Screening of several biological activities induced by different sesquiterpene lactones isolated from <i>Centaurea behen</i> L. and <i>Rhaponticum repens</i> (L.) Hidalgo

Abstract

This study aims to evaluate the in vitro cytotoxic, in vitro and in ovo anti-angiogenic effects and antimicrobial activity of sesquiterpene lactones (SLs) from two plants Centaurea behen and Rhaponticum repens (L.). Five SLs, including cynaropicrin (1), 4β,15-dehydro-3-dehydrosolstitialin A (2), aguerin B (3), janerin (4), cebellin E (5), and a flavone hispidulin (6) were isolated from C. behen (compounds 1-3) and R. repens (compounds 4-6). Cynaropicrin (1) and aguerin B (3) were characterised by strong cytotoxic activities against A2780 cells with IC₅₀ values of 1.15 and 1.62 μg mL^-1, respectively, comparable to that of doxorubicin (IC₅₀ = 1.17 μg mL^-1). The anti-angiogenic study showed the remarkable inhibitory effect of cynaropicrin (1) and aguerin B (3) on the proliferation and migration of HUVECs. In addition, cynaropycrin and aguerin B exhibited significant angio-inhibitory effects in CAM assay. These findings may be useful for the development of novel chemotherapeutic agents for the treatment of cancer.