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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Freischmidt, A. Jürgenliemk, G. Kraus, B. Okpanyi, S. N. Müller, J. Kelber, O. Weiser, D. Heilmann, J. |
| Description | Country affiliation: Germany Author Affiliation: Freischmidt A ( Lehrstuhl für Pharmazeutische Biologie, Universität Regensburg, 93040 Regensburg, Germany.) |
| Abstract | INTRODUCTION: A quantified aqueous Willow bark extract (STW 33-I) was tested concerning its inhibitory activity on TNF- induced ICAM-1 expression in human microvascular endothelial cells (HMEC-1) and further fractionated to isolate the active compounds. RESULTS: At 50 µg/ml the extract, which had been prepared from Salix purpurea L., decreased ICAM-1 expression to 40% compared to control cells without showing cytotoxic effects. Further liquid-liquid partition revealed an ethyl acetate phase with potent reduction of ICAM-1 expression to 40% at 8 µg/ml. This fraction was comprehensively characterised by the isolation of flavanone aglyca and their corresponding glycosides, chalcone glycosides, salicin derivatives, cyclohexane-1,2-diol glycosides, catechol and trans-p-coumaric acid. All compounds were investigated for their activity on TNF- induced ICAM-1 expression. The flavonoid and chalcone glycosides were not active up to 50 µM, whereas catechol and eriodictyol at the same concentration showed a significant reduction of ICAM-1 expression to 50% of control. Interestingly, other isolated flavanone aglyca like taxifolin, dihydrokaempferol and naringenin showed only weak or moderate inhibitory activity. Eriodictyol was a minor compound in the extract, whereas the catechol content in the extract (without excipients) reached 2.3%, determined by HPLC. One of the isolated cyclohexan-1,2-diol glucosides, 6'-O-4-hydroxybenzoyl-grandidentin, is a new natural compound. CONCLUSION: As catechol is quantitatively important in Willow bark extracts it can be concluded from the in vitro data that not only flavonoids and salicin derivatives, but also catechol can probably contribute to the anti-inflammatory activity of Willow bark extracts. |
| File Format | HTM / HTML |
| ISSN | 09447113 |
| Issue Number | 3-4 |
| Volume Number | 19 |
| e-ISSN | 1618095X |
| Journal | Phytomedicine |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2012-02-15 |
| Publisher Place | Germany |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Complementary Therapies Catechols Pharmacology Endothelial Cells Drug Effects Flavonoids Intercellular Adhesion Molecule-1 Metabolism Plant Bark Chemistry Plant Extracts Acetates Anti-inflammatory Agents Isolation & Purification Cell Survival Chemical Fractionation Instrumentation Methods Chromatography, High Pressure Liquid Coumaric Acids Flavanones Humans Molecular Structure Quercetin Analogs & Derivatives Salix Tumor Necrosis Factor-alpha Adverse Effects Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Drug Discovery Molecular Medicine Pharmacology Complementary and Alternative Medicine Pharmaceutical Science |
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