狭苞橐吾中一个新的艾里莫芬烷型倍半萜

利用各种色谱分离技术,从狭苞橐吾Ligularia intermedia地上部分75%乙醇提取物中分离得到4个化合物,通过理化数据和波谱数据鉴定化合物的结构分别为（3aR,4R,5S,7S,7aS）-2-acetyl-7,7a-dihydroxy-3a,4-dimethyl-3a,4,5,6,7,7a-hexahydro-3H-inden-5-yl acetate（1）,10β-羟基-艾里莫芬-7（11）-烯-12,8α-内酯（2）,β-谷甾醇（3）和β-胡萝卜苷（4）。其中化合物1为新的降二碳艾里莫芬烷型倍半萜。     

黑骨藤中神经酰胺类化学成分

目的: 研究黑骨藤化学成分. 方法: 采用反复硅胶柱色谱法、Sephadex LH-20柱色谱法等进行分离纯化,并通过理化常数测定和质谱、一维、二维核磁共振等波谱方法分析鉴定其化学结构. 结果: 从黑骨藤中分离鉴定了2个神经酰胺类化合物,分别为1-O-β-D-葡萄糖-(2S, 3S, 4R, 10E)-2-[(2R)-2-羟基二十四烷酰氨基]-10-十八烷-3, 4-二醇(1),(2S, 3S, 4R, 10E)-2-[(2R)-2-羟基二十四烷酰氨基]-10-十八烷-1, 3, 4-三醇(2). 结论: 所有化合物均首次从黑骨藤中分离得到,采用二维核磁技术确定化合物2的结构,并对其二维谱数据进行归属.     

鬼针草化学成分研究

对鬼针草Bidens bipinnata中的化学成分进行研究,筛选具有抗肝纤维化活性单体。采用大孔树脂、硅胶、MCI树脂、Sephadex LH-20等方法进行分离纯化,得到15个化合物,并运用波谱技术测试,鉴定其结构为槲皮素（1）,槲皮素-3-O-α-L-鼠李糖苷（2）,紫云英苷（3）,山柰酚-3-O-α-L-鼠李糖苷（4）,5,3’-二羟基-3,6,4’-三甲氧基-7-O-β-D-吡喃葡萄糖苷黄酮（5）,7,8,3’,4’-四羟基二氢黄酮（6）,（R/S）-异奥卡宁-7-O-β-D-葡萄糖苷（7）,（R/S）-异奥卡宁-3’-甲氧基-7-O-β-D-葡萄糖苷（8）,6,7,3’,4’-四羟基橙酮（9）,海生菊苷（10）,6,7-二羟基香豆素（11）,3-咖啡酸酰基-2-甲基-D-赤藓糖酸-1,4内酯（12）,（7S,8R）苯并二氢呋喃新木脂素-4-O-β-D-葡萄糖苷（13）,丁香酚-O-β-D-呋喃芹糖-（1"-6’）-O-β-D-吡喃葡萄糖苷（14）,（+）丁香脂素-4-O-β-D-吡喃葡萄糖苷（15）。其中化合物8,13~15为首次从本属植物中分离得到。在初步的活性筛选中化合物 1,6有较强体外抑制肝星状细胞增殖的能力;化合物1,2,6,7有较强体外抑制腹腔巨噬细胞分泌炎症因子的能力。     

美洲刺人参酚类化学成分研究

利用正向硅胶、反相硅胶、Sephadex LH-20和制备液相色谱等多种分离技术进行分离纯化,依据理化性质和波谱数据鉴定结构,从美洲刺人参Oplopanax horridus的根皮醇提物乙酸乙酯和正丁醇萃取部位分离并鉴定了16个酚类化合物,其中7个苯丙素类成分阿魏酸（1）,3-乙酰咖啡酸（2）,咖啡酸（3）,3-甲氧基二氢肉桂醇-4-O-β-D-葡萄糖苷（4）,3-羟基二氢肉桂醇-4-O-β-D-葡萄糖苷（5）,3,5-二甲氧基肉桂醇-4-O-β-D-葡萄糖苷（6）,3-甲氧基肉桂醇-4-O-β-D-葡萄糖苷（7）;3个香豆素类成分,东莨菪内酯（8）,6,7-二羟基香豆素（9）,反式-3’-当归酰基-4’-乙酰基角型吡喃香豆素（10）;6个木脂素类成分,（+）-异落叶松脂素9’-O-β-D-葡萄糖苷（11）,3,3’-二甲氧基-4,9,9’-三羟基-4’,7-环氧-5’,8-木脂素-4,9-O-β-D-二葡萄糖苷（12）,（+）-5,5’-二甲氧基落叶松脂素 4’-O-β-D-葡萄糖苷（13）,（-）-5,5’-二甲氧基落叶松脂素 4’-O-β-D-葡萄糖苷（14）,（-）-松脂醇 4’-O-β-D-葡萄糖苷（15）,（±）-5,5’-二甲氧基落叶松脂素 9’-O-β-D-葡萄糖苷（16）。所有化合物均为首次从该植物中分离得到,除化合物4,6,12和13外,其余化合物均为首次从该属植物中报道。     

多刺锦鸡儿化学成分研究

目的:研究多刺锦鸡儿Caragana spinifera全草的化学成分。方法:采用硅胶柱色谱等方法分离化合物,采用理化性质和波谱分析法鉴定其结构。结果:分离并鉴定了6个化合物,分别为(6aR,11aR)-3-羟基-4,9-二甲氧基紫檀烷(1),(6aR,11aR)-4,9-二羟基-3-甲氧基紫檀烷(2),5,4′-二羟基-7-甲氧基异黄酮(3),7-羟基-4′-甲氧基异黄酮(4),6,7-二羟基-4′-甲氧基异黄酮(5),β-谷甾醇(6)。其中化合物1的结构还得到X-ray单晶衍射的证实。结论:化合物1~6均首次从该植物中分离得到。     

云南独蒜兰的化学成分研究

采用正、反相硅胶柱色谱,凝胶柱色谱,薄层制备及高效液相色谱等分离方法,对中药山慈菇来源之一——云南独蒜兰假鳞茎的乙醇提取物的乙酸乙酯萃取部位的化学成分进行了研究,分离得到14个化合物,其中二氢菲类5个,联苄类4个,三萜类2个,苯丙酸类3个;根据化合物的理化性质与波谱数据分别鉴定为4,7-二羟基-2-甲氧基-9,10-二氢菲（1）,4,7-二羟基-1-（p-羟苄基）-2-甲氧基-9,10-二氢菲（2）,（2,3-trans）-2-（4-hydroxy-3-methoxyphenyl）-3-hydroxymethyl-10-methoxy-2,3,4,5-tetrahydro-phenanthro [2,1-b]furan-7-ol（3）,pleionesin B（4）,blestriarene A（5）,山药素Ⅲ（6）,3,3’-二羟基-2-（p-羟苄基）-5-甲氧基联苄（7）,3’,5-二羟基-2-（p-羟苄基）-3-甲氧基联苄（8）,3,3’-二羟基-2,6-二（p-羟苄基）-5-甲氧基联苄（9）,triphyllol（10）,pholidotin（11）,对羟基反式桂皮酸（12）,反式阿魏酸（13）,反式阿魏酸二十六烷基酯（14）。化合物 5,10~14 为首次从独蒜兰属分离得到。     

白英中的倍半萜类化合物

采用硅胶柱色谱、Sephadex LH-20柱色谱及制备薄层等方法对白英中的倍半萜进行分离纯化,根据理化性质和波谱数据鉴定其化学结构,发现并鉴定了10个倍半萜,分别为1β-羟基-1,2-二氢-α-山道年（1）,boscialin（2）,布卢门醇C（3）,3β-hydroxy-5α,6α-epoxy-7-megastigmen-9-one（4）,去氢催吐萝芙木醇（5）,布卢门醇 A（6）,（1'S,2R,5S,10R）-2-（1',2'-dihydroxy-1'-methylethyl）-6,10-dimethylspiro[4,5] dec-6-en-8-one（7）,（1'R,2R,5S,10R）-2-（1',2'-dihydroxy-1'-methylethyl）-6,10-dimethylspiro [4,5] dec-6-en-8-one（8）,2-（1',2'-dihydroxy-1'-methylethyl）-6,10-dimethyl-9-hydroxyspiro [4,5] dec-6-en-8-one（9）,蚱蜢酮（10）。10个倍半萜均为首次从白英中发现。     

杜鹃兰假鳞茎化学成分研究

为了研究杜鹃兰Cremastra appendiculata干燥假鳞茎95%乙醇提取物的化学成分,采用多种色谱方法进行分离纯化,通过波谱数据及核对文献鉴定化合物结构。从其石油醚和乙酸乙酯萃取部位分离得到13个化合物,分别是4,4’-二甲氧基-9,9’10,10’-四氢-（1,1’-双菲）-2,2’,7,7’-四醇（1）,4,4’,7,7’-四羟基-2,2’-二甲氧基-1,1’-双菲（2）,3,5-二羟基-2,4-二甲氧基菲（3）,大黄素甲醚（4）,大黄酚（5）,大黄素（6）,芫花素（7）,槲皮素（8）,槲皮素3’-O-β-D-吡喃葡萄糖苷（9）,3-甲氧基-4-羟基苯乙醇（10）,丁香酸（1）,香草醛（12）,对羟基苯甲醛（13）。化合物 1~3,5~12 为首次从该属植物中分离得到。     

贡山八角中的倍半萜类成分

目的 对贡山八角Illicium wardii种子的化学成分进行研究。方法 采用桂胶色谱柱、Sephadex LH-20色谱柱、MCI色谱柱等方法进行分离纯化,根据化合物的理化性质和波谱数据鉴定其结构。结果 从贡山八角种子的95%乙醇提取物中分离得到11个倍半萜类化合物,分别鉴定为八角醇C(1)、7,8-epoxy-1(12)-caryophyllene-9β-ol(2)、merrilliortholactone(3)、2α-羟基新莽草毒素(4)、2,6-dihydroxyhumlan-9(E)-3(12),7(13),9-trien(5)、莽草毒素(6)、伪大八角素(7)、8α-hydroxy-10-deoxycyclomerrillianolide(8)、2α-羟基莽草毒素(9)、rel-5-(3S,8S-dihydroxy-1R,5S-dimethyl-7-oxa-6-oxobicyclo-[3,2,1]-oct-8-yl)-3-methyl-2Z,4E-pentadienoic acid(10)、菜豆酸(11)。结论 化合物1为新化合物,命名为八角醇C;其他化合物均为首次从该植物中分离得到。     

接骨木根皮的化学成分研究(I)

目的 研究接骨木Sambucus williamsii根皮的化学成分。方法 采用硅胶、ODS、制备液相等分离方法对化合物进行分离,通过核磁共振和质谱等波谱数据鉴定化合物结构。结果 从接骨木根皮95%乙醇提取部位中分离得到18个化合物,分别鉴定为7α-乙氧基莫诺苷（1）、7β-乙氧基莫诺苷（2）、去氢莫诺苷（3）、马钱子苷（4）、7-脱氢马钱子苷（5）、7-甲酸裂环马钱子苷（6）、獐牙菜苷（7）、松柏醇-9-O-β-D-葡萄糖苷（8）、3-甲氧基-4-（2-丙三醇氧基）-苯丙醇（9）、（7R,8R）-7,8-二氢-9'-羟基-3'-甲氧基-8-羟甲基-7-（4-羟基-3-愈创木基）-1'-苯骈呋喃丙醇-9'-O-β-D-吡喃葡萄糖苷（10）、（7R,8R）-4,7,9,9'-四羟基-3-甲氧基-8-O-4'-新木脂素-3'-O-β-D-吡喃葡萄糖苷（苏式）（11）、（7R,8R）-3-甲氧基-8,4'-氧新木脂素-3',4,7,9,9'-戊醇（苏式）（12）、5-（1'-羟乙基）-烟酸甲酯（13）、3-（羟乙酰基）吲哚（14）、4'-羟基-N-（4-羟基-3-甲氧基苯甲酰基）-3',5'-二甲氧基苯甲酰胺（15）、3-甲氧基-1H-吡咯（16）、（1S,3S）-1-甲基-1,2,3,4-四氢-β-咔啉-3-羧酸（17）、丁香酸-4-O-α-L-鼠李糖（18）。结论 化合物8～10、13～17是从忍冬科植物中首次分离得到,1～4、6、11、18是首次从接骨木属中分离得到。     

α-Glucosidase inhibitory activity of selected Philippine plants

Ethnopharmacological relevance

Antidesma bunius Spreng. (Phyllantaceae), Averrhoa bilimbi L. (Oxalidaceae), Biophytum sensitivum (L.) DC. (Oxalidaceae), Ceriops tagal (Perr.) C.B. Rob. (Rhizophoraceae), Kyllinga monocephala Rottb. (Cyperaceae), and Rhizophora mucronata Lam. (Rhizophoraceae) are used as remedies to control diabetes. In the present study, these plants were screened for their potential α-glucosidase inhibitory activity.

Materials and methods

The 80% aqueous ethanolic extracts were screened for their α-glucosidase enzyme inhibitory activity using yeast alpha glucosidase enzyme.

Results

Except for A. bilimbi with IC₅₀ at 519.86±3.07, all manifested a significant enzyme inhibitory activity. R. mucronata manifested the highest activity with IC₅₀ at 0.08±1.82 μg mL⁻¹, followed by C. tagal with IC₅₀ at 0.85±1.46 μg mL⁻¹ and B. sensitivum with IC₅₀ at 2.24±1.58 μg mL⁻¹.

Conclusion

This is the first report on the α-glucosidase inhibitory effect of the six Philippine plants; thus, partly defining the mechanism on why these medicinal plants possess antidiabetic properties.     

European medicinal polypores – A modern view on traditional uses

Ethnopharmacological relevance

In particular five polypore species, i.e. Laetiporus sulphureus, Fomes fomentarius, Fomitopsis pinicola, Piptoporus betulinus, and Laricifomes officinalis, have been widely used in central European folk medicines for the treatment of various diseases, e.g. dysmenorrhoea, haemorrhoids, bladder disorders, pyretic diseases, treatment of coughs, cancer, and rheumatism. Prehistoric artefacts going back to over 5000 years underline the long tradition of using polypores for various applications ranging from food or tinder material to medicinal–spiritual uses as witnessed by two polypore species found among items of Ötzi, the Iceman. The present paper reviews the traditional uses, phytochemistry, and biological activity of the five mentioned polypores.

Materials and methods

All available information on the selected polypore taxa used in traditional folk medicine was collected through evaluation of literature in libraries and searches in online databases using SciFinder and Web of Knowledge.

Results

Mycochemical studies report the presence of many primary (e.g. polysaccharides) and secondary metabolites (e.g. triterpenes). Crude extracts and isolated compounds show a wide spectrum of biological properties, such as anti-inflammatory, cytotoxic, and antimicrobial activities.

Conclusions

The investigated polypores possess a longstanding ethnomycological tradition in Europe. Here, we compile biological results which highlight their therapeutic value. Moreover, this work provides a solid base for further investigations on a molecular level, both compound- and target-wise.     

真菌的中药干预研究近5年进展

近年来真菌感染率逐年上升,传统抗真菌药物易产生耐药性,而中药在防治真菌感染方面具有一定的优势。本文就近5年来中药对白念珠菌、皮肤癣菌、曲霉菌、马拉色菌、串珠镰孢菌、申克孢子丝菌、新生隐球菌及真菌生物膜的干预研究进展进行综述。     

Antiplasmodial activity of extracts from seven medicinal plants used in malaria treatment in Cameroon

Aim of the study

In a search for new plant-derived biologically active compounds against malaria parasites, we have carried out an ethnopharmacological study to evaluate the susceptibility of cultured Plasmodium falciparum to extracts and fractions from seven Cameroonian medicinal plants used in malaria treatment. We have also explored the inhibition of the Plasmodium falciparum cysteine protease Falcipain-2.

Materials and methods

Plant materials were extracted by maceration in organic solvents, and subsequently partitioned or fractionated to afford test fractions. The susceptibility of erythrocytes and the W2 strain of Plasmodium falciparum to plant extracts was evaluated in culture. In addition, the ability of annonaceous extracts to inhibit recombinant cysteine protease Falcipain-2 was also assessed.

Results and discussion

The extracts showed no toxicity against erythrocytes. The majority of plant extracts were highly active against Plasmodium falciparumin vitro, with IC₅₀ values lower than 5 μg/ml. Annonaceous extracts (acetogenin-rich fractions and interface precipitates) exhibited the highest potency. Some of these extracts exhibited modest inhibition of Falcipain-2.

Conclusion

These results support continued investigation of components of traditional medicines as potential new antimalarial agents.     

列当属、肉苁蓉属和草苁蓉属植物传统药物学调查

通过野外资源调查、整理各大标本馆标本原始记录和查阅文献记载等方法,系统整理、总结、归纳了列当属、肉苁蓉属和草苁蓉属民族药用植物种类、功效及民间使用情况,结果表明列当属6种药用植物在4个少数民族间作为7种民族药应用,草苁蓉属2种药用植物在8个少数民族间作为10种民族药应用,肉苁蓉属2种药用植物在3个少数民族间作为3种民族药应用,且同种药用植物常作不同民族药;发现3属植物的传统疗效主要集中在补肾壮阳、止血和止痛3个方面,并且该传统疗效与现代药理研究结果基本吻合。因此深入研究植物种类丰富的列当属植物资源对缓解肉苁蓉植物资源匮乏局面和扩大药源具有积极意义。     

金银花类药用植物IspE和IspH基因克隆和生物信息学分析

目的:克隆金银花类药用植物4-二磷酸胞苷-2-C-甲基赤藓糖激酶(4-diphosphocytidyl-2-C-methyl-D-erythritol kinase,IspE)和4-羟基-3-甲基-2-邻苯基二磷酸还原酶(4-hydroxy-3-methylbut-2-enyl diphosphate reductase,IspH)基因,并对其基因序列、蛋白特性和转录活性进行分析、比较.方法:从忍冬Lonicera japonica转录组测序结果中分析获得了IspE,IspH基因.分别以忍冬、红白忍冬L.japonica var.chinensis、红腺忍冬L.hypoglauca和水忍冬L.dasystyla新鲜花蕾为材料,利用RT-PCR技术克隆获得了4种金银花类药用植物IspE和IspH基因的全长cDNA.运用生物信息学分析软件,预测编码蛋白的结构和功能,并通过RT-PCR检测IspE和IspH在忍冬、红白忍冬、红腺忍冬、水忍冬花蕾中的转录情况.结果:金银花类药用植物IspE基因含有1个完整的开放阅读框,长度为1 221 bp,编码406个氨基酸;IspH含有一个完整的开放阅读框,长度为1 380 bp,编码459个氨基酸.IspE和IspH均为非分泌蛋白,均定位于叶绿体中.RT-PCR分析结果表明在忍冬、红腺忍冬和水忍冬的花蕾中IspE,IspH基因的转录水平没有显著差异,但红白忍冬花蕾中IspE,IspH基因的转录水平均显著高于忍冬.结论:克隆获得忍冬、红白忍冬、红腺忍冬和水忍冬中IspE,IspH基因,并证实了其在不同金银花类药用植物中的表达,为进一步研究IspE,IspH基因对萜类化合物生物合成和花香气以及颜色的影响奠定了基础.     

Comparative “in vitro” evaluation of the antiresorptive activity residing in four Ayurvedic medicinal plants. Hemidesmus indicus emerges for its potential in the treatment of bone loss diseases

Ethnopharmacological relevance

Four Indian plants, traditionally used in Ayurvedic medicine: Asparagus racemosus Willd., Emblica officinalis Gaertn., Hemidesmus indicus R. Br., and Rubia cordifolia L. were selected on the basis of their ethnobotanical use and of scientific evidence that suggests a potential efficacy in the treatment of bone-loss diseases. The antiresorptive properties of the four plants have been investigated. The aim was to provide adequate evidence for the exploitation of natural compounds as alternative therapeutics for the treatment of diseases caused by increased osteoclast activity.

Materials and methods

Decoctions were prepared from dried plant material according to the traditional procedure and standardization by HPLC was performed using marker compounds for each species. Total polyphenols, flavonoids and radical scavenging activity of the decoctions were also determined. The bioactivity of the plant decoctions was evaluated in subsequent phases. (1) A cytotoxicity screening was performed on the mouse monocytic RAW 264.7 cell line to define the concentrations that could be utilized in the following step. (2) The antiresorptive properties of plant decoctions were compared with that of a “gold standard” drug (alendronate) by measuring osteoclastogenesis inhibition and osteoclast apoptosis. (3) The toxic effect on bone forming cells was excluded by evaluating the impact on the proliferation of osteogenic precursors (mesenchymal stem cells, MSC).

Results

All the decoctions inhibited osteoclastogenesis similarly to alendronate at the highest doses, but Hemidesmus indicus and Rubia cordifolia were also effective at lower concentrations. Apoptosis increased significantly when cells were exposed to the highest concentration of Emblica officinalis, Hemidesmus indicus, and Rubia cordifolia. All concentrations of Emblica officinalis tested inhibited the proliferation of osteogenic precursors, while only the highest doses of Asparagus racemosus and Rubia cordifolia were toxic. On the contrary, Hemidesmus indicus did not affect osteogenic precursor growth at any concentration tested.

Conclusion

Among the medicinal plants included in the study, Hemidesmus indicus showed the greatest antiosteoclastic activity without toxic effect on osteogenic precursors. Therefore, Hemidesmus indicus exhibits the properties of an antiresorptive drug and represents the ideal candidate for further clinical investigations.     

泽漆化学成分

目的:研究大戟属植物泽漆的化学成分。方法:采用正相硅胶色谱、葡聚糖凝胶Sephadex LH-20、反相制备色谱等手段进行分离纯化,并通过理化性质和光谱数据进行结构鉴定。结果:从石油醚层和乙酸乙酯层中分离得到12个化合物,分别鉴定为大戟苷(Ⅰ)、大戟苷D(Ⅱ)、豆甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅲ)、胡萝卜苷(Ⅳ)、柚皮素(Ⅴ)、木犀草素(Ⅵ)、木犀草苷(Ⅶ)、4,2’,4’-三羟基查尔酮(Ⅷ)、山柰酚(Ⅸ)、槲皮素-3-O-β-D-半乳糖苷(Ⅹ)、咖啡酸(Ⅺ)和没食子酸乙酯(Ⅻ)。结论:化合物Ⅲ～Ⅶ为首次从该种植物中分离得到。     

贝母类药材湖北贝母Fritillaria hupehensis系统位置的探讨——来自ITS,rpl16,matK序列的证据

湖北贝母为传统中药,然而《Flora of China》将其基原植物湖北贝母Fritillaria hupehensis归并于天目贝母F.monantha项下。该实验采用分子系统学方法,以川百合Lilium davidii为外类群,用核基因ITS序列和叶绿体基因rpl16序列、matK序列等3个片段对湖北贝母及其近缘类群天目贝母F.monantha、安徽贝母F.anhuiensis等进行联合建树分析,对湖北贝母植物的系统位置进行了探讨,为湖北贝母药材的安全使用提供分子证据。结果显示,分子系统树上,3种贝母各自的居群聚为一支,之后天目贝母与安徽贝母聚为一支,最后与湖北贝母聚为一支。表明湖北贝母与天目贝母的亲缘关系可能要远于安徽贝母与天目贝母之间的关系,因此不适宜将湖北贝母归并于天目贝母。     

Antifungal activity of Brazilian medicinal plants involved in popular treatment of mycoses

A survey of medicinal plants used to treat common mycoses was done in the Curituba district, Sergipe State, Brazil. One hundred inhabitants were interviewed by health agents and traditional healers. Four different plants were the most cited (more than 50% of the citations): Ziziphus joazeiro, Caesalpinia pyramidalis, Bumelia sartorum and Hymenea courbaril. The aqueous extracts obtained following traditional methods and using different parts of these plants, were submitted to drop agar diffusion tests for primary antimicrobial screening. Only the water infusion extract of Ziziphus joazeiro and Caesalpinea pyramidalis presented a significant antifungal activity against Trichophyton rubrum, Candida guilliermondii, Candida albicans, Cryptococcus neoformans and Fonsecaea pedrosoi, when compared to the antifungal agent amphotericin B. The minimal inhibitory concentration (MIC) of the bioactive extracts was evaluated by the microdilution method. Best activity with a MIC of 6.5 microg/ml for both extracts was observed against Trichophyton rubrum and Candida guilliermondii. Ziziphus joazeiro and Caesalpinea pyramidalis extracts presented also low acute toxicity in murine models. The present study validates the folk use of these plant extracts and indicates that they can be effective potential candidates for the development of new strategies to treat fungal infections.