Abstract
Lignans, which are recognized as main constituents in Justicia procumbens, have attracted considerable attention due to their pharmacological activities, including antitumor, anti-hepatitic, cytotoxic, anti-microbial, and anti-virus properties. Preparative high-speed counter-current chromatography (HSCCC) was successfully applied to the isolation and purification of four lignans (justicidin B (1), justicidin A (2), 6'-hydroxyjusticidin C (3) and lignan J1 (4)) from J. procumbens using stepwise elution with a pair of two-phase solvent systems composed of n-hexane–ethyl acetate–methanol–water at (1.3:1:1.3:1, v/v) and (2.5:1:2.5:1, v/v). The preparative HSCCC separation was performed on 300 mg of crude sample yielding compounds 1 (19.7 mg), 2 (9.86 mg), 3 (11.26 mg), and 4 (2.54 mg) in a one-step separation, with purities over 95% as determined by HPLC. The structures of these compounds were identified by MS, 1H-NMR and 13C-NMR. This is the first report on the application of HSCCC to the efficient separation of lignans from J. procumbens.
Highlights
Justicia procumbens (Acanthaceae), known as “Juechuang” in Chinese, is one of the most popular traditional Chinese medicines (TCMs) used to treat fever, pain, and cancer [1,2,3]
The present paper describes the successful preparative separation and purification in one-step of the four lignans justicidin B (1), justicidin A (2), 6'-hydroxyjusticidin C (3) and lignan J1 (4) (Figure 1) from a crude sample of J. procumbens using high-speed counter-current chromatography (HSCCC) in stepwise elution mode for the first time
The stepwise elution mode consisted of a pair of two-phase solvent systems composed of n-hexane-ethyl acetate-methanol-water at different ratios
Summary
Justicia procumbens (Acanthaceae), known as “Juechuang” in Chinese, is one of the most popular traditional Chinese medicines (TCMs) used to treat fever, pain, and cancer [1,2,3]. In the past few years, the bioactive principles isolated from J. procumbens were identified as arylnaphthalide and diarylbutane lignans, and their glycosides [10,11,12]. They exhibit antitumor [13], anti-hepatitis [14], cytotoxic [15], anti-microbial [16], and antiviral activities [17]. This motivated us to develop an efficient preparation method for the bioactive lignans
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