Current Pharmaceutical Design, 2010, 16(16):1801-12.

Lesson Learned from Nature for the Development of Novel Anti-Cancer Agents: Implication of Isoflavone, Curcumin, and their Synthetic Analogs

Yiwei Li, et al

Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, MI, USA

In recent years, naturally occurring dietary compounds have received greater attention in the field of cancer prevention and treatment research. Among them, isoflavone genistein and curcumin are very promising anti-cancer agents because of their non-toxic and potent anti-cancer properties. However, it is important to note that the low water solubility, poor in vivo bioavailability and unacceptable pharmacokinetic profile of these natural compounds limit their efficacy as anti-cancer agents for solid tumors. Therefore, the development of synthetic analogs of isoflavone and curcumin based on the structure-activity assay, and the encapsulation of isoflavone and curcumin with liposome or nanoparticle for enhancing the anti-tumor activity of these natural agents, is an exciting area of research. Emerging in vitro and in vivo studies clearly suggest that these analogs and formulations of natural compounds could be much more potent for the prevention and/or treatment of various cancers. In this review article, we will summarize the current knowledge regarding the anti-cancer effect of natural compounds and their analogs, the regulation of cell signaling by these agents, and the structure-activity relationship for better design of novel anti-cancer agents, which could open newer avenues for the prevention of tumor progression and/or treatment of human malignancies.

荷兰《现代药物设计》，2010年6月

从自然中学到的新型抗癌剂的发展︰异黄酮、 姜黄素及其合成类似物的作用

李一伟等

美国韦恩州医科大学芭芭拉 安 卡尔诺斯癌症研究所病理部

近年来，天然膳食化合物在癌症预防和治疗研究领域受到更多的关注。其中，异黄酮金雀异黄素和姜黄素因其无毒和强有力的抗癌特性成为有前途的抗癌药物。然而，由于水溶解度低、 体内生物利用度低和无法接受的药动学特征，这些天然化合物作为实体瘤的抗癌药物治疗限制了它们的功效。因此，大豆异黄酮和姜黄素基于结构-活性测定合成类似物的发展，以及用脂质体或纳米颗粒封装异黄酮和姜黄素来增强这些自然试剂抗肿瘤活性是一个令人兴奋的研究领域。新兴的体外和体内研究清楚地表明这些天然化合物的类似物和配方可能对预防和/或治疗多种癌症更有效。在这篇综述中，我们将总结天然化合物及其类似物的抗肿瘤效应，通过这些试剂调节的细胞信号，以及结构-活性关系用于更好的设计新型抗癌药物，从而开辟一条预防肿瘤发展和 （或）治疗人类恶性肿瘤的新路。