Abstract
Ent-kaurane diterpenoids were studied as a biologically active ingredient group of Sigesbeckia pubescens (Makino) Makino. Here, five known ent-kaurane diterpenoids were isolated and identified, named ent-16β,17-dihydroxy-kauran-19-oic acid (1), ent-16β,17-dihydroxy-kauran-19-oate (2), ent-18-acetoxy-17-hydroxykauran-19-oic acid (3), ent-16β,17,18-trihydroxy-kauran-19 -oic acid (4), and ent-17-hydroxy-kauran-16βH-19-oic acid (5). Their inhibitory effects of these compounds on MDA-MB-231 breast cancer migration were firstly tested in a chemotaxis invasion assay. Among them, compound 1 (DKA) showed superior inhibitory activities with IC50 value of 1.96 µM. Then, a wound healing assay and BALB/c nude mice were used for further studying the inhibitory activity of DKA on MDA-MB-231 breast cancer migration in vitro and in vivo, respectively. The wound healing assay showed that DKA (1, 5, and 25 μM) can significantly inhibit cell migration and the mouse model of lung metastasis showed that DKA (2.5, 5, and 10 mg/kg) could strongly suppress the lung metastasis of MDA-MB-231 breast cancer cells.
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