Abstract
Investigation of the seeds of Thevetia peruviana resulted in the isolation of 15 new (2-16) and 18 known (1 and 17-33) cardiac glycosides. Eight 19-nor-cardenolides (1-8), including two rare 19-nor-10-hydroperoxycardenolides, were obtained from T. peruviana for the first time. All the structures were characterized by NMR spectroscopy and chemical derivatization. The inhibitory effects of cardiac glycosides 1-33 against three cancer cell lines (human lung cancer cells, P15; human gastric cancer cells, MGC-803; and human pancreatic cancer cells, SW1990) and one normal hepatocyte cell line, LO2, were evaluated, and a preliminary structure-activity relationship is discussed. In addition, cardiac glycosides 1, 22, 26, and 28 were evaluated for their apoptosis-inducing activities in MGC-803 cells, showing IC50 values in the range 0.02-0.53 μM.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents, Phytogenic / chemistry
-
Antineoplastic Agents, Phytogenic / isolation & purification*
-
Antineoplastic Agents, Phytogenic / pharmacology
-
Cardenolides / chemistry
-
Cardenolides / isolation & purification*
-
Cardenolides / pharmacology
-
Cardiac Glycosides / chemistry
-
Cardiac Glycosides / isolation & purification*
-
Cardiac Glycosides / pharmacology
-
Drug Screening Assays, Antitumor
-
Drugs, Chinese Herbal / chemistry
-
Drugs, Chinese Herbal / isolation & purification*
-
Drugs, Chinese Herbal / pharmacology
-
Humans
-
Inhibitory Concentration 50
-
Molecular Structure
-
Nuclear Magnetic Resonance, Biomolecular
-
Seeds / chemistry*
-
Structure-Activity Relationship
-
Thevetia / chemistry*
Substances
-
Antineoplastic Agents, Phytogenic
-
Cardenolides
-
Cardiac Glycosides
-
Drugs, Chinese Herbal