Abstract：
:The Src-homology 2 domain-containing phosphatase 2 (SHP2), encoded by PTPN11, has been reported oncogenic tyrosine phosphatase associated with various tumors and played critical roles in many cell signaling events. Targeting SHP2 by small molecules may be a promising way for cancer therapy. Herein, a new abietane diterpenoid, named 3-acetoxylteuvincenone G (3-AG), was isolated from the whole plants of Ajuga ovalifolia var. calantha. The structure of the new compound was elucidated by means of extensive spectroscopic analyses. Using recombinant enzyme activity assay and cellular thermal shift assay, we found that 3-AG was a selective inhibitor of SHP2. Molecular docking suggested 3-AG displayed an orientation favorable to nucleophilic attack in the catalytic domain of SHP2. 3-AG suppressed A549 cell proliferation (IC50 = 10.79 ± 0.14 μM), invasion and induced cell apoptosis through SHP2/ERK1/2 and SHP2/AKT pathways. In summary, 3-AG, a potent, selective, and efficacious SHP2 inhibitor, may be a promising small molecule to treat human lung epithelial cancer.
journal_name
Fitoterapiajournal_title
Fitoterapiaauthors
Liu DM,Cao ZX,Yan HL,Li W,Yang F,Zhao WJ,Diao QC,Tan YZdoi
10.1016/j.fitote.2020.104484subject
Has Abstractpub_date
2020-03-01 00:00:00pages
104484eissn
0367-326Xissn
1873-6971pii
S0367-326X(20)30066-6journal_volume
141pub_type
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