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Article in Chinese | WPRIM | ID: wpr-879155


This paper aims to investigate the chemical constituents of the seeds of Herpetospermum pedunculosum. One new coumarin and two known lignans were isolated from the ethanolic extract of the seeds of H. pedunculosum with thin layer chromatography(TLC), silica gel column chromatography, Sephedax LH-20 chromatography, Semi-preparative high performance liquid chromatography and recrystallization, etc. Their structures were elucidated as herpetolide H(1), phyllanglaucin B(2), and buddlenol E(3) by analysis of their physicochemical properties and spectral data. Among them, compound 1 was a new compound, and compounds 2 and 3 were isolated from this genus for the first time. In vitro anti-inflammatory activity test showed that herpetolide H had certain NO inhibitory activity for LPS-induced RAW 264.7 cells, with its IC_(50) value of(46.57±3.28) μmol·L~(-1).

Chromatography, High Pressure Liquid , Coumarins/pharmacology , Cucurbitaceae , Lignans , Seeds
Article in Chinese | WPRIM | ID: wpr-921694


Phenylpropanoids are one of the major chemical constituents in Zanthoxylum species. They include simple phenylpropanoids, coumarins, and lignans and possess anti-tumor, anti-inflammatory, anti-platelet aggregation, anti-bacterial, anti-viral, insecticidal, and antifeedant activities. This review summarizes the chemical constituents and pharmacological activities from the Zanthoxylum plants in hopes of providing reference for the research and application of phenylpropanoids from this genus.

Anti-Inflammatory Agents/pharmacology , Coumarins/pharmacology , Lignans , Plant Extracts , Zanthoxylum
Braz. j. microbiol ; 49(2): 407-413, Apr.-June 2018. tab, graf
Article in English | LILACS | ID: biblio-889247


Abstract Fungal infections have become a concern for health professionals, and the emergence of resistant strains has been reported for all known classes of antifungal drugs. Among the fungi causing disease, we highlight those that belong to the genus Aspergillus. For these reasons, the search for new antifungals is important. This study examines the effects of a coumarin derivative, 4-acetatecoumarin (Cou-UMB16) both alone and together with antifungal drugs, and its mode of action against Aspergillus spp. Cou-UMB16 was tested to evaluate its effects on mycelia growth, and germination of Aspergillus spp. fungal conidia. We investigated its possible action on cell walls, on the cell membrane, and also the capacity of this coumarin derivative to enhance the activity of antifungal drugs. Our results suggest that Cou-UMB16 inhibits Aspergillus spp. virulence factors (mycelia growth and germination of conidia) and affects the structure of the fungal cell wall. When applying Cou-UMB16 in combination with azoles, both synergistic and additive effects were observed. This study concludes that Cou-UMB16 inhibits mycelial growth and spore germination, and that the activity is due to its action on the fungal cell wall, and that Cou-UMB16 could act as an antifungal modifier.

Antifungal Agents/isolation & purification , Antifungal Agents/pharmacology , Aspergillus/drug effects , Coumarins/isolation & purification , Coumarins/pharmacology , Drug Synergism , Aspergillus/growth & development , Azoles/pharmacology , Cell Membrane/drug effects , Cell Wall/drug effects , Hyphae/drug effects , Hyphae/growth & development , Spores, Fungal/drug effects , Spores, Fungal/growth & development
Braz. j. med. biol. res ; 51(7): e7220, 2018. tab, graf
Article in English | LILACS | ID: biblio-889115


An abnormality in the Lin28/let-7a axis is relevant to the progression of hepatitis B virus (HBV)-positive hepatocellular carcinoma (HCC), which could be a novel therapeutic target for this malignant tumor. The present study aimed to investigate the antiproliferative and anti-invasive effects of urolithin A in a stable full-length HBV gene integrated cell line HepG2.2.15 using CCK-8 and transwell assays. The RNA and protein expressions of targets were assessed by quantitative PCR and western blot, respectively. Results revealed that urolithin A induced cytotoxicity in HepG2.2.15 cells, which was accompanied by the cleavage of caspase-3 protein and down-regulation of Bcl-2/Bax ratio. Moreover, urolithin A suppressed the protein expressions of Sp-1, Lin28a, and Zcchc11, and elevated the expression of microRNA let-7a. Importantly, urolithin A also regulated the Lin28a/let-7a axis in transient HBx-transfected HCC HepG2 cells. Furthermore, urolithin A decelerated the HepG2.2.15 cell invasion, which was involved in suppressing the let-7a downstream factors HMGA2 and K-ras. These findings indicated that urolithin A exerted the antiproliferative effect by regulating the Lin28a/let-7a axis and may be a potential supplement for HBV-infected HCC therapy.

Humans , RNA-Binding Proteins/drug effects , Carcinoma, Hepatocellular/drug therapy , Coumarins/pharmacology , MicroRNAs/drug effects , Liver Neoplasms/drug therapy , Reference Values , Sincalide/analysis , Time Factors , Virus Replication/drug effects , Cell Survival/drug effects , Blotting, Western , Reproducibility of Results , Analysis of Variance , RNA-Binding Proteins/analysis , Carcinoma, Hepatocellular/genetics , Carcinoma, Hepatocellular/virology , MicroRNAs/analysis , Cell Proliferation/drug effects , Hep G2 Cells , Real-Time Polymerase Chain Reaction , Liver Neoplasms/genetics , Liver Neoplasms/virology
Braz. j. med. biol. res ; 50(11): e6455, 2017. tab, graf
Article in English | LILACS | ID: biblio-888957


Series of novel coumarin derivatives [I (a-d) and II (a-d)] were successfully synthesized and their structures were determined based on infrared 1H-nuclear magnetic resonance (NMR), HRMS, and single crystal X-ray crystallography. Additionally, the new synthesized compounds were evaluated to identify the molecular characteristics that contribute to their cytotoxicity, which was tested against SK-LU-1, SPC-A-1 and 95D human lung cancer cell lines, using the MTT assay. The results of this study showed that compounds Ic, Id, IIc, and IId exhibited an efficient percentage of inhibition of cell proliferation.

Humans , Antineoplastic Agents/pharmacology , Coumarins/pharmacology , Lung Neoplasms/drug therapy , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Coloring Agents , Coumarins/chemical synthesis , Coumarins/chemistry , Crystallography, X-Ray/methods , Drug Screening Assays, Antitumor , Lung Neoplasms/pathology , Magnetic Resonance Spectroscopy/methods , Reference Values , Reproducibility of Results , Tetrazolium Salts , Thiazoles
Rev. bras. plantas med ; 17(4,supl.2): 865-874, 2015. tab, graf
Article in English | LILACS | ID: lil-771170


ABSTRACT The extracts and fractions of leaves and branches of Protium hebetatum D. C. Daly (Burseraceae) were investigated for their antibacterial activity and chemical composition. The methanol extract of branches (EMG) was considered active against the Escherichia coli and the Proteus vulgaris, showing an inhibition zone of 13 mm, and was selected for bioassay-guided phytochemical fractionation. From the technique of broth microdilution, the extract was considered a moderate inhibitor against Staphylococcus aureus, Pseudomonas aeruginosa and Enterococcus faecalis, with a minimum inhibitory concentration (MIC) of 1 mg/mL. The dichloromethane fraction was considered a moderate inhibitor against S. aureus (MIC of 1 mg/mL) and a potent inhibitor against E. faecalis (MIC of 0.5 mg/mL). F1, F2, F5 and F6 from chromatographic column of dichloromethane fraction were considered moderate inhibitors against S. aureus (MIC of 1 mg/mL). Through analysis by a gas chromatography mass spectrometry, eighteen compounds were identified, from which thirteen (isoeugenol, p-vinylguaiacol, metoxyeugenol, coumarin, 5-hydroxy-scopoletin, 4,7-dihydroxy-6-metoxicromam-2-one, 4[(1E]-3-hydroxy-1-propenyl)-2-methoxyphenol, piperonal, scoparon, o-guaiacol, spathulenol, seringol and antiarol) are unprecedented in these species. We also identified the triterpenes α-amyrin and β-amyrin, the steroids stigmasterol and sitosterol and the coumarin scopoletin, which was closely linked to the antibacterial activity of the samples.

RESUMO Atividade antibacteriana e compostos químicos de folhas e galhos de Protium hebetatum. Extratos e frações de folhas e galhos de Protium hebetatum D. C. Daly (Burseraceae) foram investigados quanto sua atividade antibacteriana e composição química. O extrato metanólico dos galhos (EMG) foi considerado ativo contra Escherichia coli e Proteus vulgaris, apresentando um halo de inibição de 13 mm, sendo selecionado para um fracionamento fitoquímico biomonitorado. A partir da técnica de microdiluição em caldo o EMG foi considerado um inibidor moderado contra Staphylococcus aureus, Pseudomonas aeruginosa e Enterococcus faecalis, apresentando uma concentração inibitória mínima (CIM) de 1mg/mL. A fração diclorometânica foi considerada inibidora moderada contra S. aureus (CIM de 1 mg/mL) e inibidora potente contra E. faecalis (CIM de 0,5 mg/mL). F1, F2, F5 e F6 provenientes da fração diclorometânica foram consideradas inibidoras moderadas contra S. aureus (CIM de 1 mg/mL). Através da análise por cromatografia gasosa acoplada a espectrometria de massa, foram identificados dezoitos compostos, dos quais treze (isoeugenol, p-vinilguaiacol, metoxieugenol, cumarina, 5-hidroxi-escopoletina, 4,7-dihidroxi-6-metoxicromam-2-ona, 4[(1E]-3-hidroxi-1-propenil)-2-methoxifenol, piperonal, escoparona, o-guaiacol, espatulenol, seringol e antiarol) foram identificados pela primeira vez nesta espécie. Foram também identificados os triterpenos α-amirina e β-amirina, os esteroides estigmasterol e sitosterol e a cumarina escopoletina, que estão intimamente ligados à atividade antibacteriana da espécie.

Chemical Compounds/analysis , Burseraceae/classification , Anti-Infective Agents/classification , Staphylococcus aureus/classification , Enterococcus faecalis/classification , Coumarins/pharmacology
Article in English | WPRIM | ID: wpr-57306


Scoparone, which is a major constituent of Artemisia capillaries, has been identified as an anticoagulant, hypolipidemic, vasorelaxant, anti-oxidant and anti-inflammatory drug, and it is used for the traditional treatment of neonatal jaundice. Therefore, we hypothesized that scoparone could suppress the proliferation of VSMCs by interfering with STAT3 signaling. We found that the proliferation of these cells was significantly attenuated by scoparone in a dose-dependent manner. Scoparone markedly reduced the serum-stimulated accumulation of cells in the S phase and concomitantly increased the proportion of cells in the G0/G1 phase, which was consistent with the reduced expression of cyclin D1, phosphorylated Rb and survivin in the VSMCs. Cell adhesion markers, such as MCP-1 and ICAM-1, were significantly reduced by scoparone. Interestingly, this compound attenuated the increase in cyclin D promoter activity by inhibiting the activities of both the WT and active forms of STAT3. Similarly, the expression of a cell proliferation marker induced by PDGF was decreased by scoparone with no change in the phosphorylation of JAK2 or Src. On the basis of the immunofluorescence staining results, STAT3 proteins phosphorylated by PDGF were predominantly localized to the nucleus and were markedly reduced in the scoparone-treated cells. In summary, scoparone blocks the accumulation of STAT3 transported from the cytosol to the nucleus, leading to the suppression of VSMC proliferation through G1 phase arrest and the inhibition of Rb phosphorylation. This activity occurs independent of the form of STAT3 and upstream of kinases, such as Jak and Src, which are correlated with abnormal vascular remodeling due to the presence of an excess of growth factors following vascular injury. These data provide convincing evidence that scoparone may be a new preventative agent for the treatment of cardiovascular diseases.

Animals , Humans , Rats , Active Transport, Cell Nucleus , Biomarkers , Cell Cycle Proteins/genetics , Cell Movement/drug effects , Cell Proliferation/drug effects , Cells, Cultured , Coumarins/pharmacology , Gene Expression Regulation/drug effects , Hep G2 Cells , Muscle, Smooth, Vascular/cytology , Myocytes, Smooth Muscle/metabolism , Proto-Oncogene Proteins c-sis/metabolism , STAT3 Transcription Factor/genetics , Signal Transduction/drug effects , Transcription, Genetic
Rev. bras. enferm ; 67(6): 881-885, Nov-Dec/2014.
Article in English | LILACS, BDENF | ID: lil-732816


Interdisciplinary collaboration is widely recognized and considered essential for optimizing the development of knowledge and practice. However, interdisciplinarity is commonly accepted as an unquestioned good; rarely examined as both a source of benefit as well as difficulty for nursing and other disciplines. The aim of this article is to critically examine the opportunities and challenges that interdisciplinarity can provide for research in nursing and other disciplines. Based on a North American perspective, I describe the emergence of uni-disciplinary nursing research and the knowledge exchanges that occurred between nursing and other disciplines. I discuss the rise of interdisciplinary research, outline several examples of nursing participation in interdisciplinarity, and highlight the prominent benefits and difficulties associated with interdisciplinary research. I argue that authentic collaboration is required to conduct meaningful interdisciplinary research and describe how this can be promoted.

Colaboração interdisciplinar é amplamente reconhecida e considerada essencial para a otimização do desenvolvimento do conhecimento e prática. No entanto, a interdisciplinaridade é comumente aceita como um bem inquestionável, raramente examinado tanto como uma fonte de benefícios, bem como dificuldade para a enfermagem e outras disciplinas. O objetivo deste artigo é analisar criticamente as oportunidades e desafios que a interdisciplinaridade pode oferecer para a pesquisa em enfermagem e outras disciplinas. Com base em uma perspectiva norte-americana, descreve-se o surgimento de pesquisas em enfermagem unidisciplinar e as trocas de conhecimento que ocorreram entre a enfermagem e outras disciplinas. Discute-se a ascensão da pesquisa interdisciplinar, delineiam-se vários exemplos de participação da enfermagem na interdisciplinaridade, e destacam-se os benefícios proeminentes e dificuldades associadas com a pesquisa interdisciplinar. Defende-se que a colaboração autêntica é necessária para conduzir a pesquisa interdisciplinar significativa e descreve-se como isso pode ser promovido.

La colaboración interdisciplinaria es ampliamente reconocida y considerada esencial para optimizar el desarrollo del conocimiento y la práctica. Sin embargo, la interdisciplinariedad es comúnmente aceptada como un bien incuestionable; rara vez examinada tanto como una fuente de beneficio, así como de dificultad para la enfermería y otras disciplinas. El objetivo de este artículo es examinar críticamente las oportunidades y desafíos que la interdisciplinariedad puede proporcionar para la investigación en enfermería y otras disciplinas. Sobre la base de una perspectiva norteamericana, describe-se el surgimiento de la investigación en enfermería unidisciplinaria y los intercambios de conocimientos que se produjeron entre la enfermería y otras disciplinas. Se discute el aumento de la investigación interdisciplinaria, esbozan-se varios ejemplos de la participación de enfermería en la interdisciplinariedad, y destacan-se los beneficios y las dificultades asociadas con la investigación interdisciplinaria. Argumenta-sé que se requiere auténtica colaboración para llevar a cabo la investigación interdisciplinaria significativa y describe-se la forma en que esto puede ser promovido. .

Humans , Female , Catechol O-Methyltransferase/biosynthesis , /biosynthesis , Placenta/enzymology , Pregnancy/metabolism , Steroid Hydroxylases/biosynthesis , Xenobiotics/pharmacology , Butylated Hydroxyanisole/pharmacology , Carcinogens , Coumarins/pharmacology , Enzyme Induction , Naphthols/pharmacology , Pregnancy Trimester, First
Rev. cuba. farm ; 48(3)jul.-set. 2014. tab, Ilus
Article in English | LILACS, CUMED | ID: lil-740921


INTRODUCTION: Justicia pectoralis Jacq. (Acanthaceae) is medicinal plant species commonly used in Cuba for the treatment of nervous disorders because of its sedative effect. Coumarin is one of its main active phytochemicals present in the extracts obtained from this plant and used as analytic marker in quality control. On the other hand, this compound contributes to the sedative effect attributed to this plant. OBJECTIVE: to evaluate the influence of harvest time on the coumarin and umbelliferone (7-hydroxycoumarin) in Justicia pectoralis extracts. METHODS: the experiment lasted two years. The harvest was performed at 4, 6 and 8 months after planting. Aqueous and hydroalcohol extracts were produced and the coumarin and umbelliferone contents were determined by high resolution liquid chromatography. RESULTS: the achieved results showed the presence of coumarin and umbelliferone in both extracts. Both methods can be used for the extraction of these components from the plant, although in the case of umbelliferone, the best extraction results were achieved by using aqueous extract. In both cases, the recovery percentages were more than 98 percent. This study confirmed that the harvest time significantly influences on the coumarin and umbelliferone contents. CONCLUSIONS: the best results are observed in the first two harvests (4 and 6 months at summer time), which indicates that the industry should process the vegetal material in these two periods of the year(AU)

INTRODUCCIÓN: Justicia pectoralis Jacq. (Acanthaceae) es una planta medicinal comúnmente usada en Cuba para el tratamiento de enfermedades nerviosas por su efecto sedante. La cumarina es uno de los fitocomponentes mayoritarios en los extractos obtenidos con esta planta y empleado como marcador analítico en los controles de calidad. Por otro lado, este componente contribuye con el efecto sedante atribuido a esta planta. OBJETIVO: evaluar la influencia del tiempo de cosecha sobre el contenido de cumarina y umbelliferona (7 hidroxicumarina) en extractos de Justicia pectoralis. MÉTODOS: se desarrolló el experimento durante 2 años. Se realizaron las cosechas a los 4, 6 y 8 meses de plantada. Se elaboraron extractos acuosos e hidroalcohólicos y se determinó el contenido de cumarina y umbelliferone por cromatografía líquida de alta resolución. RESULTADOS: se mostró la presencia de cumarina y umbelliferona en ambos extractos. Además, en el caso de la umbelliferona, los mejores resultados se alcanzaron al aplicar extracción acuosa. En ambos casos, los por cientos de recobrados fueron superiores al 98 por ciento. Se confirmó que el tiempo de cosecha influyó significativamente sobre el contenido de cumarina y umbelliferona. CONCLUSIONES: los mejores resultados se obtienen en la primeras dos cosechas (4 y 6 meses que coincide con el verano), lo que sugiere que el material de la planta debe procesarse por la industria en esos periodos del año(AU)

Umbelliferones/pharmacology , Coumarins/pharmacology , Cuba , Tilia
Bol. latinoam. Caribe plantas med. aromát ; 11(1): 74-76, ene. 2012. tab
Article in English | LILACS | ID: lil-654803


The in vitro anti-bacterial activity of auraptene and four prenyloxycinnamic and benzoic acids was evaluated against a panel of three bacterial strain. All compounds were shown to be active as inhibitory agents of the growth of Staphylococcus aureus.

La actividad antibacteriana in vitro del auraptene y de cuatro ácidos preniloxycinámicos y benzoicos ha sido evaluada sobre un grupo de tres distintas cepas bacterianas. Todos los compuestos mostraron ser activos como agentes inhibitorios del crecimiento del Staphylococcus Aureus.

Anti-Bacterial Agents/pharmacology , Cinnamates/pharmacology , Coumarins/pharmacology , Staphylococcus aureus
Rev. bras. plantas med ; 14(2): 400-409, 2012. ilus
Article in Portuguese | LILACS | ID: lil-650684


As plantas medicinais vêm sendo cada vez mais utilizadas devido às suas propriedades preventivas, paleativas e curativas, além de ser uma terapia alternativa que traz inúmeros benefícios aos usuários. As espécies Mikania glomerata e M. laevigata pertencem à família Asteraceae e são popularmente conhecidas como guaco sendo utilizadas no tratamento de enfermidades do trato respiratório. Além disso, as duas espécies são frequentemente confundidas ou citadas na literatura de forma errada. O presente trabalho teve por objetivo realizar uma revisão bibliográfica sobre a farmacologia, farmacobotânica e fitoquímica dos metabólitos secundários de Guaco, tendo destaque a cumarina, a biossíntese e as ações biológicas. As ações broncodilatadora, expectorante, anti-inflamatória e antialérgica, além de interações com alguns antibióticos e anticoagulantes, também foram descritas neste estudo.

Medicinal plants have been increasingly used due to their preventive, palliative and curative properties, besides being an alternative therapy that brings a large number of benefits to their users. The species Mikania glomerata belongs to the Asteraceae family and is popularly known as guaco, being employed to treat diseases of the respiratory tract. This study aimed to carry out a literature review about the pharmacology, pharmacobotany and phytochemistry of the secondary metabolites of M. glomerata, particularly coumarin, its biosynthesis and biological actions. The bronchodilator, expectorant, anti-inflammatory and antiallergic actions, as well as the interactions with some antibiotics and anticoagulants, were also described in this study.

Pharmacology/methods , Mikania/chemistry , Phytotherapy , Plants, Medicinal/adverse effects , Coumarins/pharmacology
Rev. salud pública ; 16(3): 361-370, 2012. ilus, tab
Article in Portuguese | LILACS | ID: lil-729647


Objetivo Visando conhecer o impacto das demandas judiciais sobre a organização dos serviços públicos de saúde, realizou-se uma revisáo sistemática com enfoque na "judicialização da saúde" para fornecimento de medicamentos. Métodos Foram analisados artigos originais publicados no período de 2007 a 2011, na literatura nacional e internacional, resultando no total de 49239 artigos disponíveis nas bases de dados Science Direct e BIREME. Resultados A pesquisa indicou predominância da bibliografia proveniente do Brasil, principalmente do sudeste, bem como de estudo realizado na Colômbia. Discursáo Dentre os pleitos, configuraram-se como principais agravos relatados as doenças crônicas, podendo-se citar: diabetes, hipertensáo, cânceres e artrite reumatóide. Por serem afecções parte de programas específicos do Sistema Único de Saúde, a dificuldade de acesso a esses fármacos e consequente judicialização da saúde demonstrou a fragilidade das políticas públicas existentes. Conclusão Por fim, conclui-se que a via judicial, apesar de ser uma estratégia para garantir o acesso ao medicamento, apresenta inabilidade para lidar com o julgamento das ações e gera, dessa forma, distorções no fluxo dos sistemas públicos.

Objective A systematic review, focusing on the judicialisation of health regarding gaining access to medicines, was aimed at understanding the impact of lawsuits on the organisation of public health services. Method Original articles published between 2007 and 2011 in the pertinent national and international literature were analysed, resulting in 49,239 articles being found in Science Direct and BIREME databases. Results The survey indicated a predominance of literature from Brazil, mainly the southeast, as well as a study from Colombia. Discussion The aforementioned chronic disease-related claims involved diabetes, high blood pressure, cancer and rheumatoid arthritis. Forming part of specific Unified Healthcare System programmes highlighted the difficulty in gaining access to the appropriate medicine and consequent health judicialisation demonstrated the fragility of existing public policy. Conclusion It was concluded that the courts (despite being a strategy for ensuring access to medicine) were unable to deal with the current spate of lawsuits, thereby leading to disruption regarding the flow of public systems.

Objetivo El estudio tiene como objetivo evaluar el impacto de las demandas judiciales sobre la organización de los servicios públicos de salud, mediante la realización de una revisión sistemática centrada en el uso de los tribunales para el suministro de medicamentos. Método Fueron identificados 49239 artículos en las bases de datos Science Direct e BIREME. Resultado El estudio indicó que la mayor parte de la bibliografía es de Brasil, con uno estudio en Colombia. Discusión Aparecen como los principales trastornos de salud relatados a las enfermedades crónicas, se pueden citar: la diabetes, la hipertensión, el cáncer y la artritis reumatoide. Debido a que son parte de los programas específicos de lo sistema de salud, la dificultad de acceso a estos fármacos y la consiguiente judicialización de la salud de manifiesto la fragilidad de las políticas públicas existentes. Conclusiones Por último, está la conclusión de que los tribunales, a pesar de ser una estrategia para garantizar el acceso a la medicina, presenta incapacidad para hacer frente al juicio de las acciones y por lo tanto genera distorsiones en el flujo de los sistemas públicos.

Aspartic Acid Endopeptidases/genetics , Cacao/enzymology , Leucine/analogs & derivatives , Seeds/enzymology , Amino Acid Sequence , Aspartic Acid Endopeptidases/drug effects , Aspartic Acid Endopeptidases/metabolism , Cacao/genetics , Cloning, Molecular , Coumarins/pharmacology , DNA, Complementary/chemistry , DNA, Complementary/genetics , DNA, Complementary/isolation & purification , Gene Expression Regulation, Enzymologic , Gene Expression Regulation, Plant , Hydrogen-Ion Concentration , Isoenzymes/drug effects , Isoenzymes/genetics , Isoenzymes/metabolism , Leucine/pharmacology , Molecular Sequence Data , Pepstatins/pharmacology , Phylogeny , Plant Proteins/genetics , Plant Proteins/metabolism , RNA, Messenger/genetics , RNA, Messenger/metabolism , Seeds/genetics , Sequence Analysis, DNA , Sequence Homology, Amino Acid , Yarrowia/genetics , Yarrowia/metabolism
Rev. venez. cir ; 62(1): 30-33, mar. 2009. ilus
Article in Spanish | LILACS | ID: lil-539978


Evaluar la eficacia del tratamiento de las úlceras venosas de los miembros inferiores por vía intradérmica. Estudio realizado en la Clínica Santa Sofía, Caracas. Se trata de un estudio prospectivo en 19 pacientes, 10 del sexo femenino y 9 del sexo masculino, los cuales presentaron úlceras en miembros inferiores de etiología vascular, con un promedio de edad de 60 años. Se trataron por vía intradérmica con sustancias que estimulan elementos importantes del tejido conectivo. El proceso de cicatrización de la úlcera se hizo progresivo a partir de la cuarta semana de tratamiento, con un cierre total de la úlcera a las 12 semanas. La intradermoterapia puede ser una alternativa en el tratamiento de las úlceras venosas de los miembros inferiores cuando no respondan a otras terapias aplicadas.

Humans , Male , Female , Aged , Vasodilator Agents/administration & dosage , Coumarins/administration & dosage , Lower Extremity/injuries , Lower Extremity/pathology , Intradermal Tests/methods , Varicose Ulcer/etiology , Varicose Ulcer/pathology , Varicose Ulcer/drug therapy , Vasodilator Agents/pharmacology , Tibial Arteries/injuries , Cicatrix/etiology , Coumarins/pharmacology
Mem. Inst. Oswaldo Cruz ; 103(5): 431-436, Aug. 2008. ilus, tab
Article in English | LILACS | ID: lil-491963


Calophyllum brasiliense and Mammea americana (Clusiaceae) are two trees from the tropical rain forests of the American continent. A previous screening showed high trypanocidal activity in the extracts of these species. Several mammea-type coumarins, triterpenoids and biflavonoids were isolated from the leaves of C. brasiliense. Mammea A/AA was obtained from the fruit peels of M. americana. These compounds were tested in vitro against epimastigotes and trypomastigotes of Trypanosoma cruzi, the etiologic agent of Chagas disease. The most potent compounds were mammea A/BA, A/BB, A/AA, A/BD and B/BA, with MC100 values in the range of 15 to 90 g/ml. Coumarins with a cyclized ,-dimethylallyl substituent on C-6, such as mammea B/BA, cyclo F + B/BB cyclo F, and isomammeigin, showed MC100 values > 200 g/ml. Several active coumarins were also tested against normal human lymphocytes in vitro, which showed that mammea A/AA and A/BA were not toxic. Other compounds from C. brasiliense, such as the triterpenoids, friedelin, canophyllol, the biflavonoid amentoflavone, and protocatechuic and shikimic acids, were inactive against the epimastigotes. The isopropylidenedioxy derivative of shikimic acid was inactive, and its structure was confirmed by X-ray diffraction. Our results suggest that mammea-type coumarins could be a valuable source of trypanocidal compounds.

Adult , Animals , Humans , Male , Biflavonoids/pharmacology , Coumarins/pharmacology , Mammea/chemistry , Triterpenes/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effects , Biflavonoids/chemistry , Biflavonoids/isolation & purification , Coumarins/chemistry , Coumarins/isolation & purification , Dimethyl Sulfoxide/pharmacology , Lymphocytes/drug effects , Plant Extracts/pharmacology , Triterpenes/chemistry , Triterpenes/isolation & purification , Trypanocidal Agents/chemistry , Trypanocidal Agents/isolation & purification
Braz. j. med. biol. res ; 37(12): 1847-1852, Dec. 2004. ilus
Article in English | LILACS | ID: lil-388065


Several natural compounds have been identified for the treatment of leishmaniasis. Among them are some alkaloids, chalcones, lactones, tetralones, and saponins. The new compound reported here, 7-geranyloxycoumarin, called aurapten, belongs to the chemical class of the coumarins and has a molecular weight of 298.37. The compund was extracted from the Rutaceae species Esenbeckia febrifuga and was purified from a hexane extract starting from 407.7 g of dried leaves and followed by four silica gel chromatographic fractionation steps using different solvents as the mobile phase. The resulting compound (47 mg) of shows significant growth inhibition with an LD50 of 30 æM against the tropical parasite Leishmania major, which causes severe clinical manifestations in humans and is endemic in the tropical and subtropical regions. In the present study, we investigated the atomic structure of aurapten in order to determine the existence of common structural motifs that might be related to other coumarins and potentially to other identified inhibitors of Leishmania growth and viability. This compound has a comparable inhibitory activity of other isolated molecules. The aurapten is a planar molecule constituted of an aromatic system with electron delocalization. A hydrophobic side chain consisting of ten carbon atoms with two double bonds and negative density has been identified and may be relevant for further compound synthesis.

Animals , Antiprotozoal Agents/pharmacology , Coumarins/pharmacology , Leishmaniasis/drug therapy , Rutaceae , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/isolation & purification , Coumarins/chemistry , Coumarins/isolation & purification , Parasitic Sensitivity Tests , Plant Extracts/pharmacology
Indian J Exp Biol ; 2003 Nov; 41(11): 1273-8
Article in English | IMSEAR | ID: sea-56032


Well known antioxidants-coumarins (7,8-dihydroxy-4-methyl coumarin-DHMC and 7,8-diacetoxy-4-methyl coumarin-DAMC) and flavonoids (quercetin-Q and quercetin penta-acetate-QPA) were investigated for their pro-oxidant effects in two human tumor cell lines. The breast carcinoma cell line (MDA-MB-468) was found to be more sensitive to treatment by the drugs-DAMC, Q and QPA at 10 microM than the glioma cell line (U-87MG), while DHMC was non toxic in both cell lines at this concentration. In MDA-MB-468 distinct growth inhibition was observed by 48 hr post treatment. Paradoxically, an increase in the formazan production was revealed by MTT assay at this time indicating an increase in the production of free radicals. An increase in the levels of reactive oxygen species (ROS) was also confirmed by DCFH-DA assay. In cells treated with DAMC, Q and QPA an increase in the percentage of cells with the hypodiploid DNA content was suggestive of apoptotic cell death. Taken together, these results suggest that an increase in oxidative stress caused by the pro-oxidant action of these drugs is responsible for cell death.

Antioxidants/pharmacology , Apoptosis/drug effects , Breast Neoplasms/metabolism , Cell Cycle/drug effects , Cell Division/drug effects , Coumarins/pharmacology , Female , Glioma/metabolism , Humans , Oxidative Stress/drug effects , Ploidies , Quercetin/analogs & derivatives , Reactive Oxygen Species/metabolism , Tumor Cells, Cultured
Bol. Hosp. San Juan de Dios ; 47(1): 25-8, ene.-feb. 2000.
Article in Spanish | LILACS | ID: lil-258138


Se ha aprendido mucho con respecto al uso de la terapia antitrombótica para prevenir el stroke en pacientes con fibrilación auricular. Los cumarínicos son mucho más efectivos que la aspirina. Cuando se usan cumarínicos, en INR < 1,5 sólo o en combinación con aspirina son inefectivos. Todo paciente con fibrilación auricular debe ser evaluado para determinar su riesgo de tromboembolismo y especialmente de stroke. Los pacientes de riesgo alto o moderado deben ser tratados con cumarínicos, mientras los pacientes de bajo riesgo pueden ser tratados con aspirina. Un problema que está por dilucidarse es si el buen control de la hipertensión arterial disminuye el riesgo de stroke cardioembólico en los pacientes con fibrilación auricular

Humans , Atrial Fibrillation/complications , Thromboembolism/etiology , Aspirin/pharmacology , Brain Ischemia/etiology , Coumarins/pharmacology , Atrial Fibrillation/drug therapy , Ischemic Attack, Transient , Risk Factors
Bulletin of Faculty of Pharmacy-Cairo University. 1998; 36 (3): 65-72
in English | IMEMR | ID: emr-47801


New parabanic acids and thiazolines derived from different coumarinyloxyacetic acid hydrazides have been prepared and subjected to preliminary pharmacological screening. Some of the tested compounds showed anticonvulsant activity

Coumarins/pharmacology , Thiazoles/chemical synthesis , Anticonvulsants/chemical synthesis