Filippi Alexandru, Ciolac Oana-Alina, Ganea Constanța, Mocanu Maria-Magdalena
Department of Biophysics, Carol Davila University of Medicine and Pharmacy, Bucharest, Romania.
J Oncol. 2017;2017:1532534. doi: 10.1155/2017/1532534. Epub 2017 Feb 13.
ErbB proteins overexpression, in both normal and mutated forms, is associated with invasive forms of cancer prone to metastasis and with stronger antiapoptotic mechanisms and therefore more challenging to treat. Downstream effectors of ErbB receptors mediating these phenotypic traits include MAPK, STAT, and PI3K/AKT/mTOR pathways. Various phytochemical compounds were studied for their large number of biological effects including anticancer activity. Among these compounds, epigallocatechin-3-gallate (EGCG), the main catechin from green tea leaves, and curcumin, component of the curry powder, constituted the object of numerous studies. Both compounds were shown to act directly either on ErbB expression, or on their downstream signaling molecules. In this paper we aim to review the involvement of ErbB proteins in cancer as well as the biologic activity of EGCG and curcumin in ErbB expressing and overexpressing malignancies. The problems arising in the administration of the two compounds due to their reduced bioavailability when orally administered, as well as the progress made in this field, from using novel formulations to improved dosing regimens or improved synthetic analogs, are also discussed.
ErbB蛋白的正常和突变形式的过表达都与易于转移的侵袭性癌症形式以及更强的抗凋亡机制相关,因此治疗更具挑战性。介导这些表型特征的ErbB受体的下游效应器包括MAPK、STAT和PI3K/AKT/mTOR途径。人们研究了各种植物化学化合物的大量生物学效应,包括抗癌活性。在这些化合物中,表没食子儿茶素-3-没食子酸酯(EGCG),即绿茶中的主要儿茶素,以及姜黄素,即咖喱粉的成分,成为了众多研究的对象。这两种化合物都被证明可直接作用于ErbB的表达或其下游信号分子。在本文中,我们旨在综述ErbB蛋白在癌症中的作用,以及EGCG和姜黄素在表达和过表达ErbB的恶性肿瘤中的生物学活性。还讨论了由于口服给药时这两种化合物的生物利用度降低而在给药过程中出现的问题,以及该领域从使用新型制剂到改进给药方案或改进合成类似物所取得的进展。