GROWTH-INHIBITORY EFFECT OF QUERCETIN AND PRESENCE OF TYPE-II ESTROGEN-BINDING SITES IN PRIMARY HUMAN TRANSITIONAL-CELL CARCINOMAS
GROWTH-INHIBITORY EFFECT OF QUERCETIN AND PRESENCE OF TYPE-II ESTROGEN-BINDING SITES IN PRIMARY HUMAN TRANSITIONAL-CELL CARCINOMAS
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DOI：
10.1016/s0022-5347(17)32649-6
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发表时间：
1994-09-01
影响因子：
6.6
通讯作者：
CAPELLI, A
中科院分区：
文献类型：
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作者：
LAROCCA, LM;GIUSTACCHINI, M;CAPELLI, A
对8例膀胱移行细胞癌（TCC）进行了雌激素受体（ER）和Ⅱ型雌激素结合位点（Ⅱ型EBS）的研究。所有这些肿瘤特异性表达II型EBS，而8例中只有3例含有少量ER。所有的情况下，分析核和细胞质II型EBS的存在下，揭示了这些结合位点的存在下，在两个隔室。细胞质和细胞核受体类似于在其他组织中描述的II型EBS，相对于它们对雌激素和槲皮素的结合特异性以及它们对还原剂的敏感性。槲皮素，10 μ M，有效地抑制体外由TCC细胞的溴脱氧尿苷（BrdUdR）掺入。大黄素，结合很少，如果有的话，II型EBS，并没有表现出任何抑制作用，在体外BrdUdR掺入肿瘤细胞，表明II型EBS介导的黄酮类化合物的影响。虽然槲皮素的抗增殖活性的机制仍有待充分阐明，槲皮素和相关的黄酮类化合物的可能的治疗潜力应被考虑。
Eight cases of transitional cell carcinoma (TCC) of the bladder were investigated for the presence of estrogen receptors (ER) and Type II estrogen binding sites (Type II EBS). All these tumors specifically expressed type II EBS, while only 3 of 8 cases contained low amounts of ER. All the cases assayed for the presence of both nuclear and cytoplasmic type II EBS revealed the presence of these binding sites in the two compartments. Both cytoplasmic and nuclear receptors were similar to type II EBS described in other tissues relative to their binding specificity for estrogens and quercetin and their sensitivity to reducing agents. Quercetin, 10 mu M., was effective in inhibiting in vitro bromodeoxyuridine (BrdUdR) incorporation by TCC cells. Rutin, which bound little if any to type II EBS, did not show any inhibitory effect on in vitro BrdUdR incorporation by tumor cells, suggesting a type II EBS mediated effect of flavonoids. Although the mechanism of the antiproliferative activity of quercetin remains to be fully clarified, the possible therapeutic potential of quercetin and related flavonoids should be considered.