Zhai Jinxiao, Dong Xiaoru, Yan Fenglian, Guo Hongsong, Yang Jinling
Institute of Forensic Medicine and Laboratory Medicine, Jining Medical University, Jining, China.
Department of Forensic Medicine, School of Basic Medical Sciences, Fudan University, Shanghai, China.
Front Pharmacol. 2022 Feb 21;13:822726. doi: 10.3389/fphar.2022.822726. eCollection 2022.
Oleandrin is a highly lipid-soluble cardiac glycoside isolated from the plant (Apocynaceae) and is used as a traditional herbal medicine due to its excellent pharmacological properties. It is widely applied for various disease treatments, such as congestive heart failure. Recently, oleandrin has attracted widespread attention due to its extensive anti-cancer and novel anti-viral effects. However, oleandrin has a narrow therapeutic window and exhibits various toxicities, especially typical cardiotoxicity, which is often fatal. This severe toxicity and low polarity have significantly hindered its application in the clinic. This review describes natural sources, structural properties, and detection methods of oleandrin. Based on reported poisoning cases and sporadic animal experiments, the pharmacokinetic characteristics of oleandrin are summarized, so as to infer some possible phenomena, such as enterohepatic circulation. Moreover, the relevant factors affecting the pharmacokinetics of oleandrin are analyzed, and some research approaches that may ameliorate the pharmacokinetic behavior of oleandrin are proposed. With the toxicology of oleandrin being thoroughly reviewed, the development of safe clinical applications of oleandrin may be possible given potential research strategies to decrease toxicity.
夹竹桃苷是一种从夹竹桃科植物中分离出的高度脂溶性强心苷，因其优异的药理特性而被用作传统草药。它被广泛应用于各种疾病的治疗，如充血性心力衰竭。近年来，夹竹桃苷因其广泛的抗癌和新型抗病毒作用而备受关注。然而，夹竹桃苷的治疗窗较窄，并表现出多种毒性，尤其是典型的心脏毒性，这往往是致命的。这种严重的毒性和低极性显著阻碍了其在临床上的应用。本文综述了夹竹桃苷的天然来源、结构特性和检测方法。基于已报道的中毒病例和零星的动物实验，总结了夹竹桃苷的药代动力学特征，以推断一些可能的现象，如肠肝循环。此外，分析了影响夹竹桃苷药代动力学的相关因素，并提出了一些可能改善夹竹桃苷药代动力学行为的研究方法。随着对夹竹桃苷毒理学的深入研究，考虑到降低毒性的潜在研究策略，夹竹桃苷安全临床应用的发展可能成为现实。
