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Type-II estrogen binding sites in a lymphoblastoid cell line and growth-inhibitory effect of estrogen, anti-estrogen and bioflavonoids

✍ Scribed by Giovanni Scambia; Franco O. Ranelletti; Pierluigi Benedetti Panici; Mauro Piantelli; Carlo Rumi; Francesco Battaglia; Luigi M. Larocca; Amaldo Capelli; Salvatore Mancuso

Publisher
John Wiley and Sons
Year
1990
Tongue
French
Weight
566 KB
Volume
46
Category
Article
ISSN
0020-7136

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✦ Synopsis

Type4 estrogen-binding sites (type-ll EBS) have been demonstrated in the human lymphoblastoid cell line IM-9 using a whole-cell assay with (6,7-'H) estradiol ('H-E,) as tracer. Competition analysis showed that the anti-estrogen tamoxifen and the flavonoids quercetin and rutin competed for (lH)-E, binding to type-It EBS. Growth experiments demonstrated that diethylstilbestrol (DES) tamoxifen (TAM), quercetin and rutin exerted a reversible dose-dependent inhibition of cell proliferation in the range of concentrations between I 0 nM and 10 WM. The relative binding affinity of quercetin, rutin, DES and TAM for type-ll EBS correlated well with their potency as cell growth inhibitors. Moreover, hesperidin, a flavonoid which does not bind to type-ll EBS, was ineffective in inhibiting cell growth. Cell-cycle analysis showed that the growth-inhibitory effect of DES, TAM or quercetin was due to a blocking effect in the G,-G, phases. Our results suggest that high estrogen and anti-estrogen concentrations and flavonoids may regulate IM-9 cell growth through a common mechanism involving a binding interaction with type-ll EBS.

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