丹皮抗内毒素性急性肺损伤活性的谱效关系研究

分析丹皮及对照药材赤芍、白芍的高效液相特征图谱与抗内毒素性急性肺损伤活性之间的相互关系。通过HPLC-MS测定分析丹皮、赤芍、白芍各提取部位的HPLC特征图谱,用内毒素诱导大鼠急性肺损伤模型测定样品抑制蛋白和肿瘤坏死因子-α浓度的活性,运用偏最小二乘回归分析法研究谱效相关性,并用HPLC-MS/MS指认样品主要成分峰。结果显示,各样品对急性肺损伤均有一定的药效,谱效相关性研究得出4个对药效贡献率较大的成分。其中丹皮具有良好的抗急性肺损伤活性,没食子酸、芍药苷、没食子酰芍药苷和丹皮酚是其主要有效成分。     

波棱瓜子乙酸乙酯部位抗免疫性肝损伤活性谱效关系分析

目的:探讨波棱瓜子乙酸乙酯部位HPLC特征图谱与其抗免疫性肝损伤活性的相互关系。方法:采用硅胶柱色谱分离结合均匀设计获得不同化学成分组成的9批波棱瓜子乙酸乙酯部位样品,应用HPLC建立9批样品特征图谱并通过聚类分析评价9批样品的差异性;建立卡介苗+脂多糖诱导小鼠免疫性肝损伤模型测定给药组小鼠血清中丙氨酸氨基转移酶(ALT),天门冬氨酸氨基转移酶(AST)活性及肝组织匀浆中丙二醛(MDA)含量;结合灰色关联分析法及偏最小二乘回归分析法(PLSR)研究其谱效相关性。结果:9批不同组合的样品HPLC图谱有明显差异,从其共有模式中标定了16个特征峰。与模型组相比,9批波棱瓜子给药组小鼠血清中ALT,AST活性和肝匀浆中MDA含量明显降低。谱效相关性研究发现6,7,10,15,16号峰(分别代表化合物波棱甲素、波棱素、波棱醇、波棱酮、波棱醛)是与抗免疫性肝损伤作用关联性较大的正相关色谱峰。结论:各样品对免疫性肝损伤均具有治疗作用,其护肝作用主要活性成分为波棱甲素、波棱素、波棱醇、波棱酮、波棱醛。     

基于灰色关联分析探索艾纳香非挥发性部位的抗炎活性谱效关系

目的:研究艾纳香非挥发性部位UPLC指纹图谱与抗炎药效之间的相关性,为明确艾纳香抗炎药效物质基础提供实验依据。方法:采用UPLC建立12批艾纳香非挥发性部位的指纹图谱,运用UPLC-Q-TOF-MS对艾纳香非挥发性部位的共有指纹峰进行指认,通过二甲苯致小鼠耳廓肿胀炎症模型获取相应的药效数据,通过灰色关联分析建立其谱效关系。结果:UPLC指纹图谱显示艾纳香非挥发性部位有14个共有峰,与抗炎药效的关联度处于0.717 1~0.550 5,各特征峰所代表的化学成分对其抗炎药效贡献的大小顺序为3号峰 9号峰 4号峰 11号峰 2号峰 1号峰 14号峰 7号峰 6号峰 5号峰 12号峰 8号峰 10号峰 13号峰,并指认了其中9个共有峰,对抗炎药效贡献较大的前2个共有峰(3号和9号)对应的化学成分分别为3-O-咖啡酰基奎宁酸和3,5-O-二咖啡酰基奎宁酸。结论:通过谱效关系研究获得了艾纳香非挥发性部位的抗炎药效物质群,其抗炎药效是多种成分共同作用的结果,明确咖啡酰基奎宁酸类化合物为艾纳香非挥发性部位发挥抗炎药效的主要物质基础。     

唐古特大黄二氯甲烷部位抗炎活性谱效关系研究

目的 建立唐古特大黄二氯甲烷部位抗炎活性谱效关系。方法 采用脂多糖刺激RAW264.7细胞制备炎性细胞模型，通过检测RAW264.7细胞一氧化氮的分泌情况，考察唐古特大黄不同萃取部位的抗炎活性；建立唐古特大黄二氯甲烷部位的HPLC指纹图谱；采用灰色关联度、双变量相关分析法和偏最小二乘法分析抗炎活性部位HPLC特征峰与其抗炎药效之间的谱效关系。结果 唐古特大黄二氯甲烷部位为抗炎活性部位；活性部位指纹图谱中共有峰有9个；灰色关联度分析结果表明，各成分抗炎关联度依次为1号>8号(大黄素)>3号>4号>5号(大黄酸)>2号(芦荟大黄素)>9(大黄酚)>6号>7号；双变量相关分析结果表明，7个共有峰与抗炎药效指标呈正相关，其中5号(大黄酸)与8(大黄素)峰含量变化与抗炎药效指标呈正相关(P<0.05);偏最小二乘法分析结果表明，各成分抗炎关联度为1号、3号、4号、5号、7号、8号、9号峰与抗炎活性呈正相关，2号、6号峰呈负相关。结论 通过谱效关系确定唐古特大黄发挥抗炎活性的主要物质基础为大黄酸与大黄素，其抗炎作用是多成分共同作用的结果。     

唐古特大黄不同极性部位体外抗炎作用谱效关系研究

目的 研究唐古特大黄甲醇提取物及其不同极性部位的指纹图谱与体外抗炎作用的相关性，为揭示其抗炎作用物质基础提供依据。方法 采用HPLC建立唐古特大黄甲醇提取物及其不同极性部位的指纹图谱，采用脂多糖刺激RAW264.7小鼠巨噬细胞制备炎性细胞模型，通过检测RAW264.7细胞一氧化氮（NO）分泌情况，考察唐古特大黄甲醇提取物及其不同极性部位的抗炎活性，采用偏最小二乘回归法（PLSR）建立谱效关系。结果 PLSR结果表明，30个特征峰中有7个峰与抗炎率呈正相关（偏回归系数>0）,23个色谱峰与抗炎率呈负相关（偏回归系数<0），其中1、11、27（大黄酸）、12、28（大黄素）、10、14、23（芦荟大黄素）、22、30号峰（大黄素甲醚）的变量重要性投影（VIP）>1。结论 大黄酸、大黄素、芦荟大黄素、大黄素甲醚等对唐古特大黄抗炎药效的贡献最大。初步表明唐古特大黄的抗炎药效物质主要集中在二氯甲烷部位，抗炎作用是这些成分共同作用的结果。     

加味四妙丸有效部位群HPLC指纹图谱归属分析及谱效关系研究

目的:明确加味四妙丸有效部位群中指纹图谱共有峰与组方药材有效部位及药效的相关性,表征加味四妙丸有效部位群药效物质基础。方法:用指纹图谱共有峰相对保留时间的相对偏差△t和紫外光谱夹角余弦特征相似度,考察共有峰与药材有效部位的相关性;将加味四妙丸中各有效部位及各组方药中的有效部位进行正交组合,测定指纹图谱及评价抗炎、镇痛及降尿酸作用,运用数理统计学的方法将药理数据与指纹图谱各色谱峰相对面积相关联,研究谱效相关性。结果:该方有效部位群12个共有峰分别来源于组方药苍术皂苷、黄柏皂苷、黄柏生物碱、土茯苓皂苷部位,与抗炎、镇痛、降尿酸作用均有相关性。结论:研究有效部位群指纹图谱共有峰的成分特征及谱效关系,是表征复方整体成分-配伍-药效相关性的有效途径。     

基于偏最小二乘回归法分析五味子抑菌活性部位谱效关系

目的基于偏最小二乘回归法研究五味子抑菌活性部位谱效关系。方法五味子抗耐甲氧西林金黄色葡萄球菌(MRSA)体外抑菌活性组分甲醇溶液的分析采用色谱柱Acquity UPLC BEH C_(18)(100 mm×2.1 mm,1.7μm);流动相乙腈-0.1%甲酸水,梯度洗脱;柱温45℃;体积流量为0.3 mL/min。采用管碟法测定相应的抑菌活性药效数据,运用偏最小二乘回归分析法进行谱效相关性研究。结果 9批样品特征指纹图谱中有11个共有峰,其中有5个共有峰的回归系数与抑菌活性呈正相关,且变量重要性值均较大,贡献度均较高,综合评价各特征峰的贡献大小排序为峰10峰9峰3(苹果酸异构体)峰2(柠檬酸)峰11。结论五味子抗MRSA抑菌活性为多个成分协同作用的结果,揭示了五味子抑菌活性药效物质基础。     

加味四妙丸有效部位群HPLC指纹图谱归属分析及谱效关系研究

目的: 明确加味四妙丸有效部位群中指纹图谱共有峰与组方药材有效部位及药效的相关性, 表征加味四妙丸有效部位群药效物质基础。方法: 用指纹图谱共有峰相对保留时间的相对偏差△t和紫外光谱夹角余弦特征相似度, 考察共有峰与药材有效部位的相关性; 将加味四妙丸中各有效部位及各组方药中的有效部位进行正交组合, 测定指纹图谱及评价抗炎、镇痛及降尿酸作用, 运用数理统计学的方法将药理数据与指纹图谱各色谱峰相对面积相关联, 研究谱效相关性。结果: 该方有效部位群12个共有峰分别来源于组方药苍术皂苷、黄柏皂苷、黄柏生物碱、土茯苓皂苷部位, 与抗炎、镇痛、降尿酸作用均有相关性。结论: 研究有效部位群指纹图谱共有峰的成分特征及谱效关系, 是表征复方整体成分-配伍- 药效相关性的有效途径。     

细辛不同极性部位HPLC指纹图谱与其镇痛抗炎活性的谱效关系研究

目的:研究细辛不同极性部位高效液相色谱(HPLC)指纹图谱与其镇痛、抗炎作用的谱效关系。方法:建立细辛不同极性部位的HPLC指纹图谱;采用小鼠热板法和二甲苯致小鼠耳肿胀法测定细辛不同极性部位的镇痛、抗炎活性;采用偏最小二乘回归分析法分析不同极性部位HPLC特征指纹峰与其镇痛、抗炎药效之间的谱效关系。结果:在标定的31个特征指纹峰中,有15个特征峰与镇痛活性呈正相关,其中8、11、13、20、21、22、26号峰贡献较大;有20个特征峰与抗炎活性呈正相关,其中2、5、7、9、10、11号峰贡献较大。结论:细辛中含有镇痛、抗炎作用的特征效应物质。     

加味四妙丸有效部位群GC指纹图谱谱效关系及配伍变化研究

目的:研究加味四妙丸有效部位群配伍药效物质基础特征,表征君药挥发油部位化学-配伍-药效的相关性。方法:评价不同工艺全方及不同组合有效部位抗炎、镇痛及降尿酸作用,并测定GC指纹图谱,运用数理统计方法将药理数据与指纹图谱各共有峰相对面积相关联;比较挥发油部位、有效部位群及全方GC指纹图谱有效共有峰的变化特征。结果:挥发油指纹图谱25个共有峰中,除1、4、6、12号共有峰外,均与抗炎、镇痛、降尿酸活性相关;挥发油部位在与全方及有效部位群配伍组合后,有效共有峰减少,大多数共有峰峰面积比值减小,少数共有峰峰面积比值增大。结论:用指纹图谱谱效关系是表征复方整体成分-配伍-药效的相关性的有效途径     

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.     

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。     

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。