Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno D'Alcontres 31, 98166 Messina, Italy.
Molecules. 2022 Mar 8;27(6):1775. doi: 10.3390/molecules27061775.
Liver cancer is one of the most common causes of cancer mortality worldwide. Chemotherapy and radiotherapy are the conventional therapies generally employed in patients with liver tumors. The major issue associated with the administration of chemotherapeutics is their high toxicity and lack of selectivity, leading to systemic toxicity that can be detrimental to the patient's quality of life. An important approach to the development of original liver-targeted therapeutic products takes advantage of the employment of biologically active ligands able to bind specific receptors on the cytoplasmatic membranes of liver cells. In this perspective, glycyrrhetinic acid (GA), a pentacyclic triterpenoid present in roots and rhizomes of licorice, has been used as a ligand for targeting the liver due to the expression of GA receptors on the sinusoidal surface of mammalian hepatocytes, so it may be employed to modify drug delivery systems (DDSs) and obtain better liver or hepatocyte drug uptake and efficacy. In the current review, we focus on the most recent and interesting research advances in the development of GA-based hybrid compounds and DDSs developed for potential employment as efficacious therapeutic options for the treatment of hepatic cancer.
肝癌是全球癌症死亡的主要原因之一。化疗和放疗是一般用于肝肿瘤患者的常规疗法。化疗药物的主要问题是其高毒性和缺乏选择性，导致全身毒性，可能对患者的生活质量造成损害。开发原创肝靶向治疗产品的一个重要方法是利用能够与肝细胞质膜上特定受体结合的生物活性配体。在这方面，甘草次酸 (GA) 是甘草根和根茎中的一种五环三萜，由于其在哺乳动物肝细胞的窦状表面表达 GA 受体，因此被用作靶向肝脏的配体，可用于修饰药物传递系统 (DDS) 并获得更好的肝脏或肝细胞药物摄取和疗效。在当前的综述中，我们重点介绍了基于 GA 的杂合化合物和 DDS 的最新研究进展，这些化合物和 DDS 被开发用于作为治疗肝癌的有效治疗选择。
