Effects of the flavonoid baicalin and its metabolite baicalein on androgen receptor expression, cell cycle progression and apoptosis of prostate cancer cell lines
Effects of the flavonoid baicalin and its metabolite baicalein on androgen receptor expression, cell cycle progression and apoptosis of prostate cancer cell lines
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DOI：
10.1046/j.0960-7722.2001.00213.x
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发表时间：
2001-10-01
影响因子：
8.5
通讯作者：
Darzynkiewicz, Z
中科院分区：
文献类型：
--
作者：
Chen, S;Ruan, Q;Darzynkiewicz, Z
最近对中草药 PC SPES 的研究表明，其在体外、体内和晚期患者体内具有抗前列腺癌的生物活性。在研究其作用方式时，我们分离出了一些活性化合物。 HPLC测定，PC SPES乙醇提取物中黄芩苷含量最高（约6%）。已知黄芩苷在体内通过糖苷部分的裂解转化为黄芩素。因此，比较它们的体外活性是有用的。分别在雄激素阳性和阴性人类前列腺癌细胞系 LNCaP 和 JCA-1 中研究了黄芩苷和黄芩素的作用。在浓度分别为 60.8 +/- 3.2 和 29.8 +/- 2.2 muM 黄芩苷和黄芩素时，观察到 LNCaP 细胞中细胞生长被抑制 50% (ED50)。在雄激素阴性 JCA-1 细胞中观察到更有效的生长抑制作用，黄芩苷和黄芩素的 ED50 值分别为 46.8 +/- 0.7 和 17.7 +/- 3.4。因此，这些类黄酮对细胞生长的抑制似乎与雄激素受体状态无关。两种药物 (1) 在 ED50 浓度下引起 G(1) 细胞明显积聚，(2) 在较高浓度下诱导细胞凋亡，以及 (3) 降低 LNCaP 细胞中雄激素受体的表达。
Recent studies on the Chinese herbal medicine PC SPES showed biological activities against prostate cancer in vitro, in vivo and in patients with advanced stages of the disease. In investigating its mode of action, we have isolated a few of the active compounds. Among them, baicalin was the most abundant (about 6%) in the ethanol extract of PC SPES, as determined by HPLC. Baicalin is known to be converted in vivo to baicalein by the cleavage of the glycoside moiety. Therefore, it is useful to compare their activities in vitro. The effects of baicalin and baicalein were studied in androgen-positive and -negative human prostate cancer lines LNCaP and JCA-1, respectively. Inhibition of cell growth by 50% (ED50) in LNCaP cells was seen at concentrations of 60.8 +/- 3.2 and 29.8 +/- 2.2 muM baicalin and baicalein, respectively. More potent growth inhibitory effects were observed in androgen-negative JCA-1 cells, for which the ED50 values for baicalin and baicalein were 46.8 +/- 0.7 and 17.7 +/- 3.4, respectively. Thus, it appears that cell growth inhibition by these flavonoids is independent of androgen receptor status. Both agents (1) caused an apparent accumulation of cells in G(1) at the ED50 concentration, (2) induced apoptosis at higher concentrations, and (3) decreased expression of the androgen receptor in LNCaP cells.