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Int. J. Mol. Sci. 2012, 13(9), 11247-11259; doi:10.3390/ijms130911247

Bio-Guided Isolation of the Cytotoxic Terpenoids from the Roots of Euphorbia kansui against Human Normal Cell Lines L-O2 and GES-1

Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China
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Received: 26 July 2012 / Revised: 27 August 2012 / Accepted: 29 August 2012 / Published: 10 September 2012
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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Abstract

The dried roots of Euphorbia kansui (kansui) have been used for centuries in China as a herbal medicine for edema, ascites, and asthma. The 95% ethanol extract showed a significant inhibition of cell proliferation against human normal cell lines L-O2 and GES-1. Bioassay-guided separation of the 95% ethanol extract from the roots of E. kansui led to the isolation of 12 diverse terpenoids whose structures were identified by 1H, 13C NMR spectroscopy and ESI-MS as kansuinine A (1), kansuinine B (2), kansuinine C (3), kansuiphorin C (4), 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (5), 3-O-(2'E,4'E-decadienoyl)-20-O-acetylingenol (6), 3-O-(2'E,4'Z-decadienoyl)-20-deoxyingenol (7), 3-O-benzoyl-20-deoxyingenol (8), 5-O-benzoyl-20-deoxyingenol (9), kansenone (10), epi-kansenone (11), euphol (12). All these 12 terpernoids were evaluated in vitro for cytotoxicity on L-O2 and GES-1 cell lines. Most ingenane-type diterpenoids and 8-ene-7-one triterpenoids (511) exhibited a relatively lower IC50 value; therefore, these compounds had stronger cytotoxicity against human normal cell lines L-O2 and GES-1 with dose-dependent relationships. These results will be significantly helpful to reveal the mechanism of toxicity of kansui and to effectively guide safer clinical application of this herb. View Full-Text
Keywords: Euphorbia kansui; terpenoids; cytotoxicity; bio-guided separation; human normal liver cell lines L-O2; human normal gastric epithelial cell line GES-1 Euphorbia kansui; terpenoids; cytotoxicity; bio-guided separation; human normal liver cell lines L-O2; human normal gastric epithelial cell line GES-1
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Zhang, L.; Gao, L.; Li, Z.; Yan, X.; Yang, Y.; Tang, Y.; Cao, Y.; Ding, A. Bio-Guided Isolation of the Cytotoxic Terpenoids from the Roots of Euphorbia kansui against Human Normal Cell Lines L-O2 and GES-1. Int. J. Mol. Sci. 2012, 13, 11247-11259.

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