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。     

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。     

蜜环菌的化学成分研究

对蜜环菌Armillaria mellea发酵培养物的化学成分进行研究。采用硅胶、Sephadex LH-20柱色谱等方法进行分离纯化,根据波谱数据及与对照品对照鉴定化合物结构。从蜜环菌发酵培养物中分离鉴定了10个化合物,分别为2-羟基-4-甲氧基-6-甲基苯甲酸(1),苔藓酸(2),蜜环菌戊素(3),麦角甾醇(4),染料木素(5),大豆素(6),胡萝卜苷(7),染料木苷(8),尿嘧啶(9)和甘露醇(10)。化合物 1~10 均为首次从蜜环菌发酵培养物中分离得到,其中,化合物 1~4,6,10 在蜜环菌菌丝体或菌索中已有报道。通过二维核磁波谱确证,首次报道化合物3以DMSO为溶剂的氢、碳谱数据,是对该类成分波谱数据的补充。     

三白草木脂素类化学成分的研究

目的: 研究三白草Saururus chinensis抗尼古丁戒断症状有效部位中木脂素类化学成分。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木脂素类化合物的结构。结果: 从三白草抗戒断症状有效部位中分离鉴定得到13个化合物,分别为三白脂酮(1),三白脂酮A(2),1'-表三白脂酮 (3),里卡灵B (4),里卡灵A (5),5-甲氧基-里卡灵A (6),三白脂素(7),5,5'-二甲氧基-三白脂素(8),nectandrin B (9),5,5'-dimethoxy-nectandrin B (10),3',4'-methylenedioxy-3,4,5,5'-tetramethoxy-7,7'-epoxylignan(11),3',4'-methylenedioxy-3,4,5-trimethoxy-7,7'-epoxylignan (12),machilin D (13)。结论: 化合物6,8,10~12为首次从该植物中分离得到。     

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.     

蒙药长松萝的化学成分研究

目的: 研究长松萝的化学成分。 方法: 用正相硅胶、Sephadex LH-20、制备高效液相色谱等方法进行分离纯化, 根据理化性质、光谱数据以及结合文献报道的波谱数据鉴定化合物的结构。 结果: 分离得到10个化合物, 分别鉴定为(4aR,9bS)-2,6-二乙酰基-3,4a,7,9-四羟基-8,9b-二甲基-1-氧代-1,4,4a,9b-四氢二苯骈呋喃酮(1), (+)-松萝酸(2),苔黑酚(3),18R-hydroxydihydroalloprotolichensterinic acid(4),3β-羟基-5α,8α-桥二氧麦角甾-6,22-二烯(5), 扁枝衣酸乙酯(6),阿拉伯糖醇(7), 芹菜素-7-O-β-D-葡萄糖醛酸苷(8), 3-羟基-5-O-甲基-2-甲基苯甲酸(9),木栓酮(10)。 结论: 化合物1为新化合物,化合物8为首次从松萝属地衣分离得到,化合物3,4,7为首次从长松萝中分离得到。     

接骨木中的木脂素类化学成分及其对UMR106 细胞增殖作用的影响

研究接骨木Sambucus williamsii茎枝中的木脂素类化学成分,并讨论它们对大鼠骨肉瘤细胞UMR106增殖的影响。该研究采用D101大孔吸附树脂,硅胶,ODS,Sephadex LH-20,Toyopearl HW-40和RP-HPLC等色谱分离手段对接骨木茎枝60%乙醇提取物进行分离纯化,并运用波谱方法对所分离的化合物进行结构鉴定。从中分离鉴定了6个木脂素类化合物和1个酚酸类化合物,经波谱解析鉴定为threo-guaiacylglycerol-β-O-4’-conifery ether（1）,lirioresinol A（2）,1-hydroxypinoresinol（3）,5-甲氧基蛇菰宁（4）,蛇菰宁（5）,5-methoxy-trans-dihydrodehydrodiconiferyl alcohol（6）和对羟基苯甲醛（7）,化合物 3~7首次从该属植物中分离得到。对所有分离得到的化合物进行了类成骨UMR106细胞增殖活性的测定,化合物 1~7 均能一定程度上促进UMR106细胞的增殖。     

藏药甘青乌头化学成分研究

对甘青乌头Aconitum tanguticum全草的化学成分进行研究。应用硅胶,ODS,Sephadex LH-20,制备HPLC等各种色谱技术进行分离纯化,采用MS,NMR等波谱技术鉴定化合物结构。甘青乌头乙醇总提取物经石油醚、乙酸乙酯萃取后的剩余水溶液经AB-8大孔吸附树脂,依次用水,30%,60%,95%乙醇洗脱,合并回收溶剂分别得到各洗脱部分。从30%,60%乙醇洗脱部分共分离得到19个化合物,分别鉴定为紫丁香苷(1),香草酸4-O-β-D-阿洛糖苷(2),阿魏酸4-O-β-D-阿洛糖苷(3),阿魏酸4-O-β-D-葡萄糖苷(4),芥子酸4-O-β-D-葡萄糖苷(5),4-羟基-肉桂醇-4-O-β-D-葡萄糖苷(6),槲皮素-3-O-α-L-鼠李糖基-(1→2)-[α-L-鼠李糖基-(1→6)]-β-D-半乳糖苷-7-O-α-L-鼠李糖苷(7),山柰酚-3-O-α-L-鼠李糖基-(1→2)-[α-L-鼠李糖基-(1→6)]-β-D-半乳糖苷-7-O-α-L-鼠李糖苷(8),槲皮素-3-O-α-L-鼠李糖基(1→6)-β-D-半乳糖苷-7-O-α-L-鼠李糖苷(9),山柰酚-3-O-[β-D-葡萄糖基-(1→3)-(4-O-反式-对香豆酰基)]-α-L-鼠李糖基-(1→6)-β-D-半乳糖苷-7-O-α-L-鼠李糖苷(10),槲皮素-3-O-[β-D-葡萄糖基-(1→3)-(4-O-反式-对香豆酰基)]-α-L-鼠李糖基-(1→6)-β-D-半乳糖苷-7-O-α-L-鼠李糖苷(11),红景天苷(12),2-(3,4-二羟基苯基)乙醇 1-O-β-D-葡萄糖苷(13),(7S,8R)-去氢二松柏醇-9'-O-β-D-葡萄糖苷(14),citrusin B (15),异叶乌头碱(16),tanaconitine(17),山栀苷甲酯(18)和淫羊藿次苷B₁(19)。除化合物 4,13,16和17 外,其余化合物均为首次从甘青乌头中分离得到。     

中药千年健的化学成分研究

采用正相硅胶柱色谱、葡聚糖凝胶SephadexLH-20柱色谱、重结晶等方法对中药千年健进行了化学成分研究,并运用波谱方法对所分离得到的化合物进行结构鉴定。结果从中药千年健中分离并鉴定了12个化合物,分别为5-pentylresorcinol-β-glucoside(1),原儿茶酸(2),对羟基苯甲酸(3),香草酸(4),5-羟甲基-2-呋喃甲酸(5),2-呋喃甲酸(6),5-羟甲基-2-糠醛(7),(R)-苹果酸(8),(R)-苹果酸二甲酯(9),1,2,3-丙烷三羧酸三甲酯(10),4-羟基-四氢呋喃-2-酮(11)和三羟基薄荷烷(12)。其中,化合物1为新的天然产物,化合物4~12为首次从该属植物中分离得到。     

柳叶蜡梅叶氯仿部位化学成分的研究

为寻找柳叶蜡梅Chimonanthus salicifoliu叶中的抗肿瘤活性成分,对其氯仿部位进行了化学成分研究。通过正相硅胶柱色谱技术进行分离纯化,根据理化性质和光谱数据鉴定了12个化合物的结构,分别为9-epi-blumenol C(1),blumenol C(2),(+)-去氢催吐萝芙叶醇(3),(+)-催吐萝芙叶醇(4),robinlin(5),(-)-黑麦交酯(6),异秦皮定(7),东莨菪素(8),6, 7-二甲氧基香豆素(9),6, 7, 8-三甲氧基香豆素(10),β-谷甾酮(11),β-谷甾醇(12)。其中化合物1~6为蜡梅科植物中首次分离到的降倍半萜类化合物,化合物1 为首次分离到的天然产物,化合物7,11和12为本植物中首次分离得到。     

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。     

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.     

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.     

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.     

不同类型的桑螵蛸与其基原昆虫对应关系研究

桑螵蛸为常用中药,因其入药部位为螳螂的卵鞘,无法直接判断其基原昆虫.同时螳亚科动物种类繁多,均产卵鞘,目前关于桑螵蛸对应的基原昆虫尚无一致的结论,而二者准确的对应关系是保证桑螵蛸质量的基础,也是桑螵蛸条形码研究的基础.文章采用人工孵化与捕捉活体螳螂2种方式,分别鉴定了药材及其原动物,系统地研究了桑螵蛸与基原昆虫的对应关系,发现基原昆虫为大刀螳属、斧螳属、污斑螳属的多种昆虫,该研究为桑螵蛸深入开发与利用研究奠定了基础.