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J Agric Food Chem. 2011 Mar 23;59(6):2347-55. doi: 10.1021/jf105003n. Epub 2011 Feb 18.

Identification and anti-human glioblastoma activity of tagitinin C from Tithonia diversifolia methanolic extract.

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1
Department of Nutrition and Health Sciences, Chang Gung Institute of Technology, Taoyuan 333, Taiwan.

Abstract

The Tithonia diversifolia methanolic extract (TDM), which showed antiproliferative activity against human glioblastoma U373 cells, with an IC50 value of 59.2±3.7 μg mL(-1), was passed through silica gel chromatography and successively eluted with different percentages of EtOAc/hexane. The 10-60% EtOAc/hexane subfractions, which exhibited a comparatively higher antiproliferative activity, were isolated, and then structural identification was proceeded with 1H nuclear magnetic resonance. The isolated compound was tagitinin C, a kind of sesquiterpenoid. The IC50 value was 6.1±0.1 μg mL(-1) in U373 treated with tagitinin C. In flow cytometric analysis and inhibition of pan-caspase, the results showed that the anti-glioblastoma effect was apoptosis-independent. In PARP, p-p38, ULK1, and LC3-II expression, the anti-glioblastoma induced by tagitinin C was likely via autophagy. In the ULK1 siRNA transfection experiment, autophagy blockade counteracted the suppression induced by tagitinin C. The result suggested that tagitinin C induces U373 cell death dependent upon autophagy under certain conditions.

PMID:
21332189
DOI:
10.1021/jf105003n
[Indexed for MEDLINE]
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