Cardenolide glycosides of Thevetia peruviana and triterpenoid saponins of Sapindus emarginatus as TRAIL resistance-overcoming compounds.
A screening study for TRAIL resistance-overcoming activity was carried out, and activity-guided fractionations of Thevetia peruviana and Sapindus emarginatus led to the isolation of four cardenolide glycosides (1-4) and four triterpenoid saponins (5-8), respectively. In particular, cardenolide glycosides (1 and 2) from T. peruviana were shown to have a significant reversal effect on TRAIL resistance in human gastric adenocarcinoma cells, and real-time PCR showed that thevefolin (2) enhanced mRNA expression of death receptor 4 (DR4) and DR5. In addition, 1H and 13C NMR characterizations are shown for thevefolin (2) for the first time.
Miyagawa
Takashi
T
Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan, Temko Corporation, 4-27-4 Honcho, Nakano, Tokyo 164-0012, Japan.
Ohtsuki
Takashi
T
Koyano
Takashi
T
Kowithayakorn
Thaworn
T
Ishibashi
Masami
M
D001483:Base Sequence; D002298:Cardenolides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D010946:Plants, Medicinal / Q000737:chemistry*; D053220:Receptors, TNF-Related Apoptosis-Inducing Ligand / Q000235:genetics; D032127:Sapindus / Q000737:chemistry*; D012503:Saponins / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D013274:Stomach Neoplasms / Q000378:metabolism; D053221:TNF-Related Apoptosis-Inducing Ligand / Q000187:drug effects*; D013785:Thailand; D031052:Thevetia / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D002298:Cardenolides; D053220:Receptors, TNF-Related Apoptosis-Inducing Ligand; D012503:Saponins; D053221:TNF-Related Apoptosis-Inducing Ligand