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爪哇姜代谢组学分析及基于低成本开源斑马鱼生物测定指导的抗惊厥代谢产物的鉴定。

Metabolite Profiling of Javanese Ginger and Identification of Antiseizure Metabolites via a Low-Cost Open-Source Zebrafish Bioassay-Guided Isolation.

机构信息

School of Pharmaceutical Sciences, University of Geneva, Geneva, Switzerland.

Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva, CMU-Rue Michel-Servet 1, CH-1211 Geneva 4, Switzerland.

出版信息

J Agric Food Chem. 2020 Jul 29;68(30):7904-7915. doi: 10.1021/acs.jafc.0c02641. Epub 2020 Jul 19.

Abstract

The rhizomes of "Bangle", were investigated for its antiseizure properties using a streamlined and cost-effective zebrafish screening strategy and a mouse epilepsy assay. Its hexane extract demonstrated strong antiseizure activity in zebrafish epilepsy assay and was, therefore, selected for bioactivity-guided fractionation. Twelve compounds (-) were isolated, and two bioactive phenylbutenoids, - () and -banglene (), reduced up to 70% of pentylenetetrazole (PTZ)-induced seizures. These compounds showed moderate activity against PTZ-induced seizures in a mouse epilepsy assay. To understand the specificity of active compounds, its chemical profile was compared to that of . Their composition was assessed by differential metabolite profiling visualized by a molecular network, which revealed only vanillin derivatives and terpenoids as common metabolites and gave a comprehensive view of composition. This study demonstrates the efficacy of a streamlined zebrafish epilepsy assay, which is therefore suitable for routine screening in phytochemistry laboratories.

摘要

采用简化且经济有效的斑马鱼筛选策略和小鼠癫痫模型对“八角枫”的根茎进行抗惊厥作用研究。其正己烷提取物在斑马鱼癫痫模型中表现出较强的抗惊厥活性,因此被选择进行基于生物活性的分离。分离得到 12 个化合物(-),其中两个生物活性苯丁烯类化合物(-)和(-)banglene 可将戊四氮(PTZ)诱导的癫痫发作减少 70%。这些化合物在小鼠癫痫模型中对 PTZ 诱导的癫痫发作显示出中等活性。为了了解活性化合物的特异性,将其化学特征与八角枫的化学特征进行比较。通过分子网络可视化的差异代谢物分析来评估它们的组成,该网络显示只有香草醛衍生物和萜类化合物是共同代谢物,从而全面了解八角枫的组成。本研究证明了简化的斑马鱼癫痫模型的有效性,因此适合于植物化学实验室的常规筛选。

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