Chemical constituents of Plectranthus amboinicus and the synthetic analogs possessing anti-inflammatory activity
Journal
Bioorganic and Medicinal Chemistry
Journal Volume
22
Journal Issue
5
Pages
1766-1772
Date Issued
2014
Author(s)
Abstract
This study demonstrates that compounds 1-4 from an extract of Plectranthus amboinicus inhibit the binding of AP-1 to its consensus DNA sequence. Thymoquinone (5) was further identified as a nonpolar ingredient from the hexane extract of P. amboinicus to suppress the expression of lipopolysaccharide-induced tumor necrosis factor-alpha (TNF-α). We then synthesized 2-alkylidenyl-4-cyclopentene-1,3-diones as the designed biomimetics of thymoquinone, and found that compounds 8a, 8b and 8d were more potent TNF-α inhibitors.
Type
journal article