Although traditional therapies using natural sources have been used for
thousands of years, neither the active components nor their molecular targets have been very well
defined. Identification of the active
chemical entities and molecular targets
of these natural products is an active
area of research. Up to 70% of all drugs currently used for the
treatment of cancer were derived from natural sources . In
particular, studies have shown that
xanthohumol (XN; 2’,4’,6’,4-tetrahydroxy-3’-prenylchalcone), a prenylated chalcone isolated from the hop
plant (Humulus lupulus L.) (2) , inhibits the growth
of different types of human cancer
cells, including breast,
colon, ovarian, and prostate cancer cells; leukemia cells; and adipocytes (3-11) , and prevents the development of carcinogen-induced preneoplastic lesions in mouse
mammary gland organ culture (5) . Researchers also
showed that this chalcone inhibits tumor cell invasion (12) angiogenesis (13) , and bone resorption (7).
XN has been shown to inhibit
NF-kB activation I3, 14, suppresses the activity of diacylglycerol acyltransferase which is involved in triglyceride
synthesis (15, 16), downregulate topoisomerase 1 (17) and aromatase (18), and
inhibit nitric oxide (19) and
prostaglandin E2 production (5). Additionally, others have
described both caspase-dependent (3) and -independent (6) activation of apoptosis by XN.
Furthermore, this compound inhibits phase I
cytochrome P450 enzyme which is involved in metabolic activation of carcinogens (20) and induces phase II
enzyme NAD(P)H:quinone reductase (21). XN was found
to activate the famesoid X receptor (FXR) (22) , inhibits triglyceride and apolipoprotein B secretion (23), and
exhibits antidiabetic activity through the inhibition of lipid and
glucose metabolism (22).
Xanthohumol is contained in the yellow pollen of the female hops flowers. It has anti-bacterial, anti-fungal, and anti-viral properties to protect the flowers, as part of the survival of the plant.