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Bioorg Chem. 2014 Oct;56:34-40. doi: 10.1016/j.bioorg.2014.05.009. Epub 2014 Jun 2.

Synthesis and anti-tumor activity evaluation of Matijin-Su derivatives.

Author information

1
The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, China.
2
School of Chinese Medicine, The University of Hong Kong, Hong Kong Special Administrative Region.
3
School of Chinese Medicine, The University of Hong Kong, Hong Kong Special Administrative Region. Electronic address: yfeng@hku.hk.
4
The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, China. Electronic address: guangyi_liang@126.com.

Abstract

A series of Matijin-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-l-phenylalanol) derivatives was synthesized and evaluated for their anti-tumor activities in hepatocellular carcinoma cells. The IC50 of compounds 1, 3, 4, 11, 13 were less than 20μM, and compound 1 and 3 showed an IC50 value of less than 9μM. Expansion inhibition could be found significantly in compound 1 and 3-treated human hepatoma cell HepG2 and PLC/PRF/5, while both compounds exhibit lower toxicity to human hepatocyte cell line L-02. Compound 1 and 3 could induce cell cycle arrest at G1/S phase. This may be attributed to increase level of intracellular reactive oxygen species (ROS). Up-regulation of p38 MAPK activity in responding the ROS stabilize p53 and activate p21 transcription, the critical regulatory in G1/S checkpoint. Observations in this study shed light on the potential of MTS derivatives compound 1 and 3 as novel suppressors to human liver cancer.

KEYWORDS:

Anti-tumor activity; Hepatocellular carcinoma; MTS derivatives; Synthesis

PMID:
24930072
DOI:
10.1016/j.bioorg.2014.05.009
[Indexed for MEDLINE]

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