不同产地南五味子中木脂素分析研究

采用UPLC-TQ-MS技术对不同产地南五味子药材中的7种木脂素类成分进行分析评价,为南五味子的科学药用提供实验依据。结果显示秦岭以南,东侧的商洛市柞水县、山阳县所产南五味子中主要含五味子酯甲、五味子甲素;宝鸡市眉县,安康市石泉县、宁陕县,汉中市略阳县所产的南五味子主要含有安五酯素,其中宁陕县样品中五味子甲素含量也较高;而位于秦巴山区腹地的汉中市南郑县所产的南五味子主要含五味子酚、五味子甲素。总之不同产地的南五味子所含木脂素种类和含量差别很大,在实际应用中应结合现代药理实验和临床研究,根据所治疗疾病相关的主要功效成分对不同产地南五味子药材加以区别入药,以达到药物的最佳疗效。     

高效液相色谱法测定五味子属药用植物木脂素的含量

目的 :对五味子属植物的木脂素成分进行含量测定 ,探讨五味子药物资源问题。方法 :用HPLC对五味子属 14个种 (变种 ) 18个样品 (果实、茎藤和根 )中木脂素成分五味子醇甲 (schisandrin) ,五味子醇乙 (gomisinA) ,五味子酯甲 (schisantherinA) ,五味子甲素 (deoxyschizandrin) ,表 加巴辛 (d-epigalbacine) ,安五脂素 [(+) anwulig nan],五味子乙素 (wuweizisuB) ,6O 苯甲酰戈米辛O(6-O-benzoylgomisinO)和五味子丙素 (wuweizisuC)进行含量测定。结果 :5种不同种的五味子果实中 ,9种木脂素总量为 0.52%～1.96% ,其中以五味子和华中五味子含量最高 ,11种 (包括变种 )茎的 9种木脂素总量为 0.02%～1.51% ;小花五味子果实含有与华中五味子相似的木脂素成分 ,其中甲素的含量较高 (0.59%) ;绿叶五味子与五味子成分相似 ,其醇甲、醇乙和乙素的含量均较高 ;翼梗五味子果实、华中五味子果实、小花五味子茎、毛脉五味子茎和二色五味子根的安五脂素含量较高 ,分别 0.77% ,0.42% ,0.50% ,0.26% ,0.38% ;毛脉五味子茎、毛叶五味子茎和金山五味子茎的表 加巴辛含量较高 (分别为0.89% ,1.51% ,0.17% )。结论 :五味子属植物果实的木脂素含量高于根和茎 ;翼梗五味子果实、小花五味子茎、华中五味子果实、二色五味子根、毛脉五味子和毛脉五味子茎、金山五味子茎可分别作为安五脂素和表-加巴辛的植物资源。     

内南五味子中木脂素类化学成分研究

目的:研究内南五味子的化学成分。方法:采用硅胶柱色谱,羟丙基葡聚糖凝胶Sephadex LH-20、ODS及HPLC等多种色谱技术进行分离纯化,根据理化性质和波谱学方法鉴定化合物结构。结果:从内南五味子体积分数90%乙醇水提取物中分离得到了15个木脂素类化合物,分别为利卡灵A(1)、南五味子素(2)、异形南五味子丁素(3)、异形南五味子庚素(4)、8α-羟基松脂醇(5)、内南五味子素丙(6)、异形南五味子戊素(7)、扁核木醇(8)、阿里山五味子灵C(9)、苄基氧代南五味子醇(10)、松脂醇(11)、香豆木脂素(12)、川椒脂醇(13)、异形南五味子壬素(14)、二氢去氢二松柏醇(15)。结论:化合物1、5、7、8、10~15是首次从内南五味子中分离得到。     

异型南五味子木脂素的HPLC法测定

建立了异型南五味子木脂素的HPLC测定法，测定南五味子素（kadsurin）、内南五味子素（interiorin）、异型南五味子丁素（heteroclitinD）和异型南五味子庚素（heteroclitinG）的加样回收率为93．3％～102．3％．变异系数1．62％～2．78％。     

异型南五味子藤茎中1个新的木脂素

目的:研究异型南五味子藤茎的化学成分。方法:采用各种柱色谱法分离,通过波谱法进行结构鉴定。结果:化合物1是1个新的二芳基丁烷类木脂素二聚体。结论:五味子科植物中二芳基丁烷类木脂素以二聚体的形式存在属于首次发现。     

南五味子木脂素成分的HPLC含量测定及其变异规律

目的 :对南五味子的木脂素成分进行含量测定 ,探讨南五味子类药材木脂素成分的变异规律及其与地理分布的关系。方法 :高效液相色谱法。色谱柱 :SpherecloneLunaC1 8(2 ) (2 5 0× 4 6mm ,5 μm) ;流动相 :A .水 ,B .甲醇 ;梯度洗脱 :0～ 2 5min ,6 5 %～ 75 %B ,2 5～ 30min ,75 %B ,30～ 70min ,75 %～ 1 0 0 % ;检测波长 :2 5 4nm、2 80nm。结果与结论 :随着地理分布的不同 ,华中五味子果实木脂素成分的结构类型及其含量有显著差异。产于秦岭南侧、东侧、中条山及太行山南端的华中五味子果实含有主要的活性木脂素成分五味子酯甲、五味子甲素、安五脂素等 ,且总木脂素含量也较高 ,质量较优     

南五味子、五味子HPLC指纹图谱研究和木脂素成分测定

目的 采用HPLC法建立南五味子和五味子药材的指纹图谱,并同时测定4种木脂素.方法 以五味子酯甲、五味子甲素、五味子醇甲和五味子乙素为对照,采用Eclipse XDB-C18色谱柱(150 mm×4.6 mm,5 μm),乙腈-四氢呋喃-水梯度洗脱;检测波长220 nm;体积流量1.0 mL/min进行试验,用中国药典委员会颁布的中药色谱指纹图谱相似度评价系统软件(版本:2004AB)计算处理,分别建立南五味子、五味子甲醇提取物的指纹图谱,并同时测定4种木脂素.结果 南五味子药材指纹图谱中标定了25个共有峰,五味子药材指纹图谱中标定了24个共有峰;不同产地南五味子指纹图谱相似度均大于0.9,但其主要木脂素成分量差异较大;不同产地五味子指纹图谱相似度亦大于0.9,但南五味子、五味子指纹图谱相似度小于0.3.结论 南五味子、五味子药材的指纹图谱特征性和专属性强,结合木脂素成分的测定,可为全面控制药材的质量提供科学方法.     

南五味子总木脂素软胶囊制备工艺优选

目的:优选南五味子总木脂素软胶囊的制备工艺.方法:采用紫外分光光度法测定总木脂素含量.选择玉米油和聚乙二醇600(PEG600)为分散剂,氢化植物油和羧甲基纤维素钠(CMC-Na)为稳定剂,聚山梨酯80(Tween80)为助溶剂,筛选内容物最佳处方.以胶囊收率和轧囊现象为综合评价指标,通过正交试验考察进料口温度、胶囊出口温度和转篮干燥时间对制备工艺的影响.结果:内容物最佳处方为主药-玉米油-PEG600-1,2-丙二醇-CMC-Na-氢化植物油-Tween80-水(44∶10∶ 15∶ 1∶8∶9∶3∶ 10),最佳制备工艺为进料口温度50℃,胶囊出口温度20℃,转篮干燥时间24 h.结论:优选的制备工艺稳定可行.     

南北五味子中木脂素类成分含量的比较

目的:建立同时测定南、北五味子中5种木脂素成分(五味子醇甲、五味子醇乙、五味子酯甲、五味子甲素和五味子乙素)含量的超高效液相色谱法,并比较不同产地五味子类药材中木脂素类成分含量。方法:Acquity UPLC BEH C18色谱柱(2.1 mm×50 mm,1.7μm),流动相乙腈-水,梯度洗脱,流速0.4 m L·min-1,检测波长235 nm,柱温45℃,进样量1μL。以5种成分含量为评价指标,采用聚类分析法对南北五味子进行种类识别。结果:分析时间内,上述5种木脂素成分在10 min内分离度良好,在0.001~0.222μg线性关系良好,相关系数均0.999 8,平均加样回收率在97.7%~105.1%,RSD均3.0%。南北五味子中5种木脂素类成分含量差异显著,聚类分析结果也表明,南北五味子能完全被区分为两大类。结论:该方法重复性好,准确可靠,灵敏度高,可为五味子类药材的分类和质量控制提供参考。     

南五味子属药用植物的化学成分及其生物活性

综述了自上世纪90年代初以来对五味子科南五味子属药用植物的化学成分及其生物活性的研究工作。我们从5种南五味子属药用植物的藤茎中共分离鉴定了80余种化合物,并主要探讨了这些化合物的抗脂质过氧化、钙拮抗和PAF拮抗等与补血活血作用相关的生物活性,同时也尝试抗HIV方面的研究工作,发现部分木脂素和三萜类化学成分具有显著的生物活性。     

Antimicrobial activity of South African medicinal plants

This paper reviews the antimicrobial research undertaken on South African medicinal plants during the period 1997-2008. Antimicrobial methods (disc diffusion, minimum inhibitory concentration (MIC), bio-autography) are briefly discussed and an analysis of the publications reviewed indicates that the majority of papers use MIC assays for antimicrobial determination. Antimicrobial investigations on extracts are presented where the most active plants are identified from screening publications. A summary of some bioactive compounds are given with data restricted to papers reporting quantitative antimicrobial activity equivalent to or below 200 microg/ml. Antimicrobial activities on the essential oils of indigenous medicinal aromatic plants are also reviewed. An overview is given on what activities (extracts, compounds and oils) should be considered noteworthy for publication. Studies focusing on geographical ethnobotany, specific pathogenesis, formulation aspects and in vivo investigations are examined. Future recommendations to consider include pathogen selection, interactive studies and dosage administrations.     

Ethnobotanical studies of medicinal plants used in the management of diabetes mellitus in South Western Nigeria

This survey was carried out in targeted areas of South West Nigeria in order to inventory plants used by traditional healers in the area for the management of diabetes mellitus. One hundred traditional healers who know and use medicinal plants for treating diabetes mellitus were interviewed. The inventory contains scientific, vernacular, common names of the plants used and method of preparation. Thirty-one plants commonly used by traditional healers in the region were identified. The survey shows plants from the Rutaceae, Leguminosae and Cucurbitaceae families are commonly used by traditional healers in South West Nigeria for the treatment of diabetes mellitus.     

Inhibitory properties of selected South African medicinal plants against Mycobacterium tuberculosis

Ethnopharmacological relevance

Tuberculosis (TB), caused by Mycobacterium tuberculosis (MTB) is the most commonly notified disease and the fifth largest cause of mortality. One in 10 cases is resistant to treatment in some areas. Several plants are used locally to treat TB-related disease.

Aims of the study

The aim was to screen selected South African medicinal plants used to treat TB and related symptoms by traditional healers for antimycobacterial activity.

Materials and methods

Ethnobotanical information on these plants was obtained. Crude acetone, methanol, hexane and ethanol extracts of 21 selected medicinal plants obtained in Venda, South Africa were screened for their ability to inhibit MTB H₃₇Ra and a clinical strain resistant to first-line drugs and one second-line drug using tetrazolium microplate assay to determine the minimum inhibitory concentration (MIC). Results were analyzed using Microsoft Excel 2007 and One way ANOVA; p < 0.05 was considered for statistical significance.

Results

Few acetone extracts were active against MTB with MIC under 100 μg/mL. Four plants showed lower MIC values; Berchemia discolor Klotzsch Hemsl 12, 5 μg/mL on H₃₇Ra and 10.5 μg/mL on the clinical isolate, Bridelia micrantha Hochst. Baill (25 μg/mL), Warbugia salutaris Bertol. F Chiov (25 μg/mL), and Terminalia sericea Burch ex D. F (25 μg/mL) on both H₃₇Ra and clinical isolate. However, the roots of Ximenia caffra Sond. Var. caffra, barks of Sclerocarya birrea (A Rich) Hochst, Asclepias fruticosa L, tubers of Allium sativum L, leaves of Carica papaya L, Solanum panduriforme E. Mey C, and roots of Securidaca longepedunculata Fresen gave MIC greater than 100 μg/mL.

Conclusion

The acetone extracts of Berchemiadiscolor, Bridelia micrantha, Terminalia sericea and Warbugia salutaris could be important sources of mycobactericidal compounds against multidrug-resistant MTB.     

Pharmacological activity of South American plants: effects on spontaneous in vivo lipid peroxidation

The in vivo protective effects of methanol extracts of eight South American medicinal plants traditionally used as antiinflammatory were determined by means of spontaneous lipid peroxidation of liver tissue in rats. The production of TBARS was reduced in a dose dependent manner for A. macrocarpa (IC50 = 132 mg/kg), A. urundeuva (IC50 = 176 mg/kg), C. reticulata (IC50 = 561mg/kg) and S. obtusifolium (IC50 = 918 mg/kg). The extracts of P. peltata and U. tomentosa were only effective at a high concentration (300 mg/kg), although these values were not significant. The lyophilized latex of C. lechleri decreased the production of TBARS at a 200 mg/kg dose, although pro-oxidant effects were observed at lower doses (50 mg/kg). The extract of H. pallida was pro-oxidant at lower concentrations (50 mg/kg).     

Antimalarial activities of medicinal plants traditionally used in the villages of Dharmapuri regions of South India

Ethnopharmacological relevance

An ethnopharmacological investigation of medicinal plants traditionally used to treat diseases associated with fevers in Dharmapuri region of South India was undertaken. Twenty four plants were identified and evaluated for their in vitro activity against Plasmodium falciparum and assessed for cytotoxicity against HeLa cell line.

Aim of the study

This antimalarial in vitro study was planned to correlate and validate the traditional usage of medicinal plants against malaria.

Materials and methods

An ethnobotanical survey was made in Dharmapuri region, Tamil Nadu, India to identify plants used in traditional medicine against fevers. Selected plants were extracted with ethyl acetate and methanol and evaluated for antimalarial activity against erythrocytic stages of chloroquine (CQ)-sensitive 3D7 and CQ-resistant INDO strains of Plasmodium falciparum in culture using the fluorescence-based SYBR Green I assay. Cytotoxicity was determined against HeLa cells using MTT assay.

Results

Promising antiplasmodial activity was found in Aegle marmelos [leaf methanol extract (ME) (IC₅₀ = 7 μg/mL] and good activities were found in Lantana camara [leaf ethyl acetate extract (EAE) IC₅₀ = 19 μg/mL], Leucas aspera (flower EAE IC₅₀ = 12.5 μg/mL), Momordica charantia (leaf EAE IC₅₀ = 17.5 μg/mL), Phyllanthus amarus (leaf ME IC₅₀ = 15 μg/mL) and Piper nigrum (seed EAE IC₅₀ = 12.5 μg/mL). The leaf ME of Aegle marmelos which showed the highest activity against Plasmodium falciparum elicited low cytotoxicity (therapeutic index > 13).

Conclusion

These results provide validation for the traditional usage of some medicinal plants against malaria in Dharmapuri region, Tamil Nadu, India.     

An ethnobotanical study of medicinal plants used by the Yaegl Aboriginal community in northern New South Wales, Australia

Ethnopharmacological relevance

Documentation of Australian bush medicines is of utmost importance to the preservation of this disappearing and invaluable knowledge. This collaboration between the Yaegl Aboriginal community in northern New South Wales (NSW), Australia and an academic institution, demonstrates an effective means of preserving and adding value to this information.

Materials and methods

Questionnaire-guided interviews were performed with community Elders under a framework of participatory action research. Medicinal plant knowledge was collated in a handbook to aid interviews and to be used as an ongoing resource by the community. Specimens for all non-cultivar plants that were discussed were collected and deposited in herbaria with unique voucher numbers. This medicinal knowledge was checked against the literature for reports of related use and studies of biological activity.

Results

Nineteen Elders were interviewed, leading to discussions on fifty four plant preparations used for medicinal purposes. These plant preparations involved thirty two plants coming from twenty one families, reflecting the botanical diversity of the area. The plants retained in the Yaegl pharmacopoeia correspond to their accessibility and ease of preparation, reflected in their ongoing utilisation. Several plant uses did not appear elsewhere in the literature.

Conclusions

This study is the first comprehensive documentation of the medicinal knowledge of the Yaegl Aboriginal community. It has been conducted using participatory action research methods and adds to the recorded customary knowledge of the region. The customary medicinal knowledge retained by the Yaegl Aboriginal community is related to the evolving needs of the community and accessibility of plants.     

Anti-parasitic activity and cytotoxicity of selected medicinal plants from Kenya

Indigenous rural communities in the tropics manage parasitic diseases, like malaria and leishmaniasis, using herbal drugs. The efficacy, dosage, safety and active principles of most of the herbal preparations are not known. Extracts from 6 selected plant species, used as medicinal plants by indigenous local communities in Kenya, were screened for in vitro anti-plasmodial and anti-leishmanial activity, against 2 laboratory-adapted Plasmodium falciparum isolates (D6, CQ-sensitive and W2, CQ-resistant) and Leishmania major (IDU/KE/83 = NLB-144 strain), respectively. The methanol extract of Suregada zanzibariensis leaves exhibited good anti-plasmodial activity (IC₅₀ 4.66 ± 0.22 and 1.82 ± 0.07 μg/ml for D6 and W2, respectively). Similarly, the methanol extracts of Albizia coriaria (IC₅₀ 37.83 ± 2.11 μg/ml for D6) and Aspergillus racemosus (32.63 ± 2.68 and 33.95 ± 2.05 μg/ml for D6 and W2, respectively) had moderate anti-plasmodial activity. Acacia tortilis (IC₅₀ 85.73 ± 3.36 μg/ml for W2) and Albizia coriaria (IC₅₀ 71.17 ± 3.58 μg/ml for W2) methanol extracts and Aloe nyeriensis var kedongensis (IC₅₀ 87.70 ± 2.98 and 67.84 ± 2.12 μg/ml for D6 and W2, respectively) water extract exhibited mild anti-plasmodial activity. The rest of the extracts did not exhibit any anti-plasmodial activity. Although the leishmanicidal activity of extracts were lower than for pentosam (80%), reasonable activity was observed for Aloe nyeriensis methanol (68.4 ± 6.3%), Albizia coriara water (66.7 ± 5.0%), Maytenus putterlickoides methanol (60.0 ± 6.23%), Asparagus racemosus methanol and water (58.3 ± 8.22 and 56.8 ± 6.58%, respectively), Aloe nyeriensis water (53.3 ± 5.1%) and Acacia tortilis water (52.9 ± 6.55%) extracts at 1000 μg/ml. Leishmania major infected macrophages treated with methanol extracts of Suregada zanzibariensis and Aloe nyeriensis var kedongensis and Pentostam^® had infection rates of 28 ± 2.11, 30 ± 1.22 and 40 ± 3.69%, respectively at 1000 μg/ml, indicating better anti-leishmanial activity for the extracts. The methanol extract of Albizia coriara (44.0 ± 3.69%) and aqueous extracts of Asparagus racemosus (42 ± 3.84%) and Acacia tortilis (44 ± 5.59%) had similar activity to pentosam^®. Multiplication indices for Leishmania major amastigotes treated with methanol extracts of Albizia coriaria, Suregada zanzibariensis and Aloe nyeriensis var kedongensis, aqueous extract of Acacia tortilis and pentosam^® were 28.5 ± 1.43, 29.4 ± 2.15, 31.1 ± 2.22, 35.9 ± 3.49 and 44.0 ± 3.27%, respectively, at 1000 μg/ml, confirming better anti-leishmanial activity for the extracts. Aqueous extracts of Aloe nyeriensis (46.7 ± 3.28%) and Albizia coriaria (47.5 ± 3.21%) had similar activity level to pentosam^®. The plant extracts have better inhibitory activity while pentosam^® has better leishmanicidal activity. All extracts exhibited very low cytotoxicity (CC₅₀ > 500 μg/ml) against human embryonic lung fibroblast (HELF) cells. The investigations demonstrated the efficacy and safety of some extracts of plants that are used by rural indigenous communities for the treatment of parasitic diseases.     

Antimalarial and cytotoxic activities of ethnopharmacologically selected medicinal plants from South Vietnam

Malaria is a major global public health problem and the alarming spread of drug resistance and limited number of effective drugs now available underline how important it is to discover new antimalarial compounds. An ethnopharmacological investigation was undertaken of medicinal plants traditionally used to treat malaria in the South Vietnam. Forty-nine plants were identified, 228 extracts were prepared and tested for their in vitro activity against Plasmodium falciparum, and assessed for any cytotoxicity against the human cancer cell line HeLa and the embryonic lung MRC5 cell line. In a first screening at a concentration of 10 microg/ml, 92 extracts from 46 plants showed antiplasmodial activity (parasite growth inhibition >30%). The IC(50) values of the most active extracts were determined as well as their selectivity towards Plasmodium falciparum in comparison to their cytotoxic effects against the human cell lines. Six plants showed interesting antiplasmodial activity (IC(50) ranging from 0.4 to 8.6 microg/ml) with a good selectivity: two Menispermaceae, Arcangelisia flava (L.) Merr. and Fibraurea tinctoria Lour., and also Harrisonia perforata (Blanco) Merr. (Simaroubaceae), Irvingia malayana Oliv. ex Benn. (Irvingiaceae), Elaeocarpus kontumensis Gagn. (Elaeocarpaceae) and Anneslea fragrans Wall. (Theaceae).     

Mutagenic and antimutagenic properties of extracts from South African traditional medicinal plants

Aim of the study

The aim of this paper was to summarize the results of our investigations on the in vitro genotoxic as well as antigenotoxic effects of a great number of selected South African traditional medicinal plants.

Materials and methods

Investigations of methanol and dichloromethane extracts of selected plants were conducted with the bacterial Ames, Umu-C and VITOTOX^® tests, and with the cytochalasin B micronucleus test and alkaline comet assay in human white blood cells.

Results

A number of extracts were found to have genotoxic properties. Amongst the genotoxic plant extracts, especially methanol extracts of Helichrysum simillimum DC. (Asteraceae) should be highlighted. On the other hand, some plant extracts also showed antimutagenic potential. Here Bauhinia galpinii N.E.Br. (Fabaceae) and especially Chlerodendrum myricoides (Hochst.) Vatke (=Rotheca myricoides (Hochst.) Steane &; Mabb.; Lamiaceae) appear to have antimutagenic properties.

Conclusion

The safe use of Helichrysum similimum should be questioned and further investigations on its mutagenicity and overall biological properties should be encouraged. Antimutagenic properties of especially Bauhinia galpinii and Rotheca myricoides are considered of particular interest as it may be assumed that these antimutagenic natural substances are able to lower the cancer risk from everyday exposures to environmental mutagens as well as to mutagenic pharmaceuticals.     

In vitro anticancer screening of South African plants

Aim of the study

The purpose of the present study is to evaluate South African plants for their anticancer activity.

Materials and methods

Plant species were collected throughout South Africa and voucher specimens were deposited and identified at the South African National Biodiversity Institute. Plant extracts were prepared and screened for in vitro anticancer activity against a panel of three human cell lines (breast MCF7, renal TK10 and melanoma UACC62) at the CSIR. Plant extracts that exhibited anticancer activity against these three human cell lines were screened by the NCI against sixty human cancer cell lines organized into sub-panels representing leukaemia, melanoma, cancer of the lung, colon, kidney, ovary, central nervous system, breast and prostate.

Results

A total of 7500 plant extracts were screened for in vitro anticancer activity against breast MCF7, renal TK10 and melanoma UACC62 human cell lines between the period 1999 and 2006. Hits were classified into four categories based on their total growth inhibition of the cell lines. A hit rate of 5.9% was obtained for extracts which showed moderate activity and these were screened by the NCI against a panel of sixty human cancer cell lines. The extracts of plant species with limited published information for their anticancer properties were subjected to bioassay-guided fractionation and the active constituents isolated and identified. The largest number of plant specimens in this study was from the family Asteraceae, which is rich in sesquiterpene lactones.

Conclusions

Although the extracts of the plants were randomly selected, 68% of these plant species which were hits in the screening programme are reported to be used medicinally. Based on our data, it appears that unrelated medicinal use of the source plants may serve as an initial guide to selection of plants for anticancer screening.