Abstract: The invention relates to a use of an urushiol compound (code named GQ-5) in preparation of pharmaceutical compositions for inhibiting Smad3 phosphorylation. We verify that GQ-5 inhibited the interaction of Smad3 with TGF-? type I receptor (T?RI), inhibited subsequent phosphorylation of Smad3, reduced nuclear translocation of Smads complex, and suppressed the transcription of major fibrotic genes such as ?-smooth muscle actin (?-SMA), collagen I and fibronectin. Therefore, GQ-5 could be a potent and selective inhibitor of TGF-?1-induced Smad3 phosphorylation, and be used to prepare pharmaceutical compositions for inhibiting Smad3 phosphorylation.
Type:
Grant
Filed:
November 3, 2014
Date of Patent:
September 22, 2015
Assignees:
SOUTHERN HOSPITAL, SOUTHERN MEDICAL UNIVERSITY, KUNMING INSTITUTE OF BOTANY, CHINESE ACADEMY OF SCIENCES
Inventors:
Fan Fan Hou, Yongxian Cheng, Jing Nie, Jun Al, Jiangbo He
Abstract: The invention relates to a use of an urushiol compound (code named GQ-5) in preparation of pharmaceutical compositions for inhibiting Smad3 phosphorylation. We verify that GQ-5 inhibited the interaction of Smad3 with TGF-? type I receptor (T?RI), inhibited subsequent phosphorylation of Smad3, reduced nuclear translocation of Smads complex, and suppressed the transcription of major fibrotic genes such as ?-smooth muscle actin (?-SMA), collagen I and fibronectin. Therefore, GQ-5 could be a potent and selective inhibitor of TGF-?1-induced Smad3 phosphorylation, and be used to prepare pharmaceutical compositions for inhibiting Smad3 phosphorylation.
Type:
Application
Filed:
November 3, 2014
Publication date:
June 25, 2015
Applicants:
SOUTHERN HOSPITAL, SOUTHERN MEDICAL UNIVERSITY, Kunming Institute of Botany, Chinese Academy of Sciences
Inventors:
Fan Fan HOU, Yongxian CHENG, Jing NIE, Jun AI, Jiangbo HE
Abstract: The present invention provides a series of penta-substituted tetrahydropyrimidines with aggregation-induced emission (AIE) characteristics and preparation method and use thereof. The AIE penta-substituted tetrahydropyrimidines have structures shown as formula (I). R1 is selected from a group consisting of linear or branched alkyls and substituted alkyls. R2 and R4 is respectively selected from a group consisting of linear or branched alkyls, substituted alkyls, cycloalkyls, substituted cycloalkyls, aryls, substituted aryls, polycyclic aryls, substituted polycyclic aryls, heterocyclyls, substituted heterocyclyls, aromatic heterocyclyls and substituted aromatic heterocyclyls. R3 is selected from a group consisting of aryls, substituted aryls, polycyclic aryls, substituted polycyclic aryls, aromatic heterocyclyls and substituted aromatic heterocyclyls. The penta-substituted tetrahydropyrimidines can be prepared by multi-component reactions (MCR).
Abstract: The present invention provides a series of penta-substituted tetrahydropyrimidines with aggregation-induced emission (AIE) characteristics and preparation method and use thereof. The AIE penta-substituted tetrahydropyrimidines have structures shown as formula (I). R1 is selected from a group consisting of linear or branched alkyls and substituted alkyls. R2 and R4 is respectively selected from a group consisting of linear or branched alkyls, substituted alkyls, cycloalkyls, substituted cycloalkyls, aryls, substituted aryls, polycyclic aryls, substituted polycyclic aryls, heterocyclyls, substituted heterocyclyls, aromatic heterocyclyls and substituted aromatic heterocyclyls. R3 is selected from a group consisting of aryls, substituted aryls, polycyclic aryls, substituted polycyclic aryls, aromatic heterocyclyls and substituted aromatic heterocyclyls. The penta-substituted tetrahydropyrimidines can be prepared by multi-component reactions (MCR).