Bio-active constituents from Schisandra grandiflora: Isolation, semi-synthesis and evaluation of their anticancer activities

Abstract

• Two new widdarane-sesquiterpenes were isolated from the fruits of Schisandra grandiflora . • The structures of new compounds were characterized by NMR and Mass spectral techniques. • A series of derivatives from a major compound, gomosin N ( 4 ) were prepared by esterification with different acids. • Among the tested derivatives, 8a and 8h were manifested promising activity against MCF-7 and MIA PaCa cell lines. In continuation of our efforts in the exploration of Indian flora and development of new natural product-based therapeutics, bio-activity directed investigation of Schisandra grandiflora led to the isolation of two new widdarane-sesquiterpenes ( 1 and 2 ) along with four known compounds ( 3 - 8 ). Further, a series of derivatives from a major compound, gomosin N ( 4 ) were prepared by ring-opening of methylenedioxy group using Pb(OAc) 4 and followed by esterification with different acids. The structures of isolates and synthesized derivatives were confirmed by interpretation of spectral studies (NMR and Mass) and screened for their potentials against a panel of cancer cell lines. Among the tested derivatives, 8a and 8h were manifested promising activity than gomisin N ( 3 ) against MCF-7 and MIA PaCa cell lines.