1."Discussion on ""Tong Yang Bu Zai Wen Er Zai Li Xiao Bian"" Combined with Shang Han Lun"
Tao LIU ; Yi ZHANG ; Juan LI ; Jintian LI ; Senhao YU ; Qian LAI ; Qiyu ZENG
Chinese Journal of Information on Traditional Chinese Medicine 2017;24(9):106-107
This article analyzed, organizde, and summarized the specific meaning of yin and yang in Shang Han Lun, holding the idea that Zhongyang in Shang Han Lun contains fluid. YE Tian-shi's Tong Yang Bu Zai Wen Er Zai Li Xiao Bian is derived from Zhong jing method, and is more suitable to be used in damp-heat syndromes, reflecting that YE Tian-shi is not confined to traditional methods, but follows traditional prescriptions and flexible thoughts, which provides references for learning and flexibly applying prescription ideas.
2.A potent PGK1 antagonist reveals PGK1 regulates the production of IL-1β and IL-6.
Liping LIAO ; Wenzhen DANG ; Tingting LIN ; Jinghua YU ; Tonghai LIU ; Wen LI ; Senhao XIAO ; Lei FENG ; Jing HUANG ; Rong FU ; Jiacheng LI ; Liping LIU ; Mingchen WANG ; Hongru TAO ; Hualiang JIANG ; Kaixian CHEN ; Xingxing DIAO ; Bing ZHOU ; Xiaoyan SHEN ; Cheng LUO
Acta Pharmaceutica Sinica B 2022;12(11):4180-4192
Glycolytic metabolism enzymes have been implicated in the immunometabolism field through changes in metabolic status. PGK1 is a catalytic enzyme in the glycolytic pathway. Here, we set up a high-throughput screen platform to identify PGK1 inhibitors. DC-PGKI is an ATP-competitive inhibitor of PGK1 with an affinity of K d = 99.08 nmol/L. DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. In addition, DC-PGKI unveils that PGK1 regulates production of IL-1β and IL-6 in LPS-stimulated macrophages. Mechanistically, inhibition of PGK1 with DC-PGKI results in NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2) accumulation, then NRF2 translocates to the nucleus and binds to the proximity region of Il-1β and Il-6 genes, and inhibits LPS-induced expression of these genes. DC-PGKI ameliorates colitis in the dextran sulfate sodium (DSS)-induced colitis mouse model. These data support PGK1 as a regulator of macrophages and suggest potential utility of PGK1 inhibitors in the treatment of inflammatory bowel disease.