FBA-TPQ，一种新型海洋来源化合物，作为前列腺癌的实验治疗方法。
FBA-TPQ, a novel marine-derived compound as experimental therapy for prostate cancer.
机构信息
Division of Clinical Pharmacology, Department of Pharmacology and Toxicology, University of Alabama at Birmingham, 1670 University Blvd, 113 Volker Hall, Birmingham, AL 35294, USA.
出版信息
Invest New Drugs. 2010 Jun;28(3):234-41. doi: 10.1007/s10637-009-9232-x. Epub 2009 Mar 10.
Abstract
We recently synthesized a series of novel makaluvamine compounds, and found that the most potent was FBA-TPQ. The effects of FBA-TPQ on human (LNCaP and PC3) and murine (TRAMP C1) prostate cancer cells were evaluated. Potential mechanisms of action of the compound were also determined. FBA-TPQ exhibited dose-dependent cytotoxicity in the low micromolar range, inhibited proliferation, caused cell cycle arrest, and induced apoptosis in prostate cancer cell lines. The compound also decreased the expression of the androgen receptor and PSA. The results presented herein support the further development of FBA-TPQ as a novel agent for prostate cancer.
摘要
我们最近合成了一系列新型的马卡鲁瓦明化合物，发现其中最有效的是 FBA-TPQ。我们评估了 FBA-TPQ 对人（LNCaP 和 PC3）和鼠（TRAMP C1）前列腺癌细胞的影响。还确定了该化合物的潜在作用机制。FBA-TPQ 在低微摩尔范围内表现出剂量依赖性细胞毒性，抑制增殖，导致细胞周期停滞，并诱导前列腺癌细胞系凋亡。该化合物还降低了雄激素受体和 PSA 的表达。本文提供的结果支持进一步开发 FBA-TPQ 作为一种新型前列腺癌药物。
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