Natural products for the prevention and treatment of cholestasis: A review

Cholestasis is a common manifestation of decreased bile flow in various liver diseases. It results in fibrosis and even cirrhosis without proper treatment. It is believed that a wide range of factors, including transporter dysfunction, oxidative stress, inflammatory damage, and immune disruption, can cause cholestasis. In recent years, natural products have drawn much attention for specific multiple‐target activities in diseases. Many attempts have been made to investigate the anticholestatic effects of natural products with advanced technology. This review summarizes recent studies on the biological activities and mechanisms of recognized compounds for cholestasis treatment. Natural products, including various flavonoids, phenols, acids, quinones, saponins, alkaloids, glycosides, and so on, function as comprehensive regulators via ameliorating oxidative stress, inflammation, and apoptosis, restoring bile acid balance with hepatic transporters, and adjusting immune disruption. Moreover, in this progress, nuclear factor erythroid 2‐related factor 2, reactive oxygen species production, heme oxygenase‐1, NF‐κB, cholesterol 7 alpha‐hydroxylase, and farnesoid X receptors are thought as main targets for the activity of natural products. Therefore, this review presents the detailed mechanisms that include multiple targets and diverse signalling pathways. Natural products are the valuable when seeking novel therapeutic agents to treat cholestatic liver diseases.     

The 2,11-cyclized cembranoids: cladiellins, asbestinins, and briarellins (period 1998-2010)

The 2,11-cyclized cembranoids are isolated from marine invertebrates of Octocorallia species. They are a very interesting class of natural products sharing a common oxatricyclo[6.6.1.0(2,7)]pentadecane core and carrying a varied substituent pattern. This review presents their structural diversity along with the reported biological activities. The 2,11-cyclized cembranoids were comprehensively reviewed previously in 1998, and this contribution will serve as an update of that work. Since 1998 a number of structural assignments of the isolated products have been revised, some as a result of total synthesis efforts. The chemical reactivity of several of the natural compounds has been studied, and the relevance of these findings to the biosynthesis or the generation of isolation artifacts is discussed. The wide range of biological activities displayed by the 2,11-cyclized cembranoids justifies the interest shown within the synthetic chemistry community and suggests that this class of natural products remains a fruitful area for future synthetic and biological research.     

黄酮类化合物的构效关系研究进展

天然黄酮类化合物是以C6-C3-C6为基本结构骨架,结构亚型多种多样;其在自然界中的分布极为广泛,从水果、蔬菜到中药中都有发现,生物活性具有多样性,一直是药物研发的热点领域。以天然黄酮类化合物为先导化合物或直接开发成的药物已经得到广泛应用。由于黄酮类化合物的结构具有极强的规律性,对于该类化合物的构效关系研究也很活跃,也为药物研发提供了丰富的理论依据。总结了近年来黄酮类化合物构效关系的研究进展,为分离或合成具有更强药理活性的黄酮类先导化合物提供理论参考。     

海绵药物的研究进展:化学和生物活性

近年来国际上对海洋天然产物的研究日益深入，依托现代大规模药理筛选，目前已有多种结构新颖、药理活性显著且作用机制特殊的海洋天然产物进入临床试验阶段或正在进行临床前研究。海绵种类繁多，代谢途径独特，生存环境多样，共生现象复杂而普遍，多年来一直是海洋天然产物领域最富成果的研究领域之一。本文简要介绍近几年海绵化学成份及其药理活性的研究进展，以供国内同行参考。     

海绵中活性化学成分的研究进展

海洋生物海绵的活性化学成分研究一直都是海洋药物研究的焦点。目前,从海绵中发现了大量的具有抗微生物、抗炎、抗肿瘤、抗病毒和免疫调节等活性的化学成分,其按照化学结构类型可分为脂类、大环内酯类、肽类、生物碱类、甾醇类和萜类等,并且有很多化合物已经进入临床研究。对近年来从海绵中发现的活性化学成分进行综述。     

Biologically active sesquiterpene coumarins from Ferula species

Extracts from different species of the genus Ferula (Apiaceae) have had various biomedical applications for many centuries. Many biological features of this genus such as cytotoxicity, antibacterial, antiviral, P-glycoprotein (P-gp) inhibitory and antiinflammatory activity have been attributed to sesquiterpene coumarins; structures containing a common coumarin group and a sesquiterpene moiety. This both highlights the importance of sesquiterpene coumarins as biologically active natural products and necessitates further studies on these compounds. Taking into account the versatile biological properties of compounds isolated from Ferula and the unprecedented interest in the application of natural products as a new generation of therapeutics, the present review will discuss reports on biological activities of sesquiterpene coumarins of the genus Ferula, from 1990 onwards.     

海洋天然产物研究概述

近年来海洋天然产物越来越引起科学家们的注意,在浩瀚的海洋中存在着大量令人激动、活性独特、结构新颖的次生代谢产物。海洋天然产物已成为发现重要先导药物和新的生物作用机制的主要源泉。对目前海洋天然产物研究概况进行综述,其中重点介绍大环内酯类和聚醚类等化合物。     

吩噻嗪类化合物的合成及其生物活性研究进展

吩噻嗪是含杂原子的三环化合物,于19世纪后半叶在染料工业中发现并被应用。近年来,陆续发现以吩噻嗪结构为母核的部分衍生物具有抗癌、抗菌、抗阿尔兹海默症、抗氧化以及抗病毒等多种药理活性。笔者综述了吩噻嗪类化合物的合成及其相关生物活性研究进展,总结不同活性类型吩噻嗪衍生物的构效关系,为吩噻嗪类化合物的深入系统研究提供参考。     

Bioactive marine natural products, with emphasis on handling of water-soluble compounds

Recent progress in separation techniques has enabled us to work with water-soluble components which, more often than not, are responsible for biological activities found in marine organisms. Isolation techniques and chemical and biological aspects of water-soluble marine natural products will be discussed with some representative examples.     

天然黄酮苷的药理活性及合成研究进展

黄酮苷类化合物广泛存在于自然界，具有显著的生物活性，是一类重要的天然有机化合物。本文简要综述了近十几年天然黄酮苷的药理活性、构效关系及合成方面的研究进展。     

近10年甾体皂苷的生物活性研究进展

甾体皂苷具有广泛的药理作用和生物活性,如抗肿瘤、抗真菌、降血糖、免疫调节、驱虫等。近10年来,从天然植物中又发现一些新结构的甾体皂苷类化合物,它们具有强度不一的新活性。为了加快甾体皂苷化合物的药物创新研究,该文概述此类化合物的研究新进展。     

生物转化在天然甘草药物活性成分中的研究进展

药用甘草活性成分的生物转化一直是国内外研究的热点。文章从植物细胞培养、微生物和游离酶为生物催化剂角度综述了天然甘草活性成分的生物转化,其反应包括水解、羟基化、糖基化、酰基化等多种类型,并在生物转化体系的筛选、转化条件的优化、转化率的提高及酶的分离纯化方面取得了一些进展。这增加天然产物结构多样性、寻找药物先导化合物、促进珍稀物种资源可持续利用、提高生产效率、降低成本等多个环节均有广泛的应用价值。     

ChemGPS-NP: tuned for navigation in biologically relevant chemical space

Natural compounds are evolutionary selected and prevalidated by Nature, displaying a unique chemical diversity and a corresponding diversity of biological activities. These features make them highly interesting for studies of chemical biology, and in the pharmaceutical industry for development of new leads. Of utmost importance, for the discovery of new biologically active compounds, is the identification and charting of the corresponding biologically relevant chemical space. The primary key to this is the coverage of the natural products' chemical space. Here we introduce ChemGPS-NP, a new tool tuned for handling the chemical diversity encountered in natural products research, in contrast to previous tools focused on the much more restricted drug-like chemical space. The aim is to provide a framework for making compound classification and comparison more efficient and stringent, to identify volumes of chemical space related to particular biological activities, and to track changes in chemical properties due to, for example, evolutionary traits and modifications in biosynthesis. Physical-chemical properties not directly discernible from structural data can be discovered, making selection more efficient and increasing the probability of hit generation when screening natural compounds and analogues.     

福建药用植物金线莲研究进展

福建药用植物金线莲具有丰富的营养物质,为高效安全的天然药物。本文对金线莲的化学成分、 提取分析、生物活性等方面的最新研究进展进行综述,并讨论金线莲药用植物的研究与开发。     

抗艾滋病毒生物活性天然多糖类化合物研究进展

目的：探讨抗艾滋病毒（HIV）生物活性天然多糖类化合物研究进展,为临床治疗艾滋病（AIDS）提供依据。方法：通过总结、归纳和分析近年来治疗艾滋病毒感染者和艾滋病患者（HIV/AIDS）的相关文献,对具有抗HIV生物活性的天然多糖类化合物的来源与种类、抗HIV机制、结构及其构效关系进行概括和总结,并探讨研究中存在的主要问题。结果：天然多糖类化合物广泛存在于自然界各类有机体中,具有多种重要的生物活性和药理作用,特别是其抗HIV活性,越来越受到科学界的重视。结论：对抗HIV活性天然多糖类化合物的研究为临床应用提供了理论基础。     

Research progress of Chinese herbal medicine compounds and their bioactivities: Fruitful 2020

Traditional Chinese medicines (TCMs) have continued to be a treasure trove. The study of chemodiversity and versatility of bioactivities has always been an important content of pharmacophylogeny. There is amazing progress in the discovery and research of natural components with novel structures and significant bioactivities in 2020. In this paper we review 271 valuable natural products, including terpenoids, steroids, flavonoids, phenylpropanoids, phenolics, nitrogen containing compounds and essential oil, etc., isolated and identified from TCMs published in journals of Chinese Traditional and Herbal Drugs (Zhong Cao Yao) and Chinese Herbal Medicines (CHMs), and focus on their structures, source organisms, and relevant bioactivities, paying special attention to structural characteristics of novel compounds and newly revealed pharmacological properties of known compounds. It is worth noting that natural products with antitumor activity still constitute the primary object of research. Among the reported compounds, two new triterpenoids, i.e., ursolic acid 3-O-β-cis-caffeate and mollugoside E, display remarkable cytotoxicity against PC-9 and HL-60 cell lines, respectively. Three known phenolic compounds, i.e., pyoluteorin, 4-hydroxy-3-methoxy cinnamaldehyde and 3,7-dimethoxy-5-hydroxy-1,4-phenanthrenequinone, exhibit significant cytotoxicity against multiple cell lines. Numerous studies on the free radical scavenging activity of reported compounds are currently underway. In vitro, three known phenolic compounds, i.e., 3,4-O-dicaffeoylquinic acid methyl ester, 3,4,5-O-tricaffeoylquinic acid methyl ester and arbutin, had more considerable antioxidant activities than vitamin C. The anti-inflammatory, anti-diabetic, hypolipidemic, neuroprotective and antimicrobial activities of isolated compounds are also encouraging. The structural characteristics and bioactivities of TCM compounds highlighted here reflect the enormous progress of CHM research in 2020 and will play a positive role in the future drug discovery and development. According to pharmacophylogeny, the phylogenetic distribution of compounds with different natures and flavors can be explored, with view to better mining TCM resources.     

Woodfordia fruticosa: traditional uses and recent findings

Woodfordia fruticosa Kurz of the family Lythraceae is a plant of tropical and subtropical region with a long history of medicinal use. A wide range of chemical compounds including tannins (especially those of macrocyclic hydrolysable class), flavonoids, anthraquinone glycosides, and polyphenols have been isolated from this species in recent times. Extracts and metabolites of this plant, particularly those from flowers and leaves, possess useful pharmacological activities. A comprehensive account of the chemical constituents and the biological activities is presented and a critical appraisal of the ethnopharmacological issues is included in view of the many recent findings of importance on this plant.     

茶黄素生物活性与开发应用的研究进展

茶黄素是一类具有苯骈卓酚酮环结构的天然化合物,具有抗氧化、调血脂、降血糖、抗病毒、抗炎、降尿酸、抗菌、抗肿瘤、抗骨质疏松等药理作用。茶黄素是茶叶天然活性成分的研究重点之一,其在保健食品、医药、化妆品、动物饲料、植物农药等终端产品的开发上越来越广泛。通过查阅近年来有关茶黄素的文献资料,以茶黄素结构的认识为出发点,综述茶黄素的生物活性,关注茶黄素在保健食品、医药等领域中的科学研发与应用,以期为茶黄素的应用开发提供参考。     

岩黄连的化学成分及生物活性研究进展

岩黄连Corydalis saxicola是我国西南地区的民间传统药物,临床上用于乙型肝炎、肝硬化、肝癌等肝病的治疗,极具开发价值。研究表明岩黄连中含丰富的生物碱、甾体、三萜、黄酮与核苷等类化合物,生物碱类为主要成分,多数化合物具有显著的生物活性,如抗病毒、抗炎、抗肿瘤、保肝、抑菌、抑制乙酰胆碱酯酶、镇痛等活性,特别是对乙肝、肝癌以及肝硬化等疾病的缓解作用比较显著。对岩黄连化学成分及生物活性的研究进展进行综述,以期为岩黄连的后续研究和深入开发提供参考。     

Natural antagonists of platelet-activating factor

Several groups of antagonists of platelet-activating factor (PAF) are reviewed. The characteristics of PAF binding sites on mammalian cell membranes are described together with the activities of non-specific and synthetic PAF-antagonists. The specificity of the ginkgolides to bind to PAF-receptors is discussed and the effects of these natural products in a range of biological systems is emphasized. Other groups of natural PAF-antagonists described are the lignans and gliotoxin related compounds. The structural chemistry, structure-activity relationships and pharmacological properties of these drugs are compared to the ginkgolides.