Folding fan mode counter-current chromatography offers fast blind screening for drug discovery. Case study: Finding anti-enterovirus 71 agents from Anemarrhena asphodeloides

Chinese herbal medicines as a source of molecules with anti-enterovirus 71 activity

“…Components of Anemarrhena asphodeloides ( Zhi Mu ) exhibited significant pharmacological effects on the nervous system and blood, and displayed antitumor, antioxidative, antimicrobial, antiviral, anti-inflammatory, antiosteoporotic, skin-protective, and anti-aging effects [ 104 ]. By applying an isolation method called folding fan mode counter-current chromatography and CPE reduction assays, six anti-EV71 saponins were identified in A. asphodeloides , among which timosaponin B-II displayed the best medicinal potential with an EC 50 of 4.3 µM and the highest SI of 92.9 [ 105 ]. Further improvements of the isolation method were achieved using two-phase solvent systems in sample pre-treatment, which increased the production yield of the active compound [ 106 ].…”

Quantitative determination of sarsasapogenin in rat plasma using liquid chromatography-tandem mass spectrometry

“…As a typical herbal medicine, A. asphodeloides is widely used to treat febrile diseases, cough, hematochezia and hemoptysis in clinical practice [1]. Phytochemical studies revealed that A. asphodeloides contained steroidal saponins, xanthone C-glycosides, alkaloids and other components [2]. Particularly, steroidal saponins are regarded as the main active components contributing to the pharmacological efficacy of A. asphodeloides [3][4][5].…”

“…Thus, we decided to develop an easy and applicable liquid chromatography-tandem mass spectrometry (LC-MS/MS) method based on the following reasons: (1) ELISA-detecting instruments are scarcely available in most pharmacokinetics laboratories, (2) nowadays analysis by LC-MS/MS is much more common and even more specific than ELISA, and (3) given the published pharmacokinetic data of SG (determined by ELISA), the described LLOQ of 2.4 ng/mL was expected insufficient to monitor the plasma concentration-time profiles of SG for 72 h. These above mentioned factors came down to the initiative of our study. In this paper, method was developed and validated according to the FDA bioanalytical guidelines [15], and finally successfully applied to a preclinical trial in rats.…”

Anti-Enterovirus 71 Agents of Natural Products

“…Among these saponins, timosaponin B-II (48) displayed a comparable IC50 (4.3 ± 2.1 µM) and a 40-fold higher selective index (SI = 92.9) than the positive control (IC50 = 361.7 ± 104.6 µM, SI = 2.4) ribavirin [38].…”