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Biosci Biotechnol Biochem ; 84(7): 1332-1338, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32200702

RESUMO

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.


Assuntos
Adenocarcinoma Bronquioloalveolar/metabolismo , Agaricales/química , Inibidores de Checkpoint Imunológico/farmacologia , Neoplasias Pulmonares/metabolismo , Reguladores de Crescimento de Plantas/farmacologia , Proteínas Proto-Oncogênicas/antagonistas & inibidores , Receptores Proteína Tirosina Quinases/antagonistas & inibidores , Transdução de Sinais/efeitos dos fármacos , Células A549 , Adenocarcinoma Bronquioloalveolar/patologia , Antígeno B7-H1/antagonistas & inibidores , Antígeno B7-H1/metabolismo , Carpóforos/química , Humanos , Lactuca/efeitos dos fármacos , Lactuca/crescimento & desenvolvimento , Neoplasias Pulmonares/patologia , Proteína 2 Ligante de Morte Celular Programada 1/antagonistas & inibidores , Proteína 2 Ligante de Morte Celular Programada 1/metabolismo , Proteínas Proto-Oncogênicas/metabolismo , Receptores Proteína Tirosina Quinases/metabolismo , Receptor Tirosina Quinase Axl
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