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Anti-human hepatoma Hep-G2 proliferative, apoptotic, and antimutagenic activity of tagitinin C from Tithonia diversifolia leaves

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Abstract

Tagitinin C, a major sesquiterpenoid, was isolated from the leaves of Tithonia diversifolia. The high morbidity and mortality rate of hepatoma in Taiwan motivated our interest in the investigation of tagitinin C’s mechanism against the human hepatocellular carcinoma. The methanolic extract of leaves of T. diversifolia (TDM) and tagitinin C were found to have cytotoxic activities against human hepatoma Hep-G2 cells in the MTT assay with IC50 values of 40.0 ± 2.0 and 2.0 ± 0.1 μg/mL, respectively. This compound induced population increase in the sub-G1 phase and S phase arrest. Treatment with tagitinin C isolated from TDM resulted in activation of both caspase 3 and caspase 8 which suggested that the antiproliferative effect of this compound was caspase-dependent apoptosis. Magnetic resonance techniques indicated that the tumorigenisity of xenografts derived from Hep-G2 cells was retarded by the delivery of tagitinin C (15 μg/mouse/day) relative to the control counterparts.

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Acknowledgments

We thank Professor Jiunn-Guang Lo for his technical assistance of semipreparative HPLC, Professor Kong-Hwa Chiu for his chemical identification support, Yang-Kao Wang, Research Assistant Investigator, Department of Medicine, Skeleton-Joint Research Center, National Cheng-Kung University Medical College, Tainan, Taiwan for his discussion and Mackay Memorial Hospital Hsin Chu Branch for the assistance with magnetic resonance imaging and magnetic resonance spectroscopy. This work was supported by grants from the National Science Council of the Republic of China (Grant NSC 97-2113-M-264-001 and Grant NSC 98-2622-M-264-002-CC3).

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Correspondence to Hsiao-Chuan Wen.

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M.-H. Liao and Y.-N. Tsai contributed equally to this work.

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Liao, MH., Tsai, YN., Yang, CY. et al. Anti-human hepatoma Hep-G2 proliferative, apoptotic, and antimutagenic activity of tagitinin C from Tithonia diversifolia leaves. J Nat Med 67, 98–106 (2013). https://doi.org/10.1007/s11418-012-0652-0

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  • DOI: https://doi.org/10.1007/s11418-012-0652-0

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