圆锥绣球化学成分研究

目的:对圆锥绣球茎枝水提取物进行化学成分研究。方法:利用各种色谱方法进行化学成分分离,根据理化性质和波谱数据鉴定化合物的结构。结果:分离得到9个化合物,分别鉴定为茵芋苷(1),isotachioside(2),8-甲氧基香豆素-7-O-β-D-葡萄糖苷(3),6-甲氧基香豆素-7-O-β-D-葡萄糖苷(东莨菪苷,4),3,4,5-三甲氧基苯酚-1-O-6-α-L-鼠李糖基-(1→6)-O-β-D-葡萄糖苷(5),伞形花内酯-7-O-β-D-芹菜糖基-(1→6)-O-β-D-葡萄糖苷(6),伞形花内酯(7),6-甲氧基-7-羟基香豆素(东莨菪素,8)和7-羟基-8-甲氧基香豆素(9)。结论:1~7为首次从该植物中分离得到。     

长尾粗叶木根化学成分的研究Ⅰ

目的:研究茜草科粗叶木属植物长尾粗叶木Lasianthus acuminatissimus根中的化学成分。方法:利用正相、反相(RP-18)硅胶柱色谱、大孔树脂柱色谱和制备高效液相色谱分离,通过现代波谱技术(¹³C-NMR,¹H-NMR,DEPT,EI-MS)鉴定结构。结果:分离鉴定了6个化合物,分别为:异东莨菪素(isoscopletinⅠ),异东莨菪素6-O-β-D-葡萄糖苷(isoscopletin-6-O-β-D-glucopyranosideⅡ),mudanoside-A的β构型体(Ⅲ),车叶草苷(asperulosideⅣ),(-)-pinoresinol 4-O-β-D-glucopyranoside(Ⅴ),胡萝卜苷(Ⅵ)。结论:这些化合物均是首次从粗叶木属植物中得到。     

白桑叶化学成分研究

目的研究白桑叶的化学成分。方法利用各种色谱技术进行分离,根据光谱数据鉴定结构。结果从白桑叶中分离得到17个单体化合物,分别鉴定为β-谷甾醇(1)、茄尼醇(2)、(6S,9R)-6-羟基-3-氧代-α-紫罗兰醇-9-O-β-D-葡萄糖苷(3)、5α,6α-环氧-β-紫罗兰酮-3-O-β-D-葡萄糖苷(4)、5,5’-二甲氧基落叶松树脂醇-4-O-β-D-葡萄糖苷(5)、腺苷(6)、3β-羟基-5α,6α-环氧-β-紫罗兰醇-2α-O-β-D-葡萄糖苷(7)、山柰酚-3-O-β-槐糖苷(8)、山柰酚-3-O-α-L-吡喃鼠李糖基(1→2)-β-D-吡喃葡萄糖苷(9)、东莨菪苷(10)、icariside B(11)、木犀草素-7-O-β-D-葡萄糖苷(12)、山柰酚-3-O-α-L-鼠李糖苷(13)、东莨菪内酯(14)、山柰酚-3-O-β-D-葡萄糖苷(15)、马栗树皮素-7-O-β-D-葡萄糖苷(16)、左旋丁香树脂酚-4-O-β-D-吡喃葡萄糖苷(17)。结论化合物2、4、5、6、7、8、9、13为首次从该植物中分离得到。     

籽瓜汁化学成分的分离与鉴定

目的:对籽瓜汁的化学成分进行研究。方法:通过反复硅胶柱色谱和羟丙基葡聚糖凝胶柱色谱方法进行分离纯化,运用核磁共振氢谱、碳谱技术和质谱技术进行结构鉴定。结果:共分离鉴定8个化合物。分别鉴定为3,5-二甲氧基-苄醇-4-O-β-D-吡喃葡萄糖苷(1),2,6-二甲氧基-4-羟基-苯酚-1-O-β-D-吡喃葡萄糖苷(2),1-O-对香豆酰基甘油酯(3),松柏苷(4),cucumegastigmanes II(5),linarionoside C(6),δ-葡萄素(7),山柰酚-3-O-葡萄糖基1-O-β-D-葡萄糖-6-O-α-L-鼠李糖苷(8)。结论:化合物1~8均为首次从籽瓜中分离得到。     

短梗菝葜根茎的化学成分研究

目的对菝葜科菝葜属植物短梗菝葜根茎的化学成分进行研究。方法采用硅胶、反相硅胶(RP-18)、半制备HPLC色谱法,葡聚糖凝胶(Sephadex LH-20)等多种分离方法,运用NMR、MS等波谱方法以及结合文献数据对分离得到的化合物进行结构鉴定。结果从短梗菝葜根的正丁醇部位中分离得到9个化合物,通过核磁共振数据将其结构鉴定为:丁香脂素O-β-D葡萄糖苷(1),2,5-diaryltetrahydrofuran-typelignin(2),(+)-lyoniresinol 3α-O-α-L-rhamnopyranoside,(3),(1S,2R)-1-(3,4,5-三甲氧基苯基)-1,2,3-丙三醇(4),(1R,2R)-1-(3,4,5-三甲氧基苯基)-1,2,3-丙三醇(5),(+)-lyonirenisol-3α-O-β-D-glucopyranoside(6),岩白菜素(7),3,4,5,-三甲氧基苯酚(8),ethylβ-D-glucopyranoside(9)。结论化合物1~9均为首次从短梗菝葜中分离得到。     

蒿状大戟化学成分研究

采用正反相硅胶、MCI树脂、Sephadex LH-20和Rp-HPLC等色谱手段进行蒿状大戟Euphorbia dracunculoides化学成分的分离纯化,从蒿状大戟地上部分的70%丙酮提取物中得到16个化合物。利用MS、1H NMR和13C NMR等现代波谱技术确定化合物结构为西瑞香素(daphnoretin,1),异秦皮素(isofraxidin,2),东莨菪内酯(scopoletin,3),山柰酚(kaempferol,4),槲皮素(quercetin,5),番石榴苷(guaijaverin,6),紫云英苷(astragalin,7),槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,8),柚皮素-7-O-β-D-吡喃葡萄糖苷(naringenin-7-O-β-D-glucopyranoside,9),5-甲氧基芹菜素-7-O-β-D-吡喃葡萄糖苷(5-O-methyl-apigenin-7-O-β-D-glucopyranoside,10),没食子酸甲酯(methyl gallate,11),prionitiside A(12),(2S)-2,3-dihydroxypropyl-1,6,8-trihydroxy-3-methyl-9,10-dioxoanthracene-2-carboxylate(13),3,3’-O-二甲基鞣花酸(3,3’-di-O-methyl ellagic acid,14),3’-O-methyl-3,4-O,O-metheneellagic acid-4’-O-β-D-glucopyranoside(15)和3,4-methylenedioxy-3’-O-methylellagic acid(16)。其中,化合物1~3,6~9,11和14为首次从该植物中分离得到,化合物10,12,13,15和16首次从大戟属植物中分离得到。     

栀子化学成分(Ⅳ)

目的:研究栀子的干燥成熟果实中的化学成分。方法:采用各种柱色谱方法分离纯化,通过理化常数测定和光谱分析鉴定化合物的结构。结果:从栀子的果实中分离鉴定了10个化合物,分别为6″-O-[(E)-p-香豆酰基]京尼平龙胆二糖苷(1),3-O-咖啡酰基-4-O-芥子酰基奎宁酸(2),6″-O-反式-芥子酰基京尼平龙胆二糖苷(3),绿原酸(4),3-甲氧基-4-羟基苯酚(5),东莨菪内酯(6),滨蒿内酯(7),2-(3-甲氧基-4-羟基苯)乙基-β-D-呋喃芹糖氧基-(1→6)-β-D-葡萄糖苷(8),中脂素(9),5’-甲氧基异落叶松脂醇-3α-O-β-D-葡萄糖苷(10)。结论:化合物5~10为首次从该植物中分离得到。     

圆苞金足草化学成分研究

目的研究圆苞金足草Goldfussia pentstemonoides全草的化学成分。方法采用色谱技术进行分离纯化,根据波谱数据并参考文献鉴定化合物结构。结果从圆苞金足草95%乙醇提取物的正丁醇萃取部位分离得到10个芳香类化合物,分别鉴定为毛柳苷(1)、3,4,5-三甲氧基苯酚-1-O-6-L-鼠李糖基-(1→6)-O-β-D-葡萄糖苷(2)、异类叶升麻苷(3)、isonuomioside A(4)、苯甲醇-O-β-D-吡喃葡萄糖苷(5)、淫羊藿次苷F2(6)、(-)-lyoniresinol 3α-O-β-D-glucopyranoside(7)、(+)-异落叶松脂素-9-O-β-D-吡喃葡萄糖苷(8)、脱咖啡酰基毛蕊糖苷(9)、dehydrodiconiferyl alcohol 4-O-β-D-glucopyranoside(10)。结论所有化合物为首次从圆苞金足草中分离得到。     

荨麻抗风湿活性部位的化学成分研究

目的研究荨麻抗风湿活性部位的化学成分。方法运用柱色谱、制备型薄层色谱等方法对荨麻抗炎镇痛的活性部位进行分离;运用UV、IR、MS、NMR等方法进行结构鉴定。结果从活性部位中分离并鉴定了12个成分,分别为槲皮素(quercetin,)、山柰酚(kaempferol,)、山柰酚-3-O-β-D-吡喃葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside,)、槲皮素-3-O-β-D-吡喃葡萄糖苷(quercetin-3-O-β-D-glucopyranoside,)、咖啡酸(caffeicacid,)、绿原酸(chlorogenicacid,)、东莨菪苷(scopolin,)、东莨菪内酯(scopoletin,)、山柰酚-3-O-β-D-芸香糖苷(kaempferol-3-O-rutinoside,)、槲皮素-7-O-β-D-吡喃葡萄糖苷(quercetin-7-O-β-D-glucopyranoside,)、异鼠李素-3-O-β-D-芸香糖苷(isorhamnetin-3-O-β-D-rutinoside,)、β-谷甾醇(β-sitosterol,)。结论化合物~均为首次从荨麻中分得,其中化合物、、均为首次从荨麻属植物中分得。     

翻白叶树根的化学成分研究

目的 研究翻白叶树Pterospermum heterophyllum根的化学成分.方法 应用多种色谱技术进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构.结果 从翻白叶树根95％乙醇提取物中分离得到12个化合物,分别鉴定为莨菪苷(1)、2,6-二甲氧基-4-羟基-苯酚-1-O-β-D-吡喃葡萄糖苷(2)、3-甲氧基-4-羟基-苯酚-1-O-β-D-吡喃葡萄糖苷(3)、4-羟基-2-甲氧基-苯酚-1-O-β-D-吡喃葡萄糖苷(4)、甲基熊果苷(5)、(+)-南烛木树脂酚-3 α-O-β-D-吡喃葡萄糖苷(6)、(-)-南烛木树脂酚-3α-O-β-D-吡喃葡萄糖苷(7)、(-)-南烛木树脂酚-2 α-O-β-D-吡喃葡萄糖苷(8)、(-)-异落叶松树脂酚-6-O-β-D-吡喃葡萄糖苷(9)、(-)-8,8’-二甲氧基-开环异落叶松树脂酚-1-O-β-D-吡喃葡萄糖苷(10)、(+)-3-oxo-α-ionyl-O-β-D-glucopyranoside( 11)、roseoside( 12).结论 化合物1～11为首次从该属植物中分离得到.     

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.     

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.