Identification of interleukin-8-reducing lead compounds based on SAR studies on dihydrochalcone-related compounds in human gingival fibroblasts (HGF-1 cells) in vitro was written by Schueller, Katharina;Hans, Joachim;Pfeiffer, Stefanie;Walker, Jessica;Ley, Jakob P.;Somoza, Veronika. And the article was included in Molecules in 2020.Quality Control of Pyridinehydrochloride This article mentions the following:
In order to identify potential activities against periodontal diseases, eighteen dihydrochalcones and structurally related compounds were tested in an established biol. in vitro cell model of periodontal inflammation using human gingival fibroblasts (HGF-1 cells). Subsequently to co-incubation of HGF-1 cells with a bacterial endotoxin (Porphyromonas gingivalis lipopolysaccharide, pgLPS) and each individual dihydrochalcone in a concentration range of 1 μM to 100 μM, gene expression of interleukin-8 (IL-8) was determined by qPCR and cellular interleukin-8 (IL-8) release by ELISA. Structure-activity anal. based on the dihydrochalcone backbone and various substitution patterns at its aromatic ring revealed moieties 2′,4,4′,6′-tetrahydroxy 3-methoxydihydrochalcone (7) to be the most effective anti-inflammatory compound, reducing the pgLPS-induced IL-8 release concentration between 1 μM and 100 μM up to 94%. In general, a 2,4,6-trihydroxy substitution at the A-ring and concomitant vanilloyl (4-hydroxy-3-methoxy) pattern at the B-ring revealed to be preferable for IL-8 release inhibition. Furthermore, the introduction of an electroneg. atom in the A,B-linker chain led to an increased anti-inflammatory activity, shown by the potency of 4-hydroxybenzoic acid N-vanillylamide (13). Our data may be feasible to be used for further lead structure designs for the development of potent anti-inflammatory additives in oral care products. In the experiment, the researchers used many compounds, for example, Pyridinehydrochloride (cas: 628-13-7Quality Control of Pyridinehydrochloride).
Pyridinehydrochloride (cas: 628-13-7) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Quality Control of Pyridinehydrochloride