Influence of L-rhamnosyl-D-glucosyl derivatives on properties and biological interaction of flavonoids.
The anti-proliferative activity of hesperetin, hesperidin, neohesperidin and rutin was evaluated on human hepatoma cell lines (Hep G2) and correlated to their antioxidant activity. The results obtained showed strong anti-proliferative effects of hesperidin and neohesperidin, considerably higher than the other two additives. Hesperetin induced caspase-3 activation, release of LDH and endogenous accumulation of putrescine. Cell cycle distribution seems to indicate that the inhibitory effects of polyphenols on cell growth could be due to G0/G1 block, and activation of apoptotic pathway in the presence of hesperetin. Our results underline also that the glycone forms show reduced scavenging activity against DPPH, but present a remarkable inhibition of cell proliferation and low cytotoxicity.
Bellocco
Ersilia
E
Department of Organic and Biological Chemistry, University of Messina, Messina, Italy. bellocco@isengard.unime.it
Barreca
Davide
D
Laganà
Giuseppina
G
Leuzzi
Ugo
U
Tellone
Ester
E
Ficarra
Silvana
S
Kotyk
Arnost
A
Galtieri
Antonio
A
D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D015415:Biomarkers / Q000378:metabolism; D001713:Biphenyl Compounds / Q000378:metabolism; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D005419:Flavonoids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D005609:Free Radicals / Q000378:metabolism; D006569:Hesperidin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D010851:Picrates / Q000378:metabolism; D011073:Polyamines / Q000378:metabolism; D012431:Rutin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
D015415:Biomarkers; D001713:Biphenyl Compounds; D005419:Flavonoids; D005609:Free Radicals; D010851:Picrates; D011073:Polyamines; D012431:Rutin; C004931:1,1-diphenyl-2-picrylhydrazyl; D006569:Hesperidin; D053148:Caspase 3; C013015:hesperetin