2. Academic Validation
  3. Cardenolide glycosides of Thevetia peruviana and triterpenoid saponins of Sapindus emarginatus as TRAIL resistance-overcoming compounds

Cardenolide glycosides of Thevetia peruviana and triterpenoid saponins of Sapindus emarginatus as TRAIL resistance-overcoming compounds

  • J Nat Prod. 2009 Aug;72(8):1507-11. doi: 10.1021/np900202n.
Takashi Miyagawa 1,  Takashi Ohtsuki,  Takashi Koyano,  Thaworn Kowithayakorn,  Masami Ishibashi
Affiliations

Affiliation

  • 1 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.
PMID: 19594141 DOI: 10.1021/np900202n
Abstract

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.

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