天然来源的甘遂烷型三萜的结构及其药理活性研究进展

甘遂烷型三萜是以6个异戊二烯单元为基本母核的四环三萜类化合物。目前发现的天然来源的甘遂烷型三萜类虽然数量较少,但是化合物结构多样,如apo-型、侧链呈直链型及侧链成环型;药理活性广泛,如细胞毒、抗炎、抗氧化及抗疟原虫等。该文综述了近十年该类三萜化合物的植物来源、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。     

五味子科植物中羊毛脂烷型三萜类成分及其药理作用研究进展

羊毛脂烷型三萜是一类具有四环体系三萜类型的化合物,在植物中分布广泛,是五味子科中常见的三萜类化合物之一,主要具有抗HIV、抗肿瘤等药理作用。对五味子科中羊毛脂烷型三萜类成分的结构分类及药理活性方面的研究进展进行综述,为合理开发利用五味子科药用植物资源提供参考。     

葫芦烷型降三萜类化合物的研究进展

葫芦烷型降三萜类化合物是一类结构新颖的化合物,是在葫芦烷型三萜的30个碳骨架的基础上减少1个或几个碳所得.按其缺少碳原子的位置可分为2-降(a)、3-降(b)、19-降(c)、27-降(d)、29-降(e)、19,29-降(f)、25,26,27-降(g)、24,25,26,27-降(h)、23,24,25,26,27...     

胡黄连葫芦烷型四环三萜类化合物及其生物活性的研究进展

胡黄连Picrorhizae Rhizoma为中医临床清虚热要药,目前一般认为其功效与环烯醚萜类、苯乙醇糖苷类和酚苷类化合物相关,而对于胡黄连所含葫芦烷型四环三萜类化合物及其生物活性关注较少。研究表明含有α,β-不饱和酮结构的葫芦烷型四环三萜属于迈克尔反应受体小分子,具有抗肿瘤等重要药理活性。对胡黄连中的葫芦烷型四环三萜类化合物进行综述,一方面比较了2种基原胡黄连所含葫芦烷型四环三萜类化合物的差异,另一方面对此类化合物的生物活性研究进行总结,为深入探索胡黄连功效的物质基础提供参考。     

植物五环三萜类化合物生物合成途径研究进展

五环三萜类化合物是一类重要的植物次生代谢产物,由6个异戊二烯单元组成,在自然界中普遍存在,具有广泛的药理作用。五环三萜类化合物结构丰富多样,根据其苷元的不同,可分为齐墩果烷型、羽扇豆烷型、乌苏烷型和木栓烷型4大类。植物五环三萜类化合物主要由甲羟戊酸途径和戊糖磷酸途径合成,2,3-环氧角鲨烯前体在氧化鲨烯环化酶的作用下环化为不同的骨架,继而在细胞色素P450以及糖基转移酶的修饰下形成多种皂苷。综述了植物五环三萜类化合物生物合成途径的研究进展,对参与合成途径的关键家族基因进行系统分析和催化机制的解读,为寻找未知五环三萜类化合物生物合成途径关键基因和五环三萜化合物异源生物合成提供参考。     

五味子科植物中环阿屯烷型三萜类成分及其药理作用研究进展

环阿屯烷型三萜是一类具有四环体系的三萜类化合物,在植物中分布广泛,是五味子科植物中常见的三萜类型之一。对五味子科植物中环阿屯烷型三萜成分的结构分类及药理活性方面的研究进展进行了综述,为合理开发利用五味子科药用植物资源提供参考。     

乌苏烷型三萜类化合物的抗肿瘤活性及其构效关系研究进展

通过查阅整理乌苏烷型三萜类化合物的研究文献,综述了国内外有关乌苏烷类化合物抗肿瘤活性及其构效关系研究的进展,为其进一步的开发利用提供依据和参考。     

多孔菌科真菌中羊毛甾烷型三萜类成分及其药理作用研究进展

羊毛甾烷型三萜是四环三萜类化合物,是多孔菌科真菌中含量较为丰富的一类次级代谢产物。羊毛甾烷型三萜类化合物可以划分为A、B、C、D、E 5种主要骨架构型,具有抗肿瘤、抗炎、抗菌等药理活性。通过查阅国内外文献,对多孔菌科20多种真菌中分离出的161种羊毛甾烷型三萜类成分及药理作用研究进展进行了综述,为羊毛甾烷型三萜类成分的研究及多孔菌科真菌药用资源的合理应用与开发提供参考。     

金樱子根中1个新颖裂环三萜类成分

目的研究蔷薇科蔷薇属植物金樱子Rosa laevifgata根的化学成分。方法采用硅胶、Sephadex LH-20、半制备高效液相等色谱技术进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构,并进行体外抗炎活性实验。结果从金樱子根的甲醇提取物中分离得到7个三萜类化合物,分别鉴定为18,19-裂环-2α,3β,23α-三羟基-19-羰基-乌苏烷-11,13(18)-二烯-28-羧酸(1)、(2R,19R)-甲基-2-乙酰氧-19-羟基-3-羰基-乌苏烷-12-烯-28-羧酸(2)、坡模酮酸(3)、号角树酸-3-甲酯(4)、2-乙酸基委陵菜酸(5)、坡模酸(6)、2α,3α-二羟基乌苏烷-12,18-二烯-28-羧酸(7)。结论化合物1为1个新化合物,命名为金樱子裂环三萜A。体外抗炎活性实验结果表明,化合物1～7对脂多糖(LPS)刺激小鼠巨噬细胞(RAW264.7)释放NO具有明显的抑制作用,其中化合物1和7的抑制效果最为显著,显示了较好的体外抗炎活性。     

玉蕊醇型三萜的结构特征、波谱规律及药理活性研究进展

玉蕊醇型三萜是在多科植物中广泛存在的具有多羟基取代的齐墩果烷型三萜类成分。由于多羟基基团的存在,在植物次生代谢过程中,导致这类成分广泛存在不同种类酰基和糖的取代,使得玉蕊醇型三萜类化合物具有多种生物活性。玉蕊醇型三萜具有显著的抗肿瘤及改善学习记忆等作用,其在治疗肿瘤及老年退行性疾病如阿尔茨海默病方面具有极大的开发应用前景。结合文献对玉蕊醇型三萜的结构特征、波谱规律和药理活性等方面进行详细的总结,为这类化学成分的开发及应用提供重要的基础。     

Immunomodulatory effects and structure-activity relationship of botanical pentacyclic triterpenes: A review

Botanical pentacyclic triterpenes possessed a broad range of pharmacological activities such as antioxidant, anti-tumor, anti-microbial and anti-inflammatory activities. It is believed that the mechanisms involved in these bioactivities are due to the modulation of immune system. Recently, the pharmacological validation on immunomodulatory of pentacyclic triterpenes derived from higher plants is very limited and several existence review papers related for this group of compound have not been focused for this activity. In this review, we have highlighted several studies on immunomodulatory potential of botanical pentacyclic triterpenes isolated from wide array of different species of medicinal plants and herbs based on various preclinical in vitro and animal models. This review also attempts to discuss on bioactivities of compouns related with their structure-activity relationship. Hence, the evaluation of pentacyclic triterpenes offers a great opportunity to discover adjuvants and novel therapeutic agents that presented beneficial immunomodulatory properties.     

Differentiation- and apoptosis-inducing activities by pentacyclic triterpenes on a mouse melanoma cell line

In a study to investigate the relationship between the chemical structure and the differentiation-inducing activity of pentacyclic triterpenes, several lupane, oleanane, and ursane triterpenes were prepared and their effects on B16 2F2 melanoma cell differentiation and growth were examined. Eleven lupane triterpenes used in this study acted on the melanoma cells as a melanogen, but no induction of melanogenesis of B16 2F2 cells by oleanane and ursane was detected. The differences at C-17 of the lupane series and acetylation of the OH group at C-3 did not markedly influence their activities. However, the ED(50) value for up-regulation of melanin biosynthesis was markedly decreased by the oxidation of the OH group at C-3 of lupeol (1). Betulinic acid (11), its methyl ester (12), lup-28-al-20(29)-ene-3beta-ol (9), and lup-28-al-20(29)-en-3-one (10) inhibited B16 2F2 cell proliferation by induction of apoptosis. These findings suggested that the carbonyl group at C-17 might be essential for the apoptotic effects of these compounds on B16 2F2 cells.     

金粉蕨属植物化学成分及药理作用研究进展

了解金粉蕨属植物化学成分及药理作用的研究状况。通过对近年来金粉蕨属植物研究的文献分析,对该属植物的化学与药理进行分类整理。目前,从金粉蕨属植物中分离得到近30多个化学成分,包括黄酮、倍半萜和酚类等结构类型;药理作用研究表明,栗柄金粉蕨和野鸡尾金粉蕨提取物具有解毒、解痉作用;金粉蕨素和瓦利希毒苷在保护保护血管内皮细胞、抗癌、抗氧化等方面显示了较好的活性。该属一些植物提取物及其化合物在保护血管内皮细胞、抗癌、抗氧化、解毒、解痉等方面显示了较好的活性。开展金粉蕨属植物的研究,对发现新的药用活性成分有重要的意义。     

苦瓜化学成分的研究进展

系统回顾了近40年来苦瓜化学成分研究概况,着重介绍了国内外苦瓜中三萜、甾体及多肽等具显著生理活性的化学成分研究进展。苦瓜含有三萜、甾体类、生物碱、蛋白、有机酸及糖类等多种活性化学成分,具有降血糖、抗肿瘤、抗病毒及抗生育等多种药理活性。     

Ganodermataceae: natural products and their related pharmacological functions

The objective of this paper is to review the natural products and the pharmacological functions of Ganodermataceae family. Presently, studies on the bioactive components of Lingzhi are focused on polysaccharides and triterpenes/triterpenoids compounds. New Ganoderma polysaccharides, including their molecular weights, glycosyl residue compositions, glycosyl linkage and branches, are summarized in this paper. Also presented are new types of triterpenes and their characteristics from Lingzhi. Taking Ganoderma lucidum as an example, we reviewed its pharmacological functions in anti-tumor and immune-modulating activities for treating hypoglycemosis, hepatoprotection, and the effect on blood vessel system. Based on the advances in Lingzhi research in the past few decades, both G. lucidum and G. sinense are considered as the representative species of medicinal mushroom Lingzhi in China. Until 2001, G. tsugae was only advised to be used as the materials of the health products. The biologically-active components related to pharmacological functions of these three species were studied more than other Ganodermataceae family species; however, which have been used in less modern folk medicine.     

Triterpenoids from the floral spikes of Betula platyphylla var. japonica and their reversing activity against multidrug-resistant cancer cells

Four new triterpenes, together with 16 known triterpenes, were isolated from the floral spikes of Betula platyphylla var. japonica in a search for compounds capable of reversing multidrug resistance in cancer cells. The structures of the new triterpenes were elucidated as 3,4-seco-olean-4(23),13(18)-dien-3-oic acid (1), 3,4-seco-urs-4(23),20(30)-dien-3-oic acid (2), 3-O-methylmalonylepiocotillol II (6), and 3-O-methylmalonylcabraleahydroxylactone (16) by spectroscopic examination. The cytotoxicity of the isolated triterpenes against human cancer cell lines as well as multidrug-resistant cancer cell lines was evaluated. Most of the isolated triterpenes showed very weak cellular toxicities. Although no discernible differences were found in the cytotoxicities for the tested compounds against sensitive and resistant cell lines, the cytotoxicities for several triterpenes against multidrug-resistant cancer cell lines (KB-C2 or K562/Adr) were enhanced in the presence of nontoxic concentrations of colchicine or doxorubicin. Compound 10 reversed the cytotoxicity of colchicine against KB-C2 cells at 8.1 microM and showed comparable potency to 5 microM verapamil.     

Isolation of diacyl glycerol acyl transferase (DGAT) inhibitors from Pachydictyon coriaceum

The pharmacological inhibition of acyl CoA:diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) has emerged as a target for the treatment of obesity and type 2 diabetes. Chromatographic analysis of the brown alga, Pachydictyon coriaceum, led to the isolation of diterpene dictyol E and hydroxyisocrenulatin. Pharmacological assay of these compounds demonstrated DGAT inhibitory activity with IC₅₀ values of 46.0 μm and 23.3 μm , respectively. Copyright © 2011 John Wiley & Sons, Ltd.     

桂枝茯苓方治疗痛经、盆腔炎以及子宫肌瘤的活性成分和分子作用机制研究

该研究采用网络药理学的方法,探讨桂枝茯苓方治疗痛经、盆腔炎以及子宫肌瘤的主要活性成分和潜在的分子作用机制。药物-靶点网络特征分析显示分子网络度较高的多为甾醇类和五环三萜类化合物,它们在抗炎、解热镇痛、抗肿瘤以及免疫调节等方面具有较好的治疗作用;另一方面网络度较高的靶点多与炎症反应、凝血系统、血管形成、平滑肌收缩以及细胞增殖等环节有关。进一步的靶点-通路网络分析结果显示这些靶点与调控子宫平滑肌增殖、抑制子宫内新生血管形成、改善血液循环、降低性激素分泌、缓解子宫平滑肌收缩、抑制花生四烯酸代谢以及其他炎症反应等6个环节密切相关,从而揭示出其治疗痛经、盆腔炎以及子宫肌瘤的主要分子机制。该研究表明桂枝茯苓方可通过多个活性成分作用于多个靶点,调控21条生物通路,来治疗盆腔炎、痛经及子宫肌瘤。     

Chemical constituents and pharmacological activities of medicinal plants from Rosa genus

The genus Rosa (Rosaceae family) includes about 200 species spread in the world, and this genus shows unique advantages in medicine and food. To date, several scholars concentrated on compounds belonging to flavonoids, triterpenes, tannins, polysaccharide, phenolic acids, fatty acids, organic acids, carotenoids, vitamins. Pharmacological effects such as antineoplastic and anti-cancer properties, anti-inflammatory, antioxidant, liver protection, regulate blood sugar, antimicrobial activity, antiviral activity, as well as nervous system protection and cardiovascular protection were wildly reported. This article reviews the chemical constituents, pharmacological effects, applications and safety evaluations of Rosa plants, which provides a reference for the comprehensive utilization of medicine and food resources and gives a scientific basis for the development of medicinal plants of the genus Rosa.