Abstract
Various natural and synthetic compounds including alkaloids, terpenoids and phenolics were tested for inhibition of the cell surface expression of intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1), both of which are crucial in the regulation of immune response and inflammation. Of 40 compounds tested, two compounds significantly downregulated the expression of VCAM-1 on murine endothelial cells (F-2) and ten compounds that of ICAM-1 on mouse myeloid leukemia cells (M1). Sanguinarine chloride (5) and isoliquiritigenin (13) were capable of lowering the levels of both ICAM-1 and VCAM-1. The structure-activity relationships study on chalcone and flavone derivatives related to 13 suggested that the inhibitory activity of the chalcone derivatives is attributable to the 4-hydroxy group as well as the possible coplanarity between the phenyl ring and the adjacent conjugated ketone.
Abbreviations
ICAM-1:intercellular adhesion molecule-1
LFA-1:leukocyte function associated antigen-1
VCAM-1:vascular cell adhesion molecule-1
VLA-4:very late antigen-4
Key words
Chalcone - cell adhesion molecule - ICAM-1 - VCAM-1 - immunosuppressive, anti-inflammatory
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Prof. Dr. S. Tanaka
Department of Bioscience
Tokyo University of Agriculture
1-1-1 Sakuragaoka
Setagaya-ku
Tokyo 156-8502
Japan
Email: stanaka@nodai.ac.jp
Fax: +81 3-5477-2762