Chemical constituents from Xanthii Fructus / 中国中药杂志

This study was carried out to investigate the chemical constituents from Xanthii Fructus(the fruits of Xanthium sibiricum). The compounds were separated and purified by silica gel column chromatography, Sephadex LH-20 and ODS chromatography and semi-preparative HPLC. Base on HR-ESI-MS, NMR and other spectral data, their structures were identified. The anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide(LPS)-induced macrophage RAW264.7 as a screening model. A total of twenty-one compounds were isolated from the EtOAc fraction of 95% ethanol extract and identified as uracil(1), thymine(2), uridine(3), indole-3-carbaldehyde(4), indole-3-carboxylic acid(5), 2'-O-methyluridine(6), guanosine(7), 2,4(1H,3H)-quinazolinedione(8), 3-hydroxy-3-(2-hydroxyethyl)indolin-2-one(9), nicotinamide(10), N-acetyl-L-phenylalaninol(11), heliolactam(12), terresoxazine(13), caudatin(14), qingyangshengenin(15), caudatin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(16), caudatin-3-O-β-D-cymaropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(17), caudatin-3-O-α-L-cymaropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-α-L-cymaropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranoside(18), qinyangshengenin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranoside(19), qinyangshengenin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-digitoxopyranoside(20), rostratamine-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(21). Compounds 5-21 are obtained from genus Xanthium for the first time. Compounds 12 and 13 indirectly exhibited anti-inflammatory activity by suppressing LPS-induced NO production in RAW264.7 cells with IC_(50) values of(15.45±0.56) and(20.14±0.78) μmol·L~(-1), respectively.

Discussion on safety of Xanthii Fructus and consideration on its rational use / 中国中药杂志

Xanthii Fructus is a traditional Chinese medicine for the treatment of sinusitis and headache,rich in medicinal materials and is widely used for more than 1 800 years. Modern pharmacological studies have showed that Xanthii Fructus has anti-inflammatory,analgesic,anti-tumor,anti-bacterial,hypoglycemic,anti-allergic,immunomodulatory and other pharmacological effects,which can be commonly used in the treatment of diseases relating to immune abnormalities,such as rheumatoid arthritis,acute and chronic rhinitis,allergic rhinitis,and skin diseases,with a high medicinal value. Toxicological studies have shown that Xanthii Fructus poisoning can cause substantial damage to organs,such as the liver,kidney,and gastrointestinal tract,especially to liver. Because of the coexisting of its efficacy and toxicity,Xanthii Fructus often leads to a series of safety problems in the clinical application process. This study attempts to summarize its characteristics of adverse reactions,analyze the root cause of the toxicity of Xanthii Fructus from such aspects as processing,dose,course of treatment and eating by mistake,discuss the substance of its efficacy/toxicity from chemical compositions,and put forward exploratory thinking about how to promote its clinical rational application from the aspects such as strict processing,reasonable compatibility,medication information,contraindication,strict control of the dose,and course of treatment,so as to promote the safe and reasonable application of Xanthii Fructus.

Evaluación del efecto antiinflamatorio y analgésico de la asociación de los extractos de Xanthium spinosum L. y Urtica urens L. en modelo murino / Evaluation of the anti-inflammatory and analgesic effect of the association of extracts of Xanthium spinosum L. and Urtica urens L. in the murine model

La elevada incidencia de los efectos adversos provocados por el uso crónico de antiinflamatorios, ha dirigido la búsqueda de terapias alternativas o coadyuvantes basadas en la utilización de plantas medicinales. En Bolivia las especies vegetales Xanthium spinosum L. y Urtica urens L. son empleadas tradicionalmente en procesos inflamatorios. En este trabajo se investiga el efecto antiinflamatorio y analgésico de diferentes tipos de extractos: extracto acuoso, etanólico, diclorometanico, etéreo de las especies vegetales Xanthium spinosum L. y Urtica urens L. y la asociación de los extractos acuosos y etanólicos de las mismas especies vegetales, en modelos murino. Los mayores efectos de inhibición de la inflamación a una dosis de 1,5 g/kg de peso corporal se registraron a las siete horas del proceso inflamatorio para los extractos acuoso (64,8%) y etanólico (68,7%) de X. spinosum L.; el porcentaje de inhibición para el extracto acuoso y etanólico de U. urens L. fue de 57% y 51,5% respectivamente. La inhibición de la algesia fue observada en los extractos diclorometánico y etanólico de ambas especies, llegando a un máximo de inhibición de 72,8% con el extracto etanólico de U. urens L. La evaluación de la asociación de extractos acuosos de ambas especies, a una dosis de 0,75 g/kg de peso corporal de cada extracto, mostro un efecto antiinflamatorio con un porcentaje de inhibición de la inflamación de 68,95% y un porcentaje de inhibición de la algesia de 54,8%; en tanto que la asociación de los extractos etanólicos de estas especies mostró sólo efecto antiinflamatorio.

The high incidence of adverse effects caused by the chronic use of anti-inflammatory drugs has led to the search for alternative therapies or coadjuvants based on the use of medicinal plants. In Bolivia, the plant species Xanthium spinosum L. and Urtica urens L. are traditionally used in inflammatory processes. In this work the antiinflammatory and analgesic effect of different types of extracts is investigated: aqueous, ethanolic, dichloromethane, ethereal extract of the plant species Xanthium spinosum L. and Urtica urens L. and the association of aqueous and ethanolic extracts of the same plant species, in murine models. The highest effects of inhibition of inflammation at a dose of 1.5 g/kg of body weight were recorded seven hours after the inflammatory process for the aqueous (64.8%) and ethanolic (68.7%) extracts of X. spinosum L .; the percentage of inhibition for the aqueous and ethanolic extract of U. urens L. was 57% and 51.5% respectively. The inhibition of algesia was observed in the dichloromethane and ethanolic extracts of both species, reaching a maximum of 72.8% inhibition with the ethanolic extract of U. urens L. The evaluation of the association of aqueous extracts of both species, at a dose of 0.75 g/kg of body weight of each extract, showed an anti-inflammatory effect with a percentage of inhibition of inflammation of 68.95% and a percentage of inhibition of algesia of 54.8%; whereas the association of the ethanolic extracts of these species showed only anti-inflammatory effect.

A new dimeric xanthanolide from fruits of Xanthium chinense / 中国中药杂志

Through the methods of polyamide resin， Sephadex LH-20， ODS column chromatography and preparative HPLC etc.， 7 compounds were isolated from the 70% ethanol extract of the fruits of Xanthium chinense. Based on ESI-MS and NMR data， the structures of these compounds were identified as pungiolide O(1)， grasshopper ketone(2)， icariside F₂(3)， 7-[(β-D-apiofuranosyl-(1→6)-β-D-glucopyranosyl)oxymethy]-8，8-dimethyl-4，8-dihydrobenzo[1，4]thiazine-3，5-dione(4)，(6R，9S)-3-oxo-α-ionol β-D-glucopyranoside(5)， cryptochlorogenic acid methyl ester(6)， and chlorogenic acid methyl ester(7). Among them， compound 1 is a new compound.

Isolation and identification of phyllospheric bacteria possessing antimicrobial activity from Astragalus obtusifolius, Prosopis juliflora, Xanthium strumarium and Hippocrepis unisiliqousa

Background: The widespread utilization of antimicrobial compounds has caused emergence of resistant microorganisms in the world. Hence, the research to probe the products with antimicrobial features has led to finding natural habitats and discovering new pharmaceutical products

Methods: In this study, an attempt was made to explore the niche of novel habitat to isolate pyllospheric bacteria from the above ground parts [stems and leaves] of Astragalus obtusifolius, Prosopis juliflora, Xanthium strumarium, and Hippocrepis unisiliqousa to evaluate their antimicrobial features. The inhibitory effects of these strains on the growth of two fungi [Aspergillus niger, Aspergillus fumigatus], two yeasts [Saccharomyces cerevisiae, Candida albicans] and six bacteria [Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Salmonella typhi, Streptococcus pyogenes] were tested

Results: In total, 113 bacterial strains were isolated. Twenty five bacterial strains [B-1 to B-25] indicated promising antimicrobial [antibacterial and antifungal] activities against aforementioned pathogens. The identification of the bacterial strains was ascertained by morphological, physiological, biochemical tests and two strains with the strongest antimicrobial activities were further characterized based on 16s rRNA sequencing. These two strains were identified as Bacillus amyloliquefaciens

Conclusion: Our results provide evidence that phyllospheric microorganisms are capable of producing some compounds with antimicrobial properties

Toxicidad aguda de las hojas de Xanthium spinosum en ratones BALB/C / Acute toxicity of Xanthium spinosum leaves in BALB/C mice

Las hojas de la planta Xanthium spinosum se utilizan culturalmente en Paraguay por sus propiedades medicinales. Se evaluó la toxicidad aguda del extracto de hojas maduras; para el estudio se seleccionaron 35 ratones BALB/C machos que fueron distribuidos en 7 grupos, 6 de ensayo y 1 de control. El extracto fue preparado en concentraciones de 6 y 9% (g/dL); se administró la solución 6% a tres grupos y la solución 9% a los otros tres grupos, con dosis entre 200 y 1000 mg/kg. Al final de 14 días de observación, se extrajeron muestras de sangre para estudios laboratoriales de urea y transaminasas, además de órganos para estudios anatomopatológicos. Se determinaron aumentos en los niveles de GOT y urea en comparación al grupo control. Se concluye que el consumo del extracto de hojas maduras de Xanthium spinosum puede causar daño hepático...

The leaves of the Xanthium spinosum plant have been used culturally in Paraguay for their medicinal properties. Acute toxicity of mature leaf extract was evaluated. For the study, 35 Balb/c mice were selected and allocated into 7 groups, 6 test groups and 1 control group. The extract was prepared in concentrations of 6% and 9% (g/dL). The 6% concentration was administrated to 3 test groups and 9% concentration to the remaining 3 groups, with doses between 200 and 1000 mg/kg per mouse. After 14 days of observation, blood samples were taken for laboratory studies of urea and transaminases and organs were examined for pathological studies. There were increased levels of GOT and urea in the test groups compared to the control group. In conclusion, the consumption of mature leaf extract of Xanthium spinosum can cause hepatic damage...

Herbal textural research on species of Xanthii Fructus / 中国中药杂志

Xanthii Fructus is a traditional medicine for the treatment of nasal diseases in clinic, mainly come from the burs of Xanthium sibiricum with a worldwide distribution. By sorting and studying literature of Chinese medicine and comparing different figures recorded with the morphological description of several species from Xanthium (Asteraceae) in the Flora of China, combining the biological investigation in resource survey, the article pointed out that the burs or the whole herbs of X. mongolicum, as well as X. sibiricum, has been used by the traditional Chinese medicine in ancient time. It provides a reference for further studies in the future.

Screening of selected medicinal plants for their enzyme inhibitory potential - a validation of their ethnopharmacological uses

In present study four medicinal plants namely Valeriana wallichii, Xanthium strumarium, Achyranthes aspera and Duchesnea indica belonging to different families were collected in Khyber Pakhtunkhwa province and crude extract and subsequent fractions were analyzed for their inhibitory potential against acetylcholinesterase, butyrylcholinesterase and alpha-glucosidase enzymes. Valeriana wallichii, Xanthium strumarium and Achyranthes aspera were significantly active against cholinesterases. Chloroform and ethylacetate fractions of Valeriana wallichii exhibited significant activity against acetylcholinesterase [IC50: 61microg/ml] and butyrylcholinesterase enzymes [IC50: 58microg/ml], respectively. Similarly ethylacetate fraction of Achyranthes aspera showed significant activity against acetylcholinesterase [IC50: 61 microg/ml] and butyrylcholinesterase enzymes [IC50: 61 microg/ml], respectively. In case of alpha-glucosidase enzyme, the chloroform fraction of Xanthium strumarium exhibited significant inhibitory activity [IC50: 72 microg/ml] as compared to the standard compound acarbose [IC50: 483 microg/ml]. Duchesnea indica showed no such activities.

Effects of extraction methods of phenolic compounds from Xanthium strumarium L. and their antioxidant activity / Efeito de métodos de extração de compostos fenólicos de Xanthium strumarium L. e suas atividades antioxidantes

Foram avaliados os efeitos de métodos de extração e de solventes sobre o rendimento de extrato, conteúdo de fenólicos totais, atividade antioxidante, e composição dos compostos fenólicos de Xanthium strumarium L. A atividade antioxidante foi determinada pelo método do radical 2,2-difenil-1-picrilhidrazila (DPPH), e a composição dos compostos fenólicos foi determinada por cromatografia líquida de alta eficiência e por espectrometria de massas com ionização por electrospray. Todos os resultados foram afetados pelo método de extração e, principalmente pelo solvente utilizado, sendo que os melhores resultados foram obtidos com o solvente metanol. Os extratos metanólico e etanólico apresentaram forte ação antioxidante e os principais compostos fenólicos encontrados nos extratos foram os ácidos ferúlico e clorogênico.

The effect of extraction methods and solvents on overall yield, total phenolic content, antioxidant activity, and the composition of the phenolic compounds in Xanthium strumarium extracts were studied. The antioxidant activity was determined by using 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), and the composition of the phenolic compounds was determined by HPLC-DAD and LC/MS. All results were affected by the extraction method, especially by the solvent used, and the best results were obtained with the methanol extract. The methanolic and ethanolic extracts exhibited strong antioxidant activity, and the chlorogenic and ferulic acids were the most abundant phenolic compounds in the extracts.

Optimization of processing technology for xanthii fructus by UPLC fingerprint technique and contents of toxicity ingredient / 中国中药杂志

The experiment's aim was to optimize the processing technology of Xanthii Fructus which through comparing the difference of UPLC fingerprint and contents of toxicity ingredient in water extract of 16 batches of processed sample. The determination condition of UPLC chromatographic and contents of toxicity ingredient were as follows. UPLC chromatographic: ACQUITY BEH C18 column (2.1 mm x 100 mm, 1.7 microm) eluted with the mobile phases of acetonitrile and 0.1% phosphoric acidwater in gradient mode, the flow rate was 0.25 mL x min(-1) and the detection wavelength was set at 327 nm. Contents of toxicity ingredient: Agilent TC-C18 column (4.6 mm x 250 mm, 5 microm), mobile phase was methanol-0.01 mol x L(-1) sodium dihydrogen phosphate (35: 65), flow rate was 1.0 mL x min(-1), and detection wavelength was 203 nm. The chromatographic fingerprints 16 batches of samples were analyzed in using the similarity evaluation system of chromatographic, fingerprint of traditional Chinese medicine, SPSS16.0 and SIMCA13.0 software, respectively. The similarity degrees of the 16 batches samples were more than 0.97, all the samples were classified into four categories, and the PCA showed that the peak area of chlorogenic acid, 3,5-dicaffeoylquinic acid and caffeic acid were significantly effect index in fingerprint of processed Xanthii Fructus sample. The outcome of determination showed that the toxicity ingredient contents of all samples reduced significantly after processing. This method can be used in optimizing the processing technology of Xanthii Fructus.

Control de calidad y evaluación del efecto inflamatorio de los extractos de Xanthium spinosum L. y Urtica urens L. en modelo murino / Quality control and evaluation of the inflammatory effect of extracts of Xanthium spinosum L. and Urtica urens L. in murine model

La tesis se enmarca dentro de la problemática de la elevada incidencia de los efectos adversos provocados por el uso crónico de antiinflamatorios y la posibilidad de contar con una terapia alternativa o coadyuvante para el tratamiento de cuadros inflamatorios basada en la utilización de plantas medicinales empleadas tradicionalmente en Bolivia. En este sentido, la investigación se realizó con las especies vegetales Xanthium spinosum L. y Urtica urens L. procedentes de la Provincia Ingavi del Departamento de La Paz. El objetivo principal de esta investigación fue el de profundizar en el conocimiento del efecto antiinflamatorio de los extractos de Xanthium spinosum L. y Urtica urens L. a través de la evaluación de procesos inflamatorios inducidos, en modelo murino. Para alcanzar este objetivo, se desarrolló un plan de trabajo que se dividió en cuatro partes fundamentales: la autentificación de ambas especies vegetales estudiadas, el estudio de sus parámetros de calidad, el estudio fitoquímico cualitativo y el estudio farmacológico in vivo, de los diferentes extractos obtenidos. La autentificación fue realizada sobre muestras representativas de las plantas recolectadas, en el Herbario Nacional de Bolivia, identificándose posteriormente como X. spinosum L. y U. urens L. El grado de su calidad fue determinado empleando las directrices propuestas por la Real Farmacopea Española y por comparación con muestras auténticas, lo que reveló la presencia de tricomas en X. spinosum L. y pelos urticantes unicelulares y pluricelulares en U. urens L. y valores de humedad, cenizas totales, cenizas ácidas, cenizas solubles, elementos extraños, índice de hinchamiento, dentro de los límites aceptables de calidad. Por otro lado, el protocolo desarrollado para la obtención de extractos por el método de polaridad creciente permitió la obtención de extractos etéreo, diclorometánico, etanólico y acuoso, los que mediante un screening fitoquímico cualitativo reveló la presencia mayoritaria de esteroles y flavonoides en X. spinosum L. y taninos, alcaloides, compuestos reductores, esteroles, flavonoides y cumarinas en U. urens L. Adicionalmente, el perfil cromatográfico de los distintos extractos reveló la presencia de diferentes manchas en fases móviles asociadas principalmente con flavonoides. El estudio del efecto antiinflamatorio de los extractos se realizó en ratones albinos Swiss, siguiendo el protocolo de edema plantar inducido por carragenina y el estudio del efecto analgésico siguiendo el protocolo de inducción de contorciones abdominales por ácido acético. Los mayores valores de inhibición de la inflamación fue registrado para los extractos acuoso y etanólico de X. spinosum L. y de U. urens L., en tanto que la inhibición de la algesia fue más importante cuando se empleó extractos diclorometánico y etanólico de ambas especies vegetales. Finalmente, la combinación de extractos acuosos de ambas especies estudiadas mostró un efecto sinérgico antiinflamatorio y analgésico, en tanto que la combinación de los extractos etanólicos de estas especies vegetales mostró sólo un efecto antiinflamatorio, no así analgésico. (AU)

In vitro effect of Acanthospermum australe (Asteraceae) extracts on Acanthamoeba polyphaga trophozoites / Efeito in vitro de extratos de Acanthospermum australe (Asteraceae) sobre trofozoitos de Acanthamoeba polyphaga

Acanthamoeba is a free-living protozoan widely distributed in the environment, occurring in vegetative trophozoite and resistance cyst stages during its life cycle. It constitutes an etiological agent of Acanthamoeba keratitis, a disease that may cause severe ocular inflammation and blindness. New drugs can be developed from molecules found in plants and thus help in its difficult treatment. Acanthospermum australe (Asteraceae), a plant used in folk medicine, had its effect tested on Acanthamoeba polyphaga. Aqueous and ethanolic extracts of A. austral were obtained from aerial parts for infusion and static maceration, respectively. Concentrations of 10, 5, 2.5, 1.25 and 0.625 mg/ml of the extract were tested against Acanthamoeba polyphaga trophozoites. The cytotoxic effect of the extracts was tested in mammalian cells using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. RESULTS: The 10 mg/ml concentration of ethanolic extract was lethal to 100% of the A. polyphaga trophozoites in 24 h and both extracts presented cytotoxic effect against mammalian cells. These findings suggest that the A. austral ethanolic extract may have compounds with relevance to the development of new amoebicidal drugs.

Acanthamoeba é um protozoário de vida livre amplamente distribuído no ambiente, ocorrendo sob a forma trofozoítica (metabolicamente ativa) e cística (de resistência), durante seu ciclo de vida. O protozoário constitui um agente etiológico da Ceratite Amebiana, uma doença que pode causar inflamação ocular severa e cegueira. Novos fármacos podem ser desenvolvidos a partir de moléculas encontradas em plantas e assim ajudar em seu difícil tratamento. Aqui, Acanthospermum australe (Asteraceae), uma planta utilizada na medicina popular, teve seu efeito sobre trofozoítos de Acanthamoeba polyphaga testado. O extrato aquoso e etanólico de A. australe foram obtidos das partes aéreas por infusão e maceração estática, respectivamente. As concentrações 10, 5, 2,5, 1,25 e 0,625 mg/ml dos extratos foram testadas contra trofozoítos do protozoário. O efeito citotóxico dos extratos foi testado em células de mamífero utilizando o ensaio de brometo de 3-[4,5-dimetiltiazol-2-il]-2,5-difeniltetrazólio (MTT). A concentração de 10 mg/ml do extrato etanólico foi letal a 100% dos trofozoítos de A. polyphaga em 24 h e ambos os extratos apresentaram efeito citotóxico contra as células de mamífero. Estes resultados sugerem que o extrato etanólico de A. australe pode ter componentes com relevância para o desenvolvimento de novos fármacos amebicidas.

UPLC fingerprint of xanthii fructus from different habitats / 中国中药杂志

This study was establish an UPLC fingerprint of Xanthii Fructus from different habitats, to provide a comprehensive evaluation for its quality control. UPLC-PDA was adopted to analysis of 26 baches of Xanthii Fructus from different habitats. The chromatographic condition was as follow: ACQUITY BEH C18 Column (2.1 mm x 100 mm,1.7 microm) eluted with the mobile phases of acetonitrile and 0.1% phosphoric acid water in gradient mode. The flow rate was 0.25 mL x min(-1) and the detection wavelength was set at 220 nm. The fingerprints of 26 batches Xanthii Fructus were carried out by similarity comparation, cluster and the principal component analysis (PCA). There were nineteen common peaks, nine of which had been identified, and the similarity degrees of the twenty-six batches of the samples were between 0.804 and 0.990. All the samples were classified into six categories, and the PCA value of each fingerprint peak was calculated, and six principal components accounted for over 81. 140% of the total variance were extracted from the original data This method can be used to assess the quality of Xanthii Fructus.

Effects of Xanthium stramarium and Psoralea corylifolia Extracts Combined with UVA1 Irradiation on the Cell Proliferation and TGF-beta1 Expression of Keloid Fibroblasts

BACKGROUND: Xanthium stramarium (XAS) and Psoralea corylifolia (PSC), phototoxic oriental medicinal plants, has been used in traditional medicines in Asian countries. OBJECTIVE: The effects of highly purified XAS or PSC extract combined with ultraviolet A1 (UVA1) irradiation on cell proliferation and transforming growth factor-beta1 (TGF-beta1) expression of the keloid fibroblast were being investigated to define potential therapeutic uses for keloid treatments. METHODS: The keloid fibroblasts were treated with XAS or PSC alone or in the combination with UVA1 irradiation. The cell viability, apoptosis, and expression of TGF-beta1 and collagen I were investigated. RESULTS: XAS and PSC in combination with UVA1 irradiation suppressed cell proliferation and induced apoptosis of keloid fibroblasts. Furthermore, the XAS and PSC in combination with UVA1 irradiation inhibited TGF-beta1 expression and collagen synthesis in keloid fibroblasts. CONCLUSION: These findings may open up the possibility of clinically used XAS or PSC in combination with UVA1 irradiation for keloid treatments.

Effects of Xanthium stramarium and Psoralea corylifolia Extracts Combined with UVA1 Irradiation on the Cell Proliferation and TGF-beta1 Expression of Keloid Fibroblasts

BACKGROUND: Xanthium stramarium (XAS) and Psoralea corylifolia (PSC), phototoxic oriental medicinal plants, has been used in traditional medicines in Asian countries. OBJECTIVE: The effects of highly purified XAS or PSC extract combined with ultraviolet A1 (UVA1) irradiation on cell proliferation and transforming growth factor-beta1 (TGF-beta1) expression of the keloid fibroblast were being investigated to define potential therapeutic uses for keloid treatments. METHODS: The keloid fibroblasts were treated with XAS or PSC alone or in the combination with UVA1 irradiation. The cell viability, apoptosis, and expression of TGF-beta1 and collagen I were investigated. RESULTS: XAS and PSC in combination with UVA1 irradiation suppressed cell proliferation and induced apoptosis of keloid fibroblasts. Furthermore, the XAS and PSC in combination with UVA1 irradiation inhibited TGF-beta1 expression and collagen synthesis in keloid fibroblasts. CONCLUSION: These findings may open up the possibility of clinically used XAS or PSC in combination with UVA1 irradiation for keloid treatments.

Inhibition of α-glucosidase activity by water extracts of Xanthium sibiricum Patrin ex Widder and their effects on blood sugar in mice / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To investigate the effects of Xanthium sibiricum Patrin ex Widder water extracts (CEW) on α-glucosidase activity (AG) and blood sugar in mice.</p><p><b>METHODS</b>The inhibition of AG by CEW was studied with enzyme-inhibitor screening external model with acarbose as control drug. The normal mice were administrated by gavage with 40.0g*kg(-1), or 10.0 g*kg(-1) of CEW, 0.375 g*kg(-1) of acarbose, and 0.3ml of normal saline, respectively in successive 5 days; then the animals were loaded with 2.0 g*kg(-1) of glucose, 4.0 g*kg(-1) of sucrose, and 2.0 g*kg(-1) of starch and blood sugar levels were measured within 15, 30, 60, and 120min. Diabetes was induced by injection of streptozotocin (STZ) in mice, then 40.0 g*kg(-1), or 10.0 g*kg(-1) of CEW was given to diabetic mice in successive 2 weeks and 4 weeks, then the blood sugar levels were measured.</p><p><b>RESULTS</b>In the enzyme inhibition test, when the concentration of CEW was between 0.3125 g*L(-1)-10.00 g*L(-1), the inhibition rate was 55.42%-92.73% when the concentration of acarbose was 1.5625 g*L(-1)-25.00 g*L(-1), the inhibition rate was 9.28%-64.87%. In the sugar tolerance test, the blood sugar value in starch-loaded mice decreased sharply (P<0.01), followed by sucrose-loaded group (P<0.05), and there was no change in glucose-loaded group (P>0.05). In diabetic mice CEW-40 and CEW-10 groups showed significant blood sugar lowering effect (P<0.01 or P<0.05).</p><p><b>CONCLUSION</b>CEW has stronger effect in inhibition of AG activity than acarbose. CEW can increase the sugar tolerance in normal mice and decrease the blood sugar level in diabetic mice..</p>

Comparative study on acute toxicity of four extracts from Xanthii Fructus in mice / 中国中药杂志

<p><b>OBJECTIVE</b>To comparative study the acute toxicity of four extracts from Xanthii Fructus in mice.</p><p><b>METHOD</b>Observed the toxic manifestations in mice which were given the four extracts by intragastric administration and calculated the LD50 of the four extracts from Xanthii Fructus.</p><p><b>RESULT</b>The toxic manifestations of the mice given water extract by intragastric administration were repose, pilo-erection, cyanosis, intention tremor, respiratory inhibition, loss of righting reflex and convulsion . The toxic manifestations of the mice given ethanol extract by intragastric administration were repose, abdominal respiration, intention tremor, intermittent convulsions, incontinence. The LD50 of Xanthii Fructus processed water extract, processed ethanol extract, crude water extract, crude ethanol extract were material drug 155.93, 317.80, 167.6, 275.41 g x kg(-1), respectively.</p><p><b>CONCLUSION</b>The acute toxicity of water extract is distinctly stronger than that of ethanol extract, but there is no marked distinguish between crude and processed extract.</p>

Search of new Antimitotics compounds from the Cuban flora / Búsqueda de nuevos compuestos con actividad antimitótica en la flora cubana

The main objective of anti-carcinogenic chemotherapy is to stop uncontrolled cellular proliferation. This has prompted us to begin a systematic survey of new effective inhibitors with ability to react with cytoskeletal components and arrest living, dividing cells. Even for traditional populations herbs-consuming, encouraging the use of species with chemopreventive actions could be helpful as part of life expectancy improvement strategies. Herbal products have significantly lower costs, exhibit little or no toxicity during long-term oral administration and are relatively available at large scale. Current work involved the screening of 85 extracts from Cuban medicinal plants, selected on the basis of traditional use, ethnobotanics and pharmacological information (antiparasitic, antitumour, abortive, etc.). Antitubulinic activity in the hydroalcoholics extracts was evaluated by using a modified version of the conventional turbidity assay of tubulin assembly/ disassembly. The activity limits of the news isolated antitubulin agents were thoroughly investigated. According to the presented results, the extracts displaying the highest antitubulinic activity were Tamarindus indica L., Lawsonia inermes L and Xanthium strumarium L.

Detener la proliferación celular es el principal propósito de la quimioterapia anticarcinogénica. Para ello se ha realizado una búsqueda a partir de fuentes naturales de nuevos inhibidores efectivos que reaccionen con los componentes del citoesqueleto y puedan detener la división celular. En poblaciones que tradicionalmente utilizan plantas medicinales se estimula el uso de aquellas especies con acción quimiopreventivas como parte de una estrategia que contribuya a la calidad de vida. Los productos herbarios tienen costos significativamente más bajos, exhiben poca o ninguna toxicidad durante la administración oral a largo plazo y están al alcance de todos. Nuestro trabajo consistió en realizar un tamizaje de 85 extractos de plantas medicinales cubanas seleccionadas en base al uso tradicional, en las encuestas etnobotánicas e información farmacológica (actividad antiparasitaria, antitumoral, abortiva, etc). La actividad antitubulínica fue evaluada mediante una versión modificada del ensayo turbimétrico del ensamblaje/desensamblaje de la tubulina. Se determinó la actividad límite de los nuevos agentes antitubulínicos siendo los extractos de Tamarindus indica L., Lawsonia inermes L and Xanthium strumarium L. los de mejor actividad antitubulínica según las condiciones ensayadas.

Prácticas agrícolas para el cultivo de Xanthium strumarium L (guizazo de caballo) con fines terapéuticos / Agricultural practices for the culture of Xanthium strumanium L (guizazo de caballo) with therapeutic aims

Xanthium strumarium (guizazo de caballo) se encuentra entre las plantas con antividad antimitótica. OBJETIVOS: determinar en esta especie los aspectos agrícolas que garanticen el adecuado material vegetal. MÉTODOS: se realizaron estudios durante 2007-2009, donde se evaluaron dos fechas de siembra: junio y julio; dos distancias de siembra 90 x 30 cm y 90 x 50 cm y dos momentos de cosecha: 3 meses de edad (parte aérea y raíces) en plantas que presentaban estado de floración-fructificación y 4 meses de edad (solo raíces) en plantas en fructificación. Las semillas, obtenidas de areales silvestres, se sembraron en parcelas, 3 repeticiones en cada caso. Se evaluó la altura de las plantas en el momento de la cosecha, se seleccionaron 10 plantas/parcelas y se cosecharon 39 plantas/parcelas en la distancia de 90 x 30 cm y 24 plantas en la distancia de 90 x 50 cm, en el caso del follaje se evaluaron los rendimientos de 10 plantas/parcelas en cada caso. RESULTADOS: se observó que bajo cultivo la altura de las plantas fueron mayores en las que se sembraron en junio, con distancia de 90 x 30 cm, en tanto que en las de julio se comportaron de forma similar, independientemente a las distancias de siembra empleadas y en correspondencia con ello los rendimientos resultaron iguales; sin embargo, cuando se quieren cosechar también las raíces, es preferible hacer la cosecha a los 3 meses de edad y, en este caso, los mayores valores se presentaron en las siembras de julio, con distancia de 90 x 30 cm. CONCLUSIÓN: para el aprovechamiento de la planta con doble propósito: parte aérea y raíces, pues en ambas se ha encontrado la actividad antimitótica, la siembra se debe realizar entre junio y julio a la distancia de 90 x 30 cm y recolectarse el material a la edad de 3 meses

Xanthium strumarium (guizazo de caballo) is among the plants with antimitotic activity. OBJECTIVES: to determine in this species the agricultural features to guarantee the appropriate plant material. METHODS: during 2007-2009 studies were conducted to assess to sow dates: June and July; two sow distances 90 x 30 cm and 90 x 50 cm at two sow periods: three months of age (aerial parts and roots) in plants with a flowering-fructification states and four months of age (only roots) in plants in fructification process. Seeds obtained from wild aerial plants were sowed in plots, three repetitions in each case. The plants height was assessed at the harvest moment, choosing 10 plants/lots and 39 plants/lots were growed at a 90 x 30 cm distance and 24 plants at the 90 x 50 cm distance, in the case of foliage the yields of 10 plants/lots were assessed in each case. RESULTS: there was that at culture the plants heights were higher in those sowed in June at a 90 x 30 cm distance while those sowed in July behaved in a similar way independently of the sow distances used and in correspondence with it, the yields were similar; however, when we desire to grow also the roots, it is preferable to grow at three months of age, and in this case, the higher values were in sows of July at a 90 x 30 cm distance. CONCLUSION: for the plant exploitation with a double aim: aerial parts and roots, since in both there is antimitotic activity, sow must to be performed between June and July at a 90 x 30 cm distance and to harvest the material at three months age

Simultaneous determination of 4 phenolic acids in cangerzi by ultra-performance liquid chromatography / 药学学报

In this study, an analytical method was developed and used to quantify simultaneously protocatechuic acid, neochlorogenic acid, cryptochlorogenic acid and 1, 3-dicaffeoylquinic acid--four bioactive compounds contained in Fructus Xanthii using UPLC. The contents of four phenolic components of 28 batches of samples collected from different product areas and markets were determined and compared by means of this established method. The mobile phase was composed of methanol and water containing 0.1% phosphoric acid. Chromatography was monitored at dual-wavelengths--220 and 327 nm. Flow rate was 0.4 mL x min(-1) and column temperature was 35 degrees C. The correlation coefficient between concentration and chromatographic peak area of protocatechuic acid, neochlorogenic acid, cryptochlorogenic acid and 1, 3-dicaffeoylquinic acid was over 0.9999 in the range of 0.3570-35.70, 2.500-250.0, 1.060-106.1, 1.010-101.0 microg x mL(-1), respectively. The average recoveries of the four compounds were 97.68%, 99.55%, 97.92% and 100.4%, respectively. In conclusion, the established method can rapidly attain an accurate and reproducible result used to control the quality of Fructus Xanthii.