番石榴果实中三萜类成分研究

目的:研究番石榴果实的化学成分.方法:采用各种色谱技术分离,波谱法进行结构鉴定.结果:从番石榴果实中分离得到9个乌苏烷型三萜类化合物:乌苏酸(1),1β,3β-二羟基乌苏烷-12烯-28-酸(2),2α,3β-二羟基-12-烯-28-乌苏酸(3),3β,19α-二羟基-12-烯-28-乌苏酸(4),19α-羟基-12-烯-28-乌苏酸-3-O-α-L-阿拉伯吡喃糖(5),3β,23-二羟基-12-烯-28-乌苏酸(6),3β,19α,23-三羟基-12-烯-28-乌苏酸(7),2α,3β,19α,23-四羟基-12-烯-28-乌苏酸(8),3α,19α,23,24-四羟基-12-烯-28乌苏酸(9).结论:化合物2,5-9为首次在该植物中分离得到.     

山梨猕猴桃根化学成分及细胞毒活性研究

探究山梨猕猴桃Actinidia rufa根的化学成分。采用葡聚糖凝胶色谱法、薄层色谱硅胶色谱法、高效液相色谱法等方法分离得到9个化合物,鉴定为:2α,3β,19α,23,24-五羟基乌苏-12-烯-28-O-β-D-吡喃葡萄糖苷(1)、2α,3α,19α,24-四羟基乌苏-12-烯-28-O-β-D-吡喃葡萄糖苷(2)、2α,3α,24-三羟基乌苏-12-烯-28-酸(3)、2α,3α,24-三羟基齐墩果-12-烯-28-酸(4)、2α,3α,23,24-四羟基乌苏-12-烯-28-酸(5)、2α,3β,23,24-四羟基乌苏-12-烯-28-酸(6)、2α,3β,23-三羟基乌苏-12-烯-28-酸(7)、2α,3β,23-三羟基乌苏-12,20(30)-二烯-28-酸(8)、2α,3α,24-三羟基乌苏-12,20(30)-二烯-28-酸(9),其中化合物1和2为首次从该属植物中分离得到。细胞毒活性测试结果显示化合物2~4对人卵巢癌细胞株SKVO3和人甲状腺乳头状癌细胞株TPC-1具有强的细胞毒活性(IC50在10.99~16.41μmol·L~(-1)),而化合物3,4对人宫颈癌细胞株He La具有强的细胞毒活性,IC50分别为15.53,13.07μmol·L~(-1)。     

猕猴桃藤山柳茎叶中的三萜化合物

目的:进一步阐明我国特有属药用植物猕猴桃藤山柳的化学成分.方法:采用硅胶和MCI柱色谱及制备液相色谱等分离方法对该植物茎叶的化学成分进行分离纯化,经质谱和核磁共振波谱技术进行结构鉴定.结果:从猕猴桃藤山柳茎叶的甲醇提取物中分离纯化出16个化合物,其结构分别鉴定为桦木酸(1)、乌苏酸(2)、齐墩果酸(3)、科罗索酸(4)、3β-反式对香豆酰氧基-2α,23-二羟基-12-烯-28-乌苏酸(5)、3β-反式对香豆酰氧基-2α,23-二羟基-12,20(30)-二烯-28-乌苏酸(6)、2α,3α,23-三羟基乌苏-12,20(30)-二烯-28-酸(7)、2α,3α,23-三羟基乌苏-12-烯-28-酸(8)、积雪草酸(9)、2α,3α,24-三羟基乌苏-12-烯-28-酸(10)、2α,3β,23-三羟基乌苏-12,20(30)-二烯-28-酸(11)、2α,3β,19α,23-四羟基乌苏-12-烯-28-酸(12)、2α,3α,19α,24-四羟基乌苏-12-烯-28-酸(13)、2α,3β,23,24-四羟基乌苏-12-烯-28-酸(14)、2α,3α,19α,23,24-五羟基乌苏-12-烯-28-酸(15)和胡萝卜苷(16).结论:这些化合物主要为乌苏烷型三萜成分,其中化合物3～6,11,12,14和15为首次从该单种属植物中分离得到.     

夏枯草的化学成分

目的：研究夏枯草地上部位（除去果穗）的化学成分。方法：运用各种色谱方法进行化学成分的分离纯化,用理化方法解析其化学结构。结果：从该植物地上部位中分得12个化合物,均为五环三萜和三萜皂苷类成分,经与文献理化常数和波谱数据对照,分别为：乌苏酸（1）,齐墩果酸（2）,白桦酯酸（3）,2α,3α-二羟基-乌苏-12-烯-28-酸（4）,2α,3α,19α-三羟基-乌苏-12-烯-28-酸（5）,2α,3β-二羟基-乌苏-12-烯-28-酸（6）,2α,3α,23-三羟基-乌苏-12-烯-28-酸（7）,2α,3β,24-三羟基-齐墩果-12-烯-28-酸（8）,2α,3α,19α,24-四羟基-乌苏-12-烯-28-酸-β-D-吡喃葡萄糖苷（9）,2α,3β,19α,23-四羟基坞苏-12-烯-28-酸-β-D-吡喃葡萄糖苷（10）,2α,3α,24-三羟基-齐墩果-12-烯-28-酸（11）,和2α,3α,24-三羟基-乌苏-12-烯-28-酸（12）。结论：其中化合物3、9和10为首次从该植物中分离得到,化合物5、7和8为首次从该属植物中分离得到。     

猫人参化学成分研究

目的 对猫人参Actinidia valvata根的化学成分进行研究.方法 采用硅胶柱色谱法进行分离纯化,根据理化性质和光谱方法鉴定化合物的结构.结果 从猫人参根乙醇提取物的醋酸乙酯部位分离鉴定了10个化合物,结构鉴定为2α,3α,24-三羟基-12-烯-28-乌苏酸(Ⅰ)、2β,3β,23-三羟基-12-烯-28-乌苏酸(毛花猕猴桃酸B)(Ⅱ)、2α,3β,19,23-四羟基-12-烯-28-乌苏酸(Ⅲ)、2α,3β,24-三羟基-12-烯-28-乌苏酸(Ⅳ)、积雪草酸(Ⅴ),3β-(反式-P-香豆素酰基)-2α,24-二羟基-12-烯-28-乌苏酸(Ⅵ)、3β-(反式-P-香豆素酰基)-2α,23-二羟基-12-烯-28-乌苏酸(Ⅶ)、熊果酸(Ⅷ)、β-谷甾醇(Ⅸ)、胡萝卜苷(Ⅹ).结论 以上化合物均系首次从该植物中分离得到.     

乌檀化学成分的研究

目的研究乌檀Nauclea officinalis(Pierre ex Pitard) Merr. et Chun的化学成分。方法乌檀75%乙醇提取物采用硅胶、ODS、Sephadex LH-20进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果从中分离得到12个化合物,分别鉴定为没食子酸(1)、3,4-二羟基苯甲酸(2)、山柰酚(3)、2α,3β-二羟基乌苏-12-烯-28-酸(4)、2α,3β,19α-三羟基乌苏-12-烯-28-酸(5)、23-羟基-乌苏酸(6)、2α,3β,19α,23-四羟基乌苏-12-烯-28-酸(7)、2β,3β,19α-三羟基乌苏-12-烯-28-酸(8)、3-O-β-D-glucopyranosyl-23-hydroxyursolic acid(9)、3β,19α,23-三羟基乌苏-12-烯-28-酸(10)、乌苏酸(11)、胡萝卜苷(12)。结论化合物3～9均为首次从该植物中分离得到。     

黄牛奶树根的三萜酸类成分研究

目的研究黄牛奶树Symplocos laurina根的三萜酸类成分。方法采用硅胶柱色谱法、ODS、凝胶Sephadex LH-20柱色谱、半制备液相色谱等技术进行分离纯化,通过波谱数据分析及物理常数对照等方法鉴定化合物结构。结果从黄牛奶树根95%乙醇提取物中分离得到10个三萜酸类化合物,分别鉴定为19α-羟基-4-羰基-3,24-非-2,4-开环齐墩果烷-12-烯-2,28-二酸(1)、negundonorin A(2)、2α,3β,19α,23-四羟基乌苏烷-12-烯-28-酸(3)、2α,3β,19α,23-四羟基齐墩果烷-12-烯-28-酸(4)、2α,3β,23-三羟基乌苏烷-12-烯-28-酸(5)、2α,3β,23-三羟基齐墩果烷-12-烯-28-酸(6)、2α,3α,19α,23-四羟基乌苏烷-12-烯-28-酸(7)、1α,3β,19α,23-四羟基乌苏烷-12-烯-28-酸(8)、3β,19α,23-三羟基乌苏烷-12-烯-28-酸(9)、3β,19α,23-三羟基乌苏烷-2-羰基-12-烯-28-酸(10)。结论所有化合物均首次从黄牛奶树中分离得到,除化合物3、7,其他化合物均为首次从山矾属植物中分离得到。     

美味猕猴桃根中三萜类成分研究

目的 研究美味猕猴桃Actinidia deliciosa根的化学成分.方法 以95％乙醇为提取溶剂,经多种色谱方法分离,根据理化性质,结合谱学手段对化合物进行结构鉴定.结果 从美味猕猴桃根中分离得到3个化合物,分别鉴定为2β,3β,28-三羟基-12,20(30)-羽扇豆二烯(1)、2α,3β,19α,24-四羟基-12-烯-28-乌苏酸(2)、2α,3β,23,27-四羟基-12-烯-28-乌苏酸(3).结论 化合物1为1个新的羽扇豆烷型三萜,命名为猕猴桃素A.     

蓝萼香茶菜化学成分的研究

目的研究来自吉林省的蓝萼香茶菜化学成分。方法分别对蓝萼香茶菜根部和地上部分的醋酸乙酯提取相进行色谱分离,用波谱方法和理化性质鉴定各化合物的结构。结果分离得到10个化合物,分别为蓝萼甲素①、3β-乙酰氧基-12-烯-28-齐墩果酸②、3β-乙酰氧基-12-烯-28-乌苏酸③、2α-羟基乌苏酸④、2α,3α,24-三羟基-12,20(30)-二烯-乌苏酸⑤、2α,3β,23-三羟基-12-烯-28-乌苏酸⑥、正十六烷酸⑦、豆甾醇⑧、谷甾醇⑨、胡萝卜苷⑩。结论化合物2、5为首次从该属植物中得到,6、7为首次从该种植物中得到。     

蓝萼香茶菜三萜成分的研究

从蓝萼香茶菜Rabdosia japonica var.galaucocalyx茎叶的醋酸乙酯部分分得9个化合物,利用现代波谱学方法进行了结构鉴定,它们分别是:软木三萜酮(Ⅰ),3β,28-二羟基乌苏烷(Ⅱ),熊果酸(Ⅲ),3β-乙酰氧基-12-烯-28-乌苏酸(Ⅳ),2α,3α-二羟基-12-烯-28-乌苏酸(Ⅴ),2α,3α,23-三羟基-12-烯-28-乌苏酸(Ⅵ),齐墩果酸(Ⅶ),β-谷甾醇(Ⅷ),β-胡萝卜苷(Ⅸ)。化合物Ⅰ,Ⅱ,Ⅳ,Ⅴ,Ⅵ为首次从该植物中分离得到。     

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.     

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.     

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。     

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。     

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.     

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.     

中国石斛属植物文献计量研究

石斛是珍稀濒危中药材,目前正处于快速发展阶段。为全面了解我国石斛属植物研究的历史和发展现状,作者以1954～2010年"中国知网中国学术期刊网络出版总库"收录的石斛研究文献为依据,采用文献计量学的原理和方法,对我国石斛属植物研究文献从文献年代分布、期刊分布与被引频率、主题分布、研究对象分布、作者与研究机构分布等方面进行了统计与分析。结果表明,我国石斛研究明显分为起步(2个)、停滞、平稳发展、快速上升5个阶段;期刊分布存在离散性与集中性并存的现象,已形成核心期刊研究群,并以《中国中药杂志》、《中草药》和《陕西中医》为代表;研究主题广泛涉及临床与药理、组织培养与种苗繁育、成分分析等多个领域,已经形成比较稳定的研究机构和团队,但研究对象差异显著,以铁皮石斛、金钗石斛和霍山石斛最为集中。我国石斛属植物的研究已取得显著成果,但种植产业发展缓慢,供需矛盾突出,预计种苗繁育与人工种植、产品开发、化学与药理等方面是未来的研究热点,其文献报道仍将进一步上升。     

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.