期刊
CHEMMEDCHEM
卷 13, 期 19, 页码 2057-2064出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800481
关键词
macrophage repolarization; STING; tumor microenvironment; typeI interferon; -mangostin
资金
- National Natural Science Foundation of China (NSFC) [21521003, 81373326, 21290183, 81400826]
- Shenzhen Science and Technology Innovation Program [JCYJ20150529095420031, JCYJ20170412150827191, JCYJ20170818090609800]
- program of the Science and Technology Committee of Guangdong [2014A030312004, 2015A030313887]
- Adlai Nortye Biopharma Co., Ltd.
The xanthone derivate 5,6-dimethylxanthenone-4-acetic acid (DMXAA, also known as ASA404 or vadimezan) is a potent agonist of murine STING (stimulator of interferon genes), but cannot activate human STING. Herein we report that -mangostin, which bears the xanthone skeleton, is an agonist of human STING, but activates murine STING to a lesser extent. Biochemical and cell-based assays indicate that -mangostin binds to and activates human STING, leading to activation of the downstream interferon regulatory factor (IRF) pathway and production of typeI interferons. Furthermore, our studies show that -mangostin has the potential to repolarize human monocyte-derived M2 macrophages to the M1 phenotype. The agonist effect of -mangostin in the STING pathway might account for its antitumor and antiviral activities.
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