黑骨藤中的一个二萜醌类化合物

目的:利用硅胶柱色谱及重结晶对黑骨藤抗炎活性部位进行化学成分研究,从其活性部位(乙酸乙酯部位)分离得到1个化合物丹参酮ⅡA,该化合物为首次在萝藦科杠柳属植物中发现的二萜醌类化合物。     

黑骨藤抑制破骨细胞分化及骨吸收能力的活性部位研究

目的:探究黑骨藤对破骨细胞分化的影响并确定其活性部位。方法:采用维生素D3(VD3)诱导兔骨髓细胞法获得破骨细胞,以形态学观察、苏木素和伊红(HE)染色、抗酒石酸酸性磷酸酶(TRAP)染色鉴定破骨细胞,然后通过测定黑骨藤各极性部位低、中、高剂量组(1,10,100 mg·L-1)对破骨细胞TRAP酶活力,TRAP+细胞计数及骨吸收陷窝面积的影响来确定活性部位。结果:黑骨藤水饱和正丁醇层的高剂量组及乙酸乙酯层的中、高剂量组均对骨髓细胞向破骨细胞分化具有显著的抑制作用(P<0.01),并具有剂量依赖性。在抑制破骨细胞骨吸收能力实验中,黑骨藤乙酸乙酯层各剂量组均有显著抑制骨吸收陷窝面积的作用(P<0.01),而正丁醇层中、高剂量组具有显著抑制作用(P<0.01),均呈剂量依赖性。结论:黑骨藤抑制骨髓细胞向破骨细胞分化及骨吸收能力的主要活性部位是乙酸乙酯部位。     

基于网络药理学的苗药黑骨藤防治肺癌分子机制研究

目的:利用网络药理学对西南地区苗药黑骨藤防治肺癌的分子机制进行研究。方法:采用磺酰罗丹明B(SRB)比色法考察苗药黑骨藤抗肺癌活性部位,运用网络药理学的方法,通过文献检索上述各活性部位已分离得到的化合物并应用Linpinski 5原则筛选黑骨藤中与肺癌相关的活性成分。结果:黑骨藤抗肺癌活性部位为正丁醇、水、氯仿、乙酸乙酯,活性成分共42个,活性成分与疾病作用的关键靶点53个,GO富集分析显示黑骨藤作用于肺癌的关键节点为EGFR、GRB2、P53、NF-κB;主要分子功能包括调节NF-κB结合,泛素连接酶的活性;生物学过程包含氧化应激,调节转录与生长;信号通路主要富集在细胞增殖、凋亡、应激及泛素介导的水解、MAPK等16条信号通路。结论:黑骨藤抗肺癌可能是通过PI3K-AKT和MAKB信号通路发挥作用。     

桃仁凝血因子Xa抑制活性部位分析

目的:研究中药桃仁的化学成分及其对凝血因子Xa(FXa)的抑制活性。方法:采用生色底物法和连续速率法进行FXa抑制活性测定,利用多种柱色谱技术对活性部位进行分离纯化,并通过波谱分析方法鉴定各化合物的结构。结果:桃仁乙酸乙酯萃取部位对FXa的抑制率高达60.27%,为抑制FXa的活性部位;从活性部位中分离鉴定出10个化合物,分别鉴定为9-十八碳烯酸-2',3'-二羟基丙酯(1),胡萝卜苷(2),扁桃酰胺(3),苯甲酸(4),2-羟基-9-十八碳烯酸(5),正十七烷酸(6),9-十八碳烯酸甲酯(7),对羟基苯甲酸(8),棕榈酸(9),苦杏仁苷(10)。结论:桃仁乙酸乙酯萃取部位为抑制FXa的活性部位,从活性部位中分离得到的化合物1和3首次从该科植物中分离得到,化合物5~8首次从该植物中分离得到。     

基于LC-MS的蛇倒退抗肿瘤活性部位筛选及鉴定研究

目的:分离得到蛇倒退中抗肿瘤活性部位并鉴定。方法:通过硅胶柱色谱分离蛇倒退得到不同馏分，以SGC-7901的抑制率和IC₅₀为指标筛选得到抗肿瘤作用最强部位，并在倒置显微镜下观察细胞形态及应用LC-MS对其进行鉴定。结果:经分离得到4个主要馏分，其中馏分1的抗肿瘤活性最强，LC-MS鉴定得到一系列化合物。结论:蛇倒退中分离得到的PEC A部位具有良好的抗肿瘤活性，其主要成分为黄酮类化合物。     

乌骨藤化学成分及其抗肿瘤活性

目的研究乌骨藤Marsdenia tenacissima化学成分及其抗肿瘤活性。方法乌骨藤80%乙醇提取物的氯仿、乙酸乙酯、正丁醇部位通过硅胶、大孔吸附树脂、Sephadex LH-20、ODS色谱柱进行分离纯化,根据波谱数据对所得化合物结构进行鉴定,再通过MTT法评价其抗肿瘤活性。结果从中分离出10个化合物,分别鉴定为白桦脂酸(1)、乌骨藤苷H(2)、乌骨藤苷G(3)、乌骨藤苷I(4)、绿原酸(5)、野黄芩素四甲醚(6)、山柰酚-4'-甲醚(7)、山柰酚(8)、β-谷甾醇(9)、胡萝卜苷(10)。化合物8对胃癌细胞MKN-45和SGC-7901有较显著的抑制作用,IC50分别为48.87μg/m L和54.71μg/m L。结论化合物6~8为首次从该植物中分离得到,而且化合物8的抗肿瘤活性较强。     

红凉伞抗肿瘤转移化学成分研究

目的:研究红凉伞Ardisia Crenata的化学成分及其抗肿瘤转移活性.方法:采用硅胶柱色谱、凝胶柱色谱和HPLC制备色谱方法分离纯化得到单体化合物,采用有机波谱方法鉴定化合物结构,进一步以Tranawell趋化实验方法测定化合物抗肿瘤转移作用.结果:从红凉伞乙醇提取物中分离得到9个化合物,分别为5-羟甲基糠醛(1),乙基-β-D-吡喃果糖苷(2),丁香酸(3),正丁基-βD-呋喃果糖苷(4),正丁基-α-D-呋喃果糖苷(5),甲基-α-D-呋喃果糖苷(6),岩白菜素(7),百两金皂苷B(8),车叶草酸(9).抗肿瘤转移实验结果表明化合物1-9,均有明确的抗肿瘤转移作用,其中化合物1,5和8的抗肿瘤转移活性较强,化合物5在质量浓度0.8mg·L-1下对人乳腺癌细胞MDA-MB-231趋化抑制率达到93.8%.结论:化合物2～6和,均为首次从该植物中分离得到;化合物1～9,均具有明确的抗肿瘤转移作用,其中化合物1,5和8的抗肿瘤转移活性较强.     

枳椇子乙酸乙酯部位抗肿瘤活性成分筛选

目的:研究筛选枳椇子Hovenia acerba Lindl.乙酸乙酯部位中具有抗肿瘤活性的化合物。方法:利用乙酸乙酯萃取枳椇子60%乙醇水提取物,并采用300～400目硅胶与制备级HPLC对其萃取物进行分离纯化,最终得到4个化合物,通过MTT法筛选发现其中ZJZ-Z2具有最优的活性,通过ESI-MS、~1H-NMR和~(13)C-NMR检测,并通过与相关文献对比,初步推测该化合物为二氢杨梅素(dihydromyricelin),体内实验证明ZJZ-Z2具有体内抗肿瘤活性。结果:通过MTT法分别对枳椇子乙酸乙酯部位硅胶分离得到的12个组分进行测定,发现其中第4组分对肿瘤细胞Huh-7、OS-RC-2的半数抑制率(IC_(50))分别为70.4、69.8μg·mL~(-1);进一步分离纯化得到的ZJZ-Z2对肿瘤细胞OS-RC-2、Huh-7、HCT-116、CFPAC-1的IC_(50)分别为33.8、63.9、46.8、55.1μg·mL~(-1),且对H22荷瘤小鼠模型表现出一定的抑瘤作用。结论:枳椇子乙酸乙酯部位具有抗肿瘤活性,其主要的抗肿瘤活性成分为二氢杨梅素。     

文冠果壳抗氧化活性及抑制人HepG_2细胞增殖活性部位筛选

目的:筛选文冠果壳的抗氧化及抑制肝癌HepG2细胞增殖活性部位。方法:用水,10%、30%、50%、70%、95%乙醇水溶液从文冠果中提取得到A、B、C、D、E和F提取物,用清除自由基DPPH·能力筛选抗氧化活性部位,用MTT法筛选抑制肝癌细胞增殖的活性部位。结果:6个提取部位均有抗氧化活性和抑制Hep G2细胞增殖作用,其中E(70%乙醇水提取)部位的抗氧化活性最强,当质量浓度为0.2 mg·m L-1时,其对DPPH·清除率能达到70.82%;提取部位F(95%乙醇水提取)抑制Hep G2细胞增殖作用最强,当其质量浓度为75μg·m L-1时,抑制率高达70.1%。结论:文冠果壳提取物具有抗氧化及抑制人Hep G2增殖活性,具有开发前景。     

瑞香狼毒系统溶剂法分离提取部位的体外抗肿瘤活性

目的:分离筛选瑞香狼毒中抗肿瘤活性部位.方法:用系统溶剂法对瑞香狼毒95%乙醇提取物进行分离,MTT比色法对分离得到的部位进行体外抗肿瘤活性的测定.结果:石油醚提取物和氯仿提取物对体外培养肿瘤细胞表现出较强的抑制作用,在测定浓度范围内呈现出良好剂量依赖性抑制作用,而正丁醇和甲醇提取部位在测定浓度范围内则显示出很弱的抑制作用;在各提取部位中石油醚提取物的体外抗肿瘤作用最强.结论:石油醚提取部位是瑞香狼毒中的体外抗肿瘤活性部位.     

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.     

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.     

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。     

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.     

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。     

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.     

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.     

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。     

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。