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Wang X.,Nanjing University | Wang X.,China Medicine Corporation | Liu X.,Nanjing University | Liu X.,China Medicine Corporation | And 7 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2015

Fangji Huangqi Tang (FHT) is a classical formula widely used in Chinese clinical application. In this paper, a novel and advanced strategy has been developed for the multiple constituent identification of FHT in rats, which was basing on an ultra-high performance liquid chromatography equipped with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-Q-TOF-MS) method combined with dynamic background subtract (DBS) data acquisition and enhance peak list (EPL) data processing techniques. Firstly, a total of 58 potential bioactive compounds including alkaloids, flavonoids, saponins, saccharides and terpenoids were detected from FHT. Their chemical structures were identified by comparing the retention time and mass spectrometry data, as well as retrieving the reference literatures. Based on the same instrumental conditions, 33 compounds were found in rat serum after oral administration of FHT. After a considerate comparison with the former chemical identification results of FHT, 33 compounds were found, which turned out to be 8 original compounds of FHT as well as 25 metabolites, including 20 phase I and 5 phase II metabolites. The results indicated that the metabolic reactions included hydroxylation, hydrogenation, demethylation, tarine conjugation and acetylation. This study firstly reported the metabolism description of fangchinoline and tetrandrine in vivo, which could be very useful for further pharmacological and clinical studies of FHT. Meanwhile, it provided a practical strategy for rapid screening and identifying of multiple constituents and their metabolites of complex traditional Chinese medicine in biological matrix. © 2015 Elsevier B.V. Source

Hao Y.,Liaoning Institute for Food and Drug Control | Li L.,Liaoning University | Chen C.,Liaoning University | Sang Y.,Liaoning University
Zhongguo Zhongyao Zazhi | Year: 2011

Objective: To investigate the chemical constituents from Lamiophlomis rotata and the bioactivities of 8-epideoxyloganic acid. Method: The constituents were isolated by using a combination of various chromatographic techniques including column chromatography over ployamide, silica gel and Sephadex LH-20. Structures of the isolates were identified by spectroscopic data analysis. Bioactivities were screened by using models in vivo. Result: Five constituents were isolated. 8-epideoxyloganic acid was isolated for the first time in L. rotata and also in lamioplomis genus. 8-epideoxyloganic acid could significantly inhibit aectic acid-induced twisting times and slower the time of homeostatsis, also inhibit xylene-induced ear edema in mice. Conclusion: 8-epideoxyloganic acid possesses bioactivities of analgesia , homeostasis and anti-inflammatory. Source

Su G.Y.,Shenyang Pharmaceutical University | Yang J.Y.,Shenyang Pharmaceutical University | Wang F.,Shenyang Pharmaceutical University | Xiong Z.L.,Shenyang Pharmaceutical University | And 7 more authors.
Journal of Pharmacy and Pharmacology | Year: 2014

Objectives Xiaochaihutang (XCHT) has been used in China for thousands of years to treat 'Shaoyang syndrome', which involves depressive-like symptoms. However, no studies were conducted to demonstrate its antidepressant effect and mechanism. This study was designed to confirm the antidepressant effect of XCHT and explore its mechanism using the pharmacological methods. Methods Ultra-HPLC and mass spectrometry was used to identify the chemical constituents of XCHT. Forced swimming test (FST) and tail suspension test (TST) were used to determine the antidepressant-like activity of XCHT in mice and rats. The possible mechanism of XCHT was elucidated by the reserpine-induced hypothermia and 5-hydroxytryptophan (5-HTP)-induced head-twitch in mice. The levels of serotonin (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) were measured in prefrontal cortex and hippocampus tissue of both mice and rats. Moreover, the extracellular 5-HT in rat hippocampus was assessed by using microdialysis coupled to HPLC with electrochemical detection. Key findings Forty-four components were detected in XCHT. XCHT significantly reduced immobility time in the TST and the FST, antagonized reserpine-induced depressive-like behaviours, increased 5-HTP-induced head-twitches, elevated 5-HT and 5-HIAA levels, and increased 5-HT turnover at doses that did not affect general activity. Conclusions These data demonstrate that XCHT has therapeutic effects in animal models of depression by enhancing the serotoninergic system in the prefrontal cortex and hippocampus. © 2013 Royal Pharmaceutical Society. Source

Yin J.,Liaoning University of Traditional Chinese Medicine | Qu J.,Liaoning Institute for Food and Drug Control | Zhang W.,Liaoning University of Traditional Chinese Medicine | Lu D.,Liaoning University of Traditional Chinese Medicine | And 3 more authors.
Biomedical Chromatography | Year: 2014

Hawthorn leaves, a well-known traditional Chinese medicine, have been widely used for treating cardiovascular and fatty liver diseases. The present study aimed to investigate the therapeutic basis treating fatty liver disease by comparing the tissue distribution of six compounds of hawthorn leaf extract (HLE) in fatty liver rats and healthy rats after oral administration at first day, half month and one month, separately. Therefore, a sensitive and specific HPLC method with internal standard was developed and validated to determine chlorogenic acid, vitexin-4''-O-glucoside, vitexin-2''-O-rhamnoside, vitexin, rutin and hyperoside in the tissues including heart, liver, spleen, kidney, stomach and intestine. The results indicated that the six compounds in HLE presented some bioactivity in treating rat fatty liver as the concentrations of the six compounds varied significantly in inter- and intragroup comparisons (healthy and/or fatty liver group). © 2013 John Wiley & Sons, Ltd. Source

Tian Y.,Shenyang Pharmaceutical University | Wang X.,Shenyang Pharmaceutical University | Xi R.,Shenyang Pharmaceutical University | Pan W.,Shenyang Pharmaceutical University | And 5 more authors.
International Journal of Nanomedicine | Year: 2014

Realgar is a poorly water-soluble compound that exhibits poor bioavailability. To improve this, the authors reduced the particle size of realgar to nanoscale by high-energy ball milling and optimized the preparation process under which (realgar weight 40g, milling time 9 hours, milling speed 38Hz, milling temperature -20°C) realgar nanoparticles (NPs) with an average size of 78±8.3nm were prepared. The average particle size of realgar was characterized by laser scattering, and its apparent shape was observed by transmission electron microscopy and scanning electron microscopy. The solubility of realgar was enhanced after milling until the particles were in the nanoscale region without altering its properties, as confirmed by a scanning electron microscopy energy-dispersive spectrometer. Realgar NPs had higher cytotoxicity on the selected cell lines, namely human breast cancer (MCF7), human hepatoma (HepG2), and human lung cancer (A549) cell lines, than coarse realgar. In addition, a pharmacokinetics study performed in rats indicated that the relative bioavailability of realgar NPs was 216.9% compared with coarse realgar; a biodistribution study performed in mice showed that after intragastric administration of realgar NPs, higher arsenic concentration was reached in the tumor, heart, liver, spleen, lung, and kidney compared with the administration of coarse realgar, as confirmed by inductively coupled plasma mass spectrometry to determine the concentration of arsenic. This study indicated that high-energy ball milling is an effective way to reduce the average particle size of realgar, and compared with coarse realgar, the cytotoxicity and bioavailability of realgar NPs were significantly improved. © 2014 Tian et al. Source

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