卡烯内酯类化合物：从化学结构和药理学应用角度的深入了解

Cardenolides: Insights from chemical structure and pharmacological utility.

机构信息

Division of Pharmacognosy, Department of Medicinal Chemistry, Uppsala University, Biomedical Centre, Box 574, SE-75123, Uppsala, Sweden; Chemistry Department, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia; H. E. J. Research Institute of Chemistry, International Center for Chemical Sciences, University of Karachi, Karachi 75270, Pakistan; Department of Chemistry, Faculty of Science, Menoufia University, Shebin El-Kom, Egypt.

Department of Molecular Biosciences, The Wenner-Gren Institute, Stockholm University, S-106 91, Stockholm, Sweden.

出版信息

Pharmacol Res. 2019 Mar;141:123-175. doi: 10.1016/j.phrs.2018.12.015. Epub 2018 Dec 21.

DOI:10.1016/j.phrs.2018.12.015

PMID:30579976

Abstract

Cardiac glycosides (CGs) are a class of naturally occurring steroid-like compounds, and members of this class have been in clinical use for more than 1500 years. They have been used in folk medicine as arrow poisons, abortifacients, heart tonics, emetics, and diuretics as well as in other applications. The major use of CGs today is based on their ability to inhibit the membrane-bound Na/K-ATPase enzyme, and they are regarded as an effective treatment for congestive heart failure (CHF), cardiac arrhythmia and atrial fibrillation. Furthermore, increasing evidence has indicated the potential cytotoxic effects of CGs against various types of cancer. In this review, we highlight some of the structural features of this class of natural products that are crucial for their efficacy, some methods of isolating these compounds from natural resources, and the structural elucidation tools that have been used. We also describe their physicochemical properties and several modern biotechnological approaches for preparing CGs that do not require plant sources.

摘要

强心苷（CGs）是一类天然甾体样化合物，该类化合物已有 1500 多年的临床应用历史。它们在民间医学中被用作箭毒、堕胎药、心脏滋补剂、催吐剂和利尿剂，以及其他用途。CGs 的主要用途基于其抑制膜结合 Na/K-ATP 酶的能力，它们被认为是充血性心力衰竭（CHF）、心律失常和心房颤动的有效治疗方法。此外，越来越多的证据表明 CGs 对各种类型的癌症具有潜在的细胞毒性作用。在这篇综述中，我们强调了该类天然产物的一些结构特征，这些特征对其疗效至关重要，还介绍了从自然资源中分离这些化合物的一些方法以及已经使用的结构解析工具。我们还描述了它们的物理化学性质和几种不需要植物来源的现代生物技术方法来制备 CGs。