期刊
ACS OMEGA
卷 5, 期 40, 页码 25927-25935出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.0c03315
关键词
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资金
- National Natural Science Foundation of China [31672070]
- National Key Research and Development Program of China [2017YFD0201400, 2017YFD0201401]
- Changjiang Scholars and Innovative Research Team in University [IRT_15R16]
- Talent training plan of Hebei University [521000981185]
Phomoxanthone A and B (PXA and PXB) are xanthone dimers and isolated from the endophytic fungus Phomopsis sp. By254. The results demonstrated that PXB and PXA are noncompetitive inhibitors of SHP2 and PTP1B and competitive inhibitors of SHP1. Molecular docking studies showed that PXB and PXA interact with conserved domains of protein tyrosine phosphatases such as the beta 5-beta 6 loop, WPD loop, P loop, and Q loop. PXA and PXB could significantly inhibit the cell proliferation in MCF7 cells. Our results indicated that these two compounds do not efficiently inhibit PTP1B and SHP2 activity. RNA sequencing showed that PXA and PXB may inhibit SHP1 activity in MCF7 cells leading to the upregulation of inflammatory factors. In addition to PTP inhibition, PXA and PXB are multitarget compounds to inhibit the proliferation of tumor cells. In conclusion, both compounds show inhibition of cancer cells and a certain degree of inflammatory stimulation, which make them promising for tumor immunotherapy.
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