白木香叶的化学成分研究(二)

为综合利用白木香叶的丰富资源,阐明其物质基础,课题组再次对其化学成分进行了研究,采用多种色谱技术对其化学成分进行分离纯化,从白木香叶95%,70%乙醇提取物的氯仿和正丁醇萃取部位共分离得到12个化合物.经多种波谱方法鉴定其结构,分别为鸢尾酚酮2-(O-α-L)-吡喃鼠李糖苷(3),4'-羟基-5-甲氧基黄酮-7-O-葡萄糖(6-1)木糖苷(2),7,3',5'-三甲氧基黄酮苷(3),5-甲氧基芹菜素7-(O-β-D)-葡萄糖苷(4),2-苯乙基1-O-β-D-吡喃葡萄糖苷(5),红景天苷(6),苯甲醇1-O-β-D-吡喃葡萄糖苷(7),2,6-二甲氧基-4-羟基苯酚-1-O-β-D-吡喃葡萄糖苷(8),vanilloloside(9),(+)-丁香脂素(10),β-维生素E(11),豆甾-5-烯-3β,7α-二醇(12),化合物 2,3,5~9,11和12 为首次从该属植物中分离得到.另外,对氯仿萃取部位的9个流分进行了4种人体肿瘤细胞毒活性筛选,均未显示明显活性.     

苦参中非生物碱类成分研究

该文采用硅胶和HPLC等色谱手段,从苦参茎叶中分离得到5个化合物,从苦参根中分离得到10个化合物;根据化合物的波谱数据,分别鉴定为corchionoside C(1),丁香苷(2),2'-脱氧胸腺嘧啶核苷(3),松柏苷(4),benzyl O-β-D-glucopyranoside(5),番石榴酸(6),三叶豆紫檀苷(7),苦参酮(8),三叶豆紫檀苷-6'-单乙酸酯(9),槐属二氢黄酮G(10),异腐醇(11),降脱水淫羊藿素(12),4'-甲氧基异黄酮-7-O-β-D-芹糖-(1→6)-β-D-吡喃葡萄糖苷(13),kushenol O(14) 和6"-木糖-染料木素葡萄糖苷(15),其中化合物 1~6 为首次从该属植物分离得到。     

云南兔儿风中的三萜类成分

对云南兔儿风Ainsliaea yunnanensis的化学成分进行了系统的研究。利用多种色谱技术进行分离纯化,并通过现代波谱鉴定其结构。从云南兔儿风乙醇提取物中的石油醚萃取部位中分离鉴定了12个三萜类化合物,分别为冬青醇乙酸酯(1),降香萜烯醇(2),α-香树脂醇(3),伪蒲公英甾醇(4),β-香树脂醇(5),刺囊酸(6),multiflorenol (7),3β-羟基-18-烯-齐墩果烷 (8),12-齐墩果烯-11-酮-3β-棕榈酸酯(9),羊齿烯醇(10),fern-7-en-3β-ol(11)和羽扇豆醇(12)。除化合物 1,3,5,和10 外,其余化合物均为首次从该属植物中分离得到;所有化合物均为首次从云南兔儿风植物中分离得到。     

大血藤中1个新的木脂素类化合物

大血藤来源于木通科植物大血藤Sargentodoxa cuneata的干燥藤茎。该研究通过HPD-100 大孔树脂、反复硅胶柱色谱、Sephadex LH-20 和制备液相等方法,从采自安徽黄山的大血藤藤茎中分离出20个化合物;根据化合物的理化性质和波谱数据,分别鉴定为(7R,8S)-3,3'-5-三甲氧基-4,9-二羟基-4',7-环氧-5',8-木脂素-7'-烯-9'-酸 4-O-β-D-吡喃葡萄糖苷(1),1-O-香草酸-6-O-香草酰基吡喃葡萄糖苷(2),对羟基苯乙醇-6-O-香豆酰吡喃葡萄糖苷(3),枸橼苦素B(4),桂皮苷(5),(-)-异落叶松脂素4'-O-β-D-吡喃葡萄糖苷(6),(-)-异落叶松脂素4-O-β-D-吡喃葡萄糖苷(7),1-O-香草酸-6-(3",5"-二甲氧基-没食子酰)-β-D-吡喃葡萄糖苷(8),对羟基苯乙醇-6-O-(E)-咖啡酰吡喃葡萄糖苷(9),(-)-丁香树脂醇4'-O-β-D-吡喃葡萄糖苷(10),(-)-丁香树脂醇双葡萄糖苷(11),野菰苷(12),木通苯乙醇苷B(13),4-羟基-3-甲氧基苯乙酮-4-O-α-L-鼠李糖-(1→6)-β-D-吡喃葡萄糖苷(14),4-羟基-3-甲氧基苯乙酮-4-O-β-D-芹糖-(1→6)-β-D-吡喃葡萄糖苷(15),(-)-表儿茶素(16),毛柳苷(17),3,4-二羟基苯乙醇吡喃葡萄糖苷(18),绿原酸(19),原儿茶酸(20),其中化合物1为新化合物,化合物2~7首次从该植物中分离得到。     

藏飞廉中酚酸类成分研究

通过大孔吸附树脂,MCI 树脂,正相硅胶,Sephadex LH-20,ODS和反相HPLC 等多种色谱分离方法相结合,从藏飞廉乙醇提取物中分离得到14个化合物;利用多种谱学技术鉴定它们的结构分别为红景天苷(1),2-(3,4-二羟苯基)-乙基-O-β-D-吡喃葡萄糖苷(2),3,5-二羟苯基-乙醇-3-O-β-D-吡喃葡萄糖苷(3),对羟基桂皮酸(4),3-hydroxy-1-(4-hydroxy-3-methoxyphenyl) propan-1-one(5),3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl) propan-1-one(6),紫丁香苷(7),对羟基苯甲醛(8),水杨酸(9),tachioside(10),香草酸-4-O-β-D-吡喃葡萄糖苷(11),丁香醛(12),2, 6-二甲氧基-4-羟基苯酚-1-O-β-D-吡喃葡萄糖苷(13),2, 6-二甲氧基-对苯二酚-4-O-β-D-吡喃葡萄糖苷(14)。除化合物4和7外,其余均为首次从飞廉属植物中分离得到。     

五指毛桃的化学成分研究

利用各种色谱方法从五指毛桃中分离得到了17个化合物,根据理化常数和波谱数据鉴定了化合物的结构,分别为cyclomorusin(1),quercetin 3-O- -(1→2)-β-D-glucopyranoside(2),3,5,4'-三羟基-6,7,3'-三甲氧基黄酮(3),槲皮素(4),小麦黄素(5),金合欢素(6),木犀草素(7),芹菜素(8),(E)-suberenol(9),meranzin hydrate(10),丁香酚甲醚(11),3-甲氧基-4-羟基苯甲酸(12),对羟基苯甲酸(13),绿原酸甲酯(14),大黄素(15),α-香树素乙酸酯(16),β-谷甾醇(17)。其中化合物1~6,9~15为首次从该植物中分离得到。     

小果蔷薇三萜酸类化学成分的研究

采用柱色谱技术对小果蔷薇Rosa cymosa Tratt.根的95%乙醇提取物进行化学成分的研究,从小果蔷薇中分离得到11个化合物,根据波谱数据结合理化性质确定各化合物的结构,分别鉴定为坡模酸(1), 覆盆子酸(2), 乌苏酸(3), 蔷薇酸(4), 阿江榄仁尼酸(5), 委陵菜酸(6), 3β-E-feruloyl corosolic acid(7), 1β-羟基蔷薇酸(8), 千花木酸(9), 2,3-断-19α-羟基-12-稀-乌苏-2,3,28-三羧酸(10), 冬青苷 B(11)。化合物 3, 6~8, 10, 11 为首次从该植物中分离得到, 其中化合物 7, 10 为首次从蔷薇属分离得到。     

赤小豆的化学成分研究

通过大孔吸附树脂D101,正相硅胶,Sephadex LH-20,ODS,反相HPLC等多种色谱分离方法相结合,从赤小豆70%乙醇提取物中分离得到8个化合物;借助ESI-MS,NMR等光谱技术鉴定其结构为2β,15α-二羟基-贝壳杉-16-烯-18,19-二羧酸(1),2β-O-β-D-葡萄吡喃糖-15α-羟基-贝壳杉-16-烯-18,19-二羧酸 (2),2β-(O-β-D-葡萄吡喃糖)atractyligenin (3),3R-O-[β-L-阿拉伯吡喃糖基-(1→6)-β-D-葡萄吡喃糖] 辛-1-烯-3-醇 (4),(6S,7E,9R)-6,9-二羟基-megastigman-4,7-二烯-3-酮-9-O-β-D-葡萄吡喃糖苷 (5),刺五加苷D(6),白藜芦醇(7)和麦芽酚(8).结论:化合物1~7均为首次从该属植物中分离得到,化合物8为首次从该种植物中分离得到.     

鸭跖草的化学成分研究

利用常规柱色谱及半制备高效液相色谱等手段相结合对鸭跖草化学成分进行分离纯化,从鸭跖草中分离得到15个化合物,根据其NMR和MS等光谱数据以及理化性质鉴定化合物结构,所分化合物分别鉴定为柯伊利素-7-O-β-D-葡萄糖苷(1),没食子酸甲酯(2),对香豆酸(3),原儿茶酸(4),咖啡酸(5),对羟基苯甲酸(6),2-苯乙基-β-D-葡萄糖苷(7),土大黄苷(8),(7S,8R)-dihydrodehydrodiconiferyl alcohol-9-O-β-D-glucoside(9),异牡荆素(10),芹菜素-6-C-α-L-鼠李糖苷(11),isorhamnetin-3-O-β-D-glucoside(12),槲皮素-3-O-α-L-鼠李糖苷(13),异槲皮素(14),1,2-dihydro-6,8-dimethoxy-7-1-(3,5-dimethoxy-4-hydroxyphenyl)-N¹,N²-bis-[2-(4-hydroxyphenyl)ethyl]-2,3-naphthalene dicarboxamide(15).化合物 2,5-9,11,13 等8个化合物为首次从鸭跖草属中分离得到.     

毛果一枝黄花化学成分研究

目的: 对毛果一枝黄花Solidago virgaurea的化学成分进行研究。 方法: 采用硅胶柱色谱,凝胶柱色谱,ODS反相柱色谱以及重结晶等方法分离纯化,并通过理化常数和波谱分析鉴定化合物结构。 结果: 分离并鉴定出了12个化合物,分别为2'-甲氧基-2-甲氧基-6-羟基苯甲酸酯(1), 2'-甲氧基-2,6-二甲氧基苯甲酸酯(2),β-乙酰香树脂醇乙酸酯(3),α-菠菜甾醇(4),豆甾-7, 22-二烯-3-酮(5),2-羟基-6-甲氧基苯甲酸(6),胡麻素(7),槲皮素(8),山奈酚(9), 3β-acetoxyolean-12-en-11-one-acetate(10)和N-benzoylphenylalaninyl-N-benzoylphenylalaninate(11),原儿茶酸(12)。 结论: 化合物11为首次从该科植物中分离得到,化合物5, 10为该属内首次分离,化合物1,2,3,6,7,12为首次从该植物中分离得到。     

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。     

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.     

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.     

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。     

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.     

Screening of the topical anti-inflammatory activity of the bark of Acacia cornigera Willdenow, Byrsonima crassifolia Kunth, Sweetia panamensis Yakovlev and the leaves of Sphagneticola trilobata Hitchcock

Ethnopharmacological relevance

An investigation of topical anti-inflammatory activity was undertaken on plants used in Central America traditional medicine.

Aim of study

Four herbal drugs used in the folk medicine of Central America to treat inflammatory skin affections (Acacia cornigera bark, Byrsonima crassifolia bark, Sphagneticola trilobata leaves and Sweetia panamensis bark) were evaluated for their topical anti-inflammatory activity.

Materials and methods

Petroleum ether, chloroform and methanol extracts were obtained for herbal medicines and then extracts were tested on Croton oil-induced ear dermatitis model in mice.

Results

Almost all the extracts reduced the Croton oil-induced ear dermatitis in mice and the chloroform ones showed the highest activity, with ID₅₀ (dose giving 50% oedema inhibition) values ranging from 112 μg/cm² (Byrsonima crassifolia) to 183 μg/cm² (Sphagneticola trilobata). As reference, ID₅₀ of the non-steroidal anti-inflammatory drug indomethacin was 93 μg/cm².

Conclusions

Lipophilic extracts from these species can be regarded as potential sources of anti-inflammatory principles.     

红药根的化学成分研究

采用硅胶、Sephadex LH-20、高效制备液相等方法,对红药根的甲醇提取物进行分离纯化,通过质谱（MS）、波谱数据分析（¹H,¹³C-NMR）进行结构鉴定。从红药根的甲醇提取物中分离7个化合物,分别鉴定为plantainoside A（1）,plantainoside B（2）,calcedarioside C（3）,calcedarioside D（4）,platyphylloside（5）,hirsutanonol（6）和hirsutanonol-5-O-β-D-glucopyranoside（7）。化合物均5~7为首次从该科物中分离得到。     

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。     

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。     

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.