橡胶灵芝化学成分研究

利用硅胶柱色谱和Sephadex LH-20凝胶柱色谱技术对橡胶灵芝Ganoderma philippii进行化学成分研究,从中分离到16个化合物,通过波谱方法分别鉴定为2,5-二羟基苯乙酮（1）,甲龙胆酸（2）,（S）-苹果酸二甲酯（3）,muurola-4,10（14）-dien-11β-ol（4）,dihydroepicubenol（5）,5-羟甲基呋喃甲醛（6）,麦角甾-7,22E-二烯-3β-醇（7）,麦角甾-7,22E-二烯-3-酮（8）,麦角甾-7,22E-二烯-2β,3α,9α-三醇（9）,6β-甲氧基麦角甾-7,22E-二烯-3β,5α-二醇（10）,麦角甾-4,6,8（14）,22E -四烯-3-酮（11）,麦角甾-4,6,8（14）,22E-四烯-3β-醇（12）,5α,8α-过氧桥麦角甾-6,22E-二烯-3β-醇（13）,7α-甲氧基-5α,6α-epoxy麦角甾-8（14）,22E-二烯-3β-醇（14）,麦角甾-8,22E-二烯-3β,5α,6β,7α-四醇（15）,麦角甾-5,23E-二烯-3β-醇,醋酸盐（16）。化合物1~16均首次从橡胶灵芝中分离得到,其中化合物4 ,5首次从灵芝属分离得到。     

桂花果实的化学成分研究

采用硅胶、Sephadex LH-20等多种材料进行分离纯化,通过理化方法和波谱分析进行结构鉴定,从桂花果实醇提溶液的乙酸乙酯萃取部分,分离并鉴定了23个化合物,分别为尼克酰胺（1）,D-阿洛醇（2）,5-羟甲基-2-呋喃甲醛（3）,乙酰氧基齐墩果酸（4）,苯甲酸（5）,麦角甾-7,22-二烯-3-酮（6）,β-谷甾醇（7）,borreriagenin（8）,麦角甾-7,22-二烯-3β,5α,6β-三醇（9）,C-veratroylglycol（10）,甲基-2-O-β-吡喃葡糖基苯甲酸（11）,3’,7-二羟基-4’-甲氧基异黄酮（12）,7-羟基香豆素（13）,咖啡酸甲酯（14）,齐墩果酸（15）,（-）-襄五脂素（16）,莳萝油脑（17）,3β,5α,9α-三羟基-麦角甾-7,22-二烯-6-酮（18）,2α-羟基齐墩果酸（19）,桦木酸（20）,白桦脂醇（21）,3,3’-Bisdemethylpinoresinol（22）,羽扇豆醇（23）。所有化合物在桂花果实中均为首次分离;除化合物 4,7,15,19,23外,其余化合物在此种植物中为首次分离。     

紫芝中的一个新甾醇

 目的 研究紫芝Ganoderma sinense子实体的化学成分。方法 通过反复硅胶柱色谱进行分离纯化,利用多种波谱技术鉴定化合物的结构。结果 分离鉴定了5个化合物,分别为：麦角甾-7,22-二烯-2β,4α-二醇（ergosta-7, 22-dien-2β, 4α-diol,1）、麦角甾-7,22-二烯-2β,3α,9α-三醇（ergosta-7, 22-dien-2β, 3α, 9α-triol,2）、麦角甾-7,22-二烯-3β,5α,6β,9α-四醇（ergosta-7, 22-dien-3β, 5α, 6β, 9α-tetraol,3）、麦角甾-7, 22-二烯-3β-棕榈酸酯（ergosta-7, 22-dien-3β-yl palmitate,4）、5-羧基糠醛（5-formylfuran-2-carboxylic acid,5）。结论 化合物1为新化合物,其余化合物均为首次从紫芝中分离得到。     

蓖麻中的萜类和甾体及抗糖尿病活性研究

运用多种色谱方法从蓖麻地上部分甲醇提取物中分离得到7个萜类化合物和3个甾体化合物,经波谱技术分别鉴定为ficusic acid（1 ）, 叶绿醇（2）, callyspinol（3）, 羽扇豆醇（4）, 30-降羽扇豆-3β-醇-20-酮（5）, 羽扇豆-20（29）-烯-3β,15α-二醇（6）, acetylaleuritolic acid（7）, 豆甾-4-烯-3-酮（8）, 豆甾-4-烯-6β-醇-3-酮（9）, 豆甾-4-烯-3,6-二酮（10）, 其中化合物 1 ~ 3,5 ~ 10 是首次从该植物中分离得到,体外抗糖尿病活性表明,化合物 5,6 对小鼠和人11β-HSD具有显著的抑制活性和良好的选择性。     

小球藻化学成分的研究

利用硅胶柱色谱和Sephadex LH-20 凝胶柱色谱技术对小球藻石油醚部位的化学成分进行研究,并根据理化性质和光谱分析鉴定化合物的结构。从小球藻石油醚萃取部位获得脂溶性提取物M1, M2, M3,分离得到化合物5个,分别鉴定为(22E,24R)-5α,8α-过氧化麦角甾-6,22-二烯-3β-醇 (1),(24S)-麦角甾-7-烯-3β-醇(2), 黑麦草内酯(3),豆甾-7,22-二烯-3β,5α,6α-三醇(4)和3β-羟基-5α,6α-环氧-7-大柱香波龙烯-9-酮(5)。小球藻脂溶性提取物以脂肪酸酯类、烷酸类和烯酸类为主,化合物1~5均为首次从该属植物中分离得到。     

皱盖假芝中1个新的木脂素类成分

目的 对皱盖假芝Amauroderma rude子实体中的化学成分进行初步研究。方法 采用硅胶柱色谱、凝胶柱色谱、液相色谱等多种色谱方法对皱盖假芝子实体醋酸乙酯相中的化学成分进行分离纯化,并根据其理化性质和波谱数据鉴定化合物结构。结果 从皱盖假芝醋酸乙酯相中分离得到3个化合物,包括1个新的木脂素和2个已知的甾醇类化合物,分别鉴定为3,4-二羟基苯甲酰乙酰酮（1）、（22E,24R）-3β,5α-二氢-麦角甾-7,22-二烯-6-酮（2）、（22E,24R）-麦角甾-6,9,22-三烯-3β,5α,8α-三醇（3）。结论 化合物1为新的木脂素类成分,命名为假芝木脂素B。     

厚蜂窝菌的化学成分研究

目的研究厚蜂窝菌发酵液的化学成分。方法厚蜂窝菌发酵液的乙酸乙酯提取部位经过硅胶、RP-18、Seph-adex LH-20等多种材料进行分离纯化,通过理化方法和波谱分析进行结构鉴定。结果分离鉴定了11个化合物,经波谱数据分析分别鉴定为角鲨烯(1)、9(Z)-十八烷烯酸(2)、麦角甾-4,6,8(14),22-四烯-3-酮(3)、麦角甾-5,7,22-三烯-3β-醇(4)、过氧麦角甾醇(5)、麦角甾-6β-甲氧基-7,22-二烯-3β,5α-二醇(6)、麦角甾-7,22-二烯-3β,5α,6β-三醇(7)、8,14-环氧麦角甾-4,22-二烯-3,6-二酮(8)、麦角甾-3β,5α,9α-三羟基-7,22-二烯-6-酮(9)、2,2-二甲基-1-苯并吡喃-6-醇(10)、2-呋喃甲酸(11)。结论以上化合物均是首次从该种真菌中分离得到。     

木蹄层孔菌化学成分研究

 目的 研究木蹄层孔菌 [ Fomes fomentarius ( L.Ex.Fr.) ] 的化学成分。方法 采用反复硅胶柱色谱法、Sephadex LH-20 柱色谱法等进行分离纯化,并通过化合物的理化性质和波谱数据进行结构鉴定。结果 从木蹄体积分数95%乙醇提取物中分离得到6个化合物,其中1个木脂素类化合物：泡桐素 (1);2个小分子芳香族化合物：原儿茶醛 (2),4-( 3,4-二羟苯基)-3-丁烯-2-酮 (3); 3个甾类化合物：5α,8α-过氧化麦角甾-6,22-二烯-3β醇 (4),麦角甾-7,22-二烯-3β醇 (5),β-谷甾醇 (6) 。结论 化合物1～4, 6均为首次从该真菌中分离得到。     

喜热灵芝子实体化学成分研究

目的:研究喜热灵芝子实体的化学成分。方法:采用硅胶柱层析、薄层制备色谱、高压制备液相等色谱方法分离喜热灵芝子实体的化学成分,运用核磁共振氢谱、碳谱等波谱方法鉴定化合物的结构。结果:从喜热灵芝中分离12个化合物,分别鉴定为:麦角甾-7,22-二烯-3β-棕榈酸酯(1)、(22E,24R)-麦角甾-7,22-二烯-3β-醇(2)、灵芝萜烯二醇(3),6,9-环氧麦角-7,22-二烯-3β-醇(4)、灵芝酮二醇(5)、丁二酸(6)、灵芝醇F(7)、赤芝酮(8)、灵芝酮三醇(9)、灵芝醇A(10)、(22E,24R)-麦角甾-7,22-二烯-2β,3α,9α-三醇(11)、泥湖鞘胺醇(12)。结论:其中,化合物1、2、4~7、9~12为首次从该真菌中分离得到。     

云南美登木内生真菌Botryosphaeria sp. MHF次生代谢产物研究

目的:对云南美登木内生真菌Botryosphaeria sp.MHF的化学成分进行研究.方法:采用反相、正相等多种柱色谱法进行分离;应用波谱技术进行结构鉴定.结果:从云南美登木内生真菌B.sp.MHF的发酵物中分离得到8个化合物:分别是麦角甾-5-烯-3-醇(1)、麦角甾-4,6,8,22-四烯-3-酮(2)、麦角甾-3β,5α,9α-三羟基-7,22-二烯-6-酮(3)、麦角甾-7,22-二烯-3β,5α,6β-三醇(4)、麦角甾-5α,8α-环二氧-6,22-二烯-3-醇(5)、fusaproliferin (6)、脑苷脂C(7)和3,4,5-三羟基-四氢萘酮(8).结论:所有化合物均为首次从以Murashige-Skoog培养基培养的该菌株中分离得到.     

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.