A new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one suppresses prostate cancer involving p53-mediated cell cycle arrests and apoptosis.
A new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one suppresses prostate cancer involving p53-mediated cell cycle arrests and apoptosis.
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发表时间：
2012-09
影响因子：
2
通讯作者：
Yong Zhang;B. Srinivasan;Chengguo Xing;J. Lü
中科院分区：
文献类型：
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作者：
Yong Zhang;B. Srinivasan;Chengguo Xing;J. Lü
以前的研究表明查耳酮作为抗肿瘤药物的候选者。我们合成了一种新的查耳酮衍生物（E）-3-（4-甲氧基苯基）-2-甲基-1-（3，4，5-三甲氧基苯基）丙-2-烯-1-酮（CHO 27），在细胞培养试验中，其细胞毒性效力相对于其母体化合物增加高达1000倍。低纳摩尔水平的CHO 27通过细胞周期停滞和半胱天冬酶依赖性凋亡抑制前列腺癌（PCa）细胞生长。p53的激活至少部分地解释了CHO 27在体外的生长抑制作用。此外，腹腔注射CHO 27可抑制已建立的PCa 22 Rv 1异种移植肿瘤的生长，并伴有p53和p21（Cip 1）诱导。CHO 27可能是开发新的前列腺癌治疗药物的先导。
Previous studies suggested chalcones as antineoplastic drug candidates. We synthesized a new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one, (CHO27) with an up to 1000-fold increased cytotoxic potency relative to its parent compound in cell culture assays. CHO27 at low nanomolar levels, inhibited prostate cancer (PCa) cell growth through cell cycle arrest and caspase-dependent apoptosis. Activation of p53 accounted for, at least in part, the growth inhibition by CHO27 in vitro. Furthermore, i.p. administration of CHO27 suppressed the growth of established PCa 22Rv1 xenograft tumors accompanied with p53 and p21(Cip1) induction. CHO27 may be a lead for development of new therapeutic agents for PCa.