Structure-proteasome-inhibitory activity relationships of dietary flavonoids in human cancer cells
- PMID: 17127432
- DOI: 10.2741/2199
Structure-proteasome-inhibitory activity relationships of dietary flavonoids in human cancer cells
Abstract
Diet high in vegetables and fruits has been associated with reduced cancer risk. However, the involved mechanisms are unknown. Previously, we reported that the dietary flavonoid apigenin could inhibit the proteasome activity and induce apoptosis in tumor cells. To further investigate the structure-proteasome-inhibitory activity relationships, we chose and tested five dietary flavonoids, including luteolin, apigenin, chrysin, naringenin and eriodictyol. We found that the order of inhibitory potencies and apoptosis-inducing potencies of these five compounds in 20S purified proteasome and tumor cells was: (1) luteolin > apigenin > chrysin, and (2) apigenin >> naringenin, and luteolin >> eriodictyol. Therefore, flavonoids with hydroxylized B ring and/or unsaturated C ring are natural potent proteasome inhibitors and tumor cell apoptosis inducers. Furthermore, neither apigenin nor luteolin could inhibit the proteasome and induce apoptosis in non-transformed human natural killer cells. This finding may provide a molecular basis for the clinically observed cancer-preventive effects of fruits and vegetables.
Similar articles
-
Apigenin, chrysin, and luteolin selectively inhibit chymotrypsin-like and trypsin-like proteasome catalytic activities in tumor cells.Planta Med. 2010 Feb;76(2):128-32. doi: 10.1055/s-0029-1186004. Epub 2009 Aug 3. Planta Med. 2010. PMID: 19653143
-
Anti-carcinogenic effects of the flavonoid luteolin.Molecules. 2008 Oct 22;13(10):2628-2651. doi: 10.3390/molecules13102628. Molecules. 2008. PMID: 18946424 Free PMC article. Review.
-
Inhibition of proteasome activity by the dietary flavonoid apigenin is associated with growth inhibition in cultured breast cancer cells and xenografts.Breast Cancer Res. 2007;9(6):R80. doi: 10.1186/bcr1797. Breast Cancer Res. 2007. PMID: 18300387 Free PMC article.
-
The antitumor activities of flavonoids.In Vivo. 2005 Sep-Oct;19(5):895-909. In Vivo. 2005. PMID: 16097445 Review.
-
Dietary flavonoids as proteasome inhibitors and apoptosis inducers in human leukemia cells.Biochem Pharmacol. 2005 May 15;69(10):1421-32. doi: 10.1016/j.bcp.2005.02.022. Biochem Pharmacol. 2005. PMID: 15857606
Cited by
-
Evolution of Natural Product Scaffolds as Potential Proteasome Inhibitors in Developing Cancer Therapeutics.Metabolites. 2023 Mar 31;13(4):509. doi: 10.3390/metabo13040509. Metabolites. 2023. PMID: 37110167 Free PMC article. Review.
-
Hydroxylation decoration patterns of flavonoids in horticultural crops: chemistry, bioactivity and biosynthesis.Hortic Res. 2022 Jan 20;9:uhab068. doi: 10.1093/hr/uhab068. Online ahead of print. Hortic Res. 2022. PMID: 35048127 Free PMC article.
-
Phenolic Profiling and Therapeutic Potential of Certain Isolated Compounds from Parkia roxburghii against AChE Activity as well as GABAA α5, GSK-3β, and p38α MAP-Kinase Genes.ACS Omega. 2021 Jul 26;6(31):20492-20511. doi: 10.1021/acsomega.1c02340. eCollection 2021 Aug 10. ACS Omega. 2021. PMID: 34395996 Free PMC article.
-
Inhibitory Effect of Delphinidin on Oxidative Stress Induced by H2O2 in HepG2 Cells.Oxid Med Cell Longev. 2020 Nov 20;2020:4694760. doi: 10.1155/2020/4694760. eCollection 2020. Oxid Med Cell Longev. 2020. PMID: 33274001 Free PMC article.
-
Targeting Ubiquitin-Proteasome Pathway by Natural Products: Novel Therapeutic Strategy for Treatment of Neurodegenerative Diseases.Front Physiol. 2020 Apr 28;11:361. doi: 10.3389/fphys.2020.00361. eCollection 2020. Front Physiol. 2020. PMID: 32411012 Free PMC article.