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Fu Y.,China Pharmaceutical University | Chen J.,China Pharmaceutical University | Li Y.-J.,Jiangsu Kanion Pharmaceutical Co. | Zheng Y.-F.,China Pharmaceutical University | Li P.,China Pharmaceutical University
Food Chemistry | Year: 2013

Licorice, the roots and rhizomes of several Glycyrrhiza species (Leguminosae), is an important natural sweetening agent and a widely used herbal medicine. In this work, six flavonoids, 5-(1,1-dimethylal-lyl)-3,4,4′- trihydroxy-2-methoxychalcone (1), licochalcone B (2), licochalcone A (3), echinatin (4), glycy-coumarin (5) and glyurallin B (6), were isolated from the extracts of licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis). Their structures were elucidated using various spectroscopic methods. To our knowledge, compound 1 was isolated from natural plants for the first time. All the isolates were tested by antioxidant and anti-inflammatory assays. Compounds 2,4 and 5 showed strong scavenging activity toward the ABTS+ radical, and compounds 1,2,3,5 and 6 exhibited potent inhibition of lipid peroxidation in rat liver microsomes compared with the reference controls. Compounds 1-4 dose-dependently inhibited LPS induced reactive oxygen species (ROS) production in RAW 264.7 cells. Furthermore, compounds 1-5 were demonstrated to inhibit the production of nitric oxide (NO), interleukin-6 (IL-6) and prostaglandin E2 (PGE2) in LPS-induced macrophage cells. Moreover, the contents of the six compounds, in different Glycyrrhiza species, were quantified by HPLC-MS. Crown Copyright © 2013 Published by Elsevier Ltd. All rights reserved.

Niu X.S.,Jiangsu Kanion Pharmaceutical Co.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica | Year: 2012

To optimize the process for preparing genipin with enzymolyzed geniposide by an orthogonal experiment. The optimal enzymolysis process was selected by an orthogonal experiment, with the concentration of geniposide as the index as well as enzyme quantity, pH of enzymolysis solution, enzymolysis time and enzymolysis temperature as considerations. The optimal hydrolysis conditions were as follow: rough genipin samples at the concentration of 40 g x L(-1) were selected and shook on a table concentrator at a speed of 100 r x min(-1), added with beta-glucosidase-geniposide 1 : 1 (weight proportion), with pH of enzymolysis solution at 4.5, hydrolyzation temperature at 50 degrees C, the conversion rate of genipin could reach 85.8%. The process is so stable and feasible that it can provide theoretical basis for the preparation of genipin with enzymolyzed geniposide.

Bao B.,Nanjing University | Geng T.,Jiangsu Kanion Pharmaceutical Co. | Cao Y.,Nanjing University | Yao W.,Nanjing University | And 2 more authors.
International Journal of Molecular Sciences | Year: 2012

The aim of this study was to find out whether Schizonepetin influences the pharmacokinetics of the main substrates drugs of CYP1A2, CYP3A1/2, CYP2E1, CYP2C19 and CYP2D6 in rats; the influence on the levels of CYP mRNA was also studied. Phenacetin, dapsone, chlorzoxazone, omeprazole and metoprolol were selected as probe substrates for CYP1A2, CYP3A1/2, CYP2E1, CYP2C19 and CYP2D6 respectively. HPLC methods were employed for the determination of these substrates in plasma and the pharmacokinetic parameters were calculated. Real-time RT-PCR was used to determine the effects of Schizonepetin on the mRNA expression of CYP3A1, CYP1A2 and CYP2E1 in the rat liver. After the rats were orally administrated with Schizonepetin once a day for seven consecutive days, there were significant differences in plasma concentration of phenacetin, dapsone, chlorzoxazone and metoprolol, but not omeprazole, as compared with pre-administration. In addition, Schizonepetin induced the expression of CYP3A1, CYP1A and CYP2E1 at dosages of 24 and 48 mg/kg. Our results indicated that Schizonepetin had significant induction effects on CYP3A1/2 and inhibition effects on CYP1A2, CYP2E1 or CYP2D6 as oriented from the pharmacokinetic profiles of the substrates. Moreover, in the mRNA expression levels, Schizonepetin could induce the mRNA expression of CYP3A1, CYP1A and CYP2E1. In conclusion, co-administration of some CYP substrates with Schizonepetin may lead to an undesirable herb-drug interaction. © 2012 by the authors; licensee MDPI, Basel, Switzerland.

An S.Y.,Jiangsu Kanion Pharmaceutical Co.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica | Year: 2012

To determine the content of polyphenol contained samples, in order to provide basis for comprehensive quality evaluation on Echinacea extracts. LC-MS was used for qualitative analysis on relevant compounds of the samples of Echinacea extracts. Optimized USP methods, RP-HPLC and QAMS (quantitative analysis of multi-components by single-marker) were used to determine the content of polyphenol. Meanwhile, UV method was adopted for comparative analysis on content according to international standard IS014502-1-2005. The six batches of samples could not meet the export standard for polyphenol content by HPLC. UV showed four batches in line with the standard and two batches in inconformity. UV method is generally adoptedfor the content determination of domestic Echinacea extracts, but shows results that are significantly different from that by HPLC method. it is suggested to use HPLC method to standardize quality of extracts and raise market access standards.

Guo C.,China Pharmaceutical University | Han F.,China Pharmaceutical University | Zhang C.,China Pharmaceutical University | Xiao W.,China Pharmaceutical University | And 2 more authors.
Planta Medica | Year: 2014

Diabetic nephropathy, one of the most common and serious vascular complications of both type 1 and type 2 diabetes mellitus, has become a major contributor of end-stage renal failure. The aims of this study were to investigate the effects and possible underlying action mechanism(s) of oxymatrine on renal damage in diabetic rats. Diabetes was induced in male Sprague-Dawley rats by administering a high-fat diet and an intraperitoneal 30 mg/kg streptozotocin injection. The animals were treated orally with saline, metformin hydrochloride, and oxymatrine at 50, 100, and 150 mg/kg/day for 11 weeks. At the end of the treatment, renal tissue, blood, and urine samples were collected for histological and biochemical examination. The results revealed that oxymatrine significantly decreased blood glucose, urinary protein and albumin excretion, serum creatinine, and blood urea nitrogen in diabetic rats, and ameliorated diabetes-induced glomerular and tubular pathological changes. Furthermore, oxymatrine significantly prevented oxidative stress and reduced the contents of renal advanced glycation end products, transforming growth factor-β1, connective tissue growth factor, and inflammatory cytokines in diabetic rats. All these results indicate that oxymatrine has protective effects on experimental diabetic nephropathy by multiple mechanisms. © Georg Thieme Verlag KG Stuttgart New York.

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