ultra-high-performance-liquid-chromatography-mass-spectrometry-self

Ultra High-Performance Liquid Chromatography-Mass Spectrometry and Self-established Database Analysis of Chinese Herbal Medicine Components

Chinese herbal medicine is complex and has numerous unknown compounds, making qualitative research crucial. Ultra-high-performance liquid chromatography ...

Chongqing Traditional Chinese Medicine Hospital

The Src-homology 2 domain-containing phosphatase 2 (SHP2), which is encoded by PTPN11, participates in many cellular signaling pathways and is closely related to various tumorigenesis. Inhibition of the abnormal activity of SHP2 by small molecules is an important part of cancer treatment. Here, three abietane diterpenoids, named compounds -, were isolated from  var. . Spectroscopic analysis was used to identify the exact structure of the compounds. The enzymatic kinetic experiment and the cellular thermal shift assay showed compound  selectively inhibited SHP2 activity in vitro. Molecular docking indicated compound  targeted the SHP2 catalytic domain. The predicted pharmacokinetic properties by SwissADME revealed that compound  passed the majority of the parameters of common drug discovery rules. Compound  restrained A549 proliferation (IC = 8.68 ± 0.96 μM), invasion and caused A549 cell apoptosis by inhibiting the SHP2-ERK/AKT signaling pathway. Finally, compound  (Ajuforrestin A) is a potent and efficacious SHP2 inhibitor and may be a promising compound for human lung epithelial cancer treatment.

Fujin Yang

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