Tamariz Joaquín, Burgueño-Tapia Eleuterio, Vázquez Miguel A, Delgado Francisco
Departamento de Química Orgánica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Prolongación de Carpio y Plan de Ayala S/N, 11340 Mexico City, Mexico.
Departamento de Química Orgánica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Prolongación de Carpio y Plan de Ayala S/N, 11340 Mexico City, Mexico.
Alkaloids Chem Biol. 2018;80:1-314. doi: 10.1016/bs.alkal.2018.03.001. Epub 2018 Jul 6.
Naturally occurring pyrrolizidine alkaloids (PAs) are isolated from plants and other sources. The interest of the scientific community in these compounds owes itself to their high toxicity and biological activity, as well as to the challenge of synthesizing their pyrrolizidine scaffold. This review encompasses a wide range of topics found in the literature from 1995 to date, including the occurrence, biosynthesis, toxicity (hepatotoxicity, genotoxicity, and tumorigenicity), biological activity, and pharmacological properties (glycosidase inhibitory activity) of these secondary metabolites. Particular attention is given to the chemistry of PAs, addressing general strategies for formal and total syntheses via amino-based substrates, pyrroles, and pyrrolidine-based derivatives.
天然存在的吡咯里西啶生物碱（PAs）是从植物和其他来源中分离出来的。科学界对这些化合物感兴趣，是由于它们具有高毒性和生物活性，以及合成其吡咯里西啶骨架所面临的挑战。本综述涵盖了1995年至今文献中发现的广泛主题，包括这些次生代谢产物的存在、生物合成、毒性（肝毒性、遗传毒性和致癌性）、生物活性和药理特性（糖苷酶抑制活性）。特别关注了PAs的化学，阐述了通过氨基底物、吡咯和基于吡咯烷的衍生物进行形式合成和全合成的一般策略。
