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Production of Highly Active Antiparasitic Compounds from the Controlled Halogenation of the Arrabidaea brachypoda Crude Plant Extract.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-09-09 , DOI: 10.1021/acs.jnatprod.0c00433 Alexandra Neuenschwander 1 , Vinicius P C Rocha 2 , Tanira M Bastos 2 , Laurence Marcourt 1 , Hugo Morin 1 , Cláudia Q da Rocha 3 , Gabriela B Grimaldi 2 , Karoline A F de Sousa 2 , Jadson N Borges 2 , Elisabeth Rivara-Minten 1 , Jean-Luc Wolfender 1 , Milena B P Soares 2 , Emerson F Queiroz 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-09-09 , DOI: 10.1021/acs.jnatprod.0c00433 Alexandra Neuenschwander 1 , Vinicius P C Rocha 2 , Tanira M Bastos 2 , Laurence Marcourt 1 , Hugo Morin 1 , Cláudia Q da Rocha 3 , Gabriela B Grimaldi 2 , Karoline A F de Sousa 2 , Jadson N Borges 2 , Elisabeth Rivara-Minten 1 , Jean-Luc Wolfender 1 , Milena B P Soares 2 , Emerson F Queiroz 1
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Direct halogenation of phenolic compounds present in the CH2Cl2 extract of the roots of Arrabidaea brachypoda was investigated to enhance chemodiversity. The approach is based on eco-friendly reactions using NaBr, NaI, and NaCl in aqueous media to generate multiple “unnatural” halogenated natural products from crude extracts. The halogenation reactions, monitored by UHPLC-PDA-ELSD-MS, were optimized to generate mono-, di-, or trihalogenated derivatives. To isolate these compounds, the reactions were scaled up and the halogenated analogues were isolated by semipreparative HPLC-UV and fully characterized by NMR and HR-MS data. All of the original 16 halogenated derivatives were evaluated for their antiparasitic activities against the parasites Leishmania amazonensis and Trypanosoma cruzi. Compounds presenting selective antiparasitic activities against one or both parasites with IC50 values comparable to the reference were identified.
中文翻译：
从 Arrabidaea brachypoda 粗植物提取物的受控卤化生产高活性抗寄生虫化合物。
存在于CH酚类化合物的直接卤化2氯2的根部提取Arrabidaea brachypoda进行了研究以增强chemodiversity。该方法基于在水性介质中使用 NaBr、NaI 和 NaCl 的环保反应，从粗提物中生成多种“非天然”卤化天然产物。由 UHPLC-PDA-ELSD-MS 监测的卤化反应经过优化以生成单、二或三卤代衍生物。为了分离这些化合物，放大反应，通过半制备型 HPLC-UV 分离卤代类似物，并通过 NMR 和 HR-MS 数据进行充分表征。评估了所有最初的 16 种卤化衍生物对寄生虫的抗寄生虫活性亚马逊利什曼原虫和克氏锥虫。鉴定了对一种或两种寄生虫具有选择性抗寄生虫活性的化合物，其 IC 50值与参考值相当。
更新日期：2020-09-25
中文翻译：
从 Arrabidaea brachypoda 粗植物提取物的受控卤化生产高活性抗寄生虫化合物。
存在于CH酚类化合物的直接卤化2氯2的根部提取Arrabidaea brachypoda进行了研究以增强chemodiversity。该方法基于在水性介质中使用 NaBr、NaI 和 NaCl 的环保反应，从粗提物中生成多种“非天然”卤化天然产物。由 UHPLC-PDA-ELSD-MS 监测的卤化反应经过优化以生成单、二或三卤代衍生物。为了分离这些化合物，放大反应，通过半制备型 HPLC-UV 分离卤代类似物，并通过 NMR 和 HR-MS 数据进行充分表征。评估了所有最初的 16 种卤化衍生物对寄生虫的抗寄生虫活性亚马逊利什曼原虫和克氏锥虫。鉴定了对一种或两种寄生虫具有选择性抗寄生虫活性的化合物，其 IC 50值与参考值相当。
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