Plant growth regulators and Axl and immune checkpoint inhibitors from the edible mushroom Leucopaxillus giganteus
Plant growth regulators and Axl and immune checkpoint inhibitors from the edible mushroom Leucopaxillus giganteus
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DOI：
10.1080/09168451.2020.1743170
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发表时间：
2020-03-22
影响因子：
1.6
通讯作者：
Kawagishi, Hirokazu
中科院分区：
文献类型：
--
作者：
Malya, Irine Yunhafita;Wu, Jing;Kawagishi, Hirokazu
从野生食用菌Leucopaxillus acuteus的子实体中分离得到一个新化合物（R）-4-乙氧基-2-羟基-4-氧代丁酸（1）和六个已知化合物（2-7）。通过光谱数据分析确定了化合物1的平面结构。通过比较合成化合物的比旋光度确定了化合物1的绝对构型。在植物调节试验中，评价了分离的化合物（1-7）和化学制备的化合物（8-10）对莴苣（Lactuca sativa）生长的生物活性。化合物1和3-10对莴苣生长具有明显的调节活性。其中化合物1的抑菌活性最强。在肺癌测定中，通过RT-PCR评估所有化合物在人A549肺泡上皮细胞系中Axl和免疫检查点（PD-L1、PD-L2）的mRNA表达。化合物1-10显示出对Axl和/或免疫检查点的显著抑制活性。
A novel compound, (R)-4-ethoxy-2-hydroxy-4-oxobutanoic acid (1), and six known compounds (2-7) were isolated from the fruiting bodies of the wild edible mushroom Leucopaxillus giganteus. The planar structure of 1 was determined by the interpretation of spectroscopic data analysis. The absolute configuration of 1 was determined by comparing specific rotation of the synthetic compounds. In the plant regulatory assay, the isolated compounds (1-7) and the chemically prepared compounds (8-10) were evaluated their biological activity against the lettuce (Lactuca sativa) growth. Compounds 1 and 3-10 showed the significant regulatory activity of lettuce growth. 1 showed the strongest inhibition activity among the all the compounds tested. In the lung cancer assay, all the compounds were assessed the mRNA expression of Axl and immune checkpoints (PD-L1, PD-L2) in the human A549 alveolar epithelial cell line by RT-PCR. Compounds 1-10 showed significant inhibition activity against Axl and/or immune checkpoint.