Title:(Iso)Flav(an)ones, Chalcones, Catechins, and Theaflavins as Anticarcinogens: Mechanisms, Anti-Multidrug Resistance and QSAR Studies
Volume: 19
Issue: 25
Author(s): Andrew G. Mercader and Alicia B. Pomilio
Affiliation:
Keywords:
Anticarcinogens, flavonoids, (iso)flavones, flavanones, catechins, chalcones, QSAR, theaflavins, TRAIL, flavonoids/TRAIL, flavonoids/chemotherapy
Abstract: Flavonoids have shown anticarcinogenic activity in cancer cell lines, animal models, and some human studies. Quantitative
structure-activity relationship (QSAR) models have become useful tools for identification of promising lead compounds in anticancer
drug development. However, epidemiological and clinical studies are still scarce. Compounds with flavonoid scaffold have been the subject
of many mechanistic studies in cells, but information on human chemopreventive properties is still missing. The knowledge of the
mechanisms of action, anti-multidrug resistance, and QSAR studies on flavonoids and related compounds may help to enhance research
on these compounds and their bioactivity. Therefore, once the issue is introduced, the mechanisms involved, and QSAR studies developed
to predict the activity and toxicity of these chemicals to biological systems are discussed. QSAR studies on flavonoids as inhibitors
of breast cancer resistance protein (BCRP/ABCG2), 17β-hydroxysteroid dehydrogenase (17β-HSD), PIM-1 kinase and cyclin-dependent
kinases (CDKs) are analyzed. Combined treatment of flavonoids with TRAIL and current chemotherapy agents is also discussed as a
promising cancer chemoprevention and/or therapy.
