Min Yan1, Yan Lu1, Chin-Ho Chen2, Yu Zhao3, Kuo-Hsiung Lee3,4, Dao-Feng Chen1. 1. Department of Pharmacognosy, School of Pharmacy, Fudan University , Shanghai 201203, People's Republic of China. 2. Duke University Medical Center , Box 2926, SORF, Durham, North Carolina 27710, United States. 3. Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina , Chapel Hill, North Carolina 27599-7568, United States. 4. Chinese Medicine Research and Development Center, China Medical University and Hospital , Taichung, Taiwan.
Abstract
Bioassay-guided fractionation of a petroleum ether extract of the roots of Stellera chamaejasme led to the isolation of seven new (stelleralides D-J, 1-7) and 12 known (8-19) daphnane diterpenoids. The structures and relative configurations of 1-7 were established on the basis of extensive spectroscopic analysis, including HRESIMS and comprehensive NMR techniques. All isolates were evaluated for anti-HIV activity in MT4 cells. All compounds tested, except 2, showed anti-HIV activity, and, especially, five 1α-alkyldaphnane diterpenoids (3, 4, 5, 10, and 11) exhibited extremely potent anti-HIV activity, with EC50 values of 0.06-1.1 nM and selectivity index values of more than 10,000.
Bioassay-guided fractionation of a petroleum ether extract of the roots of n class="Species">Stellera chamaejasme led to the isolation of seven new (stelleralides D-J, 1-7) and 12 known (8-19) daphnanediterpenoids. The structures and relative configurations of 1-7 were established on the basis of extensive spectroscopic analysis, including HRESIMS and comprehensive NMR techniques. All isolates were evaluated for anti-HIV activity in MT4 cells. All compounds tested, except 2, showed anti-HIV activity, and, especially, five 1α-alkyldaphnanediterpenoids (3, 4, 5, 10, and 11) exhibited extremely potent anti-HIV activity, with EC50 values of 0.06-1.1 nM and selectivity index values of more than 10,000.
Authors: Luis M Bedoya; Nieves Márquez; Natalia Martínez; Silvia Gutiérrez-Eisman; Amparo Alvarez; Marco A Calzado; José M Rojas; Giovanni Appendino; Eduardo Muñoz; José Alcamí Journal: Biochem Pharmacol Date: 2008-12-03 Impact factor: 5.858