Department of Biotechnology, Maharishi Markandeshwar Engineering College, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala 133207, India.
Amity Institute of Environmental Sciences, Amity University, Noida 201303, India.
Molecules. 2022 Dec 12;27(24):8819. doi: 10.3390/molecules27248819.
Phloretin is a natural dihydrochalcone found in many fruits and vegetables, especially in apple tree leaves and the Manchurian apricots, exhibiting several therapeutic properties, such as antioxidant, antidiabetic, anti-inflammatory, and antitumor activities. In this review article, the diverse aspects of the anticancer potential of phloretin are addressed, presenting its antiproliferative, proapoptotic, antimetastatic, and antiangiogenic activities in many different preclinical cancer models. The fact that phloretin is a planar lipophilic polyphenol and, thus, a membrane-disrupting Pan-Assay Interference compound (PAIN) compromises the validity of the cell-based anticancer activities. Phloretin significantly reduces membrane dipole potential and, therefore, is expected to be able to activate a number of cellular signaling pathways in a non-specific way. In this way, the effects of this minor flavonoid on Bax and Bcl-2 proteins, caspases and MMPs, cytokines, and inflammatory enzymes are all analyzed in the current review. Moreover, besides the anticancer activities exerted by phloretin alone, its co-effects with conventional anticancer drugs are also under discussion. Therefore, this review presents a thorough overview of the preclinical anticancer potential of phloretin, allowing one to take the next steps in the development of novel drug candidates and move on to clinical trials.
根皮苷是一种天然二氢查耳酮，存在于许多水果和蔬菜中，特别是在苹果树叶子和毛樱桃中，具有多种治疗特性，如抗氧化、抗糖尿病、抗炎和抗肿瘤活性。在这篇综述文章中，探讨了根皮苷的抗癌潜力的多个方面，介绍了其在许多不同的临床前癌症模型中的抗增殖、促凋亡、抗转移和抗血管生成活性。根皮苷是一种平面亲脂性多酚，因此是一种膜干扰泛分析干扰化合物（PAIN），这影响了基于细胞的抗癌活性的有效性。根皮苷显著降低膜偶极电位，因此预计能够以非特异性方式激活许多细胞信号通路。通过这种方式，当前的综述分析了这种低浓度类黄酮对 Bax 和 Bcl-2 蛋白、半胱天冬酶和 MMPs、细胞因子和炎症酶的影响。此外，除了根皮苷单独发挥的抗癌作用外，还讨论了其与传统抗癌药物的协同作用。因此，本文全面综述了根皮苷的临床前抗癌潜力，为开发新型候选药物并推进临床试验提供了依据。
