Yuyama Kamila Tomoko, Fortkamp Diana, Abraham Wolf-Rainer
Helmholtz Center for Infection Research, Chemical Microbiology, Inhoffenstrasse 7, D-38124 Braunschweig, Germany.
Escola Superior de Agricultura 'Luiz de Queiroz' (ESALQ), Department of Exact Sciences, Piracicaba, SP, Brazil.
Biol Chem. 2017 Dec 20;399(1):13-28. doi: 10.1515/hsz-2017-0171.
Eremophilanes are sesquiterpenes with a rearranged carbon skeleton formed both by plants and fungi, however, almost no plant eremophilanes are found in fungi. These eremophilanes possess mainly phytotoxic, antimicrobial, anticancer and immunomodulatory properties and in this review fungal eremophilanes with bioactivities of potential medicinal applications are reviewed and discussed. A special focus is set on natural products bearing highly functionalized fatty acids at C-1 or C-3 position of the eremophilane backbone. Many of these fatty acids seem to contribute to the bioactivity of the metabolites enhancing the activity of the sesquiterpene moieties. Several approaches for optimization of these natural products for clinical needs and testing of the resulting derivatives are presented and discussed. The combination of identification of bioactive natural products with their subsequent improvement using a variety of genetical or chemical tools and the pharmacokinetic assessment of the products is presented here as a promising approach to new drugs.
桉叶烷类是一类倍半萜，其碳骨架经过重排，由植物和真菌均可产生，然而，在真菌中几乎未发现植物来源的桉叶烷类。这些桉叶烷类主要具有植物毒性、抗菌、抗癌和免疫调节特性，在本综述中，对具有潜在药用生物活性的真菌桉叶烷类进行了综述和讨论。特别关注在桉叶烷骨架的C-1或C-3位带有高度官能化脂肪酸的天然产物。这些脂肪酸中的许多似乎有助于代谢产物的生物活性，增强倍半萜部分的活性。本文介绍并讨论了几种针对临床需求优化这些天然产物以及测试所得衍生物的方法。将生物活性天然产物的鉴定与随后使用各种遗传或化学工具进行的改进以及产物的药代动力学评估相结合，作为一种有前景的新药开发方法在此呈现。
