Inhibition of VLA-4/VCAM-1-mediated Cell Adhesion by Triterpenoid Saponins from Bupleurum falcatum L

Bulletin of the Korean chemical society

Jin Ling¹  Min Seok Kim¹  Jong Sun Chang¹  Ju Hwan Lim¹  Mun Chual Rho¹  Seung Woong Lee¹  Woo Song Lee¹  Ki Hwan Bae¹ 

关键词: Bupleurum falcatum L;    Umbelliferae;    Vascular cell adhesion molecule-1 (VCAM-1);    Very late antigen-4 (VLA-4);    Saikosaponins;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Discovery and isolation of compounds capable of blocking the interactions between VCAM-1 and VLA-4, a major pair of adhesion molecules contributing to the different steps of leukocyte migration across the endothelium in inflammatory responses, has been a major goal of this lab. Through bioactivity-guided fractionation, five saikosaponins were subsequently isolated from the methanol extracts of the roots of Bupleurum falcatum L. Their structures were elucidated by spectroscopic analysis (¹H-, ¹³C-NMR and 2D-NMR), as follows, saikosaponins: A (1); D (2); C (3); B3 (4); B4 (5). Compounds 1 and 2 inhibited interaction of sVCAM-1 and VLA-4 of THP-1 cells with respective IC₅₀ values of 7.8 and 1.7 レM. The aglycone structure of 2 also showed cell adhesion inhibitory activity with an IC₅₀ value of 21.1 レM. With these results, we suspect these two saikosaponins from the Bupleurum falcatum L. roots to be prime candidates for therapeutic strategies towards inflammation.

【 授权许可】

Unknown