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Glutathione Transferases: Surrogate Targets for Discovering Biologically Active Compounds
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-10-01 , DOI: 10.1021/acs.jnatprod.0c00480 Muriel Barbier 1 , Thomas Perrot 2 , Guillaume Salzet 1 , Nadine Amusant 3 , Stéphane Dumarçay 4 , Philippe Gérardin 4 , Mélanie Morel-Rouhier 1 , Rodnay Sormani 1 , Eric Gelhaye 1
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-10-01 , DOI: 10.1021/acs.jnatprod.0c00480 Muriel Barbier 1 , Thomas Perrot 2 , Guillaume Salzet 1 , Nadine Amusant 3 , Stéphane Dumarçay 4 , Philippe Gérardin 4 , Mélanie Morel-Rouhier 1 , Rodnay Sormani 1 , Eric Gelhaye 1
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Glutathione transferases comprise a large class of multifunctional enzymes, some involved in detoxification pathways. Since these enzymes are able to interact with potentially toxic molecules, they could be used as targets to screen for compounds with biological activity. To test this hypothesis, glutathione transferases (GSTs) from the white-rot fungus Trametes versicolor have been used to screen for antifungal molecules from a library of tropical wood extracts. The interactions between a set of six GSTs from the omega class and 116 extracts from 21 tropical species were quantified using a high-throughput thermal shift assay. A correlation between these interactions and the antifungal properties of the tested extracts was demonstrated. This approach has been extended to the fractionation of an Andira coriacea extract and led to the detection of maackiain and lapachol in this wood. Altogether, the present results supported the hypothesis that such detoxification enzymes could be used to detect biologically active molecules.
中文翻译：
谷胱甘肽转移酶：发现生物活性化合物的替代目标
谷胱甘肽转移酶包括一大类多功能酶，其中一些参与解毒途径。由于这些酶能够与潜在的有毒分子相互作用，因此它们可以用作筛选具有生物活性的化合物的靶标。为了验证这一假设，来自白腐真菌花斑栓菌的谷胱甘肽转移酶 (GST)已被用于从热带木材提取物库中筛选抗真菌分子。欧米茄类的 6 种 GST 与 21 种热带物种的 116 种提取物之间的相互作用使用高通量热位移测定法进行量化。证明了这些相互作用与测试提取物的抗真菌特性之间的相关性。这种方法已扩展到分馏Andira coriacea提取物并导致在该木材中检测到 maackiain 和 lapachol。总之，目前的结果支持这样的假设，即这种解毒酶可用于检测生物活性分子。
更新日期：2020-10-26
中文翻译：
谷胱甘肽转移酶：发现生物活性化合物的替代目标
谷胱甘肽转移酶包括一大类多功能酶，其中一些参与解毒途径。由于这些酶能够与潜在的有毒分子相互作用，因此它们可以用作筛选具有生物活性的化合物的靶标。为了验证这一假设，来自白腐真菌花斑栓菌的谷胱甘肽转移酶 (GST)已被用于从热带木材提取物库中筛选抗真菌分子。欧米茄类的 6 种 GST 与 21 种热带物种的 116 种提取物之间的相互作用使用高通量热位移测定法进行量化。证明了这些相互作用与测试提取物的抗真菌特性之间的相关性。这种方法已扩展到分馏Andira coriacea提取物并导致在该木材中检测到 maackiain 和 lapachol。总之，目前的结果支持这样的假设，即这种解毒酶可用于检测生物活性分子。
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