounds that have ability to prevent genetic damage have been isolated from plants, and can be used to prevent or delay the development of tumor cells. Genetic toxicology evaluation is widely used in risk assessment of new drugs in preclinical screening tests. In this study, we evaluated the genotoxicity and cytotoxicity of the neolignan analogue 2-(4-nitrophenoxy)-1-phenylethanone (4NF) and its protective effect against DNA damage using the mouse bone marrow micronucleus test and the comet assay in mouse peripheral blood. Our results showed that this neolignan analogue had no genotoxic activity and was able to reduce induced damage both in mouse bone marrow and peripheral blood. Although the neolignan analogue 4NF was cytotoxic, it reduced cyclophosphamide-induced cytotoxicity. In conclusion, it showed no genotoxic action, but exhibited cytotoxic, antigenotoxic, and anticytotoxic activities.     

黏菌化学成分的研究进展

文中回顾及总结了黏菌化学成分的研究进展。迄今为止已从4个目共27种黏菌中分离得到脂肪酸、氨基酸、生物碱、萘醌、芳香族化合物、萜类化合物、酯类化合物及它们的衍生物等近百种化学成分,其中某些成分表现出重要的生物活性。研究表明黏菌不仅已经逐渐成为天然产物的重要研究对象,而且有望成为获得天然活性物质的新资源,这对于黏菌的开发利用具有重要意义。     

By-Products of Zea mays L.: A Promising Source of Medicinal Properties with Phytochemistry and Pharmacological Activities: A Comprehensive Review

Zea mays (Z. mays) is one of the main cereal crops in the world, and it′s by-products have exhibited medicinal properties to explore. This article intends to review the chemical compositions and pharmacological activities of by-products of Z. mays (corn silks, roots, bract, stems, bran, and leaves) which support the therapeutic potential in the treatment of different diseases, with emphasis on the natural occurring compounds and detailed pharmacological developments. Based on this review, 231 natural compounds are presented. Among them, flavonoids, terpenes, phenylpropanoids, and alkaloids are the most frequently reported. The by-products of Z. mays possess diuretic effects, hepatoprotective, anti-diabetic, antioxidant, neuroprotective, anti-inflammatory, anti-cancer, plant protection activity, and other activities. This article reviewed the phytochemistry and pharmacological activities of Z. mays for comprehensive quality control and the safety and effectiveness to enhance future application.     

Naturally occurring plant isoquinoline N-oxide alkaloids: Their pharmacological and SAR activities

The present review describes research on novel natural isoquinoline alkaloids and their N-oxides isolated from different plant species. More than 200 biological active compounds have shown confirmed antimicrobial, antibacterial, antitumor, and other activities. The structures, origins, and reported biological activities of a selection of isoquinoline N-oxides alkaloids are reviewed. With the computer program PASS some additional SAR (structure–activity relationship) activities are also predicted, which point toward new possible applications of these compounds. This review emphasizes the role of isoquinoline N-oxides alkaloids as an important source of leads for drug discovery.     

Allenic and cumulenic lipids

Nowadays, about 200 natural allenic metabolites, more than 2700 synthetic allenic compounds, and about 1300 cumulenic structures are known. The present review describes research on natural as well as some biological active allenic and cumulenic lipids and related compounds isolated from different sources. Intensive searches for new classes of pharmacologically potent agents produced by living organisms have resulted in the discovery of dozens of such compounds possessing high anticancer, cytotoxic, antibacterial, antiviral, and other activities. Known allenic and cumulenic compounds can be subdivided on several structural classes: fatty acids, hydrocarbons, terpenes, steroids, carotenoids, marine bromoallenes, peptides, aromatic, cumulenic, and miscellaneous compounds. This review emphasizes the role of natural and synthetic allenic and cumulenic lipids and other related compounds as an important source of leads for drug discovery.     

Medicinal and pharmaceutical uses of seaweed natural products: A review

In the last three decades the discovery of metabolites with biological activities from macroalgae has increased significantly. However, despite the intense research effort by academic and corporate institutions, very few products with real potential have been identified or developed. Based on Silverplatter MEDLINE and Aquatic Biology, Aquaculture & Fisheries Resources databases, the literature was searched for natural products from marine macroalgae in the Rhodophyta, Phaeophyta and Chlorophyta with biological and pharmacological activity. Substances that currently receive most attention from pharmaceutical companies for use in drug development, or from researchers in the field of medicine-related research include: sulphated polysaccharides as antiviral substances, halogenated furanones from Delisea pulchra as antifouling compounds, and kahalalide F from a species of Bryopsis as a possible treatment of lung cancer, tumours and AIDS. Other substances such as macroalgal lectins, fucoidans, kainoids and aplysiatoxins are routinely used in biomedical research and a multitude of other substances have known biological activities. The potential pharmaceutical, medicinal and research applications of these compounds are discussed.