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Sun Y.,Shenyang Pharmaceutical University | Peng Y.,Shenyang Pharmaceutical University | Li L.-G.,Shenyang Pharmaceutical University | Zheng L.-W.,Shenyang Pharmaceutical University | And 5 more authors.
Evidence-based Complementary and Alternative Medicine

Alzheimer's disease (AD) is a neurodegenerative disease characterized by progressive memory loss and cognitive impairment. Cholinesterase inhibitors are widely used for the symptomatic treatment of Alzheimer's disease to enhance central cholinergic transmission. In this study, a bioactivity-oriented screening platform based on a modified Ellman's method and HPLC-QTOF MS technique was developed to rapidly screen active agents of Anemarrhena asphodeloides Bge. The 60% ethanol fraction from an ethyl acetate extract exhibited the most potential anticholinesterase activity. Fifteen steroid saponins were identified by the mass spectrum, standards and literature reports. Twenty-five compounds were isolated from the active fraction. The results showed that compounds with the C6-C3-C6 skeleton probably had both AChE and BuChE inhibitory activities. Xanthone and benzene derivatives exhibited no or little activity. Lignans showed weak BuChE inhibitory activity. The steroidal saponins demonstrated moderate or weak AChE inhibitory activity. © 2014 Yu Sun et al. Source

Sun Y.,Shenyang Pharmaceutical University | Li L.,Shenyang Pharmaceutical University | Liu C.,Shenyang Pharmaceutical University | Liu Q.,Shenyang Pharmaceutical University | And 4 more authors.
Phytochemistry Letters

Two new components, anemarrhena A (1) and anemarrhena B (2), together with five known ones (3-7), were isolated from the rhizome of Anemarrhena asphodeloides Bge. Their structures were established by detailed spectral studies, including 1D-NMR (1H NMR, 13C NMR and DEPT), 2D-NMR (HSQC, HMBC and NOESY), HR-ESI-MS and by the comparison with literature data. The absolute configuration of 2 was further determined by CD analysis. The isolated compounds were evaluated for their antiplatelet aggregative activity. Compounds 1, 2, 3, 5, 6 and 7 exhibited moderate activity of antiplatelet aggregation in vitro, compound 4 showed potential antiplatelet aggregation activity. © 2013 Phytochemical Society of Europe. Source

Sun Y.,Shenyang Pharmaceutical University | Sun Y.,Key Laboratory of Structure Based | Liu L.,Shenyang Pharmaceutical University | Liu L.,Key Laboratory of Structure Based | And 7 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences

Timosaponin AIII, a major saponin found in Anemarrhena asphodeloides Bge., exhibits a wide spectrum of bioactivities. It is believed that it may be further developed into a promising new drug. To better understand the pharmacological activities of the component, the investigation of its in vivo and in vitro metabolism was necessary. In this study, the metabolic profile of timosaponin AIII was investigated using liquid chromatography-mass spectrometric (LC/MS) techniques. Two different types of mass spectrometers-aquadrupole time-of-flight (Q-TOF) mass spectrometer and hybrid quadrupole/linear ion trap (Q-TRAP) mass spectrometer were employed to acquire structural information on timosaponin AIII metabolites. Plasma, bile, urine and feces were collected from rats after a single oral dose of 400. mg/kg of water solution. A total of 19 metabolites were detected and tentatively identified based on the mass spectral fragmentation patterns, elution order or confirmed using available reference standard. Two metabolites were detected after incubating with rat liver microsomal. What's more, we isolated sarsasapogenin from the collection of urine samples after timosaponin AIII (5.0. g) giving orally to 20 rats at a dose of 150.0. mg/kg in an interval of 7 days. The present study provided important information about the metabolism of timosaponin AIII which will be helpful for fully understanding the mechanism of this compound's action. © 2015. Source

Sun Y.,Shenyang Pharmaceutical University | Sun Y.,Key Laboratory of Structure Based | Sun Y.,Qiqihar Medical University | Wu J.,Shenyang Pharmaceutical University | And 11 more authors.
Bioorganic and Medicinal Chemistry Letters

Cancer remains a major killer worldwide. To search for novel naturally occurring compounds that are cytotoxic to cancer cells to be used as lead structures for drug development, five new steroids (1-5) along with seven known ones (6-12) were isolated from the rhizome of Anemarrhena asphodeloides Bge. Their structures were established by detailed spectral studies, including 1D-NMR, 2D-NMR, HR-ESI-MS and by comparison with literature data. These compounds exhibited different levels of growth inhibition against A549, HepG2, Hep3B, Bcap37 and MCF7 cell lines in vitro. Compounds 9, 10 and 11 showed potent inhibitory against all the tested cell lines with IC50 values ranging from 0.35 ± 0.15 to 25.53 ± 0.31 μM. The three compounds displayed stronger inhibitory activities against A549, HepG2 and Hep3B cell lines compared with the positive control 5-fluorouracil. The experimental data obtained permit us to identify the roles of the sugar moieties, hydroxyl group, double bond and F-ring with regard to their cytotoxic activities. © 2016 Elsevier Ltd. All rights reserved. Source

Qin N.-B.,Shenyang Pharmaceutical University | Qin N.-B.,Key Laboratory of Structure Based | Wang A.-L.,Shenyang Pharmaceutical University | Wang A.-L.,Key Laboratory of Structure Based | And 9 more authors.
Phytochemistry Letters

Two new clerodane-type furanoditerpenoids, tinosporins A (1) and B (2), along with two known compounds columbin (3) and fibaruretin B (4), were isolated from the root of Tinospora sagittata (Oliv.) Gagnep. Their structures were elucidated by extensive spectroscopic analyses, including 1D NMR (1H and 13C NMR), 2D NMR (HMBC and NOESY) and HR-ESI-MS, and by the comparison of the spectroscopic data with literature values. The absolute configurations of compounds 1 and 2 were determined by CD analysis. Compound 1 showed moderate cytotoxicity against HL-60 and MCF-7 cell lines. © 2015 Phytochemical Society of Europe. Published by Elsevier B.V. All rights reserved. Source

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