| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Phytochemistry | ||||
| Publisher: | PERGAMON-ELSEVIER SCIENCE LTD | ||||
| Place of Publication: | OXFORD | ||||
| Volume: | 90 | ||||
| Page Range: | pp. 106-113 | ||||
| Date: | 2013 | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) | ||||
| Identification Number: |
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| Keywords: | UNDERGROUND PARTS; CYTOSTATIC ACTIVITY; HL-60 CELLS; ACULEATUS L; FORT; Ruscus aculeatus; Endothelium; Permeability; Esculin; Spirostanol saponins | ||||
| Dewey Decimal Classification: | 600 Technology > 615 Pharmacy | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 62555 |
Web of ScienceAbstract
Rusci rhizoma extracts are traditionally used against chronic venous disorders (CVD). To determine the effect of its secondary plant metabolites on the endothelium, phenolic compounds and saponins from Butcher's broom were isolated from a methanolic extract, and their activity on the thrombin-induced hyperpermeability of human microvascular endothelial cells (HMEC-1) was investigated in vitro. In ...
Abstract
Rusci rhizoma extracts are traditionally used against chronic venous disorders (CVD). To determine the effect of its secondary plant metabolites on the endothelium, phenolic compounds and saponins from Butcher's broom were isolated from a methanolic extract, and their activity on the thrombin-induced hyperpermeability of human microvascular endothelial cells (HMEC-1) was investigated in vitro. In addition to the six known spirostanol saponins deglucoruscin (5), 22-O-methyl-deglucoruscoside (6), deglucoruscoside (7), ruscin (8), ruscogenin-1-O-(alpha-L-rhamnopyranosyl-(1 -> 2)-beta-D-galactopyranoside (9) and 1-O-sulpho-ruscogenin (10), three new spirostanol derivatives were isolated and identified: 3'-O-acetyl-4'-O-sulphodeglucoruscin (1), 4'-O-(2-hydroxy-3-methylpentanoyl)-deglucoruscin (2) and 4'-O-acetyl-deglucoruscin (3). Furthermore, the coumarin esculin (4), which is also prominently present in other medicinal plants used in the treatment of CVD, was isolated for the first time from Rusci rhizoma. Five of the isolated steroid derivatives (2, 5, 8, 9 and 10) and esculin (4) were tested for their ability to reduce the thrombin-induced hyperpermeability of endothelial cells in vitro, and the results were compared to those of the aglycone neoruscogenin (11). The latter compound showed a slight but concentration-dependent reduction in hyperpermeability to 71.8% at 100 mu M. The highest activities were observed for the spirostanol saponins 5 and 8 and for esculin (4) at 10 mu M, and these compounds resulted in a reduction of the thrombin-induced hyperpermeability to 41.9%, 42.6% and 533%, respectively. For 2, 5 and 8, the highest concentration tested (100 mu M) resulted in a drastic increase of the thrombin effect. The effect of esculin observed at a concentration of 10 mu M was diminished at 100 mu M. These in vitro data provide insight into the pharmacological mechanism by which the genuine spirostanol saponins and esculin can contribute to the efficacy of Butcher's broom against chronic venous disorders. (C) 2013 Elsevier Ltd. All rights reserved.
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