冬凌草中的一个新生物碱

目的:研究冬凌草(Rabdosia rubescens (Hemls.) Hara)地上部分的化学成分。方法:利用大孔吸附树脂色谱进行分离纯化,根据化合物的理化性质和光谱数据鉴定结构。结果:从冬凌草地上部分分离得到7个化合物,分别为:冬凌草碱(1),黄嘌呤(2),芹菜素-6,8-二-C-β-D-葡萄糖苷(3),7-羟基-4(1H)-喹啉酮(4),1,5-二-(3,4-二羟基苯基)-乙烯醚(5),3-(3,4-二羟基苯基)-2-异丙氧基-丙酸(6),邻苯二甲酸双-(2-乙基己基)酯(7)。结论:化合物1为新化合物,其余化合物均为首次从该属植物中分离得到。     

延胡索中的生物碱成分

目的:研究延胡索Corydalis yanhusuo块茎60%乙醇提取物的生物碱成分.方法:采用多种色谱学方法进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构.结果:从延胡索块茎60%乙醇提取物的氯仿可溶部分分离得到9个生物碱,分别鉴定为7-醛基脱氢海罂粟碱(1),O-甲基南天竹碱(2),(+)-O-甲基球紫堇碱(3),d-紫堇碱(4),四氢黄连碱(5),8-氧黄连碱(6),巴马亭(7),四氢巴马亭(8)和去氢紫堇碱(9).结论:化合物1为首次从生物样品中获得,首次报道了其核磁数据,化合物3为首次从罂粟科植物中分离得到,化合物6为首次从该植物中分离得到.     

牡荆子的化学成分与生物活性研究

研究牡荆Vitex negundo var.cannabifolia果实的化学成分及其生物活性。利用硅胶、Sephadex LH-20柱色谱和半制备HPLC等色谱方法分离纯化,结合其理化性质和MS、NMR等波谱学数据鉴定化合物的结构。从牡荆子70%丙酮提取物的二氯甲烷萃取部位分离鉴定了19个化合物,包括13个木脂素和6个酚类化合物,分别鉴定为6-羟基-4-(4-羟基-3-甲氧基苯基)-3-羟甲基-7-甲氧基-3,4-二氢-2-萘醛(1),6-羟基-4-(4-羟基-3-甲氧基苯基)-3-羟甲基-5-甲氧基-3,4-二氢-2-萘醛(2),vitexdoin F(3),去四氢铁杉脂素(4),vitexdoin E(5),4-氧代芝麻素(6),L-芝麻素(7),(+)-beechenol(8),ligballinol(9),2-(4-hydroxyphenyl)-6-(3-methoxy-4-hydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane(10),松脂素(11),balanophonin(12),thero-guaiacylglycerol-β-coniferyl aldehyde ether(13),对羟基肉桂醛(14),松柏醛(15),5,7-二羟基色原酮(16),反-3,5-二甲氧基-4-羟基-肉桂醛(17),覆盆子酮(18)和alternariol 4-methyl ether(19)。化合物8~10,14,18,19为首次从马鞭草科植物中分离得到,化合物13为首次从牡荆属植物中分离得到,化合物6,7,12,15~17为首次从该植物中分离得到。对分离得到的化合物进行了体外抗炎和细胞毒活性评价,8个化合物(3,5,7,10,11,14,15,17)能够明显抑制LPS诱导的RAW 264.7细胞释放一氧化氮(NO),其IC_(50)在7.8~81.1μmol·L-1;4个化合物(1~4)对Hep G-2细胞具有明显的细胞毒作用,IC_(50)在5.2~24.2μmol·L~(-1)。     

蓬莪术姜黄素类化学成分研究

目的研究蓬莪术Curcuma phaeocaulis根茎的姜黄素类化学成分及其细胞毒活性。方法将蓬莪术根茎的95%乙醇提取物经石油醚、醋酸乙酯、正丁醇依次萃取,对醋酸乙酯萃取部位采用硅胶和葡聚糖凝胶Sephadex LH-20柱色谱、反相中压液相色谱、制备薄层色谱及半制备高效液相色谱等分离技术进行分离纯化,利用现代波谱学手段对分离的化学成分进行结构鉴定;采用MTT法对分离得到的化合物进行细胞毒活性筛选。结果从蓬莪术根茎的醋酸乙酯萃取部位分离得到4个姜黄素类化合物,分别鉴定为1,7-双(4-羟基苯基)-1E,6E-庚二烯-3-酮(1)、1,7-双(4-羟基苯基)-1,4,6-庚三烯-3-酮(2)、1,7-双(4-羟基苯基)-4E,6E-庚二烯-3-酮(3)和(1R,5S,6S)-1,5-环氧-6-羟基-1,7-双(3-甲氧基-4-羟基苯基)-庚烷(4)。MTT实验显示化合物1～3均可抑制人胃癌HGC-27细胞的增殖,仅化合物2对人乳腺癌MDA-MB-231细胞有抑制作用;化合物2和3还对人正常肝细胞L-02表现出强烈的毒性作用。结论从蓬莪术中分离得到4个姜黄素类成分,其中化合物1为新化合物,命名为姜黄素P。化合物1～3均具有一定的抑制HGC-27细胞增殖作用,其中化合物1可选择性抑制HGC-27细胞的增殖并对人正常肝L-02细胞无明显毒性作用。     

灰绿黄堇生物碱化学成分研究Ⅱ

目的:研究灰绿黄堇Corydalis adunca生物碱的化学成分。方法:按不同的pH值,对95%乙醇热提浸膏进行分段处理,柱色谱分离,根据理化性质和现代波谱技术等进行结构鉴定。结果:从灰绿黄堇中分离得到4个生物碱:四氢巴马亭(Ⅰ),1,2,3,4-四氢-6-甲氧基-1-[4′-羟基苯基]甲基-7-异喹啉醇(Ⅱ),黄连碱(Ⅲ),巴马亭(Ⅳ)。结论:4个化合物均是首次从该植物中得到。     

沙煲暗罗根的化学成分(英文)

目的:对沙煲暗罗根的化学成分进行研究。方法:运用硅胶和Sephadex LH-20柱色谱,以及制备薄层色谱等方法分离纯化化合物,通过波谱数据和理化性质鉴定结构。结果:从沙煲暗罗根中得到10个化合物:5,7-二羟基-8-甲酰基-6-甲基黄烷酮(1),demethoxymatteucinol(2),5,7-二羟基-6-甲基-8-甲酰基黄酮(3),5,7-二羟基-6-甲酰基-8-甲基黄酮(4),MarcanineA(5),suberosol(6),β-谷甾醇(7),香草醛(8),肉桂酸(9),烟酸(10)。结论:化合物1-4为首次从该属中分离得到,所有化合物为首次从该植物中分离得到。化合物6对人肿瘤细胞SPC-A-1和SGC-7901显示有细胞毒性。     

雷公藤叶化学成分研究

目的:对雷公藤叶水提取物进行化学成分研究.方法:利用各种色谱方法进行化学成分分离,根据理化性质和波谱数据鉴定化合物的结构.结果:分离得到9个化合物,分别鉴定为(+)-lyoniresinol(1),(+)-isolarieiresinol(2),burselignan(3),dibutyl phthalate(4),cyclo-(S-Pro-R-Phe)(5),cyclo-(S-Pro-R-Leu)(6),cyclo-(S-Pro-S-Ile)(7),3-hydroxy-1-(4-hydroxy-3.5-dimethoxyphenyl)-1-propanone(8),胡萝卜苷(9).结论:1-3为4-苯基四氢萘类木脂素,5-7为二酮哌嗪类化合物(环二肽),化合物1-3,5-8为首次从该植物中分离得到.     

博落回的生物碱成分及细胞毒活性研究

目的:研究博落回Macleaya cordata的生物碱成分及其抗肿瘤活性。方法:采用乙醇提取和液液萃取等方法提取,硅胶,反相ODS,Sephadex LH-20柱色谱,HPLC等分离技术分离其生物碱成分,利用MS,NMR等光谱技术鉴定化合物结构,采用MTT法测定化合物对MCF-7及SF-268肿瘤细胞株的细胞毒活性。结果:从博落回中分离鉴定了12种生物碱,分别为maclekarpine E(1),6-丙酮基二氢白屈菜红碱(2),岩黄连灵碱(3),6-丙酮基二氢血根碱(4),O-methylzanthoxyline(5),6-甲氧基二氢血根碱(6),spallidamine(7),6-羟基二氢白屈菜红碱(8),arnotianamida(9),二氢血根碱(10),原阿片碱(11),别隐品碱(12)。结论:化合物1,3,7~9为首次从该植物中分离得到,化合物5为新天然产物。药理实验表明,化合物6对MCF-7及SF-268细胞株具有显著的细胞毒活性,IC50值分别为0.61,0.54μmol·L-1。     

山辣子皮根茎化学成分研究

目的:研究山辣子皮Daphne papyracea var.crassiuscula根茎的化学成分.方法:对山辣子皮根茎75％乙醇提取物的乙酸乙酯部分进行反复硅胶、反相硅胶柱色谱分离,并运用波谱学方法对化合物结构进行鉴定.结果:从瑞香属植物山辣子皮根茎中分离得到8个化合物,分别鉴定为瑞香新素(1),瑞香素(2),7-羟基-8-甲氧基香豆素(3),西瑞香素(4),1-4’-羟基苯基-5-苯基-2(E)-烯-1-戊酮(5),瑞香醇酮(6),β-香树脂醇醋酸酯(7)和(+)-松萝酸(8).结论:化合物1～8为首次从山辣子皮中得到,化合物8首次从该属植物中得到.     

黔产吴茱萸化学成分研究

目的:研究黔产吴茱萸的化学成分.方法:利用各种色谱技术进行分离纯化,根据化合物的理化性质和波谱数据进行结构鉴定.结果:从黔产吴茱萸中分离并鉴定了11个化合物,分别是吴茱萸次碱(1),去氢吴茱萸碱(2),柠檬苦素(3),吴茱萸果酰胺Ⅰ(4),吴茱萸卡品碱(5),胡萝卜苷(6),蒲公英萜酮(7),乌苏-14-烯-3-醇-1-酮(8),反式咖啡酸甲酯(9),对香豆酸甲酯(10),咖啡因(11).结论:化合物7,8,10,11为首次从该植物中分离得到.     

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。     

Investigation of plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts

Aim of the study

To investigate the activities of the 217 plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts.

Materials and methods

Plant extracts were prepared by the method of maceration using solvents of different polarities. The growth inhibition of chloroquine-resistant Plasmodium falciparum strain (FcB1) was determined by measuring the radioactivity of the tritiated hypoxanthine incorporated. Activity against Leishmania (Leishmania) chagasi and Trypanosoma cruzi was measured by the MTT colorimetric assay. The antifungal tests were carried out by using the CLSI method. The active extracts were tested also by cytotoxicity assay using NIH-3T3 cells of mammalian fibroblasts.

Results

Two hundred and seventeen extracts of plants were tested against Plasmodium falciparum. The eleven active extracts, belonging to eight plant species were evaluated against L. (L.) chagasi, Trypanosoma cruzi, yeasts and in NIH-3T3 cells. The results found in these biological models are consistent with the ethnopharmacological data of these plants. The ethyl acetate extract of Diospyros hispida root showed IC₅₀ values of 1 μg/mL against Plasmodium falciparum. This extract demonstrated no toxicity against mammalian cells, resulting in a significant selectivity index (SI) of 435.8. The dichloromethane extract of Calophyllum brasiliense root wood was active against Cryptococcus gattii LMGO 01 with MIC of 1.95 μg/mL; and Candida albicans ATCC 10231 and Candida krusei LMGO 174, both with MIC of 7.81 μg/mL. The same extract was also active against Plasmodium falciparum and L. (L.) chagasi with IC₅₀ of 6.7 and 27.6 μg/mL respectively. The ethyl acetate extract of Spiranthera odoratissima leaves was active against Cryptococcus gattii LMGO 01 with MIC of 31.25 μg/mL, and against Plasmodium falciparum with IC₅₀ of 9.2 μg/mL and Trypanosoma cruzi with IC₅₀ of 56.3 μg/mL.

Conclusion

The active extracts for protozoans and human pathogenic yeasts are considered promising to continue the search for the identification and development of leading compounds.     

厚朴与凹叶厚朴群体遗传学研究

目的:对厚朴与凹叶厚朴的群体遗传学进行研究,为中药厚朴的质量控制提供分子生药学方面的依据。方法:对厚朴与凹叶厚朴15个居群应用2个叶绿体基因间序列psbA-trnH和trnL-trnF进行PCR扩增并测序,计算厚朴与凹叶厚朴单倍型频率,用程序HaploNst分析遗传多样性和遗传结构,应用TCS version 1.13软件构建单倍型网状进化树。结果:厚朴与凹叶厚朴均无特有单倍型存在,但单倍型频率存在显著差异,已开始出现遗传分化的趋势,NST略大于GST。结论:厚朴与凹叶厚朴在遗传上已出现遗传分化的趋势,但尚未完全分化成彼此独立的单系。     

Effect of feeding Mucuna pruriens on helminth parasite infestation in lambs

Ethnopharmacological relevance

Mucuna pruriens is a tropical legume anecdotally reputed to have anthelmintic properties. This study was conducted to examine the validity of such claims.

Aim of the study

The aim of this study was to determine if ingestion of Mucuna seeds reduces helminth parasite infestation in lambs.

Materials and methods

Thirty-six Dorper × Katahdin ram lambs were assigned to three treatments, a cottonseed meal based control diet, a diet in which Mucuna replaced cottonseed meal and the control diet with levamisole (7.5 mg/kg body weight) administration. All diets were isonitrogenous and isocaloric. The 12 lambs in each treatment were assigned randomly to 4 pens, each containing 3 lambs. Lambs were trickle infected three times per week by gavage with infectious Haemonchus contortus larvae (2000 larvae/lamb) for 3 weeks.

Results

Levamisole treatment decreased fecal egg counts by 87% and abomasal worm counts by 83%. Mucuna intake did not statistically affect fecal egg counts or abomasal worm counts, though numerical (P > 0.10) reductions of 7.4% and 18.1%, respectively were evident. Anemia indicators, feed intake, and lamb growth were unaffected by treatment.

Conclusions

Levamisole reduced the Haemonchus parasite burden in lambs significantly but feeding Mucuna reduced the burden by levels unlikely to eliminate the clinical effects of parasitism.     

牛耳朵和黄花牛耳朵的显微和化学鉴别

目的:为苦苣苔科唇柱苣苔属植物牛耳朵和黄花牛耳朵的鉴定和分类提供解剖学和化学依据。方法:采用石蜡制片法和水合氯醛透化法对2种药用植物的根状茎和叶横切面和粉末特征进行研究,应用光学显微镜观察显微结构。采用HPLC-UV法进行化学鉴别。结果:牛耳朵和黄花牛耳朵显微特征无明显区别,但是化学特征有明显的差异。结论:化学诞生特征鉴别方法可以作为2种药用植物的鉴定方法。     

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.     

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.     

不同类型的桑螵蛸与其基原昆虫对应关系研究

桑螵蛸为常用中药,因其入药部位为螳螂的卵鞘,无法直接判断其基原昆虫.同时螳亚科动物种类繁多,均产卵鞘,目前关于桑螵蛸对应的基原昆虫尚无一致的结论,而二者准确的对应关系是保证桑螵蛸质量的基础,也是桑螵蛸条形码研究的基础.文章采用人工孵化与捕捉活体螳螂2种方式,分别鉴定了药材及其原动物,系统地研究了桑螵蛸与基原昆虫的对应关系,发现基原昆虫为大刀螳属、斧螳属、污斑螳属的多种昆虫,该研究为桑螵蛸深入开发与利用研究奠定了基础.