2,3-Seco and 3-nor guaianolides fromAchillea alpina with antidiabetic activity / 中国天然药物

In this study, we presented the isolation and characterization of eight novel seco-guaianolide sesquiterpenoids (1-8) and two known guaianolide derivatives (9 and 10), from the aerial part of Achillea alpina L.. Compounds 1-3 were identified as guaianolides bearing an oxygen insertion at the 2, 3 position, while compounds 4-8 belonged to a group of special 3-nor guaianolide sesquiterpenoids. The structural elucidation of 1-8, including their absolute configurations, were accomplished by a combination of spectroscopic data analysis and quantum electronic circular dichroism (ECD) calculations. To evaluate the potential antidiabetic activity of compounds 1-10, we investigated their effects on glucose consumption in palmitic acid (PA)-mediated HepG2-insulin resistance (IR) cells. Among the tested compounds, compound 7 demonstrated the most pronounced ability to reverse IR. Moreover, a mechanistic investigation revealed that compound 7 exerted its antidiabetic effect by reducing the production of the pro-inflammatory cytokine IL-1β, which was achieved through the suppression of the NLRP3 pathway.

A Histopathological Study of Cisplatin-induced Acute Vascular Injuries in Vital Organs and Protective Effect of Achillea millefolium

The aim was to study the protective effect of ethanolic extract of Achillea millefoliumon acute vascular injuries induced by cisplatin in liver, heart and renal tissues 24 hour after administration and using histopathological surveys in wistar rats. 24 adult male wistar rats were randomly divided into four groups. Group I (control group) received physiological saline for 10 days. Animals of group II had single dose of injection of CP (cisplatin) (6mg/kg, IP) on the ninth day. Group III received Achillea millefoliumextract (250mg/kg, gavage) for 10 consecutive days. Group IV had both Achillea millefoliumextract (250mg/kg, gavage) for 10 consecutive days and a single dose of injection of CP (6mg/kg, IP) on the ninth day. Kidney, liver and heart organs were collected on 10thday from sacrificed rats and subjected to histopathological analysis. Then the possible histopathological vascular effects of cisplatin on liver, heart, kidney tissues and the protective effect of Achillea millefoliumextract was analysed. Obtained data showed the vascular injuries in CP group as congestion of cardiac capillaries (p=0.00) and interstitial edema (p=0.03). In the kidney, shrinkage of glomeruli (p=0.04), widening of Bowman's space (p=0.04), dilatation of cortical capillaries (p=0.01) were significantly altered. The findings of liver organ were increased sinusoidal space (p=0.00) and infiltration of neutrophils in portal space (p=0.01). Pretreatment with ethanolic extract of Achillea millefoliumcould attenuate these vascular injuries. Briefly, 24 hour after single injection of cisplatin the inflammatory process was seen in vital organs and administration of Achillea millefoliumcould mitigate these side effects

Achillea biebersteinii extracts suppress angiogenesis and enhance sensitivity to 5-fluorouracil of human colon cancer cells via the PTEN/AKT/mTOR pathway in vitro

Objective: To investigate the antiproliferative, anti-angiogenic, and apoptotic effects of extracts of Achillea biebersteinii (ABE) and combined treatments of ABE with 5-fluorouracil (5-FU) on HT-29 cells.Methods: The effects of ABE, 5-FU, and combined treatments on the viability of HT-29 cells were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Isobologram analysis was used to determine synergism between ABE and 5-FU. The apoptotic and anti-angiogenic effects were determined by cell death detection and human vascular endothelial growth factor ELISA method, respectively. Transcriptional and translational expressions of p53, Bax, Bcl-2, p38 MAPK, Akt, PTEN, and mTOR were also evaluated by real-time PCR and Western blotting analysis. Results: ABE decreased the viability of HT-29 cells in a dose-dependent manner. Combined treatment of hexane, chloroform, and methanol extracts of Achillea biebersteinii with 5-FU at IC50 doses decreased the cell viability to 26.0％, 19.1％, and 14.9％, respectively (P<0.001). Furthermore, ABE treatment alone and combination with 5-FU, induced apoptosis, significantly downregulated mTOR, Akt, Bcl-2 expression, upregulated p53, Bax, PTEN, p38 MAPK expression, and exhibited anti-angiogenetic effects. Conclusions: Our findings indicate that ABE shows synergism with 5-FU and inhibits the proliferation of HT-29 cells by inducing apoptosis and suppressing angiogenesis, which may provide biological evidence for further use of ABE in the treatment of colorectal cancer.

Achillea biebersteinii extracts suppress angiogenesis and enhance sensitivity to 5-fluorouracil of human colon cancer cells via the PTEN/AKT/mTOR pathway in vitro

To investigate the antiproliferative, anti-angiogenic, and apoptotic effects of extracts of Achillea biebersteinii (ABE) and combined treatments of ABE with 5-fluorouracil (5-FU) on HT-29 cells. Methods: The effects of ABE, 5-FU, and combined treatments on the viability of HT-29 cells were determined by 3-(4,5- dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Isobologram analysis was used to determine synergism between ABE and 5-FU. The apoptotic and anti-angiogenic effects were determined by cell death detection and human vascular endothelial growth factor ELISA method, respectively. Transcriptional and translational expressions of p53, Bax, Bcl-2, p38 MAPK, Akt, PTEN, and mTOR were also evaluated by real-time PCR and Western blotting analysis. Results: ABE decreased the viability of HT-29 cells in a dosedependent manner. Combined treatment of hexane, chloroform, and methanol extracts of Achillea biebersteinii with 5-FU at IC50 doses decreased the cell viability to 26.0%, 19.1%, and 14.9%, respectively (P0.001). Furthermore, ABE treatment alone and combination with 5-FU, induced apoptosis, significantly downregulated mTOR, Akt, Bcl-2 expression, upregulated p53, Bax, PTEN, p38 MAPK expression, and exhibited anti-angiogenetic effects. Conclusions: Our findings indicate that ABE shows synergism with 5-FU and inhibits the proliferation of HT-29 cells by inducing apoptosis and suppressing angiogenesis, which may provide biological evidence for further use of ABE in the treatment of colorectal cancer.

N-alkylamide profiling of Achillea ptarmica and Achillea millefolium extracts by liquid and gas chromatography-mass spectrometry / 药物分析学报

Achillea millefolium and Achillea ptarmica are both plants belonging to the Asteracea family and are traditionally used for their medicinal properties. It has already been shown that some N-alkylamides (NAAs) are responsible for these pharmacological actions. Therefore, in the present study, the NAA content of the two plants was analytically characterised. Different extracts were prepared from the roots, the leaves, the stems and the flowers. The structures of NAAs have been assigned in ethanolic extracts of Achillea millefolium and Achillea ptarmica using high performance liquid chromatography – electrospray ionisation – mass spectro-metry (HPLC–ESI–MS) and gas chromatography–electron impact–mass spectrometry (GC–EI–MS). Using both analytical techniques, the structures of 14 and 15 NAAs have been assigned in Achillea ptarmica and Achillea millefolium, respectively. Structures of two new NAAs, previously never observed in Achillea ptarmica, were assigned: deca-2E,6Z,8E-trienoic acid 2-methylbutylamide (homospilanthol) or a related isomeric compound and deca-2E,4E-dienoic acid N-methyl isobutylamide. The structure of homospilanthol or a related isomeric compound was also assigned in Achillea millefolium for the first time.

Achillea fragrantissima, rich in flavonoids and tannins, potentiates the activity of diminazine aceturate against Trypanosoma evansi in rats

OBJECTIVE@#To evaluate activity of methanol extract of Achillea fragrantissima (meth) (A. fragrantissima) alone or in combination with diminazine aceturate (DA) against Trypanosoma evansi (T. evansi) in experimentally infected rats.@*METHODS@#Sixty adult male Wister albino rats were divided equally into 6 groups (A-F). Rats in groups A-E were experimentally infected with T. evansi and those in group F were uninfected. The groups were treated respectively as follows: group A-with 3.5 mg/kg DA; group B- with 1000 mg/kg meth A. fragrantissima; group C-3.5 mg/kg DA plus 500 mg/kg meth A. fragrantissima; group D-3.5 mg/kg DA plus 1000 mg/kg meth A. fragrantissima. Group E was left untreated. Parasitemia, survivability, packed cell volume, hemoglobin concentration, total leucocytes count, lymphocyte count, and serum malondialdehyde and reduced glutathione (GSH) levels were estimated. Phytochemical screening of meth A. fragrantissima was also performed.@*RESULTS@#The phytochemical analysis of the meth A. fragrantissima indicated a higher content from polyphenolic tannins and non tannins and flavonoids. The efficacy percentage against trypanosomiasis in groups A - E was respectively as follows 80, 40, 90, 100, 0. The administration of meth-A. fragrantissima (1000 mg/kg b.wt.) produced a moderate efficacy against trypanosomiasis. Untreated rats in group E died between 25 and 30 d post infection. The rats given DA and meth A. fragrantissima combinations (C and D) showed faster and higher recovery rates than the uninfected control and groups A and B. The initial reduction in packed cell volume, hemoglobin, total leucocytes count, increases in serum malondialdehyde and decreases in GSH levels were reversed by the treatments.@*CONCLUSION@#The administration of the methanol extracts of A. fragrantissima and DA combination therapy was more effective than each product alone in the treatment of rats infected with T. evansi and further studies are required to isolate more active ingredients.

Analysis of liposoluble chemicals from Achillea Alpina L .by GC-MS / 药学实践杂志

Objective To identify the chemical structures for the components in the liposoluble portion of Achillea alpi-na L .by gas chromatography/mass spectrometry (GC-MS) .Methods Achillea alpina L .was extracted with 95% alcohol and petroleum ether .The chemical compositions in the extract were analyzed with GC-MS .The structures were identified by comparing to the authentic samples and searching NIST 10 database .The relative content of each compound in the extract was calculated by area normalization method .Results Twenty-nine compounds were separated and identified ,which accounted for 82 .74% of petroleum ether extract .The major constituents were octamethylpicen-3-ol (33.16% ) ,Lup20(29)-en-3-ol ,acetate (3b) (10 .99% ) , n-Hexadecanoic acid (7 .98% ) , Stigmasterol (3 .68% ) , Octadecanoic acid (3 .55% ) , Friedelan-3-one (3 .51% ) .Conclusion This simple and accurate method can be used for the assay of liposoluble chemicals from Achillea alpi-na L .The results provide a foundation for pharmacological research and better use the resource of Achillea alpina L .

HPLC DETERMINATION OF GLYCYRRHIZIC ACID TABLETAE FROM HERBAL / Монголын эм зүй, эм судлал

Introduction: It is very important to develop traditional medicine, connecting it with modern medicine, and studying medicines, herbal medicines, and raw materials, which have been used by people for hundreds of years, and to use them to treat various diseases.1 In every country of the world as well as in our country, viral hepatitis has become widespread. Thus the number of chronic liver diseases, such as liver hardening and liver cancer, is increasing. The main ingredients are those of four herbs, that people have been using in both Tibetan and Mongolian traditional medicine for hundreds of years for liver diseases, namely Saussurea amara L., Salsola collina Pall., Glycyrrhiza uralensis Fisch., Achillea aziatica Serg. The aim of this research is to determine the quality assessment criteria for herbal preparation tablets and to develop pharmacopeia articles. As a result of the study the quality criteria of the tablet were defined, which have completely satisfied the requirements of common tablets. Material and methods: The research was carried out by the Accredited Pharmaceutical Laboratory of the School of Pharmacy and Bio-Medicine. The qualitative and quantitative assessment was measured according to the methods published in the Mongolian National Pharmacopeia /first edition/ and CP 2005, Vol. 1. The quantitative analysis of the amount of glycyrrhizic acid was determined by HPLC. Using HPLC, applications were performed on an Octadecylsilaine, С18 (5 m, 4.0 mm, 250 nm); mobile phase: acetic acid-methanol-0.2 mol/L ammonium acetate (1:33:67); detection wavelength: 250nm: flow rate 0.8 ml/min; column temperature 220 C. 2 Results: Identification and quantification of some of the biological active components of preparation, including glycyrrhizic acid components, were determined, using HPLC, and it was established that glycyrrhizic acid 18.3mg %±0.04. Key words: Saussurea Amara L., Achillea asiatica Serg., Salsola Collina Pall., Glycyrrhiza Uralensis Fisch.

Achillea fragrantissima, rich in flavonoids and tannins, potentiates the activity of diminazine aceturate against Trypanosoma evansi in rats

Objective: To evaluate activity of methanol extract of Achillea fragrantissima (meth) (A. fragrantissima) alone or in combination with diminazine aceturate (DA) against Trypanosoma evansi (T. evansi) in experimentally infected rats. Methods: Sixty adult male Wister albino rats were divided equally into 6 groups (A-F). Rats in groups A-E were experimentally infected with T. evansi and those in group F were uninfected. The groups were treated respectively as follows: group A-with 3.5 mg/kg DA; group B- with 1. 000 mg/kg meth A. fragrantissima; group C-3.5 mg/kg DA plus 500 mg/kg meth A. fragrantissima; group D-3.5 mg/kg DA plus 1. 000 mg/kg meth A. fragrantissima. Group E was left untreated. Parasitemia, survivability, packed cell volume, hemoglobin concentration, total leucocytes count, lymphocyte count, and serum malondialdehyde and reduced glutathione (GSH) levels were estimated. Phytochemical screening of meth A. fragrantissima was also performed. Results: The phytochemical analysis of the meth A. fragrantissima indicated a higher content from polyphenolic tannins and non tannins and flavonoids. The efficacy percentage against trypanosomiasis in groups A - E was respectively as follows 80, 40, 90, 100, 0. The administration of meth-A. fragrantissima (1. 000 mg/kg b.wt.) produced a moderate efficacy against trypanosomiasis. Untreated rats in group E died between 25 and 30 d post infection. The rats given DA and meth A. fragrantissima combinations (C and D) showed faster and higher recovery rates than the uninfected control and groups A and B. The initial reduction in packed cell volume, hemoglobin, total leucocytes count, increases in serum malondialdehyde and decreases in GSH levels were reversed by the treatments. Conclusion: The administration of the methanol extracts of A. fragrantissima and DA combination therapy was more effective than each product alone in the treatment of rats infected with T. evansi and further studies are required to isolate more active ingredients.

Comparative chemical composition of the essential oils of Iranian Achillea oxyodonta from different ecological regions.

Hydro-distilled volatile oils from the aerial parts of Achillea oxyodonta (collected from two different locations), which is endemic to Iran, was analysed by GC and GC–MS. In the oil of A. oxyodonta from Shemshak sample, 54 compounds representing 95.68% of the total oil were characterized with camphor 13.18%; spathulenol 11.19%; 1,8-cineole 10.51%; salvial-4(14)-en-1-one 4.82%; eudesm-4-en-6-one 3.17%; caryophyllene oxide 3.07%; filifolone 3.03% as the major components. In the oil obtained from A. oxyodonta sample collected in Soleghan, 49 compounds representing 97.98% of the oil were characterized. spathulenol 13.13%; camphor 12.83%; 1,8-cineole 11.15%; cis-β-Farnesene 8.21%; α-Cadinol 4.83%; salvial-4(14)-en-1-one 4.19%; bornyl acetate 4.16%; isospathulenol 3.64%; germacrene D 3.45%; endo-1,5-Epoxysalvial-4(14)-ene 3.09% was found as the main components. The results showed that there are qualitative similarities between the oils although the amounts of some corresponding compounds are different indicating that environmental factors strongly influence its chemical composition.

Cell viability, anti-proliferation and antioxidant activities of Sideritis syriaca, Tanacetum argenteum sub sp. argenteum and Achillea aleppica subsp. zederbaueri on human breast cancer cell line (MCF-7).

The breast cancer is one of the most common types of cancer. Many scientists have focused on the treatment of this disease for a long time by studying anti-cancer activities of plant extracts as well as synthetics. Lamiaceae and Asteraceae have been used in anticancer studies due to their phytochemical content. The genus Sideritis, Achillea and Tanacetumare the members of these families. Sideritis, Achillea and Tanacetum are used as herbal medication for the treatment ofvariety of diseases. In present study, we demonstrated the biological activity of Sideritis syriaca (SS), Achillea aleppica (AAZ) and Tanacetum argenteum (TAA) methanol extracts on cell viability of the breast cancer line MCF7. MTT (3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was used to determine the cell viability and proliferation of MCF7 cells. In a dose dependent manner, methanol extracts (0, 1, 5, 25, 100 and 250 μg/ml) of SS, AZZ and TAA were examined on MCF7, and viability of cells were determined with MTT staining. Especially, concentrations in 100 and 250 μg/ml of extracts decreased the cell viability (p<0.001). The results of the current study showed that methanol extracts of SS, AZZ and TAA effectively inhibited the cell proliferation by decreasing the cell viability of MCF7 cells. Suggesting that SS, AZZ and TAA can be considered as natural herbal-based anti-cancerous agents.

Produção de biomassa e do rendimento do óleo essencial de melissa em cultivo solteiro e consorciado com mil-folhas e alface / Biomass production and essential melissa oil output evaluation in a single and linked crop cultivation to both yarrow and lettuce

O trabalho teve como objetivo avaliar a produção da biomassa e o rendimento de óleo essencial da melissa, quando em cultivo solteiro e consorciada com mil-folhas e alface. Os tratamentos consistiram em melissa em cultivo solteiro, melissa em consórcio com mil-folhas, melissa consorciada com alface, mil-folhas e alface em cultivo solteiro. O delineamento experimental utilizado foi o inteiramente casualizado com cinco tratamentos e seis repetições. Foram avaliados o teor e o rendimento do óleo essencial da melissa e a matéria fresca e a matéria seca da parte aérea de todas as espécies. Notou-se, a partir dos valores das médias, que o cultivo consorciado de melissa com alface proporcionou maior rendimento de óleo essencial, matéria fresca e matéria seca. Os menores valores de todas as variáveis foram observados no cultivo solteiro da melissa. Considerando o Uso Eficiente da Terra (UET), o cultivo consorciado da mil-folhas e da alface com a melissa gerou bons rendimentos de biomassa das plantas, pois os valores calculados para as espécies foram superiores a 1,0. O cultivo consorciado das espécies não interferiu significativamente no teor do óleo essencial da melissa.

The research aimed to evaluate melissa's biomass production and its essential oil output, both single cultivation and linked cultivation to yarrow and lettuce. The treatments were consisted in single cultivantion melissa, melissa linked to yarrow, melissa linked to lettuce, yarrow and lettuce in single cultivation. The experimental design used was a totally randomized design with five treatment and six repetitions. Was evaluated the content and the yield of essential oil of melissa, the fresh matter and the dry matter of the aerial part of all species. It was seen from the average valuations that the melissa linked cultivation to the lettuce obtained the greatest output, fresh matter and dry matter. The smaller values of all variables was observed in melissa in single cultivation. To the the Effective Land Use (ELU), the yarrow and lettuce linking cultivated to the melissa generated good species biomass output, because the calculated results to the plants were higher than 1,0. The species linking cultivation did not interfere significantly in melissa's essential oil content.

Biological Activities of the Hydro-alcoholic and Aqueous Extracts of Achillea falcata L. (Asteraceae) Grown in Jordan.

Aim: This study aimed to screen the aqueous and hydro-alcoholic extracts of Achillea falcata L. (Asteraceae) grown in Jordan for their antioxidant, antibacterial, antiplatelet and anti-proliferative efficacy. Study Design: HPLC-MS evaluation of the aqueous and hydro-alcoholic extracts and in vitro investigations. Place and Duration of Study: Faculties of Pharmacy and Science, The University of Jordan and Centre of Misanalysis, National Institute for Biological Sciences, between August 2012 and June 2013. Methodology: Total phenols and flavonoids were determined colorimetrically. The radical scavenging activities were evaluated using 2,2′-azino-bis-3-ethylbenzthiazoline-6- sulphonic acid (ABTS) radical scavenging activity assay. Antimicrobial activities were determined by the disc-diffusion method, and the minimum inhibition concentration and the minimum bactericidal concentration tests. In vitro antiplatelet activity was tested on human whole blood using an electrical impedance method. Anti-proliferative activity was investigated using the MTT assay. High performance liquid chromatography-mass spectrometry (HPLC-MS) evaluation was performed. Results: Hydro-alcoholic extract had a bactericidal activity against Streptococcus pneumoniae, Bacillus cereus and Klebsiella pneumoniae rather than inhibitory effect. No significant activity was observed against gram negative bacteria and Candida albicans. In vitro antiplatelet activity was tested on human whole blood using an electrical impedance method. At concentrations (50, 100, and 200 μg/ml), hydro-alcoholic extract did not show effect on platelet aggregation. Extracts did not possess cytotoxic activity against the MCF- 7 cells at concentrations up to 200 μg/ml. HPLC-MS analysis resulted in the identification of 8 phenolic compounds in the hydro-alcoholic extract and 6 compounds in the aqueous extract; quercetin 3-β-D-glucoside was the main component for both extracts. Conclusion: The present investigation supported the traditional use A. falcata in the Jordanian folk medicine as a depurative agent and as an antimicrobial active representative of the genus Achillea.

НИЙЛМЭЛ НАЙРЛАГА БҮХИЙ УРГАМЛЫН ГАРАЛТАЙ БЭЛДМЭЛИЙН ЭЛЭГНИЙ ӨВЧЛӨЛД НӨЛӨӨЛӨХ ҮЙЛДЛИЙН СУДАЛГАА / Монголын эм зүй, эм судлал

Introduction: Achillea asiatiсa has been used in traditional medicine for one hundreds of years. Many compounds have been isolated from /Achillea asiatica/, including flavonoids, sesquiterpenes and essential oils. Salsola collina herb grows in Siberia, Baikal and Altai. It contains a variety of amino acids, flavonoids, glycosides, and vitamins. It has a positive effect on metabolism of fats in liver, regulates cholesterol and sugar in the blood and is recommended for weight reduction. Salsola collina is widely distributed in droughty and semi-droughty area, which is used as a kind of folk remedy in traditional Chinese and Mpngolian traditional medicine for treatment of hypertension and liver protectevity . Goal: The aim of study is to choose optimal extragent and determination liver protecting activity in Achillea asiatiсa, Salsola colina and to determine main substances in these herbals. Material and Methods: Achillea asiatiсa was collected from Dorgonot mountain Tuv province in June of 2012, Salsola colina were collected from Medicinal botanical garden of Drug Research Institute in August of 2012. Maceration was chosen by suitable extraction method and optimal extragent was ethanol. Flavonoids were determined in evaporated extract of Achillea asiatiсa, Salsola colina using the method by Mongolian National first Pharmacopeia. We use non line wistar rats, determination liver protecting activity biochemical analysis by Hospitex analyzer. Result: Liquid extracts were obtained from Achillea asiatiсa, Salsola colina with maceration method. Liquid extracts were evaporated on Vacuum rotor. The tehnological parameters of liquid extracts are the main important index to calculate the extragent correctly, to establish the material balance exactly, and to extract the process efficiently. 70% ethanol (1:10 sample/extragent) was determined by optimal extragent for Achillea asiatiсa, 80% ethanol (1:10) for Salsola colina. Achillea asiatiсa, Salsola colina were have liver protecting activity. Conclusion: Some technological parameters of liquid extract were determined such as optimal extragent and the effective extracting method of Achillea asiatiсa, Salsola colina. As the result of determining these parameters, it has much practical significant for establishing the technological condition to extract the biological activity compounds completely from their plants. Key words: Achillea asiatiсa, Salsola collina, technological pharameters, flavonoid, anthraquinons, liver protecting activity

Chemical constituents from Achillea alpina / 中草药

Objective: To investigate the chemical constituents from the aerial parts of Achillea alpina. Methods: The compounds were isolated and purified by various chromatographic techniques and their structures were characterized on the basis of physicochemical properties and their spectral analyses. Results: Eleven compounds were isolated. Their structures were identified as epifriedelanol (1), spinasterol (2), β-sitosterol (3), 5, 6-epoxy-24(R)-methylcholesta-7, 22-dien-3β-ol (4), β-daucosterol (5), schensianol A (6), negunfurol (7), (3S, 5S, 8R)-3, 5-dihydroxymegastigma-6, 7-dien-9-one (8), saropeptate (9), (+)-syringaresinol (10), and (±)-lariciresinol (11). Conclusion: All the compounds are isolated from the aerial parts of A. alpina for the first time, and compounds 1, 2, 4, 6-11 are reported to obtain from the plants in Achillea L. for the first time.

Radiolabeling of methanol extracts of yarrow (Achillea millefolium l) in rats / Radiomarcação do extrato metanólico de yarrow (Achillea millefolium l) em ratos

PURPOSE: Current study is focused on extraction with methanol, purification, labeling with 131I using iodogen method of the yarrow plant and investigating in vivo biological activity using biodistribution and imaging studies on healthy animal models. The aim of the study is to contribute plant extracts to discover new drugs in the diagnosis and treatment of several diseases. METHODS: Nine female and nine male healthy Wistar albino rats, which were approximately 100-150 g in weight, were used for biodistribution studies. For imaging studies four healthy male Balb-C mice were used. Quality control studies were done utilizing thin layer radio chromatography (TLRC) and high performance liquid chromatography (HPLC) methods. For biodistribution studies, 131I radiolabeled Peak 7 (131I-Peak 7) was sterilized and injected into the tail veil of rats and imaging studies were obtained using Kodak FX PRO in vivo Imaging System. RESULTS: The radiolabeling yield of each purified the bioactive extracts of the yarrow plant, seven peaks was between 79 and 92%. The highest radiolabeling yield was calculated for 131I radiolabeled seventh peak (131I-Peak 7) (92.78±5.04, n=5). For this reason the biodistribution and imaging studies were done for 131I-Peak 7. That's why; these studies with Peak 7 were carried out. CONCLUSION: Peak 7 was radiolabeled with 131I in high yield for using imaging and therapeutic studies in nuclear medical applications.

OBJETIVO: O atual estudo tem por objetivo a extração com metanol, purificação, marcação com I131 usando o método direto de marcação da planta Achillea, para investigar in vivo a atividade biológica usando biodistribuição e estudos de imagem em modelos animais saudáveis. O objetivo do estudo é contribuir com extratos de plantas para descobrir novas drogas para o diagnóstico e tratamento de várias doenças. MÉTODOS: Nove fêmeas e nove machos ratos Wistar albino saudáveis, com aproximadamente 100 a 150g de peso foram usados para estudos de biodistribuição. Para estudos de imagem, quatro camundongos Balb-C machos e saudáveis foram usados. Estudos de controle de qualidade foram realizados usando métodos de cromatografia de camada fina e cromatografia líquida de alta performance. Para estudos de biodistribuição, pico 5 radiografado com I131 (I131-Peak 7) foi esterilizado e injetado na veia da cauda dos ratos e estudos de imagem foram obtidos usando Sistema de Imagem Kodak FX PRO in vivo. RESULTADOS: O retorno radiomarcado de cada extrato bioativo purificado da planta Achillea sete picos estavam entre 79 e 92%. O retorno com maior marcação foi calculado para I131 sétimo pico (I131-Peak 7) (92,78±5,04, n=5). Por esta razão os estudos de biodistribuição e de imagem foram feitos para I131-Peak 7. CONCLUSÃO: Peak 7 foi radiomarcado com I131 em alto retorno para uso em estudos terapêuticos e de imagens nas aplicações médicas nucleares.

Cytotoxic and genotoxic activity of Achillea millefolium L., Asteraceae, aqueous extracts

The yarrow, Achillea millefoilum L. is an important species of Asteraceae family with common utilization in folk medicine of many countries. The aim of this study was to investigate the cytotoxic and genotoxic effects of aqueous extracts from yarrow leaves on Lactuca sativa (lettuce) root tip meristem cells by cytogenetic studies, since studies of this nature do not exist for the yarrow extracts. For this, lettuce seeds were treated for 72 h with different concentrations of yarrow aqueous extracts (5, 10, 20 and 30 mg/mL). The percentage of germination, root development and cellular behavior were analyzed and the results showed that the highest concentration of aqueous extracts reduced the mitotic index (MI), the seed germination and the root development of L. sativa. More yet, the extracts also induced chromosome aberrations (CA) and cellular death in the roots cells of L. sativa indicating precaution in the therapeutic use of A. millefolium and reinforcing the utilization of L. sativa in the screening of cytogenotoxic substances once that this species showed a good sensibility to the extract application.

Determinação da atividade antifúngica dos óleos essenciais de curcuma longa l. (zingiberaceae) e de achillea millefolium (asteraceae) cultivadas no noroeste do Paraná / Determination of antifungal activity of essential oils of curcuma longa l. (zingiberaceae) and achillea millefolium (asteraceae) grown in the northwest paraná

No presente estudo, utilizou-se o óleo essencial das plantas Curcuma longa L. e Achillea millefolium, cultivadas no Horto Medicinal da Universidade Paranaense, localizado na cidade de Umuarama-PR região Noroeste do Paraná-Brasil. Para isso, os óleos foram obtidos pelo processo de extração por Clevenger modificado, e determinada a ação antimicrobiana frente a 20 cepas de microorganismos isolados de material clínico humano, sendo 16 leveduras da espécie Candida albicans isoladas da cavidade oral de pacientes portadores do Vírus da Imunodeficiência Adquirida (HIV), 3 leveduras isoladas de candidíase vulvovaginal (C. albicans, C. glabrata e C. tropicalis) e uma amostra de S. aureus isolado de lesões cutâneas. Por intermédio dos testes de microdiluição em caldo, os óleos de Achillea millefolium e de Curcuma longa demonstraram ação antimicrobiana considerada moderada (0,625 mg mL-1) em 63,2% e 68,4% das leveduras testadas, respectivamente. Ambos os óleos não apresentaram atividade frente ao S. aureus. Desta forma, sugere-se estudos adicionais para uso na incorporação dos óleos em formas farmacêuticas, com vistas ao uso no tratamento tópico de Candidíase mucocutânea.

It was used in this research the essential oil of the plants Curcuma longa and Achillea millefolium cultivated on the Medicinal garden of Universidade Paranense located on the city of Umuarama-PR. The oils were obtained by the process of steam distillation and was determined the microbial activity against 20 microorganisms isolated from clinical human material, being 16 yeasts of Candida albicans species isolated from the oral cavity from patients infected with Human Immunodeficiency Virus (HIV), 3 yeasts isolated from vulvovaginal candidiasis (C. albicans, C. glabrata and C. tropicalis) and one sample of S. aureus isolated from skin injuries. Through broth microdilution tests, the oils of Achillea millefolium and Curcuma longa showed moderated action (0,625 mg mL-1) on 63,2% e 68,4% of tested yeasts, respectively. Both Oils didn?t show activity against S. aureus. Therefore it is suggested further studies for use in the incorporation of oils in dosage forms with a view to use in the topical treatment of mucocutaneous candidiasis.

Comparação da atividade antimicrobiana entre os sabonetes contendo digluconato de clorexidine, triclosan e óleo essencial de achillea milefollium L (asteraceae) / Comparision of the antimicrobial activity of soap containing clorhexidine digluconate, triclosan, and the essential oil of the achillea millefolium achillea millefolium L (asteraceae)

Amostras de sabonete contendo, como agentes antissépticos, triclosan, na concentração de 1,0%; digluconato de clorexidine a 2,0%; óleo essencial de Achillea millefolium nas concentrações de 1,0% e 2,0%, foram avaliadas quanto à atividade antimicrobiana frente aos microorganismos S. aureaus, E. coli, P. aeruginosa e C. albicans pela técnica de Pour Plate. Os resultados demonstraram um poder inibitório total do triclosan frente aos microorganismos testados e observou-se poder inibitório superior do óleo essencial de achillea millefolium na concentração de 2,0% em relação ao sabonete de digluconato de clorexidine, muito utilizado em ambientes hospitalares.

Soap samples containing antiseptics agents such as 1%-triclosan, 2%-clorexidine digluconato, and 1-2% essential oil of Achillea millefolium was assessed according to its antimicrobial activity against Sthaphylococus aureus, E. coli, P. aeruginosa, and C.albicans by the Pour Plate technique. The results demonstrated a total inhibition of the triclosan to the tested microorganisms and a superiorinhibition of the essential oil of Achillea millefolium was observed at the concentration of 2% in relation to the clorhexidine digluconate soap, very used in hospital atmospheres.

Anatomy of root, stem and leaf and identification of secretory structures of Achillea millefolium L. (Asteraceae)- DOI: 10.4025/actascibiolsci.163 / Anatomia de raiz, caule e folha e identificação de estruturas secretoras de Achillea millefolium L. (Asteraceae) - DOI: 10.4025/actascibiolsci.163

An anatomic study of the vegetative organs: root, stem and leaf was made. The essential oils were extracted from the plant identifying the possible secretory structures. Fresh material was used in order to perform histochemical tests and to prepare semi-permanent slides, which were colored with Safrabau. For the preparation of the semi-permanent slides, material fixed in FAA 50% was used including historesina. Tector hairs can be observed in the scape and flower. Secretory channels of schizogeneous origin follow the vascular bundles in the rhizome, scape, leaf and bract of the flower. In the root, these channels are absent. In the leaf and in the unopened inflorescence there is a greater quantity of the essential oils. The leaf is amphistomatic and the stomata of anomocytic type are present in the scape as well. The general structure of the Achillea millefolium is similar to the structures of the other species of Asteraceae family.

Realizou-se o estudo anatômico dos órgãos vegetativos raiz, caule e folha, e extraíram-se os óleos essenciais das diferentes partes da planta, identificando-se as possíveis estruturas secretoras desses óleos. Utilizou-se material fresco para a realização dos testes histoquímicos e para a confecção de lâminas semipermanentes, as quais se coraram com Safrablau. Para a confecção de lâminas permanentes, utilizou-se material fixado em FAA 50%, incluído em historesina. Observaram-se pêlos tectores no escapo e na folha, enquanto que pêlos glandulares foram encontrados no escapo e na flor. Canais secretores de origem esquizógena acompanham os feixes vasculares no rizoma, no escapo, na folha e na bráctea da flor. Na raiz, esses canais estão ausentes. Na folha e na inflorescência fechada, observouse maior quantidade de óleos essenciais. A folha é anfistomática e os estômatos, do tipo anomocítico, estão presentes também no escapo. A estrutura geral de Achillea millefolium é semelhante à de outras espécies da família Asteraceae.