Chemistry Department and Centre for Biotechnology, Brock University, 1812 Sir Isaac Brock Way, St. Catharines, Ontario, L2S 3A1, Canada.
Department of Organic Chemistry, Faculty of Science, Charles University, Hlavova 8, 12843, Prague, Czech Republic.
Angew Chem Int Ed Engl. 2019 Dec 16;58(51):18338-18387. doi: 10.1002/anie.201901564. Epub 2019 Sep 23.
This review provides a comprehensive coverage of the history, biology and chemistry of tetrodotoxin (TTX). It traces the origin of this remarkable molecule all the way back to the ancient Chinese medicine records. The discovery of biological activity, isolation, and a brief overview of structure elucidation are summarized. Next, the biology of TTX is discussed, primarily in the context of its activity in the sodium channels, its anesthetic properties, and its potential use in cancer treatment or drug addiction. Biosynthesis of TTX is covered before the discussion of the total syntheses. All total, formal or partial syntheses are covered but those total syntheses that have been discussed in previous reviews are only briefly summarized. Finally, the synthesis of natural and unnatural derivatives is surveyed, and a conclusion and outlook are provided for this very extensive field of endeavor. To the best of our knowledge the literature coverage is complete up to December 2018.
这篇综述全面介绍了河豚毒素（TTX）的历史、生物学和化学。它追溯了这种非凡分子的起源，可以一直追溯到中国古代的医学记录。本文总结了该分子的生物活性发现、分离和结构解析的简要概述。接下来，本文讨论了 TTX 的生物学特性，主要集中在其对钠离子通道的活性、麻醉特性以及在癌症治疗或药物成瘾方面的潜在用途。在讨论 TTX 的生物合成之前，本文先介绍了它的全合成。本文涵盖了所有的全合成或部分合成，但对于之前综述中已经讨论过的全合成，本文仅做简要总结。最后，本文还调查了天然和非天然衍生物的合成，并对这个非常广泛的研究领域提供了结论和展望。就我们所知，文献综述的内容截止到 2018 年 12 月。
