Planta Med 2012; 78 - CL30
DOI: 10.1055/s-0032-1320265

Briarane Diterpenoids: Potential tumor cell growth inhibitor

W Zhang 1, C Li 1, M Jiang 1, T Kurtan 2
  • 1Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, 325 Guo-He Road, Shanghai 200433, P. R. China
  • 2Department of Organic Chemistry, University of Debrecen, P.O.B.: 20, H-4010 Debrecen, Hungary

The structural complexity of briarane diterpenoids challenges the chemical synthesis and SAR studies of the intriguing metabolites. Our systematic study on briarane deterpenoids concerning their chemistry and bioactivities led the isolation and structural elucidation of a series of briaranes, gemmacolides G-Y. The absolute configuration was determined by a TDDFT/CD approach. In in vitro bioassays, gemmacolide J, V, and Y (1, 2, 3), showed potent growth inhibition towards tumor cell lines of A549 and MG63, being stronger than the positive control of adriamycin. The identification of possible new targets of compound 1 was conducted using the Inverse Virtual Screening approach, which showed significant interactions in the binding sites gamma, ftase, tank1, and jmjd3. The tumor cell growth inhibitory mechanism of compound 1 is currently under investigation.