Antitumor Agents. 261. 20(S)-Protopanaxadiol and 20(S)-Protopanaxatriol as Antiangiogenic Agents and Total Assignment of 1H NMR Spectra

Abstract

Angiogenesis is a critical step in tumor progression and involves several steps including endothelial cell (EC) proliferation, migration, and matrix remodeling. We investigated the antiangiogenic effects of 20(S)-protopanaxadiol (1) and 20(S)-protopanaxatriol (2), the sapogenins of two major ginseng saponins, in an angiogenesis model of human umbilical vein endothelial cells (HUVECs). These compounds inhibited the proliferative activity of HUVECs in a dose-dependent manner and have potential as anticancer drug candidates. In addition, we report the complete and unambiguous assignment of ¹H NMR spectra of 1 and 2, based on analyses of 2D NMR spectra including COSY, NOESY, HSQC, and HMBC. This report is the first to completely assign the ¹H NMR signals of 2, together with correction of data for 1 from prior reports.