Abstract

Cancelled due to Travelling Problems

Wei Li, Associate Professor, Toho University

Historically, natural products have provided the most successful inspiration for new drug development due to both great structural diversity and potent biological activity. Herein, we report our recent progresses on the discovery of novel biologically active natural products as lead compounds for new drug development, through approaches of screening of plant extracts and compounds libraries, bioactivity-guided fractionation, chemical structure analyses and biological evaluations. Glycybenzofuran was found as the first example of 2-aryl-3-methylbezofuran-type flavonoids from the roots of Glycyrrhiza uralensis, and exhibited potent protein tyrosine phosphatase 1B inhibitory activity. Its action profile on insulin stimulated signaling pathway revealed its potentials as a new anti-insulin-resistant drug. Stelleralides A is a novel daphnane-type diterpenoids from the roots of Stellera chamaejasme, and showed extremely potent anti-HIV activity (EC90 at sub-nM) but with low cytotoxicity. Stelleralides A appears to be a promising compound into clinical trials as a new anti-AIDS drug candidate. Ardisianoside B is a novel 13,28-epoxy triterpenoid saponin from Ardisia japonica, and showed a potent but selective anti-proliferative activity against human liver cancer cells without affecting normal liver cells. The activity is bene?cial for development of a speci?c and ef?cient anti-cancer agent with low toxic side effects.