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

Autor: Claudia S. Maier, Adrian F. Gombart, Malcolm B. Lowry, Cristobal L. Miranda, Jan F. Stevens, Isabelle E. Logan
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Cell cycle checkpoint
Colorectal cancer
dietary agent
phytochemical
lcsh:Chemistry
chemistry.chemical_compound
0302 clinical medicine
Cytotoxic T cell
chemoprevention
lcsh:QH301-705.5
Spectroscopy
0303 health sciences
Propiophenones
Communication
Cell Cycle
Liver Neoplasms
apoptosis
General Medicine
Hep G2 Cells
Cell cycle
3. Good health
Computer Science Applications
colon cancer
030220 oncology & carcinogenesis
Xanthohumol
Colonic Neoplasms
Liver cancer
HT29 Cells
Carcinoma
Hepatocellular
Antineoplastic Agents
tetrahydroxanthohumol
Catalysis
Inorganic Chemistry
03 medical and health sciences
In vivo
medicine
Humans
flavonoid
Physical and Theoretical Chemistry
Molecular Biology
030304 developmental biology
Cell Proliferation
Flavonoids
Organic Chemistry
medicine.disease
HCT116 Cells
digestive system diseases
xanthohumol
polyphenol
dihydroxanthohumol
chemistry
lcsh:Biology (General)
lcsh:QD1-999
Apoptosis
Cancer research
Zdroj: International Journal of Molecular Sciences
International Journal of Molecular Sciences, Vol 20, Iss 5, p 1203 (2019)
ISSN: 1422-0067
Popis: 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.
Databáze: OpenAIRE
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