[Effect of baicalin on pattern recognition receptor TLR2/4-NOD2 and its significance of druggability].
Activation pattern recognition receptors can cause the startup of downstream signaling pathways, the expression of inflammatory factors, and finally immunological inflammatory reaction. Either exogenous pathogenic microorganisms or endogenous tissue components can activate these pattern recognition receptors as ligands at varying degrees, and then cause the immunological inflammatory reaction. Therefore, it is of great significance to inhibit relevant receptors, as well as the immunological inflammatory reaction, in order to avoid tissue injury during the course of disease. Baicalin is able to specifically inhibit the expression of TLR2/4-NOD2, inhibit the expression of inflammatory factors IL-1beta, IL-6 and TNF-alpha, and thereby reducing the injury of the tissue cells during the course of disease. This effect is non-specific with tissues, which is of great theoretical and practical significance in druggability. In addition, the drug metabolism and toxicity of baicalin are also discussed for its druggability in this article.
Protein Science Laboratory of the Ministry of Education, Laboratory of Molecular Pharmacology and Pharmaceutical Sciences, School of Life Sciences and School of Medicine, Tsinghua University, Beijing 100084, China.
Yu-Shuang
YS
Chai
Fan
F
Lei
Dong-Ming
DM
Xing
Yi
Y
Ding
Li-Jun
LJ
Du
D000818:Animals; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D053473:Nod2 Signaling Adaptor Protein / Q000378:metabolism*; D051195:Toll-Like Receptor 2 / Q000378:metabolism*; D051197:Toll-Like Receptor 4 / Q000378:metabolism*
D005419:Flavonoids; D053473:Nod2 Signaling Adaptor Protein; D051195:Toll-Like Receptor 2; D051197:Toll-Like Receptor 4; C038044:baicalin