US 12,064,405 B2
Immunosuppressant comprising TSAHC or a pharmaceutically acceptable salts thereof as an active ingredient
Jung Weon Lee, Seoul (KR); and Eunmi Kim, Seoul (KR)
Assigned to SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION, Seoul (KR)
Filed by Seoul National University R&DB Foundation, Seoul (KR)
Filed on Nov. 5, 2021, as Appl. No. 17/520,499.
Claims priority of application No. 10-2020-0148087 (KR), filed on Nov. 6, 2020.
Prior Publication US 2022/0160663 A1, May 26, 2022
Int. Cl. A61K 31/18 (2006.01); A61P 1/16 (2006.01); A61P 37/06 (2006.01)
CPC A61K 31/18 (2013.01) [A61P 1/16 (2018.01); A61P 37/06 (2018.01)] 12 Claims
 
1. An immunosuppressive method, comprising:
administering 4′-(p-toluenesulfonylamido)-4-hydroxychalcone (TSAHC) to a subject in an amount effective for the TSAHC to inhibit:
(i) secretion of inflammatory cytokines or chemokines dependent on the expression of TM4SF5;
(ii) activation of M1 type macrophages by inhibiting (a) binding of TM4SF5 and GLUT1, (b) sensitivity of glycolysis to extracellular glucose, or (c) glycolysis in macrophages;
(iii) conversion of M1 type macrophages to M2 type macrophages; and
(iv) chronic activation of M2 type macrophages by inhibiting the expression of mannose receptor C-type 1 (MRC1, CD206), fibronectin (FN1), arginase I (Arg1), and peroxisome proliferator-activated receptor gamma (Pparγ) in macrophages,
in the subject, thereby suppressing immunity in the subject,
wherein the subject has excessive inflammatory response caused by liver resection or liver tissue resection, abnormality in metabolic function of liver or liver tissue, liver transplant rejection or liver tissue transplant rejection, or exposure to substance(s) toxic to the liver or liver tissue.