Antimicrobial activity of natural ecdysteroids from Serratula coronata L. and their acyl derivatives

Natural ecdysteroids isolated from Serratula coronata L., including 20-hydroxyecdysone (20-HE), 25-S-inokosterone, and ecdysone, did not exhibit antimicrobial activity with respect to most standard test microbe cultures. The introduction of the acetyl group into the 20-HE molecule significantly increased the antibacterial activity with respect to microbes inducing inflammatory and purulent processes. Acyl derivatives of 20-hydroxyecdysone can be suggested for use in wound-healing compositions __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 40, No. 5, pp. 34–36, May, 2006.     

Ecdysteroid sources in the Carpathian basin. 11-hydroxy substituted ecdysteroids from the Serratula wolffii Andrae

Seven ecdysteroids have been isolated from the methanolic extract of the herb Serratula wolffii Andrae. The isolation process involved the removal of polar and apolar contaminants, and also included the separation of the target ecdysteroids from each other by using combined chromatographic methods. Isolation of the pure compounds required a minimum of 2 and a maximum of 7 consecutive chromatographic steps with different selectivity. Six of the isolated ecdysteroids showed the presence of an 11alpha-hydroxyl group on the steroidal skeleton, which structure may enhance the increasing effect of ecdysteroids on the protein synthesys of mammals, according to literature data. Ajugasterone C, one of these compounds was found to be present in remarkable amount in the plant. One ecdysteroid, 11 alpha-hydroxypoststerone was identified as a new natural compound.     

Identification and determination of ecdysones and flavonoids in Serratula strangulata by micellar electrokinetic capillary chromatography

The simultaneous determination of 20-hydroxyecdysone ( 1), 25-deoxy-11,20-dihydroxyecdysone ( 2), kaempferol 4',7-dimethyl ether ( 3) and biochanin A ( 4) in the fruit, leaf and root of Serratula strangulata Iljin has been investigated by micellar electrokinetic capillary chromatography for the first time. With an electrolyte containing 15 mmol/L borate, 60 mmol/L SDS, 20 % (v/v) methanol, at pH 9.08 and 20 kV applied voltage, the four analytes were completely separated within 22.7 min. The effects of concentration of borate, electrolyte pH, the concentrations of SDS and organic modifier and the applied voltage on electrophoretic behavior and separation were studied. Regression equations revealed linear relationships (correlation coefficients: 0.9986 - 0.9997) between the peak areas of the analytes and the corresponding concentrations. The levels of analytes in the different parts of S. strangulata were easily determined with recoveries ranging from 95.3 % to 104.0 %.     

New Ecdysteroids from Serratula tinctoria

Six new ecdysteroids have been isolated from SERRATULA TINCTORIA; these are: the 2,22- and 3,22-diacetates of 20-hydroxyecdysone, 5beta-hydroxyrubrosterone, 3-epi-poststerone, 3-epi-rubrosterone, and 22-oxo-20-hydroxyecdysone. These minor compounds were found together with the known ecdysteroids, 20-hydroxyecdysone, its 2-, 3-, and 22-monoacetates, rubrosterone, poststerone, polypodine B (5beta,20-dihydroxyecdysone), pterosterone (25-deoxy-20,24-dihydroxyecdysone), and makisterone C (24-ethyl-20-hydroxyecdysone). All these ecdysteroids were isolated by a combination of several chromatographic techniques (liquid chromatography on alumina, DCCC, and HPLC), then identified using standard mass spectrometric and 2D (1)H-NMR techniques.     

The influence of ecdysteroid fraction from Serratula coronata on transmembrane ionic currents of snail neurons

Changes of the transmembrane potassium, calcium, and sodium ion currents in isolated neurons of Lymnaea stagnalis snail under the action of ecdysteroid fraction (serpisten) from Serratula coronata L. applied from outside in 0.01 -1000 microg/ml concentrations have been studied using the voltage-clamp technique. It is established for the first time that serpisten non-selectively activates the potassium and calcium ion currents (the currents amplitude increases by 2 - 15%) and reduces nonspecific membrane leakage currents in the entire range of concentrations. The sodium ion current also increased by 4 - 7% under the action of Serpisten in low concentrations (0.01 -10 microg/ml) in comparison with control, but this current decreased by 5 -10% at serpisten concentrations of 100 and 1000 microg/ml. The effects were reversible. The kinetics of currents was not changed under the action of serpisten.     

In vitro antiplatelet activity of flavonoids from Leuzea carthamoides

Plants and their secondary metabolites, including flavonoids, exhibit a wide range of biological effects. Consequently, natural substances are receiving an increased attention in medicinal research. Owing to these facts, in vitro antiplatelet activity of ethanol summary extract and four flavonoids from Leuzea carthamoides was determined in human platelet-rich plasma. Arachidonic acid (AA), adenosine diphosphate (ADP), collagen (COL), and thrombin were used as agonists of platelet aggregation. The summary extract showed a significant inhibition of the aggregation induced by COL and ADP. Of the tested flavonoids, eriodictyol (1) and patuletin (2) influenced COL- and AA-induced aggregation. Their IC(50) values are presented. Flavonoid glycosides eriodictyol-7-beta-glucopyranoside (3) and 6-hydroxykaempferol-7-O-(6'-O-acetyl-beta-D[small cap]-glucopyranoside) (4) were found to be weak antiplatelet agents. These results confirmed the fact that glucosylation decreases the antiplatelet activity. Quantitative composition of tested flavonoids in L. carthamoides extract was also determined. Though two of the tested flavonoids inhibited platelet aggregation, further evaluation of L. carthamoides, in order to discover other antiplatelet active compounds and possible adverse health effects, is needed.     

基于无机元素、有效成分银柴胡产地特征及关联分析

目的 比较不同产地银柴胡和土壤无机元素及药材有效成分特征,分析土壤与药材无机元素和有效成分的相关性。方法 收集来自9个产地银柴胡药材和生境土壤样品,采用ICP-MS技术测定样品16种无机元素含量,绘制无机元素指纹图谱;采用紫外可见分光光度法测定银柴胡总甾醇和总黄酮含量,并对土壤与药材无机元素和总甾醇、总黄酮含量进行Pearson相关性分析。结果 不同产地银柴胡药材和土壤具有相对一致的无机元素特征,但因无机元素不同表现出不同的特征差异;药材总甾醇和总黄酮含量亦因产地不同存在较大差异;银柴胡药材无机元素间及其与土壤无机元素存在不同水平的相关性,药材中S元素与总甾醇含量呈显著负相关性,土壤和药材中Mg元素以及土壤中Ca元素与药材总黄酮含量呈显著负相关性,药材中As元素与药材总黄酮含量呈显著正相关性。结论 银柴胡及生境土壤的无机元素,表现出不同的协同或拮抗作用,并与药材有效成分表现出一定的相互作用关系,研究结果为银柴胡道地产区建设和科学种植提供了一定的参考。     

Effects of 20-hydroxyecdysone, Leuzea carthamoides extracts, dexamethasone and their combinations on the NF-κB activation in HeLa cells

Objectives The plant steroid 20‐hydroxyecdysterone (20E) and 20E‐containing extracts from Leuzea carthamoides (Willd.) DC are sold with claims of anabolic and immunomodulatory effects. Yet their effect on the activation of nuclear factor kappa B (NF‐κB), a key player in immune response and cell fate, and their influence on the NF‐κB‐inhibiting activity of steroidal anti‐inflammatory drugs is still unknown. Methods The ability of 20E, Leuzea extracts and selected steroidal/non‐steroidal anti‐inflammatory drugs to influence the activation of NF‐κB was explored using, as the experimental model, human cervical cancer HeLa‐IL‐6 cells stably transfected with an IL‐6‐bound reporter gene. Effects on cell viability and proliferation were monitored (MTT assay). HPLC‐DAD was used to establish links between chemical patterns of Leuzea extracts and their bioactivities. Key findings 20E inhibited NF‐κB activation (IC50 31.8 µm ) but was less active than other plant metabolites (xanthohumol 3.8 µm , withaferin A 1.4 µm ). Leuzea extracts with high content in 20E had a fair activating effect, but in contrast, some extracts with low 20E content significantly inhibited NF‐κB activation at IC50s ranging from 3.5 to 6.2 µg/ml. Combination tests confirmed that 20E does not explain the NF‐κB modulation achieved by Leuzea extracts. The extracts but not 20E itself showed a significant modulation of the NF‐κB inhibitory effect of dexamethasone. Conclusions 20E is unlikely a major player in the NF‐κB inhibitory effects displayed by some Leuzea extracts in vitro. If confirmed in vivo, caution should prevail towards marketed Leuzea extracts that are non‐standardised or standardised on 20E only, since different starting materials and extracts may even cause opposite effects. More importantly, our results indicate the interaction potential of Leuzea with steroidal anti‐inflammatory drugs.     

Effect of Rhaponticum carthamoides extract on hemorheological properties of blood in rats with arterial hypertension

The hemorheological activity of a dry extract from Rhaponticum (Leuzea) carthamoides (Willd.) Iljin. was studied in spontaneously hypertensive rats (SHRs). A 14-day treatment of the test rats with a daily dose of 150 mg/kg improved the rheological characteristics, as manifested by a reduced viscosity of the whole blood and plasma, increased spontaneous erythrocyte aggregation and fibrinogen concentration, and increased erythrocyte deformability and electrophoretic mobility against the untreated control level.     

Structural diversity of ecdysteroids of Lychnis flos-cuculi

Eleven ecdysteroids have been isolated from Lychnis floscuculi; we are the first who report eight ecdysteroids of the eleven compounds in this plant. Two of these ecdysteroids, dihydrorubrosterone and 20-hydroxyecdysone 3-acetate are newly discovered natural products. The success of isolation of these new ecdysteroids has been based on the use of separation methods in a proper order; these separation procedures were completing each others. At the beginning steps of isolation simple separation methods were used, such a solvent-solvent distribution and fractionated precipitation. Two third of the contaminants were removed thereby. High capacity low resolution methods were used then, such as classical adsorption column chromatography and preparative thin-layer chromatography. The major component (20-hydroxyecdyssone) and certain minor ecdysteroids (polypodine B and rubrosterone) were isolated in pure form here. Purification of the further minor components (poststerone, 2-deoxy-20-hydroxyecdysone, vitikosterone E, dihydrorubrosterone, makisterone A, taxisterone, 20-hydroxyecdysone 2-acetate, 20-hydroxyecdysone 3-acetate) required HPLC and other absorption chromatographic methods. Our recent separation scheme means a generally applicable guiding principle for isolation of any plant ecdysteroid, major and minor alike. Structural identification of the known ecdysteroids was based on their spectral data and that of their literature information. Structural elucidation of 20-hydroxyecdysone 3-acetate was done by the help of a standard component prepared by acetylation of 20-hydroxyecdysone. From the mixture of seven acetates the corresponding compound (20-hydroxyecdysone 3-acetate) was isolated, and used for identification. Structural diversity of ecdysteroids of Lychnis flos-cuculi is evaluated, and a tentative explanation is introduced for the formation and biosynthesis of the versatility of phytoecdysteroids.     

Analysis of phytoecdysteroids in cultured plants of Ajuga nipponensis makino

Cultured plants of Ajuga nipponensis contained cyasterone (1), ajugasterone C (2), cyasterone-22-acetate (3) and 22-dehydrocyasterone (4) based on HPLC and NMR data, whereas 20-hydroxyecdysone was not detectable. The presence of compounds 2-4 is reported for the first time in this species. Compound 1 is the main phytoecdysteroid component found in both preblossom and blossom plants, but the latter contained higher amount than the former. Compared with other parts of the plant, the highest percentage of 1 and 3 occurred in leaves, amounting to 60.1% and 88.0% respectively, whereas the flowers contained mainly 2, which represented 72.8% of the total amount in whole plant. The contents of phytoecdysteroids in stems were very low.     

鹿根的研究进展

目的对鹿根的生态学、化学成分、药理活性研究进展进行综述。方法参考近30年国内外40余篇文献,简述其生态学相关内容,按照化合物的结构类型对其化学成分进行分类,对其药理作用进行总结。结果鹿根为一类喜阳植物,对环境有较好的适应性;含有多种化学成分,主要含有黄酮类,甾体类,三萜皂苷类,酚酸类,挥发油和多糖等化合物;具有促细胞生长、降血脂、抗动脉粥样硬化、抑菌、增强免疫系统、强壮机体、调节抗应激等药理作用。结论目前对鹿根在化学成分和药理活性方面的研究较多,关于其临床应用和作用机制尚有待于更深入的研究。     

法定药用植物论述

目的 对法定药用植物这一概念进行诠释,并对其内容和范围进行概括,阐明提出法定药用植物这一概念的意义。方法 查询我国历版中国药典、国家标准、地方标准和国外药典,对其收载的传统药、植物药和天然药物的基源植物进行分析,概括其基源植物的全貌。对提出法定药用植物这一概念的背景和历史渊源进行分析综合。结果 国家药典收载植物来源中药材已有悠久的历史,我国法定药用植物数量多,种类丰富,截止目前,我国的法定药用植物总数为2 965种,种类包含菌藻、地衣、苔藓、蕨类、裸子植物和被子植物。国外药典和标准亦收载了相当数量的法定药用植物。结论 法定药用植物这一概念的提出既符合法制日益健全的社会潮流也符合传统药、植物药和天然药物发展趋势。这一概念的提出具有深远意义,为法定药用植物的进一步研究、生产和使用奠定了基础。     

Studies on antigen specifity of immunoreactive arabinogalactan proteins extracted from Baptisia tinctoria and Echinacea purpurea.

In a series of experiments the cross-reactivity of antibodies raised against arabinogalactan proteins from Baptisia tinctoria and Echinacea purpurea was studied in order to prove the antigen specificity of the extracted glycoproteins/polysaccharides. Using the antigen-antibody reaction in a competitive ELISA it was evident that antibodies against glycoproteins from Baptisia tinctoria were specific because none of the other antigens like those from Echinacea purpurea, Thuja occidentalis, arabinogalactan from larch, LPS from E. coli 055:B5, and from Salmonella typhimurium were able to inhibit the antigen-antibody reaction. The same results were obtained from ELISA experiments with Echinacea purpurea. From these studies it was concluded that the antigenic regions of immunoreactive proteins from both medicinal plants show structural differences.     

Ethnoveterinary uses of medicinal plants: A survey of plants used in the ethnoveterinary control of gastro-intestinal parasites of goats in the Eastern Cape Province,South Africa

Conventional drugs have become expensive and therefore unaffordable to resource-limited farmers, causing farmers to seek low cost alternatives, such as use of medicinal plants. In this study, a survey was conducted in order to document information on medicinal plants used by farmers in the control of internal parasites in goats in the Eastern Cape Province. Structured questionnaires and general conversation were used to collect the information from farmers and herbalists. The survey revealed 28 plant species from 20 families that are commonly used in the treatment of gastro-intestinal parasites in goats. The plant family Asphodelaceae was frequent in usage, comprising 21.4% of the plants, and the Aloe was the most utilized species (50%). Leaves were the most frequently used plant parts (45.9%), and decoctions constituted the majority of medicinal preparations (70%). Medicinal plants are generally used in combination with other plants, and/or non-plant substances, but a few plants are used on their own. These medicinal plant remedies are administered orally, mainly by use of bottles and this is done twice in summer at intervals of one month, only once in winter and when need arises thereafter. Some of the mentioned plants have been reported in literature to possess anthelmintic properties, while others possess activities ranging from anti-inflammatory, analgesic, antimicrobial, purgative, anti-edema to immuno-regulation. If their safety and efficacy could be confirmed, these plants could form an alternative cost effective strategy in managing helminthiasis in the province.     

Ethnopharmacological use of plants by Sisala traditional healers in northwest Ghana

Context and objective: The Sisala traditional healers of northwest Ghana have a rich ethnomedical tradition. The purpose of this study was to collect and analyse data on medicinal plants commonly used by Sisala traditional healers.

Methods: A total of 30 traditional healers were interviewed using a mixture of open- and closed-ended questionnaires after obtaining prior-informed consent. Plant materials of each species of medicinal plant mentioned being used were collected and processed as voucher specimens following standard ethnobotanical methods.

Results: The majority (65%) of traditional healers were males, age ≥ 38, and their knowledge about medicinal plants was acquired orally largely from their parents (81.3%). A total of 35 species of plants were reported used to treat 24 diseases. Most (55%) of the plant materials were harvested from the bush and about half (54.8%) of the healers collected plant materials in the morning. Leaf (20%) and root (17.5%) plant materials were most commonly used in the preparation of 27 herbal remedies for treatments. The modes of administration of the herbal remedies were both through internal and external routes.

Conclusion: The results of this study show that Sisala traditional healers possess rich traditional knowledge about medicinal plants and new therapeutic use claims for 34 medicinal plants used in Ghana and widely within Africa are documented for the first time.     

香鳞毛蕨化学成分的研究

目的:研究香鳞毛蕨的化学成分。方法:化学成分系统预试法。结果:香鳞毛蕨中含有氨基酸、蛋白质、糖及其苷类、酚类、鞣质、有机酸、挥发油、黄酮等各类化学物质。结论:香鳞毛蕨是一种具有较高开发价值的药用植物。     

Preliminary screening the antioxidant potential of in vitro-propagated Amsonia orientalis: An example to sustainable use of rare medicinal plants in pharmaceutical studies

Amsonia orientalis (European Bluestar) is a critically endangered plant species with medicinal and ornamental properties. The rare availability of the species in nature limits its potential to be used for various purposes. However, plant tissue culture is an effective method for the cultivation of such vulnerable species without damaging their natural populations, which are very limited in nature for scientific purposes. By taking advantage of plant tissue culture, this study aimed to measure the phenolic substance and flavonoid contents in leaf extracts of in vitro-propagated Amsonia orientalis, and to investigate their antioxidant potentials through phosphomolybdate and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays. The crude extracts prepared in water, aqueous ethanol, methanol, and acetone were tested. The highest phenolic substance content was found in the ethanolic extracts, while statistically the same flavonoid contents were found in the ethanolic, methanolic, and acetone extracts. Although the water extract had lesser flavonoid content, it exhibited a notable antioxidant property. The ethanolic leaf extract gave the highest antioxidant and DPPH radical scavenging activity, especially when used at 1 mg mL^?1 concentration. Also, the TLC fingerprint profile validated the presence of valuable phytoconstituents in the leaves of the plant. This study indicated that ultrasound-assisted extraction of minimal amounts of dried leaf samples from in vitro-propagated plants might be adequate for the pre-screening of the antioxidant capacity of rare plant species.     

基于HPLC法的黄芩和粘毛黄芩药用活性成分相似性、多样性评价

目的评价黄芩及粘毛黄芩中活性成分的相似性及多样性,研究不同干燥方法对两者的影响。方法在资源调查、收集的基础上,经不同干燥方法处理后,以HPLC法测定活性成分含量,并进行对比分析。结果 60℃烘干提高了黄芩中的黄芩素含量,对其他成分没有显著影响;但对粘毛黄芩中黄芩苷和汉黄芩苷的含量有一定程度的降低。另外,粘毛黄芩中未检出野黄芩苷;粘毛黄芩中黄芩苷和汉黄芩苷的含量(分别为9.89%和2.27%)与黄芩(分别为10.23%和2.33%)相比无显著差异(P>0.05),但黄芩素和汉黄芩素的含量(分别为0.21%和0.08%)均显著低于黄芩(分别为0.40%和0.16%)(P<0.05)。结论不同干燥方法对活性成分有一定影响,粘毛黄芩与黄芩活性成分有差异。