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

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
* Authors to whom correspondence should be addressed.
Received: 26 July 2012; in revised form: 27 August 2012 / Accepted: 29 August 2012 / Published: 10 September 2012
(This article belongs to the Section Bioactives and Nutraceuticals)
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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.
Keywords: Euphorbia kansui; terpenoids; cytotoxicity; bio-guided separation; human normal liver cell lines L-O2; human normal gastric epithelial cell line GES-1

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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.

AMA 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. International Journal of Molecular Sciences. 2012; 13(9):11247-11259.

Chicago/Turabian Style

Zhang, Li; Gao, Lan; Li, Zhengjun; Yan, Xiaojing; Yang, Yanjing; Tang, Yuping; Cao, Yudan; Ding, Anwei. 2012. "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. 13, no. 9: 11247-11259.

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