苦瓜化学成分的研究

目的研究葫芦科苦瓜属植物苦瓜Momordica charantia的未成熟果实的化学成分。方法采用树脂柱纯化,硅胶柱色谱进行分离纯化,通过理化常数和光谱分析鉴定化合物的结构。结果从苦瓜的乙醇提取物中分离、鉴定了5个化合物的结构,分别是日耳曼醇乙酸酯(germanicyl acetate,Ⅰ)、苦瓜皂苷元(aglycone of momordico-sideⅠ,Ⅱ)、苦瓜皂苷元L(aglycone of momordicoside L,Ⅲ)、苦瓜苷(charantin,Ⅳ)、β-谷甾醇(β-sitosterol,Ⅴ)。结论化合物Ⅰ为首次从苦瓜属植物中分离得到,化合物Ⅱ为首次从苦瓜中分离得到新的天然产物,化合物Ⅲ为国内首次从苦瓜中分离得到。     

苦瓜化学成分的研究

目的研究苦瓜的化学成分。方法采用乙醇提取、氯仿萃取和硅胶柱色谱分离,通过理化常数和光谱分析鉴定化合物的结构。结果从苦瓜的氯仿萃取物中分离并鉴定了5个化合物,化学结构分别为苦瓜皂苷元F1(aglycone of momordicoside F1,Ⅰ)、5,25-豆甾二烯醇(5,25-stigmastadien-3-ol,Ⅱ)、苦瓜皂苷元Ⅰ(aglycone of momordicoside,Ⅰ,Ⅲ)、苦瓜苷(charantin,Ⅳ)、β-谷甾醇(β-sitosterol,Ⅴ)。结论化合物和为首次从苦瓜中分离得到。     

苦瓜中新化合物的化学研究

目的 研究苦瓜的新活性成分.方法 采用乙醇提取、微波萃取、D-101型大孔树脂纯化、硅胶柱色谱以及制备液相色谱等方法分离,通过理化常数及光谱数据鉴定化合物的结构.结果 分离并鉴定了8个化合物,分别为charantadiol A(5β,19-epoxycucurbita-6,23(E),25(26)-triene-3β,19(R)-diol,Ⅰ)、(+)-eduesmin(Ⅱ),blueme-nol A(Ⅲ)、宽叶葱苷元D(karatavilagenin D.Ⅳ)、5β,19-epoxycucurbita-6,23-diene-3β-19,23-triol(Ⅴ)、苦瓜皂苷元Ⅰ(5,19-epoxy-5β-cucurbita-6,23(E)-diene-3β,25-diol,Ⅵ)、苦瓜皂苷L昔元(aglycone of momordicoside L,3β,7β,25-trihydroxy-cucurbita-5,23(E)-diene-19-al,Ⅶ)、β-谷甾醇(β-sitosterol,Ⅷ ).结论 化合物Ⅰ为新化合物,命名为苦瓜二醇A(charantadiol A),化合物Ⅱ、Ⅲ为从苦瓜中首次分离得到.     

苦瓜中总皂苷的比色法测定

目的：建立苦瓜中总皂苷的比色法含量测定方法,定量分析苦瓜中的总皂苷含量。方法：采用热回流法提取苦瓜干料中的苦瓜皂苷。用液液萃取法去除杂质,纯化苦瓜提取液。然后采用香草醛-高氯酸法比色体系,优化体系参数,确定标准曲线性范围、准确度、加样回收率并测定苦瓜中的总皂苷含量。结果：经验证标准曲线性良好,准确度高,加样回收率高且稳定,可用于苦瓜中总皂苷的测定。测得江苏苦瓜中的总皂苷含量为3.10%。结论：本文所建立的方法可以用于苦瓜中总皂苷含量的测定,为日后的进一步研究奠定基础。     

不同产地苦瓜中苦瓜皂苷的闪式提取及HPLC测定

目的 采用闪式提取和固相萃取相结合的方法来快速测定不同产地苦瓜中momordicoside L、kuguaglycoside C、goyaglycoside-d的量.方法 样品经过闪式提取和固相萃取处理后,采用HPLC法进行测定.色谱条件为Kromasil C18色谱柱(150 mm×4.6 mm,5μm),流动相为乙腈-水(57:43),体积流量1.0 mL/min,检测波长203 nm.结果 Momordicoside L 线性范围为0.048～0.48 μg,加样回收率为96.93％,RSD为1.95％; kuguaglycoside C线性范围为0.024～0.36 μg,加样回收率为97.80％,RSD为1.19％; goyaglycoside-d线性范围为0.006～0.192 μg,加样回收率为93.62％,RSD为1.28％.广东、广西、福建3个产地3种成分的量差异较大.结论福建产苦瓜中momordicoside L量最高,广东产苦瓜中kuguaglycoside C 和goyaglycoside-d的量均较高.此方法可作为苦瓜药材质量评价的依据.     

降血糖活性成分苦瓜皂苷的纯化工艺研究△

目的:研究苦瓜中降糖活性成分皂苷的纯化工艺.方法:以苦瓜苷计的总皂苷含量为指标,用正交试验和单因素试验等方法考查各工艺步骤的影响因素.结果:苦瓜的乙醇提取物经D-101大孔吸附树脂富集纯化后皂苷含量可达35%以上.结论:本纯化工艺可为苦瓜皂苷的工业化制备提供参考.     

降血糖活性成分苦瓜皂苷的纯化工艺研究

目的：研究苦瓜中降糖活性成分皂苷的纯化工艺。方法：以苦瓜苷计的总皂苷含量为指标，用正交试验和单因素试验等方法考查各工艺步骤的影响因素。结果：苦瓜的乙醇提取物经D-101大孔吸附树脂富集纯化后皂苷含量可达35％以上。结论：本纯化工艺可为苦瓜皂苷的工业化制备提供参考。     

降血糖活性成分苦瓜皂昔的纯化工艺研究

目的：研究苦瓜中降糖活性成分皂苷的纯化工艺。方法：以苦瓜苷计的总皂苷含量为指标，用正交试验和单因素试验等方法考查各工艺步骤的影响因素。结果：苦瓜的乙醇提取物经D-101大孔吸附树脂富集纯化后皂苷含量可达35％以上。结论：本纯化工艺可为苦瓜皂苷的工业化制备提供参考。     

苦瓜根总皂苷的提取及其对α-葡萄糖苷酶活性抑制作用的研究

目的研究了苦瓜根总皂苷的提取工艺及其对α-葡萄糖苷酶活性的抑制作用。方法以人参皂苷Rb1为对照,采用分光光度法对苦瓜根总皂苷的含有量进行定量分析,通过正交试验L16(45)对其进行以提取温度、浸泡时间、乙醇体积分数和料液比为考察因素的工艺优化试验,同时对最优条件下制备得到的总皂苷进行了α-葡萄糖苷酶的抑制活性实验。结果在浸提温度40℃,浸提时间6 h,乙醇体积分数70%及料液比1∶5的最佳提取条件下,苦瓜根总皂苷的提取率为2.3%,纯度达98%,而且对α-葡萄糖苷酶具有良好的抑制作用,IC50为1 538μg/m L。结论通过正交试验得到了苦瓜根总皂苷的最佳提取工艺,而且其对α-葡萄糖苷酶表现出抑制作用,显示出一定的降糖活性。     

糖康胶囊中苦瓜的提取工艺研究

目的考察糖康胶囊中苦瓜的提取工艺。方法采用正交实验法,以苦瓜总皂苷含量和浸膏收率为指标筛选苦瓜的提取工艺。结果确定苦瓜的提取工艺为:采用12,10,8倍水,提取3次,前两次提取时间2 h/次,第3次30 min。结论该实验确定的苦瓜提取工艺方法合理,稳定可行。     

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.     

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.     

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.     

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。     

Antifungal activity of Brazilian medicinal plants involved in popular treatment of mycoses

A survey of medicinal plants used to treat common mycoses was done in the Curituba district, Sergipe State, Brazil. One hundred inhabitants were interviewed by health agents and traditional healers. Four different plants were the most cited (more than 50% of the citations): Ziziphus joazeiro, Caesalpinia pyramidalis, Bumelia sartorum and Hymenea courbaril. The aqueous extracts obtained following traditional methods and using different parts of these plants, were submitted to drop agar diffusion tests for primary antimicrobial screening. Only the water infusion extract of Ziziphus joazeiro and Caesalpinea pyramidalis presented a significant antifungal activity against Trichophyton rubrum, Candida guilliermondii, Candida albicans, Cryptococcus neoformans and Fonsecaea pedrosoi, when compared to the antifungal agent amphotericin B. The minimal inhibitory concentration (MIC) of the bioactive extracts was evaluated by the microdilution method. Best activity with a MIC of 6.5 microg/ml for both extracts was observed against Trichophyton rubrum and Candida guilliermondii. Ziziphus joazeiro and Caesalpinea pyramidalis extracts presented also low acute toxicity in murine models. The present study validates the folk use of these plant extracts and indicates that they can be effective potential candidates for the development of new strategies to treat fungal infections.     

Experimental study on anti-inflammatory activity of a TCM recipe consisting of the supercritical fluid CO2 extract of Chrysanthemum indicum, Patchouli Oil and Zedoary Turmeric Oil in vivo

Ethnopharmacological relevance

Chrysanthemum indicum (Compositae) Linné, Pogostemon cablin (Blanco) Benth and Curcuma wenyujin (Zingiberaceae) Y. H. Chen et C. Ling are three of the extensively used herbal remedies among traditional Chinese medicines for the purpose of anti-inflammation. A traditional Chinese medicine (TCM) recipe named CPZ consisting extracts of the above three herbs, has shown noteworthy anti-influenza activity, which is closely related to its anti-inflammatory feature.

Aim of this study

To investigated the anti-inflammtory activity of CPZ in vivo for a further exploration of the recipe's anti-inflammatory properties.

Materials and methods

The anti-inflammatory property of CPZ on acute inflammation was evaluated by inflammatory models of dimethylbenzene (DMB)-induced ear vasodilatation and acetic acid-induced capillary permeability enhancement in mice, as well as the carrageenan-induced paw edema rat model, in which inflammation-related cytokine including prostaglandin E₂ (PGE₂), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), and nitric oxide (NO) in the edematous paw tissue were determined by enzyme linked immunosorbent assay (ELISA). Moreover, effect of CPZ on chronic inflammation was observed through granuloma formation in rats subjected to cotton pellet implantation.

Results

CPZ (340, 170, and 85 mg/kg for mice, p.o.) not only decreased the DMB-induced ear vasodilatation but also attenuated capillary permeability under acetic acid challenge in mice. And the significant inhibition on carrageenan-induced paw edema was observed. Further more, the ELISA results showed that CPZ (170, 85, and 42.5 mg/kg for rats, p.o.) could up-regulate the level of IL-1β in the edema paw tissue of rats significantly while down-regulate that of PGE₂, but no apparent effect on TNF-α or NO was observed in the test. Besides, CPZ had a certain degree of restraining effect on the cotton pellet-induced granuloma formation in rats and the highest dose of 170 mg/kg even showed a significant suppression on it.

Conclusion

The above results indicated that CPZ possessed a potent anti-inflammatory activity, which is indicated to be closely associated with its regulation on IL-1β and PGE₂ thereby mediating the inflammatory response acting at an appropriate level.     

Regulation effects on abnormal glucose and lipid metabolism of TZQ-F,a new kind of Traditional Chinese Medicine

Aim of the study

Based on the recipe of the traditional anti-diabetic formula TZQ, we developed TZQ-F, a new formula including 8 fractions isolated from Red Paeony root, Mulberry leaf, Lotus leaf, Danshen root and Hawthorn leaf with a good quality assurance. The study was aimed at fraction preparation and effects of the fractions on abnormal glucose and lipid metabolism.

Materials and methods

The active fractions were obtained by macroporous resin, ion-exchange resin and polyamide resin column chromatographies. HPLC analyses were used for quality control. In vitro mechanism study included DPPH radical scavenging, AGEs formation inhibition, α-glucosidase inhibition and lipase inhibition, and rats on high-fat diet were used for in vivo study.

Results

In vitro mechanism study showed that among the 8 fractions, three of them had inhibition effects on intestinal disaccharase, three with inhibition effects on lipase, and five with effects of free radical scavenging. In vivo study showed that after 4 weeks of treatment, TZQ-F significantly decreased the levels of serum total cholesterol, TG, glucose, LDL-C and HDL-C in rats on high-fat diet. Consistent with the in vitro and in vivo results, histology study demonstrated that TZQ-F alleviated hepatic steatosis induced by high-fat diet.

Conclusions

TZQ-F possesses the potential regulation effects on abnormal glucose and lipid metabolism.     

常用藏药“蒂达”(藏茵陈)基原物种药用合理性及资源利用价值评价

目的:对“蒂达”各品种不同基原植物药用合理性及其资源利用价值作出评价.方法:采用HPLC指纹图谱共有特征峰、结合SPSS聚类分析方法,评价“蒂达”不同品种基原植物的成分组成相似性.结果:“蒂达”不同品种涉及的来源有龙胆科獐牙菜属、花锚属、扁蕾属及肋柱花属共15种1变种33个样品,指纹图谱全谱相似度较差;以10个共有峰成分的相对面积聚类,其基原植物可分别聚为4个组;上述4个属的属间成分组成差异较大;其中獐牙菜属不同种间成分组成变化较大,而其他各属种间成分组成相似度较高.结论:上述龙胆科4属植物均含有具有保肝利胆生物活性的环烯醚萜类、(山)酮类及三萜类成分,藏医学将其归为“蒂达”一类药材使用具有一定的物质基础;鉴于“蒂达”类药材不同基原各品种间在成分组成上差异较大,分别制定各品种的HPLC指纹图谱,是鉴别和控制各品种质量的有效手段,可有效控制各基原品种质量.     

虫草属EST-SSR标记系统的建立研究

目的:通过球孢虫草、蛹虫草EST设计EST-SSR引物,建立虫草属EST-SSR标记系统.方法:从NCBI公共数据库下载获得虫草EST,利用Sequece Seiners 1.2软件去除冗余序列并设计引物,进行PAGE电泳.结果:通过去除EST总序列中低质量的和冗余的序列后,得到全长为2 953 173 bp的4 556条无冗余球孢虫草EST.从中发掘出718个EST-SSR,分布于616条EST中,出现频率是15.8％.平均分布频率是每4 096 bp出现1个,三核苷酸重复序列有419个,是出现最多的重复类型.蛹虫草EST去冗余后得到1 363条无冗余EST,共含有1 117个EST-SSR,出现频率为81.95％,出现最多的重复类型是A核苷酸重复.根据球孢虫草EST-SSR序列,设计合成50对引物,有扩增产物的引物为34对,占总设计引物数的68％.根据蛹虫草EST-SSR,设计合成40对引物,有扩增产物的引物为39对,占总设计引物数的97.5％.基于SSR标记进行聚类分析,7种虫草无性型均能分开,且分为4支.结论:虫草属EST-SSR出现频率较高、类型较丰富、多态性潜能较高,具有较高的利用价值.球孢虫草和蛹虫草EST开发的SSR标记在虫草属有较好的转移性与通用性,可以很好的应用于虫草种间遗传关系的研究.应用虫草物种EST建立分子标记是一条简便而又有效的途径.     

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。