
Three new (1-3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characterized from a medicinal plant, Streblus asper Lour. (Moraceae), collected in Vietnam, with six new analogues and one known derivative (5a-g) synthesized from (+)-strebloside (5). A preliminary structure-activity relationship study indicated that the C-10 formyl and C-5 and C-14 hydroxy groups and C-3 sugar unit play important roles in the mediation of the cytotoxicity of (+)-strebloside (5) against HT-29 human colon cancer cells. When evaluated in NCr nu/nu mice implanted intraperitoneally with hollow fibers facilitated with either MDA-MB-231 human breast or OVCAR3 human ovarian cancer cells, (+)-strebloside (5) showed significant cell growth inhibitory activity in both cases, in the dose range 5-30 mg/kg.
Plants, Medicinal, Dose-Response Relationship, Drug, Molecular Structure, Antineoplastic Agents, Phytogenic, Moraceae, Cardiac Glycosides, Mice, Structure-Activity Relationship, Vietnam, Animals, Humans, Drug Screening Assays, Antitumor, HT29 Cells, Nuclear Magnetic Resonance, Biomolecular
Plants, Medicinal, Dose-Response Relationship, Drug, Molecular Structure, Antineoplastic Agents, Phytogenic, Moraceae, Cardiac Glycosides, Mice, Structure-Activity Relationship, Vietnam, Animals, Humans, Drug Screening Assays, Antitumor, HT29 Cells, Nuclear Magnetic Resonance, Biomolecular
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