Porto Conte Ricerche, Località Tramariglio, 07041 Alghero, Sassari, Italy.
J Med Chem. 2011 Mar 10;54(5):1321-32. doi: 10.1021/jm1013715. Epub 2011 Feb 9.
Molecular targeted cancer therapy mediated by nanoparticles (NPs) is a promising strategy to overcome the lack of specificity of conventional chemotherapeutic agents. In this context, the prostate-specific membrane antigen (PSMA) has demonstrated a powerful potential for the management of prostate cancer (PCa). Cancer chemoprevention by phytochemicals is emerging as a suitable approach for the treatment of early carcinogenic processes. Since (-)-epigallocatechin 3-gallate (EGCG) has shown potent chemopreventive efficacy for PCa, we designed and developed novel targeted NPs in order to selectively deliver EGCG to cancer cells. Herein, to explore the recent concept of "nanochemoprevention", we present a study on EGCG-loaded NPs consisting of biocompatible polymers, functionalized with small molecules targeting PSMA, that exhibited a selective in vitro efficacy against PSMA-expressing PCa cells. This approach could be beneficial for high risk patients and would fulfill a significant therapeutic need, thus opening new perspectives for novel and effective treatment for PCa.
纳米粒子（NPs）介导的分子靶向癌症疗法是克服传统化疗药物缺乏特异性的有前途的策略。在这种情况下，前列腺特异性膜抗原（PSMA）已显示出用于管理前列腺癌（PCa）的强大潜力。植物化学物质的癌症化学预防作为治疗早期致癌过程的一种合适方法正在出现。由于（-）-表没食子儿茶素 3-没食子酸酯（EGCG）已显示出对 PCa 的强大化学预防功效，因此我们设计并开发了新型靶向 NPs，以便将 EGCG 选择性递送至癌细胞。在此，为了探索“纳米化学预防”的最新概念，我们研究了由生物相容性聚合物组成的载 EGCG 的 NPs，该聚合物用靶向 PSMA 的小分子进行了功能化，对表达 PSMA 的 PCa 细胞表现出选择性的体外功效。这种方法可能对高危患者有益，并将满足重要的治疗需求，从而为 PCa 的新型有效治疗开辟新的前景。
