Compounds from Wedelia chinensis synergistically suppress androgen activity and growth in prostate cancer cells
Compounds from Wedelia chinensis synergistically suppress androgen activity and growth in prostate cancer cells
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DOI：
10.1093/carcin/bgm137
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发表时间：
2007-12-01
期刊：
影响因子：
4.7
通讯作者：
Hsiao, Pei-Wen
中科院分区：
文献类型：
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作者：
Lin, Feng-Min;Chen, Li-Ru;Hsiao, Pei-Wen
慢性炎症可以促进各种癌症的肿瘤发展，包括前列腺癌（PCa）。因此，减少炎症是一个重要的抗癌治疗机会。在这里，我们报告了蟛蜞菊（一种东方草药）中的四种抗增殖植物化合物，通过它们调节 PCa 细胞中前列腺特异性抗原启动子转录的雄激素受体 (AR) 激活的能力来鉴定。 3-吲哚醛、蟛蜞菊内酯、木犀草素和芹菜素的50％抑制浓度值分别为34.9、0.2、2.4和9.8μM。以与草药提取物相同比例混合植物化合物的配方减少了实现最大 AR 抑制所需的每种化合物的剂量。与 AR 抑制作用相关，这些活性化合物特异性抑制 AR 依赖性 PCa 细胞的生长，并且作为组合配方，它们还协同抑制 AR 依赖性 PCa 细胞的生长。我们的研究已经确定了W. chinensis中活性化合物的协同作用，并证明了它们在前列腺癌预防和治疗中的潜力。多种活性和协同作用的范式是研究各种药用植物物种完整提取物的治疗效果的有用框架。
Chronic inflammation can augment tumor development in various types of cancers, including prostate cancer (PCa). Reduction of inflammation is therefore an important anticancer therapeutic opportunity. Here, we report four anti-proliferative phytocompounds in Wedelia chinensis, an oriental herbal medicine, identified through their ability to modulate the androgen receptor (AR) activation of transcription from prostate-specific antigen promoter in PCa cells. The 50% inhibition concentration values of indole-3-carboxylaldehyde, wedelolactone, luteolin and apigenin, were 34.9, 0.2, 2.4 and 9.8 mu M, respectively. A formula that combined the phytocompounds in the same proportions as in the herbal extract decreased the dosage of each compound required to achieve maximal AR inhibition. In correlation with the AR suppression effect, these active compounds specifically inhibited the growth of AR-dependent PCa cells and as a combination formula they also synergistically suppressed growth in AR-dependent PCa cells. Our study has identified synergistic effects of active compounds in W. chinensis and demonstrated their potential in PCa prevention and therapy. The paradigm of multiple activities and synergism is a useful framework to investigate the therapeutic effects of whole extracts from assorted medicinal plant species.