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Abstract
Three saikosaponins were isolated from the MeOH extract of the roots of Bupleurum falcatum L.: saikosaponins B3 (1); B4 (2); and D (3). Of the three, compound 3 inhibited the interaction of selectins (E, L, and P) and THP-1 cells with IC50 values of 1.8, 3.0 and 4.3 µM, respectively. Also, the aglycone structure 4 of compound 3 showed moderate inhibitory activity on L-selectin-mediated cell adhesion. From these results, we suspect that compound 3 isolated from Bupleurum falcatum roots would be a good candidate for therapeutic strategies to treat inflammation.
Highlights
The interactions between circulating leukocytes and vascular endothelial cells play an important role in the development of inflammatory diseases such as atherosclerosis, asthma, and rheumatoid arthritis [1,2]
We investigated the potent effect of saikosaponins, isolated from the MeOH extract of B. falcatum, on selectin-mediated cell adhesion
During an investigation of selectin-mediated cell adhesion inhibitors obtained from natural sources, the MeOH extract of the roots of B. falcatum were observed to inhibit the interaction of selectin and THP-1 cells
Summary
The interactions between circulating leukocytes and vascular endothelial cells play an important role in the development of inflammatory diseases such as atherosclerosis, asthma, and rheumatoid arthritis [1,2]. Selectins are involved in the initial adhesive step in the recruitment and migration of immune cells to the inflammatory site [4,5]. P-selectin is P-selectin glycoprotein ligand-1 (PSGL-1, CD 162), constitutively expressed by leukocytes. L-selectin, which is present on leukocytes, is responsible for lymphocyte binding to endothelium and for the permeation of neutrophils in the inflammatory site stimulated by viruses and bacteria [8]. It was used as an important component of traditional oriental medicines for the treatment of chronic hepatitis and auto-immune diseases [9]. We investigated the potent effect of saikosaponins, isolated from the MeOH extract of B. falcatum, on selectin-mediated cell adhesion
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