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Structural Optimization of Caffeoyl Salicylate Scaffold as NO Production Inhibitors
- Source :
- Chemicalpharmaceutical bulletin. 67(9)
- Publication Year :
- 2019
-
Abstract
- Chlorogenic acid (CGA) has been considered as one of important active components in a number of medicinal herbs. Recently our group demonstrated that caffeoyl salicylate scaffold derived from CGA can be employed for the development of novel anti-inflammatory agents. The most active compound D104 can be a very promising starting point for the further structural optimization. A series of novel caffeoyl salicylate analogs were designed, synthesized, and evaluated by preliminary biological evaluation. The obtained results showed that the two compounds B12 and B13 can not only inhibit production of nitric oxide (NO) in RAW264.7 cells induced by lipopolysaccharides (LPS) effectively, but also have high safety in in vitro cytotoxic test, which could be comparable with D104. Molecular docking study on the peroxisome proliferator-activated receptor γ (PPARγ) protein revealed that compounds B12 and B13 can follow the same binding mode with D104, and the carboxyl group of caffeoyl salicylate scaffold might play a key role in the interaction with protein target, which implied the carboxyl group should be retained in the further optimization.
- Subjects :
- Lipopolysaccharides
Scaffold
medicine.drug_class
Cell Survival
Nitric Oxide
Anti-inflammatory
Nitric oxide
chemistry.chemical_compound
Mice
Chlorogenic acid
Drug Discovery
medicine
Cytotoxic T cell
Animals
Humans
Receptor
Binding Sites
Macrophages
General Chemistry
General Medicine
Peroxisome
In vitro
Protein Structure, Tertiary
PPAR gamma
RAW 264.7 Cells
Biochemistry
chemistry
A549 Cells
Chlorogenic Acid
Salicylic Acid
Subjects
Details
- ISSN :
- 13475223
- Volume :
- 67
- Issue :
- 9
- Database :
- OpenAIRE
- Journal :
- Chemicalpharmaceutical bulletin
- Accession number :
- edsair.doi.dedup.....fdd3b0c306a7ff03d9a32b3a01cf4736