呫吨酮类化合物及其药理活性

近年来从天然产物中分离得到大量呫吨酮类化合物，多数有异戊烯及其衍生物取代基，具有抗肿瘤、抗氧化、抗疟等多种活性，进行结构修饰后可得到活性显著的化合物。对近5年来分离的呫吨酮类化合物及其药理活性研究作一回顾。     

遍地金的生药学鉴定、化学成分和药理活性研究概况

目的:为遍地金的进一步研究与开发利用提供参考。方法:以"遍地金""生药学鉴定""化学成分""药理活性""Hypericum wightianum""Hyperium elodeoides""Chemical composition""Chemical constituents""Pharmacologic actions"等为关键词,在中国知网、万方、维普、百链外文数据库检索平台、PubMed、EBSCO等数据库中组合查询2000年-2018年8月发表的相关文献,对遍地金的生药学鉴定、化学成分、药理活性方面的研究进行归纳和总结。结果与结论:共检索到相关文献68篇,其中有效文献45篇。目前有关遍地金的生药学鉴定的研究主要集中在其分泌结构的形态特征、显微构造及类型鉴定和特征性差热图谱、近红外漫反射图谱及高效液相指纹图谱鉴定上。从遍地金及挺茎遍地金植物全草或地上部分中分离、鉴定或检测到的化学成分主要有间苯三酚类、萘骈二蒽酮类、黄酮类、呫吨酮类、异戊烯基苯甲酮类以及挥发性化学成分等。遍地金具有抗抑郁、抗菌、抗肿瘤等药理活性,但其研究主要集中在抗抑郁方面。目前,国内外有关遍地金的研究较少,药学基础理论薄弱。今后有必要进行系统而深入的研究,包括加强药效物质基础研究,尤其是抗抑郁和抗肿瘤活性成分研究;加强药理活性机制研究,尤其是抗抑郁和抗肿瘤活性机制研究;加强萘骈二蒽酮类化合物和异戊烯基苯甲酮类化合物抗病毒药理活性研究;加强对主要活性成分间苯三酚类、萘骈二蒽酮类及挥发性化学成分的分离、鉴定及发现新化合物的研究;加强对鉴定方法与药材质量标准研究。     

从南非植物中分离得到的四种新(口山)酮

近年来,(口山)酮类化合物越来越多地引起人们的注意,因为它具有了多种药理活性:单胺氧化酶抑制作用,体外细胞毒性,体内具有抗肿瘤、抗真菌、抑制结核菌、抗炎、抗菌等作用。生长于热带的藤黄属植物是(口山)酮类化合物的丰富资源。本文报道了从该属植物Garcinia livingstonei分离得到的四种新的被异戊烯基取代的(口山)酮化合物。将采于南非的G.livingstonei根皮     

呫吨酮类衍生物抗肿瘤活性研究进展

呫吨酮是含氧杂环化合物的重要组成部分.此类化合物的生物活性与其三环骨架和骨架上取代基团的性质和位置有关.该文总结了一系列天然与合成的呫吨酮类衍生物的抗肿瘤活性,并且阐述了部分重要的抗肿瘤机制,详细介绍了一些呫吨酮类衍生物的抗肿瘤及其对靶点的作用,尤其是对蛋白激酶C调变作用的研究;还列举了部分具有癌症治疗效果的呫吨酮类化合物,包括DMXAA、普梭草素、芒果苷、降阿赛里奥、曼果斯廷等.     

呫吨酮类化合物的药理活性研究进展

目的:综述近年来呫吨酮类化合物的药理活性研究进展.方法:收集国内外有关文献汇总.结果:呫吨酮类化合物具有多方面的药理活性:抗疟作用;保肝及治疗急慢性肝炎的作用;抗氧化作用;抗结核作用;抗抑郁活性;治疗热症、肝胆病及血液病;抗心肌缺血作用等.结论:呫吨酮类化合物具有多种药理活性,是一类很有发展空间的活性天然产物,药理学研究还存在很多不足,需要进一步研究.     

呫吨酮类化合物的药理作用研究进展

呫吨酮类化合物在自然界中广泛存在,它及其衍生物具有广泛的生理学和药理学活性,具有抗肿瘤、保护心血管、降低血糖、抗氧化、抗菌等药理作用,但很多药理作用机制尚处于研究探索阶段,从而使其药理活性及其与构型关系的研究倍受关注.收集国内外近几年来的有关文献,综述呫吨酮类化合物的药理研究进展.     

中药藤黄呫吨酮类化合物及其分析测定方法

介绍近年来从中药藤黄中分离得到的笼状呫吨酮类化合物及其分析测定方法,为中药藤黄抗肿瘤活性成分的进一步研究提供参考。笼状呫吨酮类化合物为中药藤黄发挥药理活性的物质基础,但由于其结构复杂,分子稳定性较差,需要借助于新型的分析检测技术方能对其进行定性定量测定。     

箭叶淫羊藿中化学成分及其体外抗肿瘤活性研究

目的 分离箭叶淫羊藿中的化学成分并对8-异戊烯基黄酮类化合物进行体外抗肿瘤活性筛选.方法 采用硅胶柱色谱、凝胶柱色谱和HPLC制备色谱方法分离纯化,根据理化性质和波谱分析方法鉴定其结构,利用MTT法对分离得到的异戊烯基黄酮类化合物进行体外抗肿瘤活性筛选.结果 分离得到7个黄酮类化合物,分别鉴定为淫羊藿苷(1)、淫羊藿素(2)、宝藿苷Ⅰ(3)、去甲淫羊藿素(4)、苜蓿素(5)、淫羊藿次苷Ⅰ(6)和朝藿定C(7).体外抗肿瘤结果表明,在0.5～1 00 μmol/L浓度,化合物2、3、4、6对人乳腺癌MDA-MB-231细胞增殖具有明显抑制作用,并随浓度的增加抑制作用更加明显,48 h的IC50分别为12.43、35.44、11.53、16.31 μmol/L,化合物1、7活性很弱.结论 化合物3、4为首次从箭叶淫羊藿植物分离得到,化合物3有望成为靶向抗乳腺癌的候选药物.     

组合分子模拟技术快速筛选天然呫吨酮类α-葡萄糖苷酶抑制剂

目的 筛选可能具有α-葡萄糖苷酶抑制活性的天然呫吨酮类化合物.方法 构建HipHop药效团模型,以最优药效团模型筛选天然产物数据库(TCMD);匹配较好的化合物进行CDOCKER分子对接,得到4个结合情况较好的呫吨酮类化合物;进一步采用分子动力学模拟验证化合物结合的稳定性.结果 3个呫吨酮化合物与α-葡萄糖苷酶结合较为...     

查尔酮类化合物的抗肿瘤活性及其构效关系研究进展

目的:了解查尔酮类化合物的抗肿瘤活性及其构效关系,为抗肿瘤新药研发奠定基础。方法:对PubMed数据库中1994-2013年查尔酮类化合物的抗肿瘤活性与其构效关系的研究进展进行综述。结果与结论:根据查尔酮类化合物母核上有效取代基类型的不同,可将其分为羟基化和甲基化查尔酮、卤取代查尔酮、硼酸基取代查尔酮和含氮基团取代查尔酮,其均具有较好的抗肿瘤活性,且结构简单、制备方便,是一种较有潜力的抗肿瘤先导化合物,在抗肿瘤新药的研究中具有广阔的应用前景。     

Cancer chemopreventive activity of terpenoid coumarins from Ferula species

Several natural products have been found to have anti-tumor promoting activity. In the present study, we carried out a primary screening of ten terpenoid coumarins isolated from plants of the Ferula species, examining their possible inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12- O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells. Auraptene (7-geranyloxycoumarin, 1) and umbelliprenin (7-farnesyloxycoumarin, 2) were found to significantly inhibit EBV-EA activation and preserved the high viability of Raji cells, suggesting that they might be valuable anti-tumor-promoting agents (IC (50) 8.3 and 9.1 nM, respectively). Our findings revealed that the presence of a prenyl moiety in the terpenoid coumarins plays an important role in anti-tumor promoting activity as previously reported for xanthones, coumarins, flavonoids and phenylpropanoids.     

Xanthones with anti-tumor activity isolated from Securidaca inappendiculata

A new xanthone, 1,2-dihydroxy-6,7,8-trimethoxyxanthone, together with ten known xanthones and nine other compounds was isolated from the stem of Securidaca inappendiculata. The structure of the new compound was elucidated based on spectroscopic data analyses, and other compounds were identified by comparison with data from the literature. The anti-tumor activities of the xanthones were evaluated by MTT assay on human lung adenocarcinoma epithelial cell line A549, and a primary structure–activity relationship analysis was carried out based on results from MTT assay. It is revealed that all the xanthones possessed anti-tumor activity in vitro in a concentration-dependent manner. The IC₅₀ values varied a lot among xanthones. 1,7-Dihydroxy-3,4-dimethoxyxanthone was proved to be the most efficient anti-tumor agent with IC₅₀ of 50.66 μM, while 1,3,7-trihydroxy-2,8-dimethoxyxanthone and 1,7-dihydroxyxanthone possessed the weakest activities. The structure–activity relationship analysis revealed that the anti-tumor activity of xanthones was affected mostly by the position and number of hydroxyl and methoxyl groups. Free hydroxyl and ortho-methoxyl groups were believed to possess important potentials to the activity.     

多靶点抗肿瘤天然产物研究进展

天然产物及其衍生物是抗肿瘤药物的重要组成部分。目前在临床上应用的天然产物来源的抗肿瘤药物以传统细胞毒类药物或靶向某一特定靶点的分子靶向药物为主,其应用受限于药物相关不良反应和肿瘤耐药。近年的研究表明,抗肿瘤活性天然产物往往能够靶向肿瘤细胞的多个靶点,影响肿瘤发生发展中的多个过程。由于肿瘤是一种多因素诱发的系统性疾病,多靶点天然产物在肿瘤治疗方面具有独特潜力。目前已发现的多靶点抗肿瘤天然产物的作用靶标和作用机制往往不够明确,限制了其进一步的开发。本文基于现代分子药理学理论,以多个典型的多靶点抗肿瘤天然产物为例进行综述,介绍了目前这些多靶点药物的作用机制、靶点确认和结构优化等研究进展,并对其作为抗肿瘤药物的研发前景进行了展望。     

Synthesis and antifungal activity of naturally occurring O- and C-prenylated flavanones

Flavonoids is one of the most important groups of naturally occurring O-heterocycles possessing a wide range of biological activity. O- and C-prenylated flavanones as members of flavonoids also show remarkable biological activity such as antibacterial, antiviral, anti-tumor, antifungal, anti-HIV and enzyme inhibition activity. O- and C-prenylated flavanones possessing remarkable biological activity are representatives of this family of natural products. In this paper efficient synthetic methods have been reported for the preparation of O-(2, 3) and C-(4, 5) prenylated flavanones isolated from Monotes engleri and their analogues (26-30; 38-43) starting from commercially available starting materials. In vitro pharmacological examinations of our compounds were performed on different Candida species (Candida albicans, Candida inconspicua, Candida dubliniensis, Candida krusei) by agardiffusion method. Our structure-activity relationship study clearly showed that any modification of the structure of selinone (2) and monotesone-A (3) led to the total loss the fungistatic activity.     

Prenylated xanthones as potential antiplasmodial substances

Mangostin, the major xanthone of Garcinia mangostana, and a series of synthetic derivatives were investigated for their in vitro antiplasmodial activity against Plasmodium falciparum. Mangostin itself showed moderate activity, but prenylated xanthones containing alkylamino functional groups exhibited quite potent antiplasmodial activity. Some structure-activity relationships are proposed.     

抗肿瘤天然药物的研究概况

目的介绍近年来一些抗肿瘤天然药物的研究概况。方法综合最新国内外文献报道,总结抗肿瘤天然药物的研究近况。结果一些抗肿瘤天然药物及其衍生物的研究取得很大进展。结论从天然活性产物中寻找开发抗肿瘤新药具有重要意义。     

Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection - an update (1998 - 2007)

The high number of citations of the previous review on anti-HIV compounds from plants published in 1998 in Planta Medica indicates the importance of natural products research in the battle against HIV. Therefore, we have decided to write an update of our previous review paper, this time covering the time span 1998 - 2007. The following antiviral chemical classes are discussed in detail: alkaloids, carbohydrates, coumarins, flavonoids, lignans, phenolics, proteins, quinones/xanthones, tannins and terpenes. If available, chemical structures, antiviral activity and selectivity, mechanism of action, and structure-activity relationship are presented.     

Recent progress in the development of natural ent-kaurane diterpenoids with anti-tumor activity

The ent-kaurane diterpenoids are widely distributed in China, some of which have high natural abundance in plants of Isodon, Pteris, Gnaphalium, Diplospora, Croton and some other species. These compounds exhibit significant anti-tumor, antibacterial and anti-inflammatory activities, which have attracted the attention of medicinal chemists. This review focuses on the recent advances in the research of derivatives, anti-tumor activity, mechanism of action, and structure-activity relationships of ent-kaurane diterpenoids. All of these will show the potential in the development of new antitumor agents in natural products.     

藤黄属植物的化学成分和药理作用研究进展

藤黄属植物在东南亚地区广泛分布,其中一些植物作为民间药物有着悠久的用药历史。该属植物普遍具有抗肿瘤、抗炎、抗菌等药理作用,而且已有呫吨酮、双黄酮、苯甲酮、萜类等多种结构类型的化学成分从该属植物中分离得到.概述了近十年来从藤黄属植物中分离得到的新化合物和首次发现的天然产物及其化学成分的药理活性研究进展,为该属植物的深入研究提供依据。     

Synthesis of prenylated and geranylated xanthones and their bioactivities

Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11% to 36%. All of the compounds were first reported. Then, the antitumor, anti-tyrosinase, anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were evaluated. Compound 9 exhibited clear antitumor activity, and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with cisplatin. Compounds 1–4 and 6–7 alsoexhibited certain activity other than the antitumor activity described above. These results demonstrated that compounds 1–4, 6–7and 9 were very promising leads for further structural modification.