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High-speed counter-current chromatography (HSCCC) was successfully applied to the isolation and purification of four xanthone glycosides from Halenia elliptica, a plant widely used in traditional Tibetan medicine. The introduction of HSCCC greatly improved the efficiency of compounds preparation from Halenia elliptica. The following were obtained from 100 mg of crude sample in one-step separation: 2.5 mg of 1-O-primeverosyl-2,3,4,5,7-pentamethoxyxanthone, 7.0 mg of 1-O-primeverosyl-2,3,4,7- tetramethoxyxanthone, 10.0 mg of 1-O-primeverosyl-2,3,5-trimethoxyxanthone (demethyoxyhaleniaside), and 8.5 mg of 1-O-primeverosyl-2,3,4,5-tetramethoxyxanthone. HPLC analysis showed that each target compound had a purity of over 98%, and UV, 1H NMR, and 13C NMR data confirmed the component chemical structures.

Introduction: Xanthones, the primary constituents of <i>Swertia mussotii</i>, are known to possess a variety of biological activities, including anti-depressant, anti-leukaemic, anti-tumour, anti-tubercular, choleretic, diuretic, anti-microbial, anti-fungal, anti-inflammatory, anti-viral, cardiotonic and hypoglycemic properties. However, high performance, environmentally friendly methods for isolating and purifying xanthones from <i>S. mussotii</i> are not currently available.<br>Objective: To develop a high performance and environmentally friendly method for the preparative separation of xanthones methylswertianin, swerchirin and decussatin from <i>S. mussotii</i> using high-speed counter-current chromatography (HSCCC).<br>Methodology: A solvent system composed of <i>n</i>-hexane:ethyl acatate:methanol:water (5:5:10:4, v/v/v/v) was developed for the separation method. The upper phase was used as the stationary phase, and the lower phase was used as the mobile phase at a flow rate of 1.5 mL/min, a rotation speed of 800 rpm and a temperature of 25 °C.<br>Results: Using the described method, 8 mg of methylswertianin, 21 mg of swerchirin and 11 mg of decussatin with purities of over 98% could be isolated from a 150 mg crude sample. They were identified by ¹H-NMR and <sup>13</sup> C-NMR analysis.<br>Conclusion: Three xanthones in <i>Swertia mussotii</i> could be systematically isolated and purified using HSCCC. Copyright © 2011 John Wiley & Sons, Ltd.