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Molecules 2015, 20(11), 20381-20390; doi:10.3390/molecules201119703

Nonprenylated Xanthones from Gentiana lutea, Frasera caroliniensis, and Centaurium erythraea as Novel Inhibitors of Vascular Smooth Muscle Cell Proliferation

1
Institute of Pharmacy/Pharmacognosy, University of Innsbruck, 6020 Innsbruck, Austria
2
Department of Pharmacognosy, University of Vienna, 1090 Vienna, Austria
3
School of Pharmacy, Yantai University, 264005 Yantai, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Pascal Richomme
Received: 30 September 2015 / Revised: 23 October 2015 / Accepted: 3 November 2015 / Published: 13 November 2015
(This article belongs to the Special Issue Coumarins, Xanthones and Related Compounds)
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Abstract

Aberrant proliferation of vascular smooth muscle cells (VSMC) plays a major role in restenosis, the pathological renarrowing of the blood vessel lumen after surgical treatment of stenosis. Since available anti-proliferative pharmaceuticals produce unfavorable side effects, there is high demand for the identification of novel VSMC proliferation inhibitors. A natural product screening approach using a resazurin conversion assay enabled the identification of gentisin (1) from Gentiana lutea as a novel inhibitor of VSMC proliferation with an IC50 value of 7.84 µM. Aiming to identify further anti-proliferative compounds, 13 additional nonprenylated xanthones, isolated from different plant species, were also tested. While some compounds showed no or moderate activity at 30 µM, 1-hydroxy-2,3,4,5-tetramethoxyxanthone (4), swerchirin (6), and methylswertianin (7) showed IC50 values between 10.2 and 12.5 µM. The anti-proliferative effect of 1, 4, 6, and 7 was confirmed by the quantification of DNA synthesis (BrdU incorporation) in VSMC. Cell death quantification (determined by LDH release in the culture medium) revealed that the compounds are not cytotoxic in the investigated concentration range. In conclusion, nonprenylated xanthones are identified as novel, non-toxic VSMC proliferation inhibitors, which might contribute to the development of new therapeutic applications to combat restenosis. View Full-Text
Keywords: atherosclerosis; bitter plants; Centaurium erythraea; Frasera caroliniensis; Gentiana lutea; Gentianaceae; gentisin; restenosis; vascular smooth muscle cell proliferation; xanthones. atherosclerosis; bitter plants; Centaurium erythraea; Frasera caroliniensis; Gentiana lutea; Gentianaceae; gentisin; restenosis; vascular smooth muscle cell proliferation; xanthones.
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Waltenberger, B.; Liu, R.; Atanasov, A.G.; Schwaiger, S.; Heiss, E.H.; Dirsch, V.M.; Stuppner, H. Nonprenylated Xanthones from Gentiana lutea, Frasera caroliniensis, and Centaurium erythraea as Novel Inhibitors of Vascular Smooth Muscle Cell Proliferation. Molecules 2015, 20, 20381-20390.

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