Phloroglucinol derivatives from Hypericum empetrifolium with antiproliferative activity on endothelial cells

Schmidt, Sebastian and Juergenliemk, Guido and Skaltsa, Helen and Heilmann, Joerg (2012) Phloroglucinol derivatives from Hypericum empetrifolium with antiproliferative activity on endothelial cells. PHYTOCHEMISTRY, 77. pp. 218-225. ISSN 0031-9422,

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Abstract

Five acylphloroglucinols substituted with monoterpenoids (empetrifelixin A-D and empetrikajaforin), three known monocyclic acylphloroglucinols and one monocyclic acylphloroglucinol were isolated from a petrol ether extract of Hypericum empetrifolium after fractionation by flash chromatography on silica gel, RP-18 and subsequent purification by preparative HPLC (RP-18). Their structures were elucidated by 1D, 2D NMR techniques and HREIMS. To determine a possible anti-angiogenic activity, inhibition of cell proliferation was measured using a human microvascular endothelial cell line (HMEC-1). Subconfluent grown HMEC-1 cells were treated with all compounds isolated in sufficient amounts and stained with crystal violet. Highest activity was observed for empetrifelixin A and empetrifelixin D showing a concentration dependent inhibition of cell proliferation with IC50 values of 6.5 +/- 0.1 and 7.3 +/- 0.4 mu M, respectively. Empetrifelixin A also showed activity in a cell migration assay with HMEC-1 cells in low micromolar concentrations. (C) 2011 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: ACYLPHLOROGLUCINOL DERIVATIVES; HYPERFORIN; ANTIBACTERIAL; INHIBITOR; PAPUANUM; ERECTUM; Hypericum empetrifolium; Hypericaceae; Acylphloroglucinols; Anti-angiogenic activity; NMR guided fractionation
Subjects: 600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann)
Depositing User: Dr. Gernot Deinzer
Date Deposited: 15 May 2020 07:16
Last Modified: 15 May 2020 07:16
URI: https://pred.uni-regensburg.de/id/eprint/18839

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