Bioassay guided discovery of apoptosis inducers from gamboge by high-speed counter-current chromatography and high-pressure liquid chromatography/electrospray ionization quadrupole time-of-flight mass
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- 作者：Quan-Bin Han ; Yan Zhou ; Chao Feng ; Gang Xu ; Sheng-Xiong Huang ; Song-Lin Li ; Chun-Feng Qiao ; Jing-Zheng Song ; Donald C. Chang ; Kathy Q. Luo ; Hong-Xi Xu
- 关键词：High-speed counter-current chromatography ; HPLC/MS ; Apoptosis inducer ; Garcinia hanburyi ; Gambogenic acid
- 刊名：Journal of Chromatography B, Analytical Technologies in the Biomedical and Life Sciences
- 出版年：2009
- 出版时间：1 February 2009
- 年：2009
- 卷：877
- 期：4
- 页码：401-407
- 全文大小：500 K
文摘
A screening system, composed of high-speed counter-current chromatography and high-pressure liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectrometry, was established to find bioactive lead compound. This system succeeded in discovering apoptosis inducers from gamboge, the resin of Garcinia hanburyi. High-speed counter-current chromatography was used to provide well-separated fractions for bioassay and the resulted active fractions were rapidly identified using high-pressure liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectrometry. The solvent system of n-hexane/ethyl acetate/methanol/water was optimized to the ratio of 7:3:7:3 (v/v/v/v) by a K value analysis. As a result, two active fractions were obtained. They showed apoptosis inducing effects as potent as that of taxol (500 nM) at the concentration of 1 μg/ml. Gambogenic acid (72.1 % ) and epimeric isogambogic acids (25.3 % ) were identified in one of the fractions. The other active fraction mainly contained two epimeric mixtures, gambogic acids (68.7 % ) and gambogoic acids (26.9 % ). Among them, gambogenic acid, without epimerization, has priority to be lead compound.