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. 2018 Nov 9;23(11):2922.
doi: 10.3390/molecules23112922.

Highly Cancer Selective Antiproliferative Activity of Natural Prenylated Flavonoids

Agnieszka Bartmańska  1 , Tomasz Tronina  2 , Jarosław Popłoński  3 , Magdalena Milczarek  4 , Beata Filip-Psurska  5 , Joanna Wietrzyk  6
Affiliations

Highly Cancer Selective Antiproliferative Activity of Natural Prenylated Flavonoids

Agnieszka Bartmańska et al. Molecules. .

Abstract

Xanthohumol (XN) and four minor hops prenylflavonoids: α,β-dihydroxanthohumol (2HXN), isoxanthohumol (IXN), 8-prenylnaringenin (8PN), and 6-prenylnaringenin (6PN), were tested for antiproliferative activity towards human cancer and normal cell lines. Nonprenylated naringenin (NG) was used as a model compound. Xanthohumol, α,β-dihydroxanthohumol and 6-prenylnaringenin were the most active compounds. Xanthohumol exhibited higher antiproliferative activity than cisplatin (CP) against five cancer cell lines: ovarian resistant to cisplatin A2780cis, breast MDA-MB-231 and T-47D, prostate PC-3, and colon HT-29. Isoxanthohumol was more potent than cisplatin against breast cancer cell lines MDA-MB-231 and T-47D whereas 6-prenylnaringenin was stronger than cisplatin against breast cancer cell line T-47D. It was found that tested chalcones possessed highly selective antiproliferative activity towards all tested breast cancer lines compared to the normal breast MCF 10A cell line (the calculated selectivity index ranged from 5 to 10). Low antiproliferative activity of naringenin indicates the importance of the prenyl group with respect to antiproliferative activity.

Keywords: antiproliferative activity; hop flavonoids; phytoestrogen; selectivity.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structures of tested flavonoids.
Figure 2
Figure 2
Antiproliferative activity of tested flavonoids and cisplatin against human cancer cell lines (marked red) and normal ones (marked blue).
Figure 3
Figure 3
The selectivity indexes (SIA) which represents IC50 for a normal cell line (HLMEC)/IC50 and for a cancerous cell line.
Figure 4
Figure 4
The selectivity indexes (SIB) which represents IC50 for a normal cell line (MCF 10A) /IC50 and for a cancerous cell line.
See this image and copyright information in PMC

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