Next Article in Journal
Plasma Levels of Preβ1-HDL Are Significantly Elevated in Non-Dialyzed Patients with Advanced Stages of Chronic Kidney Disease
Next Article in Special Issue
Moringin from Moringa Oleifera Seeds Inhibits Growth, Arrests Cell-Cycle, and Induces Apoptosis of SH-SY5Y Human Neuroblastoma Cells through the Modulation of NF-κB and Apoptotic Related Factors
Previous Article in Journal
Natural History of a Satellite DNA Family: From the Ancestral Genome Component to Species-Specific Sequences, Concerted and Non-Concerted Evolution
Previous Article in Special Issue
Thymoquinone Selectively Kills Hypoxic Renal Cancer Cells by Suppressing HIF-1α-Mediated Glycolysis
Article Menu
Issue 5 (March-1) cover image

Export Article

Open AccessCommunication
Int. J. Mol. Sci. 2019, 20(5), 1203; https://doi.org/10.3390/ijms20051203

Antiproliferative and Cytotoxic Activity of Xanthohumol and Its Non-Estrogenic Derivatives in Colon and Hepatocellular Carcinoma Cell Lines

1
Department of Biochemistry and Biophysics, Linus Pauling Institute, Oregon State University, Corvallis, OR 97331, USA
2
Department of Pharmaceutical Sciences, Linus Pauling Institute, Oregon State University, Corvallis, OR 97331, USA
3
Department of Microbiology, Linus Pauling Institute, Oregon State University, Corvallis, OR 97331, USA
4
Department of Chemistry, Oregon State University, Corvallis, OR 97331, USA
5
Linus Pauling Institute, Department of Biochemistry and Biophysics, Oregon State University, Corvallis, OR 97331, USA
*
Author to whom correspondence should be addressed.
Received: 5 February 2019 / Revised: 28 February 2019 / Accepted: 5 March 2019 / Published: 9 March 2019
(This article belongs to the Special Issue Bioactive Phytochemicals for Cancer Prevention and Treatment)
  |  
PDF [1911 KB, uploaded 9 March 2019]
  |  

Abstract

Xanthohumol (XN), a prenylated flavonoid found in hops, inhibits growth in a variety of cancer cell lines; however, its use raises concerns as gut microbiota and the host’s hepatic cytochrome P450 enzymes metabolize it into the most potent phytoestrogen known, 8-prenylnaringenin (8-PN). The XN derivatives dihydroxanthohumol (DXN) and tetrahydroxanthohumol (TXN) are not metabolized into 8-PN and they show higher tissue concentrations in vivo compared with XN when orally administered to mice at the same dose. Here we show that DXN and TXN possess improved anti-proliferative activity compared with XN in two colon (HCT116, HT29) and two hepatocellular (HepG2, Huh7) carcinoma cell lines, as indicated by their respective IC50 values. Furthermore, XN, DXN, and TXN induce extensive apoptosis in all these carcinoma cell lines. Finally, TXN induces G0/G1 cell cycle arrest in the colon carcinoma cell line HT29. Our findings suggest that DXN and TXN could show promise as therapeutic agents against colorectal and liver cancer in preclinical studies without the drawback of metabolism into a phytoestrogen. View Full-Text
Keywords: xanthohumol; polyphenol; flavonoid; apoptosis; colon cancer; dihydroxanthohumol; tetrahydroxanthohumol; cell cycle; phytochemical; chemoprevention; dietary agent xanthohumol; polyphenol; flavonoid; apoptosis; colon cancer; dihydroxanthohumol; tetrahydroxanthohumol; cell cycle; phytochemical; chemoprevention; dietary agent
Figures

Graphical abstract

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).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

Logan, I.E.; Miranda, C.L.; Lowry, M.B.; Maier, C.S.; Stevens, J.F.; Gombart, A.F. Antiproliferative and Cytotoxic Activity of Xanthohumol and Its Non-Estrogenic Derivatives in Colon and Hepatocellular Carcinoma Cell Lines. Int. J. Mol. Sci. 2019, 20, 1203.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top