1,721,164 research outputs found
Progettazione, sintesi e attività colinergica di composti strutturalmente correlati ad arecolina, furtretonio ed epibatidina
No full textInhibition of NF-kB/DNA interactions leading to alteration of IL-8 and ICAM-1 gene expression in cystic fibrosis IB3 cells
No full textThe ethanol fraction from the stem of Berberis libanotica inhibits the viability of adult T cell leukemia
No full textAim. In the Mediterranean countries, several described medicinal plants are derived from Lebanon. According to Tohme et al. there are 2597 species in Lebanon. More than fifty two percent are endemic to Lebanon. In this paper we show that the ethanol fraction of the stem of Berberis libanotica is able to inhibit the viability of HTLV-1 positive (HuT-102) and HTLV-1 negative (CEM) cell lines of malignant T-cell leukemia.
Methods. After traditional maceration to extract the ethanol fraction from Berberis libanotica stem, the in vitro viability was assayed.
Results. The results suggest that Berberis libanotica (a Lebanese medicinal plant) contains a substantial amount of secondary metabolites such as alkaloids powerful in inhibiting the viability of HuT-102 and CEM cell lines.
Conclusion. The obtained results demonstrate a novel anticancer property of Berberis libanotica stem extracts, in addition to the previously reported anti-inflammatory activity
Antiproliferative activity of essential oils derived from plants belonging to the Magnoliophyta division
No full textThe essential oils obtained from different officinal plants of Lebanon, belonging to the Magnoliophyta division, have been tested for their antiproliferative activity on human erythroleukemic K562 cells. Satureja montana showed the most interesting biological activity in inhibiting the cell growth and inducing erythroid differentiation of K562 cells. The essential oil of Satureja montana was therefore analyzed using a GC/MS (gas chromatography/mass spectrometry) system in order to identify the major constituents and compare them with analysis performed on Satureja hortensis. We demonstrated that the essential oil composition varied with the species, the major constituent of Satureja hortensis being carvacrol (50.61%) and that of Satureja montana being alpha-terpineol (12.66%). In order to identify molecules possibly responsible for the biological activity, commercially available derivatives have been assayed on the K562 cell line. Satureja montana essential oil displayed different natural derivatives characterized by higher activity than those present in Satureja hortensis. The common active principles are alpha-pinene, gamma-terpinene, 4-terpineol, alpha-terpineol, tau-cadinene, tau-cadinol and caryophyllene. Both caryophyllene and alpha-terpineol showed important antiproliferative effects on K562 cells
Derivati isossazolici come induttori di emoglobina fetale in precursori eritroidi derivati da pazienti beta-talassemici
No full textL’invenzione si riferisce all’impiego di composti isossazolici per la preparazione di un medicamento in grado di indurre sintesi di emoglobina fetale (HbF) in pazienti affetti da talassemia e anemia falciform
Use of angelicin and of its structural analogues for the treatment of thalassemia
No full textThe use of angelicin and of its structural analogues for preparation of a medicamentfor the therapeutic treatment of beta-thalassemia is described. A structural analogue which is particularly preferred for this purpose is bergapte
1,2,4-triazoles. Improved synthesis of 5-substituited 4-amino-3mercato-(4H)-1,2,4 triazoles and a facile route to 3,6-disubstituited 1,24-triazolo[3,4b][1,3,4]thiadiazoles
No full textThe reaction of thiocarbohydrazide with carboxylic acids at the melting temperature allows an improved preparation of the 5-substituted 4-amino-3-mercapto-1,2,4-triazole heterocycles. The crude 4-amino-5-mercapto-1,2,4-triazoles react easily with carboxylic acids or carboxylic acid chlorides to afford the 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole ring system
Inhibitory Effects of Bangladeshi Medicinal Plant Extracts on Interactions between Transcription Factors and Target DNA Sequences.
Full text linkSeveral transcription factors (TFs) play crucial roles in governing the expression of different genes involved in the immune response, embryo or cell lineage development, cell apoptosis, cell cycle progression, oncogenesis, repair and fibrosis processes and inflammation. As far as inflammation, TFs playing pivotal roles are nuclear factor kappa B (NF-kB), activator protein (AP-1), signal transducer and activator of transcription (STATs), cAMP response element binding protein (CREB) and GATA-1 factors. All these TFs regulate the expression of pro-inflammatory cytokines and are involved in the pathogenesis of a number of human disorders, particularly those with an inflammatory component. Since several medicinal plants can be employed to produce extracts exhibiting biological effects and because alteration of gene transcription represents a very interesting approach to control the expression of selected genes, this study sought to verify the ability of several extracts derived from Bangladeshi medicinal plants in interfering with molecular interactions between different TFs and specific DNA sequences. We first analyzed the antiproliferative activity of 19 medicinal plants on different human cell lines, including erythroleukemia K562, B lymphoid Raji and T lymphoid Jurkat cell lines. Secondly, we employed the electrophoretic mobility shift assay as a suitable technique for a fast screening of plant extracts altering the binding between NF-kB, AP-1, GATA-1, STAT-3, CREB and the relative target DNA elements
Gene Expression modulation of pro-inflammatory IL-8 in cystic fibrosis cells by active principles of olive extract
No full textCystic fibrosis (CF) is a severe and diffuse recessive genetic disease due to defects of the CF Transmembrane conductance Regulator (CFTR) gene. CF affects several organs, with the chronic pulmonary disease being the major cause of reduction of the quality and expectancy of life. The hallmark of CF lung disease is chronic infection generally sustained by the gram-negative bacterium Pseudomonas aeruginosa and excessive lung inflammation with a huge infiltrate of neutrophils in the bronchial lumen, mainly due to the release of the chemokine interleukin IL-8. The identification of innovative drugs, to reduce the excessive lung inflammation in CF patients, is considered a therapeutic target to prevent the progressive lung tissue deterioration. Extracts originated from olive processing waste and obtained by a new Molecular Imprinting procedure, have been investigated to select pure compounds able to reduce IL-8 expression in human bronchial epithelial cells (IB3-1), derived from a CF patient with a ΔF508/W1282X mutant genotype and stimulated with TNF-alpha. Initially, Electrophoretic Mobility Shift Assays (EMSAs) were performed to understand whether the different active principles were able to inhibit the binding between transcription factor (TF) NF-kB and DNA consensus sequences. Among different identified active principles, three derivatives were selected, apigenin, oleuropein and cyanidin chloride which have shown remarkable activity in inhibiting TF/DNA complexes. NF-kB is known to be a very interesting target molecule for the design of anti-tumor, pro-apoptotic and anti-inflammatory drugs; these natural derivatives have proved to be excellent lead compounds for the inhibition of NF-kB-p50 biological activity. At last, we demonstrated that apigenin and cyanidin chloride are able to modulate the expression of the NF-kB regulated IL-8 gene in CF IB3-1 cells, while oleuropein showed no effect in regulating the expression of the gene IL-8
Modulation of the expression of the proinflammatory IL-8 gene in cystic fibrosis cells by extracts deriving from olive mill waste water.
Full text linkA persistent recruitment of neutrophils in the bronchi of cystic fibrosis (CF) patients contributes to aggravate the airway tissue damage, suggesting the importance of modulating the expression of chemokines, including IL-8 during the management of the CF patients. Polyphenols rich extracts derived from waste water from olive mill, obtained by a molecular imprinting approach, have been investigated in order to discover compounds able to reduce IL-8 expression in human bronchial epithelial cells (IB3-1 cells), derived from a CF patient with a ΔF508/W1282X mutant genotype and stimulated with TNF-alpha. Initially, electrophoretic mobility shift assays (EMSAs) were performed to determine whether the different active principles were able to inhibit the binding between transcription factor (TF) NF-kappaB and DNA consensus sequences. Among different representative active principles present in the extract, three compounds were selected, apigenin, oleuropein, and cyanidin chloride, which displayed remarkable activity in inhibiting NF-kappaB/DNA complexes. Utilizing TNF-alpha-treated IB3-1 cells as experimental model system, we demonstrated that apigenin and cyanidin chloride are able to modulate the expression of the NF-kappaB-regulated IL-8 gene, while oleuropein showed no effect in regulating the expression of the gene IL-8
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