川山橙枝叶的化学成分研究

对川山橙的化学成分进行研究,通过采用硅胶柱、ODS、Sephadex LH-20等柱色谱方法进行分离纯化,根据理化性质与波谱数据鉴定了14个化合物的结构,分别为11-hydroxytabersonine(1),venalstonidine (2),sandine(3),齐墩果酸(4),熊果酸(5),白桦脂醇(6),(+)松脂醇(7),(-)丁香脂素(8),8-羟基-松脂素(9),(-)-latifolin (10),甲基条叶蓟素(11),马钱素(12),对苯二甲酸二丁酯(13),β-谷甾醇(14),其中化合物4～14为首次从该植物中分离得到.     

缬草的化学成分研究

目的研究败酱科缬草属植物缬草Valeriana officinalis根及根茎的化学成分。方法反复利用柱色谱方法进行分离纯化,通过理化性质及波谱数据鉴定化合物结构。结果从缬草氯仿和正丁醇部位分离得到11个化合物,分别鉴定为橄榄树脂素-4-O-β-D-葡萄糖苷(1)、落叶松脂醇-4,4′-O-β-D-双葡萄糖苷(2)、落叶松脂醇-4-O-β-D-葡萄糖苷(3)、落叶松脂醇(4)、8-羟基-松脂素-4′-O-β-D-葡萄糖苷(5)、松脂素-8-O-β-D-葡萄糖苷(6)、8,9′-二羟基-松脂素-4′-O-β-D-葡萄糖苷(7)、松脂素(8)、缬草苷A(9)、香草醛(10)、β-谷甾醇(11)。结论化合物1～3、6、7、10为首次从该植物中分离得到。     

黑水缬草治疗老年痴呆有效部位化学成分研究

目的:研究黑水缬草(Valeriana amurensis Smir.ex Kom.)治疗老年痴呆有效部位化学成分。方法:采用大孔树脂吸附柱色谱、正相硅胶柱色谱、ODS反相柱色谱、HPLC等分离方法及各种波谱学鉴定方法。结果:从大孔树脂吸附柱色谱的50%乙醇洗脱组分中分离并鉴定了13个化合物,分别为:(+)松脂素-4,4'-O-β-D-双葡萄吡喃糖苷(1),(+)8-羟基-松脂素-4'-O-β-D-葡萄吡喃糖苷(2),(+)8-羟基-松脂素-4-O-β-D-葡萄吡喃糖苷(3),(+)松脂素-8-O-β-D-葡萄吡喃糖苷(4),(+)松脂素-4-O-β-D-葡萄吡喃糖苷(5),(+)8-羟基-松脂素(6),(+)8,9'-二羟基-松脂素-4'-O-β-D-葡萄吡喃糖苷(7),(+)8-羟基-松脂素-4,4'-O-β-D-双葡萄吡喃糖苷(8),橄榄树脂素-4'-O-β-D-葡萄糖苷(9),落叶松脂醇-4,4'-O-β-D-双葡萄吡喃糖苷(10),橄榄树脂素-4-O-β-D-葡萄吡喃糖苷(11),8-羟基-落叶松脂醇-4'-O-β-D-葡萄吡喃糖苷(12),落叶松脂醇-4-O-β-D-葡萄吡喃糖苷(13)。结论:13个化合物全部为该植物中首次发现,其中包括8个双环氧木脂素(1～8)和5个单环氧木脂素(9～13)。     

瑞香狼毒中的1个新木脂素

利用各种色谱技术对瑞香狼毒的化学成分进行研究,从瑞香狼毒95%乙醇提取物中分离得到9个化合物。采用MS,NMR等波谱方法鉴定化合物的结构,分别为stellerachamin A(1),8-hydroxypluviatolide(2),荛花酚(3),松脂醇(4),马台树脂醇(5),dextrobursehernin(6),扁柏脂内酯(7),(-)-glaberide I(8),(-)-皮树脂醇(9),其中化合物1为新的木脂素类化合物,化合物2和7为首次从瑞香科植物中分离得到。     

短梗五加果中木脂素类成分的分离和鉴定

目的:分离和鉴定短梗五加果提取物中木脂素类化学成分。方法:采用硅胶柱色谱、ODS柱色谱和制备液相等方法对短梗五加果提取物中的化学成分进行分离纯化,并通过NMR和MS等谱学技术确定结构。结果:从短梗五加叶提取物中分离得到7个木脂素类化合物,分别鉴定为丁香树脂酚-4-O-β-D-吡喃葡萄糖苷(1),短梗五加苷E(2),杜仲树脂醇双吡喃葡萄糖苷(3),松脂醇二吡喃葡萄糖苷(4),松脂素-4-O-β-D-吡喃葡萄糖苷(5),(7S,8R)-urolignoside(6),新短梗五加酚(7)。结论:化合物3、5、6为首次从五加属中分离得到。     

瑞香狼毒细胞培养物的化学成分研究

采用常压与减压硅胶柱色谱、半制备HPLC、Sephadex LH-20等方法,从瑞香狼毒Stellera chamaejasme细胞培养物85％乙醇提取物的乙酸乙酯部分分离纯化得到了17个化合物,依据理化性质和各种波谱技术分别鉴定为:丁香脂素(1),杜仲树脂酚(2),松脂素(3),(1R,2S,5R,6S) -2-(4-hydroxyphenyl) -6-( 3-methoxy-4- hydroxyphenyl)-3,7-dioxabicyclo[3,3,0]octane(4),表松脂酚(5),caruilignan D(6),3-羰基愈创木烷-4-烯-11,12-二醇(7),落叶松脂素(8),tetrahydro-2-( 4-hydroxy-3-methoxyphenyl) -4-[ (4-hydroxyphenyl) methyl] -3-furanmethanol(9),5′-甲氧基落叶松脂醇(10),vladinol D( 11),环(L-脯氨酸-L-缬氨酸)(12),7′-羰基马台树脂醇(13),(+) -guayarol( 14),acutissimalignanB(15),异落叶松脂素(16)以及β-谷甾醇(17).其中化合物12为环二肽类化合物,7为倍半萜类化合物.除化合物7,12与17外,其余均为木脂素类化合物.17个化合物均首次从该植物组织培养物中获得.     

东北铁线莲地上部位化学成分研究

目的研究东北铁线莲Clematis manshurica地上部位的化学成分。方法采用硅胶柱色谱、ODS柱色谱和制备HPLC等技术方法进行分离纯化,运用理化性质和波谱数据鉴定化合物结构。结果从东北铁线莲地上部位乙醇提取物中分离得到17个化合物,分别鉴定为(+)-表松脂醇(1)、(+)-松脂醇(2)、(-)-表丁香树脂醇(3)、(+)-梣皮树脂醇(4)、(+)-松脂醇-4-O-β-D-吡喃葡萄糖苷(5)、(+)-丁香树脂醇-4-O-β-D-吡喃葡萄糖苷(6)、(+)-表丁香树脂醇-4-O-β-D-吡喃葡萄糖苷(7)、罗汉松脂素(8)、(+)-珍珠花环木脂素(9)、(+)-异落叶松脂素(10)、(7R,8R)-4,7,9,9′-四羟基-3,3′-二甲氧基-8-O-4′-新木脂素(11)、(7R,8S)-4,7,9,9′-四羟基-3,3′-二甲氧基-8-O-4′-新木脂素(12)、(7S,8R)-二氢脱氢双松柏醇(13)、木犀草素(14)、3″-O-(2′′′-甲基丁酰基)异当药苷(15)、2″-O-(2′′′-甲基丁酰基)异当药苷(16)、6″-O-(2′′′-甲基丁酰基)异当药苷(17)。结论所有化合物均为首次从该植物地上部位中分离得到,其中化合物1、3、4、7~9、11、12、15~17为首次从该属植物中分离得到。     

望春玉兰花蕾中木脂素类化学成分的研究

研究木兰科植物望春玉兰花蕾(辛夷)Magnolia biondii中木脂素类化学成分。利用Diaion HP-20,硅胶,Sephadex LH-20及半制备液相等多种色谱技术进行分离纯化,根据化合物的谱学数据和理化性质鉴定化学结构。从该植物中分离得到18个木脂素类化合物,分别鉴定为木兰脂素(1),epimagnolin(2),桉脂素(3),kobusin(4),aschantin(5),里立脂素B二甲醚(6),松脂素单甲醚(7),(+)-de-O-methylmagnolin(8),isoeucommin A(9),丁香树脂醇4-O-β-D-葡萄糖苷(10),连翘脂素(11),落叶松树脂醇-4'-O-β-D-葡萄糖苷(12),conicaoside(13),3,5'-二甲氧基-4',7-环氧-8,3'-新木脂素-4,9,9'-三醇(14),(7R*,8S*)-3,3'-二甲氧基-9,9'-二羟基-苯骈呋喃木脂素-4-O-β-D-葡萄糖苷(15),7S,8R-顺式-7,9,9'-三羟基-3,3'-二甲氧基-8-O-4'-新木脂素-4-O-β-D-葡萄糖苷(16),7S,8R-顺式-4,9,9'-三羟基-3,3'-二甲氧基-8-O-4'-新木脂素-7-O-β-D-葡萄糖苷(17)和(+)-异落叶松树脂醇(18)。化合物7~18为首次从该植物中分离得到。     

粗壮润楠中的木脂素类成分

通过萃取、正相硅胶、Sephadex LH-20、中压柱色谱以及反相HPLC柱色谱等多种分离方法相结合,从粗壮润楠树皮乙醇提物中分离得到18个木脂素类化合物;通过质谱和核磁共振等波谱学分析方法鉴定结构为:异落叶松脂素9'-0-β-D-吡喃木糖苷(1),5'-甲氧基异落叶松脂素9 '-O-β-D-吡喃木糖苷(2),南烛木树脂酚9 '-O-β-吡喃木糖苷(3),(+)-(8S,8'S)-4,4 '-二羟基-3,3 ',5,5'-四甲氧基木脂烷-9,9'-二醇9-O-β-D-吡喃木糖苷(4),南烛木树脂酚(5),内消旋二氢愈创木脂酸(6),(+)-(8S,8 'R)-3',4,4'-三羟基-3'-甲氧基木脂烷(7),(8S,8'R)-4'-羟基-3,3',4-三甲氧基木脂烷(8),(+)-愈创木素(9),异愈创木素(10),(-)-(7'R,8R,8 'R)-4,4'-二羟基-3,3',5-三甲氧基-2,7'-环木脂烷(11),翼梗五味子木脂素B(12),(-)-(7S,7'S,8R,8'R)-4,4'-二羟基-3,3',5,5'-四甲氧基-7,7'-环氧木脂素-9,9'-二醇(13),(+)-(7R,8R,7'E)-4-羟基-3,5'-二甲氧基-7,4'-环氧-8,3'-氧新木脂素-7'-烯(14),甘密树皮素B(15),桢楠素Ⅰ(16),(-)-松脂素(17)和(-)-丁香树脂酚(18).以上化合物均为首次从该植物中分离得到.经体外活性筛选,在10 μmol·L-1时,化合物17对小鼠腹腔巨噬细胞分泌NO具有较强的抑制活性,抑制率为72.2％.     

白叶藤中苯丙素类化学成分分析

目的:研究萝藦科白叶藤属白叶藤的化学成分,为其药效成分及作用机制的深入研究奠定基础。方法:采用硅胶柱色谱、反相RP-18柱色谱、羟丙基葡萄糖凝胶色谱方法进行成分分离,并利用1H-NMR,13C-NMR和MS等波谱学方法进行结构鉴定。结果:从白叶藤乙醇提取液的三氯甲烷部分分离得到11个苯丙素类化合物,分别鉴定为(+)-松脂素(1),(+)-8-羟基松脂素(2),丁香脂素(3),horsfieldin(4),(-)-蛇菰宁(5),ficusesquilignan A(6),ficusesquilignan B(7),6-羟基-7-甲氧基香豆素(8),7-羟基-6,8-二甲基香豆素(9),藤菊黄素(10)和methyl sinapate(11)。结论:所有化合物均为首次从白叶藤中分离得到。     

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.