黄根化学成分的研究

目的:研究黄根Prismatomeris tetrandra的化学成分。方法:通过反复的硅胶柱色谱进行分离纯化,根据理化性质和光谱数据进行结构鉴定。结果:分离并鉴定了6个化合物:1-羟基-2-甲基蒽醌(Ⅰ),2-羟基-3-甲氧基蒽醌(Ⅱ),1,3-二羟基-2-甲氧基蒽醌(Ⅲ),甲基异茜草素(Ⅳ),甲基异茜草素-1-甲醚(Ⅴ)和β-谷甾醇(Ⅵ)。结论:化合物Ⅰ,Ⅱ和Ⅲ为首次从黄根中分离得到。     

黄根中的蒽醌苷成分(英文)

目的:对黄根中的蒽醌苷类化合物及其细胞毒活性进行研究。方法:采用大孔吸附树脂柱、硅胶柱、凝胶柱及反相柱色谱法分离单体化合物,根据波谱技术鉴定结构,采用MTT法进行细胞毒活性测定。结果:从黄根乙醇提取物的正丁醇部分离得到6个蒽醌苷类化合物,1-O-methylrubiadin 3-O-β-primeveroside(1),damnacanthol 3-O-β-primeveroside(2),rubiadin3-O-β-primerveroside (3),lucidin 3-O-β-primeveroside(4),1,3-dihydroxy-2-(methoxymethyl) anthraquinone 3-O-β-primerveroside (5)and digiferruginol ω-gentiobiose(6)。结论:化合物16均为首次从该植物中分离得到,蒽醌成苷后生物活性减弱。     

决明子蒽醌类化学成分研究

决明子为豆科植物决明 Cassia obtusifolia L.或小决明 C.tora L.的干燥成熟种子 ,为临床常用中药。现代研究证明决明子具有降血压 ,调血脂 ,保肝及抑菌等活性 ,同时又可作为食品 ,是保健饮料的良好原料。决明子在我国资源丰富 ,不仅具有广泛的药用价值 ,而且还是一味较好的保健药品 ,对许多疾病均有较好的治疗作用。但其有效成分和作用机制并不十分清楚 ,所以深入研究其有效成分 ,对进一步开发利用决明子具有重要的意义。作者对其化学成分进行了系统研究 ,从中得到6个蒽酯类化合物 ,通过化学和波谱分析 ,分别鉴定为大黄酚 ( chrysophanol…     

何首乌蒽醌类化学成分研究

何首乌为蓼科植物何首乌Polygonum multiflo-rum Thunb.的干燥块根,为常用中药。现代研究发现何首乌含有二苯乙烯苷类、蒽醌类、黄酮类等多种成分[1],具有抗衰老、增强免疫力、抗菌、调血脂等多方面的药理作用[2]。我国植物资源丰富,分布于东北、中南、华东、西南各省。国内外学者对四川和广东产的何首乌进行了较多的研究,为了更好的开发和利用植物资源,进一步寻找活性成分,笔者对采自泰山的何首乌化学成分进行了系统的研究,从中得到9个蒽醌类化合物,分别鉴定为大黄素(emodin,)、大黄素甲醚(physcion,)、拟石黄衣醇(迷人醇,fallacinol,)、…     

黄根的生药鉴定

本文对黄根进行了药材性状、显策特征及紫外吸收光谱测定研究,为鉴别其真伪提供依据。     

对叶豆蒽醌类化学成分的研究

目的:分离鉴定对叶豆(Cassia alata L.)中的化学成分,为其药效物质研究奠定基础。方法:采用溶剂萃取、正相硅胶色谱、凝胶色谱等方法进行分离;应用1D-NMR、2D-NMR、IR、UV、MS等谱学方法进行结构鉴定。结果:分离得到11个化合物:大黄酸、芦荟大黄素、大黄素、芦荟大黄素-8-O-β-D-葡萄糖苷、芦荟大黄素-3-(羟甲基)-O-β-葡萄糖苷、-生育酚、羽扇豆-20(29)-烯-3-酮、β-谷甾醇、2-乙基-3-甲基-马来酸酐、邻二甲氧基对羟基-E-肉桂酸、2,3-二乙酰基丁四醇分别鉴定。结论:除前三个化合物1、2和3外,其余8个化合物均是首次从对叶豆中分离得到。     

对叶豆蒽醌类化学成分的研究

目的：分离鉴定对叶豆（Cassia alata L．）中的化学成分，为其药效物质研究奠定基础。方法：采用溶剂萃取、正相硅胶色谱、凝胶色谱等方法进行分离；应用1D—NMR、2D—NMR、IR、UV、MS等谱学方法进行结构鉴定。结果：分离得到11个化合物：大黄酸、芦荟大黄素、大黄素、芦荟大黄素-8-O—β—D-葡萄糖苷、芦荟大黄素-3-（羟甲基）-O-β-葡萄糖苷、-生育酚、羽扇豆-20（29）-烯-3-酮、β-谷甾醇、2-乙基-3-甲基-马来酸酐、邻二甲氧基对羟基-E-肉桂酸、2，3-二乙酰基丁四醇分别鉴定。结论：除前三个化合物1、2和3外，其余8个化合物均是首次从对叶豆中分离得到。     

决明子中游离蒽醌类化学成分研究

目的:研究决明子中的游离蒽醌类化学成分.方法:采用各种现代色谱方法对决明子进行提取分离,并运用1H-NMR和13C-NMR波谱方法鉴定其结构. 结果:分离鉴定了8个化合物,分别为橙钝叶决明素(1)、甲基钝叶决明素(2)、大黄素(3)、钝叶素(4)、 Questin(5)、2-hydroxyemodin-1-methyl ether(6)、大黄酚(7)、大黄素甲醚(8).结论:其中化合物6为首次从决明Cassia obtusifolia中分离得到,化合物4、5为首次对其波谱数据进行了全归属.     

红大戟中的蒽醌类化学成分

目的:研究茜草科红芽大戟属植物红大戟根的化学成分,并对其在多种体外药理模型上进行了活性筛选.方法:运用硅胶、Sephadex LH-20柱色谱和制备薄层色谱等方法进行分离和纯化,通过理化性质和NMR,MS等波谱数据鉴定化合物的结构;在细胞水平模型上,筛选化合物在抗氧化、抗HIV、神经细胞保护及肿瘤细胞毒等方面的活性.结果:从95％乙醇提取物中分离鉴定了21个蒽醌类化合物,包括去甲虎刺醛(1)、1,3-二羟基-2-乙氧甲基-9,10-蒽醌(2)、甲基异茜草素(3)、虎刺醇(4)、1,3,5-三羟基-2-乙氧甲基-6-甲氧基-9,10-蒽醌(5)、3-羟基巴戟醌(6)、红大戟素(7)、1,3,5-三羟基-2-甲酰基-6-甲氧基-9,10-蒽醌(8)、芦西丁(9)、异茜草素(10)、1,3-二羟基-2-甲氧基-9,10-蒽醌(11)、1,3-二羟基-2-甲氧甲基-9,10-蒽醌(12)、1-羟基-2-羟甲基-9,10-蒽醌(13)、3-羟基-2-甲基-9,10-蒽醌(14)、3-羟基-1-甲氧基-2-甲基-9,10-蒽醌(15)、1,3-二羟基-2-乙氧甲基-6-甲氧基-9,10-蒽醌(16)、1,3,6-三羟基-2-甲基-9,10-蒽醌(17)、1,3-二羟基-2-羟甲基-6-甲氧基-9,10-蒽醌(18)、1,3,6-三羟基-2-甲氧甲基-9,10-蒽醌(19)、3,6-二羟基-2-羟甲基-9,10-蒽醌(20)和1,6-二羟基-2-甲基-9,10-蒽醌(21).在1.0×10-5 mol·L-1浓度下,在肿瘤细胞(MTT法,HCT-8,Bel7402,BGC-823,A549,A2780)、去血清和谷氨酸损伤神经细胞、Fe2 -Cys诱导大鼠肝微粒体丙二醛生成和小鼠腹腔巨噬细胞分泌NO模型,以及抗HIV( VSVG/HIV-luc)和抗糖尿病(PTPB酶抑制)模型上,以上化合物均未显示出显著活性.结论:化合物9～21为首次从本属植物中分离得到.     

Biological activity of Anthraquinones and Triterpenoids from Prismatomeris fragrans

A new 1,3-dihydroxy-2-methyl-5,6-dimethoxyanthraquinone (1); six known anthraquinones, nordamnacanthal (2), damnacanthal (3), rubiadin (4), rubiadin-1-methyl ether (5), lucidin-ω-methyl ether (6), and 1-hydroxy-2-hydroxymethyl-3-methoxyanthraquinone (7); a β-sitosterol (8); together with two known triterpenoids, β-acetylolean-12-en-28-olic acid (9), and 3β-O-acetyl-11,12-epoxyolean-28,13-olide (10) were isolated from the roots and stems of Prismatomeris fragrans. Their structures were established on the basis of spectral data. This is the first isolation of compounds 2, 6, 7, 9 and 10 from Prismatomeris genus. The isolated compounds were evaluated in antiplasmodial, antituberculosis, antifungal and anticancer cell lines tests. The bioactivity assays showed that only 9 exhibited moderate antimalarial activity, 2 and 3 exhibited antifungal activity while 2, 3, 4, 7 and 9 showed antituberculosis activity. In addition, compounds 2, 3 and 7 exhibited cytotoxicity to BC cell line while 1, 1a (the methyl ether derivative of 1), 2, 3, 4, 5, and 9 exhibited cytotoxicity to NCI-H187 cell line.     

Effects of Rubiadin isolated from Prismatomeris connata on anti‐hepatitis B virus activity in vitro

Prismatomeris connata was a kind of Rubiaceae plant for treatment of hepatitis, hepatic fibrosis and silicosis. Whereas, the effective components of Prismatomeris connata remains unexplored. The aim of this study was to investigate the inhibitory effects and mechanisms of Rubiadin isolated from Prismatomeris connata against HBV using HepG2.2.15 cells. The levels of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and hepatitis B core antigen (HBcAg) in the supernatants or cytoplasm were examined using by enzyme‐linked immunosorbent assay. HBV DNA was qualified q‐PCR. Rubiadin was isolated by silica gel column. The structure of the compound was elucidated by HPLC, FT‐IR, ¹H‐NMR, ¹³C‐NMR and identified as 1,3‐Dihydroxy‐2‐methyl‐9, 10‐anthraquinone. Rubiadin significantly decreased HBeAg,HBcAg secretion level and inhibit HBV DNA replication. Rubiadin inhibits the proliferation of the cells and HBx protein expression in a dose‐dependent manner. The intracellular calcium concentration was significantly reduced. These results demonstrated that Rubiadin could inhibit HepG2.2.15 cells proliferation, reduce the level of HBx expression, and intracellular free calcium, which might become a novel anti‐HBV drug candidate.     

Longipinane derivatives from Stevia connata

The hexane extracts of the roots of Stevia connata afforded three new longipinene derivatives, longipinane-7beta,8alpha, 9alpha-triol-1-one 7-angelate-8-methylbutyrate (1), longipin-2-ene-7beta,8alpha,9alpha-triol-1-one 8,9-diangelate (6), and longipin-2-ene-7beta,8alpha,9alpha-triol-1-one 8-angelate-9-methylbutyrate (8), together with the known longipinane-7beta,8alpha,9alpha-triol-1-one 8,9-diangelate (2), longipinane-7beta,8alpha,9alpha-triol-1-one 7,9-diangelate (3), longipinane-7beta,8alpha,9alpha-triol-1-one 7,8-diangelate (4), longipin-2-ene-7beta,8alpha,9alpha-triol-1-one 7,8-diangelate (5), longipin-2-ene-7beta,8alpha,9alpha-triol-1-one 7-angelate-8-methylbutyrate (12), and stigmasterol. The structures of the new compounds were determined by chemical transformations and spectral methods including 2D NMR measurements. Spontaneous intramolecular transesterifications starting from the 8-angelate-9-methylbutyrate 8 provided an equilibrated mixture of the 7-angelate-9-methylbutyrate 10, the 7-angelate-8-methylbutyrate 12 and the starting material when stored in MeOH-H(2)O solution, while the 8,9-diangelate 6 only provided a binary mixture of the 7, 9-diangelate 7 and the starting material under the same conditions. The structures of 6-8, 10, and 12 and those of the nonisolable reaction intermediates 9, 11, and 14 were further evaluated by AM1 semiempirical calculations.     

黄根醇提物对四氯化碳所致大鼠肝纤维化的保护作用

目的研究黄根醇提物对四氯化碳所致大鼠肝纤维化的保护作用。方法大鼠首次于背部皮下注射纯CCl4 5ml／k，以后每周2次注射40％（V/V）CCl4花生油3ml／kg，连续注射8周。8周后取血，计算大鼠的肝脾指数，检测大鼠血清中ALT，AST的活性及其总蛋白（TP）、白蛋白（Alb）的含量，计算白蛋白与球蛋白的比值；检测血清中透明质酸（HA）、层黏连蛋白（LN）、Ⅲ型前胶原（PcⅢ）、Ⅳ型胶原（CⅣ）的含量；检测肝脏组织中超氧化物歧化酶（SOD）活性、羟脯氨酸（Hyp）含量、丙二醛（MDA）和谷胱甘肽过氧化物酶（GSH—Px）水平。结果黄根醇提物能明显降低CCl4所致的大鼠肝纤维化肝脾指数的升高（P〈0．01）和血清中ALT，AST活性的升高（P〈0．01），降低血清中HA，LN，PCⅢ，CIV，GLB的含量（P〈0．01），升高血清中的TP，ALB含量和A／G的比值（P〈0．01）；降低肝组织中MDA的水平和Hyp的含量（P〈0．01），亦能升高肝组织中SOD的活性和GSH—Px的水平（P〈0．01）。结论黄根醇提物具有显著的抗肝纤维化的作用。     

大黄游离蒽醌的制备与纯化

从中药大黄中提取总蒽醌（结合和游离２类）,经水解后用水化学试剂或大孔树脂制备总游离蒽醌（含大黄素、大黄酸、芦荟大黄素、大黄酚和大黄素甲醚）,进一步纯化得大黄酸和大黄素。     

Anthraquinones from Polygonum cuspidatum as tyrosinase inhibitors for dermal use

Four anthraquinones, physcion (1), emodin (2), citreorosein (3) and anthraglycoside B (6), and two stilbenes, resveratrol (4), and piceid (5), were isolated previously from the root of Polygonum cuspidatum. These bioactive compounds were examined for their antityrosinase potency. No antityrosinase activity was detected with treatment using stilbenes. On the other hand, the anthraquinones showed moderate to strong inhibition of tyrosinase. Physcion exhibited the most potent tyrosinase inhibition among the four anthraquinones examined, which was comparable to kojic acid. The ability of anthraquinones to permeate the skin was also examined. Based on the same thermodynamic activity, physcion showed a higher permeation compared with emodin (48-fold), suggesting it as a potent candidate for dermal use. As naturally occurring tyrosinase inhibitors, anthraquinones from P. cuspidatum may be useful as skin-whitening agents to inhibit tyrosinase for dermal use.     

CO2-超临界流体萃取大黄中蒽醌类成分的工艺研究

目的确定采用CO2-超临界流体法提取大黄中蒽醌类成分的最佳工艺。方法采用正交试验法结合单因素考察法,优选出CO2-超临界流体萃取最佳提取条件,确定最佳工艺。结果确定CO2-超临界流体最佳提取条件为40℃条件下,维持20Mpa压力2h,并以75％乙醇为夹带剂。结论本实验优选的提取工艺合理,CO2-超临界流体萃取法可以用于大黄中葸醌类成分的提取。     

狼毒大戟萜类和蒽醌类化合物的分离鉴定

从狼毒大戟根中首次分得两个萜类化合物和一个蒽醌类化合物,经物理常数和光谱分析鉴定为boehmerone(Ⅰ)、16α,17-二羟基阿替生-3-酮(ent-16α,17-dihydroxy-atisan-3-one,Ⅱ)和大黄素甲醚(physcion,Ⅲ)。