Inhibitory Effect of Bupleuri Radix Saponins on Adhesion of Some Solid Tumor Cells and Relation to Hemolytic Action: Screening of 232 Herbal Drugs for Anti-Cell Adhesion

Abstract

Anti-cell adhesive activity and hemolytic action of herbal drugs were investigated. Among 232 herbal drugs tested, six showed a remarkable anti-cell adhesive activity, and the extract from the roots of Bupleurum falcatum (Umbelliferae), the semen of Psorala corylifolia (Leguminosae), and the semen of Areca catechu (Palmae) showed an anti-cell adhesive action at non-cytotoxic concentrations. Saikosaponins-a, d and e, isolated from the roots of Bupleurum falcatum, exhibited a potent anti-cell adhesive activity and a strong hemolytic action. In a structure-activity relationship for both activities, it seems that a sugar moiety and an ether linkage between C-13 and C-28 are required for good bioactivities. In addition, saikosaponin d with a β-hydroxy group at C-16 was more potent than saikosaponin a possessing an α-hydroxy group. Taken together, it is suggested that the mechanism for anti-cell adhesive activity of saikosaponin may resemble that for their hemolytic action.

Key words

Bupleurum falcatum - Umbelliferae - saikosaponin - anti-cell adhesion - hemolysis