滇南狸尾豆叶乙酸乙酯部分化学成分研究（Ⅱ）

目的：进一步研究滇南狸尾豆叶乙酸乙酯部分的化学成分。方法：采用硅胶柱色谱、Sephadex LH-20柱色谱等方法分离纯化;根据波谱学数据和理化性质进行结构鉴定。结果：又从中分出5个化合物：5,7,4＇-三羟基黄酮-7-O-α-L-鼠李糖基-（1→2）-β-D-葡萄糖苷（1）,柚皮素（2）,5,7-二羟基色原酮（3）,3-甲氧基-4-羟基苯甲酸（4）,二十八烷（5）。结论：5个化合物都是首次从该植物中分离得到。     

含羞云实种子中的黄酮类成分

目的:研究含羞云实种子的化学成分。方法:采用多种色谱技术对乙酸乙酯萃取物进行分离纯化。结果:从种子中分离并鉴定得到11个黄酮类化合物(包括高异黄酮),分别为:(E)-3-(3',4'-dihydroxybenzylidene)-5,7-dihydroxychroman-4-one(1)、5,7-dihydroxy-3-(4'-hydroxybenzylidene)chroman-4-one(2)、eucomin(3)、(R)-5,7-dihydroxy-3-(4'-methoxybenzyl)chroman-4-one(4)、(R)-5,7-dihydroxy-(4'-hydroxy-3'-methoxybenzyl)chroman-4-one(5)、evofolin-B(6)、kaempferol(7)、5,7,3',4'-tetrahydroxy-3-methoxyflavone(8)、柚皮素(9)、槲皮素(10)、木犀草素(11)。结论:其中,化合物1、2、4~9、11为首次从该植物中分离得到。     

九里香叶中的化学成分

目的:研究九里香叶的药效物质基础。方法:利用制备薄层、反复硅胶色谱、半制备HPLC等方法进行分离纯化,根据理化性质及波谱数据对分离的化合物进行结构鉴定。结果:分离得到11个化合物,分别鉴定为5,7,3',4'-四甲氧基黄酮(1),5,7-二羟基-3',4',5'-三甲氧基黄酮(2),5-羟基-3,7,3',4'-四甲氧基黄酮(3),3-羟基-5,6,7,4'-四甲氧基黄酮(4),川陈皮素(5),香草酸(6),咖啡酸乙酯(7),5-羟基-7,3',4'-三甲氧基黄酮(8),3,5-二羟基-6,7,3',4'-四甲氧基黄酮(9),5,6,4-三羟基-3,7,-二甲氧基黄酮(10),山柰酚(11)。结论:3,4,6,9,10为首次从九里香叶中分离得到。     

海南草珊瑚石油醚部位化学成分研究

目的:研究海南草珊瑚全草的化学成分.方法:采用各种柱色谱分离,通过波谱进行结构鉴定.结果:从海南草珊瑚全草石油醚部位中分离得到了9个化合物,分别鉴定为棕榈酸(1),花生酸(2),β-谷甾醇(3),硬脂酸(4),大黄素(5),大黄酚(6),2',3'-二羟基4',6'-二甲氧基查耳酮(7),2'-羟基4',6'-二甲氧基查耳酮(8),cardamonin(9).结论:化合物1～9均是首次从该植物中分离得到,化合物2,5～9为首次从该科中分离得到.     

云木香化学成分研究

目的:研究菊科风毛菊属植物云木香的化学成分.方法:利用硅胶柱色谱、Sephadex LH-20和反相RP-18柱色谱等手段进行分离纯化,并通过波谱数据鉴定结构.结果:分离鉴定了11个化合物,5,7-二羟基.2-甲基色原酮(5,7-dihydroxy-2-methylchromone,1),对羟基苯甲醛(p-hydroxybenzaldehyde,2),3,5-二甲氧基4一羟基苯甲醛(3,5-dimethoxy-4-hydroxy-benzalde-hyde,3),3,5-二甲氧基_4.羟基苯乙酮(3,5-dimethoxy-4-hydroxyacetophenone,4),ethyl 2-pyrrolidinone-5(s),carboxylate(5),5-羟甲基糠醛(5-hydroxymethyl-furaidehyde,6),棕榈酸(palmitic acid,7),丁二酸(succinic acid,8),葡萄糖(glucose,9),胡萝卜苷(daucosterol,10),β-谷甾醇(β-sitosterol,11).结论:化合物1,2,4,5,7,9为首次从该属植物中分离得到,且化合物5为首次从天然产物中分离得到.     

构树黄酮类化合物及其PTP1B抑制活性研究

利用正相和反相硅胶柱色谱、凝胶柱色谱和反相高效液相等分离和纯化方法,从构树Broussonetia papyrifera茎枝中分离得到11个黄酮类化合物。运用NMR,MS,UV,IR等波谱方法鉴定了它们的结构,分别为构树素A(1),5,7,3',4'-四羟基-3-甲氧基-8-香叶基黄酮(2),8-异戊烯基槲皮素-3-甲醚(3),构树醇D(4),构树黄酮醇B(5),新乌尔醇(6),构树醇E(7),8-(1,1-二甲基丙烯基)-5'-(3-甲基-2-丁烯基)-3',4',5,7-四羟基黄酮醇(8),构树黄酮醇E(9),4,2',4'-三羟基查尔酮(10),紫铆花素(11)。其中化合物1为新的异戊烯基取代的黄酮醇,化合物3,6,10,11为首次从构属植物中分离得到,化合物4和7为首次从构树中分离得到。化合物1～5和7～9具有显著的蛋白酪氨酸磷酸酶1B抑制活性,IC50为(0.83±0.30)～(4.66±0.83)μmol·L-1。     

多花黄精地上部分化学成分的研究

目的研究多花黄精Polygonatum cyrtonema地上部分的化学成分。方法采用色谱分离技术进行分离和纯化,并根据波谱学数据鉴定化合物的结构。结果从多花黄精地上部分的甲醇提取物中分离得到15个化合物,分别鉴定为(3R)-5,7-dihydroxy-3-(2'-hydroxy-4'-methoxybenzyl)-chroman-4-one(1)、5,7-dihydroxy-6-methyl-3-(2',4'-dihydroxybenzyl)-chroman-4-one(2)、5,7-dihydroxy-6-methyl-3-(4'-hydroxybenzyl)-chroman-4-one(3)、(3S)-3,7-dihydroxy-8-methoxy-3-(3',4'-methylenedioxybenzyl)-chroman-4-one(4)、芹菜素(5)、山柰酚(6)、香草酸(7)、反式对羟基桂皮酸(8)、反式对羟基桂皮酸甲酯(9)、水杨酸(10)、(+)-丁香脂酸(11)、balanophonin B(12)、咖啡酸(13)、苯丙氨酸(14)和松柏醛(15)。结论化合物1、2、7、11、14和15为首次从多花黄精中分离得到,化合物3、4和12为首次从黄精属植物中分离得到。     

桑白皮的化学成分研究(Ⅱ)

目的:研究桑白皮的化学成分.方法:采用硅胶和凝胶柱色谱分离纯化,根据理化性质和光谱数据分析鉴定化合物.结果:分离并鉴定了11个化合物,分别为:桑辛素C(moracin C,1),桑辛素M(moracin M,2),桑辛素M-3'-O-β-D-吡喃葡萄糖苷(moracin M-3'-O-β-D-glucopyranoside,3),桑辛素O(moracin O,4),桑皮酮S(kuwanon S,5),桑皮酮T(kuwanon T,6),5,7-二羟基色酮(5,7-dihydroxychromone,7),5,7,2'-三羟基二氢黄酮-4'-O-β-D-吡喃葡萄糖苷(5,7,2'-trihydroxyflawone4,-O-β-D-glucoside,steppogenin-4'-O-β-D-glucoside,8),7-羟基香豆素(7-hydroxycoumarin,9),5,7-二羟基香豆素-7-O-β-D-吡喃葡萄糖苷(5,7-dihydro-xycoumarin-7-O-β-D-glucopyranoside,10),桑叶苷C(mullberroside C,11).结论:其中化合物8为首次从该属植物中分离得到,化合物2,4,6为首次从该植物中分离得到.     

白木香叶化学成分的研究

目的:研究白木香叶的化学成分,为白木香的综合利用提供依据.方法:采用硅胶柱色谱、Sephadex LH-20柱色谱、重结晶等方法进行分离纯化,运用NMR,Ms等波谱学方法进行结构鉴定.结果:从白木香叶中分离鉴定了13个化合物,分别为7-羟基-5,4'-二甲氧基.黄酮(1),洋芹素-7,4'-二甲醚(2),木犀草素-7,3',4'一三甲醚(3),异紫堇啡碱(4),对羟基苯甲酸(5),正三十二(烷)醇(6),正三十一烷(7),α-豆甾醇(8),表木栓醇(9),木栓烷(10),木栓酮(11),芫花素(12),5,4'-二羟基_7,3'-二甲氧基黄酮(13).结论:化合物4为首次从该属中分离得到,化合物1,6～11,13为首次从该植物中分离得到.     

思茅豆腐柴中的黄酮类化学成分研究

 目的研究民族药物思茅豆腐柴(Premna szemaoensis Pei)中的黄酮类化学成分。方法利用Sephadex LH-20及硅胶等色谱技术进行分离纯化,根据理化性质、光谱数据进行结构鉴定。结果得到7个黄酮类化合物,分别鉴定为5,4'-二羟基- 3,7,3'-三甲氧基黄酮(1),5-羟基-3',4',6,7-四甲氧基黄酮(2),5,4'-二羟基-7-甲氧基黄酮醇(3),5,3'-二羟基-7,4'-二甲氧基黄酮醇(4),3',4',5-三羟基-3,7-二甲氧基黄酮(5),5,7-二羟基-4'-甲氧基黄酮(6),5-羟基-7,3',4'-三甲氧基黄酮醇(7)。结论这7个化合物均为首次从思茅豆腐柴中分离得到。     

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.     

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。     

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.     

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.     

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.