Abstract:The aim of this study was to investigate the effects of 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one, the main component in Iris tectorum which has been used as a folk proven medicine for several centuries to treat some hepatic ailments in China, on chemical-induced liver fibrosis in rats and its possible mechanism. Liver fibrosis was induced in rats by carbon tetrachloride, plus a diet of fat, cholesterol and alcohol in the drinking water. 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one treatment significantly blocked the increase of alanine aminotransferase (ALT), aspartate aminotransferase (AST), hyaluronate (HA), laminin (LN) and procollagen III N-termimal peptide (PIIIP) contents in serum and collagen contents in liver caused by chemical-induced liver fibrosis. Chemical-induced liver fibrosis led to the drop of serum albumin concentration and the ratio of albumin and globulin (A/G), and 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one made a slight increase except tectorigenin at 30 mg/kg making a remarkable increase. Tectorigenin could also remarkably block the increase of liver lipid peroxidation (LPO) production and the decrease of liver superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities caused by liver fibrosis. Furthermore tectorigenin shows no acute toxicity. In conclusion, 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one can effectively reverse chemically induced liver fibrosis in rats and it could be developed as a liver fibrosis therapeutic drug. The therapeutic effect of 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one on chemical-induced liver fibrosis in rats appears to be due, at least in part, to its antioxidant properties. These data also support the folkloric uses of I. tectorum in the treatment of hepatic diseases including hepatic fibrosis, liver cirrhosis and hepatocellular carcinoma.

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	1. Effects of 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one on chemical-induced liver fibrosis in rats
	DING Hui,LI Erguang,SHI Dahua,WANG Yurong,WU Junhua
	Pharmacy 16 January 2012
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	Abstract:The aim of this study was to investigate the effects of 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one, the main component in Iris tectorum which has been used as a folk proven medicine for several centuries to treat some hepatic ailments in China, on chemical-induced liver fibrosis in rats and its possible mechanism. Liver fibrosis was induced in rats by carbon tetrachloride, plus a diet of fat, cholesterol and alcohol in the drinking water. 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one treatment significantly blocked the increase of alanine aminotransferase (ALT), aspartate aminotransferase (AST), hyaluronate (HA), laminin (LN) and procollagen III N-termimal peptide (PIIIP) contents in serum and collagen contents in liver caused by chemical-induced liver fibrosis. Chemical-induced liver fibrosis led to the drop of serum albumin concentration and the ratio of albumin and globulin (A/G), and 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one made a slight increase except tectorigenin at 30 mg/kg making a remarkable increase. Tectorigenin could also remarkably block the increase of liver lipid peroxidation (LPO) production and the decrease of liver superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities caused by liver fibrosis. Furthermore tectorigenin shows no acute toxicity. In conclusion, 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one can effectively reverse chemically induced liver fibrosis in rats and it could be developed as a liver fibrosis therapeutic drug. The therapeutic effect of 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one on chemical-induced liver fibrosis in rats appears to be due, at least in part, to its antioxidant properties. These data also support the folkloric uses of I. tectorum in the treatment of hepatic diseases including hepatic fibrosis, liver cirrhosis and hepatocellular carcinoma.
	TO cite this article:DING Hui,LI Erguang,SHI Dahua, et al. Effects of 5,7-dihydroxy-3-(4-hydroxyphenyl)-6-methoxy-4H-chromen-4-one on chemical-induced liver fibrosis in rats[OL].[16 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4461442


	2. The Aggravatory Effect of Nicotine on Ethanol-Induced Acute Gastric Mucosa Injury: Role of Asymmetric Dimethylarginine
	LI Yuanjian,ZHANG Zhe,ZHOU Yuan,YANG Zhichun
	Pharmacy 04 January 2012
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	Abstract:effect of nicotine on ethanol-induced acute gastric injury. METHODS：Gastric mucosa injury was induced by an injection of ethanol (75%) in the stomach in Sprague-Dawley rats. Animals were pretreated with nicotine for 28 days. Nicotine was dissolved in tap water (0.05 mg/ml). The gastric mucosal ulcer index (UI), the level of ADMA and NO were determined. Mucosal epithelium cells were treated with nicotine (10 μM) for 24 h in the presence or absence of ethanol. The concentrations of ADMA in the culture medium and the rate of cell apoptosis were determined.RESULTS：In the rats treated with ethanol, the UI and ADMA level were increased and the NO level was decreased, and the effects of ethanol were intensified by pretreatment with nicotine. Incubation of nicotine (10 μM) with epithelial cells for 24 h further increased the elevated level of ADMA and rate of cell apoptosis due to ethanol. Exogenous ADMA directly induced cell apoptosis. CONCLUSIONS：The facilitatory effect of nicotine on ethanol-induced acute gastric mucosa injury is related to induction of cell apoptosis by stimulation of ADMA generation.
	TO cite this article:LI Yuanjian,ZHANG Zhe,ZHOU Yuan, et al. The Aggravatory Effect of Nicotine on Ethanol-Induced Acute Gastric Mucosa Injury: Role of Asymmetric Dimethylarginine[OL].[ 4 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4459618

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	3. Quantitative Determination of Acetylcholine and Choline with Graphene Oxide-Based MALDI-TOF-MS
	LI Yan,ZHOU Ning,DUAN Gengli,YU Yingjia
	Pharmacy 30 August 2011
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	Abstract:Purpose: The aim of this work is to establish a novel method for quick quantitative determination of acetylcholine (ACh) and choline (Ch) with mass spectrometry. Method and Results: The determination of ACh and Ch has been established by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) with grapheme oxide instead of conventional organic acid as matrix. The obtained results indicated a low limit of detection (LOD) for ACh (0.25 fmol/μL), and excellent linearity (R2=0.9998) maintained over the range of 0.5 and 250 fmol/μL. Choline was quantified over the range of 0.05 and 15 pmol/μL, also with excellent linearity (R2=0.9994) and low LOD (15 fmol/μL). Good accuracy and precision were obtained for all concentrations within the range of the standard curves. Conclusion: The developed method was quick and reliable for quantitative determination of ACh and Ch, and may have great potential in high throughput screening of acetylcholinesterase inhibitor (AChEI).
	TO cite this article:LI Yan,ZHOU Ning,DUAN Gengli, et al. Quantitative Determination of Acetylcholine and Choline with Graphene Oxide-Based MALDI-TOF-MS[OL].[30 August 2011] http://en.paper.edu.cn/en_releasepaper/content/4441258


	4. Pharmacokinetic study of isoimperatorin in rats using UPLC-MS/MS and a drug dissolution/absorption simulating system
	LI Chao,Feng Shan,HE Xin
	Pharmacy 04 June 2011
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	Abstract:A pharmacokinetic study of isoimperatorin (IO), one of the major bioactive ingredients in the herb, Angelicae dahuricae, was performed in rats (n = 10) using a newly developed ultra-performance liquid chromatography-tandem mass spectrometry method. Tandem mass spectrometry was performed and the protonated parent→daughter ion pairs at m/z 271.02→202.9 for IO and m/z 216.9→173.7 for the internal standard, bergapten, were monitored. The analysis was validated with respect to linearity, recovery, specificity, accuracy, and precision. The pharmacokinetic parameters were obtained by non-compartmental analysis. After administration, IO was extensively distributed and rapidly eliminated from the plasma. The parameters also indicate a lower IO plasma concentration and poor absorption. Factors that led to this result were the instability of IO in acidic and basic conditions, poor solubility, and low dissolution rate. The stability of IO was observed at different pH levels using high-performance liquid chromatography, and the solubility at physiological conditions was determined using a novel drug dissolution/absorption simulating system.
	TO cite this article:LI Chao,Feng Shan,HE Xin. Pharmacokinetic study of isoimperatorin in rats using UPLC-MS/MS and a drug dissolution/absorption simulating system[OL].[ 4 June 2011] http://en.paper.edu.cn/en_releasepaper/content/4431337


	5. Fluroscence-based assay to calculate dissociation rate constant of β-secretase (BACE1) inhibitors
	ZHAO Ying
	Pharmacy 17 February 2011
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	Abstract:β-secretase (BACE1) is one of the potential drug target for Alzheimer's Disease (AD). The ideal clinically available BACE1 inhibitors should have some features, such as good effect, low dose and high selectivity. The dissociation rate constant (Koff) is useful to predict the selectivity of a BACE1 inhibitor. Based on the common used fluorescent inhibitory activity measurement, we developed the assay to measure Ki and Kon of BACE1 inhibitor, and calculated Koff using the relationship of Ki = Koff / Kon. In our assay, a tight-binding inhibitor of BACE1, OM99-2, was measured to have the Koff of 9.54×10-4 S-1, which is in good accordance with previous literature. This assay is economic and simple to use, providing a rapid way for Koff measurement of BACE1 inhibitors, which may further contribute to SAR studies.
	TO cite this article:ZHAO Ying. Fluroscence-based assay to calculate dissociation rate constant of β-secretase (BACE1) inhibitors[OL].[17 February 2011] http://en.paper.edu.cn/en_releasepaper/content/4411026


	6. NQO1-mediated redox cycle underlies tanshinone IIA induced cytotoxicity and apoptosis in non-small-cell lung cancer cells
	Yu Guo,Hao Haiping,Wang Qiong,Liu Fang,Wu Xiaolan,Zhou Fang,Lai Li,Sun Shiqin,Liu Miao,Wang Guangji
	Pharmacy 20 May 2010
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	Abstract:ITanshinone IIA (TSA) has been well defined a promising anti-cancer compound; however, its intracellular target remains unclear. Based on our previous finding that the NAD(P)H:quinone oxidoreductase (NQO1) reduced TSA to form a highly unstable catechol intermediate which auto-oxidized back to TSA, we hypothesized herein that NQO1 was the potential intracellular target of TSA to elicit its anti-tumor activity. In a pair of non-small-cell lung cancer cell lines, we found TSA exhibited a potent cytotoxic and apoptotic effect in NQO1+ A549 cells, but not in NQO1- H596 cells. In contrast, TSA exhibited efficient and almost identical uptake in A549 and H596 cells. Dicoumarol (DIC), a specific inhibitor of NQO1, could reverse largely the cytotoxic and apoptotic effect of TSA in A549 cells. TSA induced an excessive generation of reactive oxygen species, DNA damage, and G0/G1 phase arrest in A549 cells, whereas very little of such effects were observed in H596 cells and DIC pretreated A549 cells. N-acetyl cysteine also abolished almost all test aspects of TSA induced cytotoxic effects. TSA induced apoptotic cell death seemed to be p53 independent, because pifithrin-α pretreatment exerted little influence on TSA induced apoptosis and cytotoxcity, and TSA synergized DIC effect on decreasing p53 protein level. In conclusion, the present study suggests that NQO1 is likely the intracellular target of TSA, and that the NQO1 catalyzed futile redox cycle leading to the generation of ROS plays a pivotal role on TSA induced apoptotic and cytotoxic effects in NSCLC cells.
	TO cite this article:Yu Guo,Hao Haiping,Wang Qiong, et al. NQO1-mediated redox cycle underlies tanshinone IIA induced cytotoxicity and apoptosis in non-small-cell lung cancer cells[OL].[20 May 2010] http://en.paper.edu.cn/en_releasepaper/content/4373134


	7. Regioselective glucuronidation of tanshinone IIa following quinone reduction: identification of human UDP-glucuronosyltransferases, species differences, and interaction potentials
	Wang Qiong,Wang Guangji,Zhu Xuanxuan,Yu Guo,Lai Li,Liu Yitong, , ,
	Pharmacy 20 January 2010
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	Abstract:We have previously identified that the NQO1 mediated quinone reduction and subsequent glucuronidation is the predominant metabolic pathway for tanshinone IIa (TSA) in rats. The present study contributes to the further research on its glucuronidation enzyme kinetics, the identification of human UDP-glucuronosyltransferase (UGT) isoforms, and the interaction potentials. A pair of regioisomers of reduced TSA glucuronides was found from human, rats and mice, whereas only M1 was found in dog liver S9 incubations. The overall glucuronidations clearance of TSA in human liver S9 was 11.8±0.8μl/min/mg protein, 0.7, 0.8, and 3 fold of that in the mice, rats and dogs, respectively. Using CLint M2/M1 as a regioselective index, opposite regioselectivity was found between human (0.7) and mice (1.3), whereas no significant regioselectitvity was found in rats. In a sequential metabolism system by applying human liver cytosol as a NQO1 donor in combination with a panel of 12 recombinant human UGTs screen, multiple UGTs were found involved in the M1 formation, whereas only UGT1A9 and to a very minor extent of UGT1A1 and 1A3 contributed to the M2 formation. Further enzyme kinetics, correlation, and chemical inhibition studies confirmed that UGT1A9 played the major role for both M1 and M2 formations. In addition, TSA presented potent inhibitory effect on the glucuronidations of typical UGT1A9 substrates propofol and MPA, with an IC50 value at 8.4±1.8μM and 8.9±1.9μM respectively. This study would be helpful for guiding the future studies on characterizing the NQO1 mediated reduction and subsequent glucuronidations of other quinones.
	TO cite this article:Wang Qiong,Wang Guangji,Zhu Xuanxuan, et al. Regioselective glucuronidation of tanshinone IIa following quinone reduction: identification of human UDP-glucuronosyltransferases, species differences, and interaction potentials[OL].[20 January 2010] http://en.paper.edu.cn/en_releasepaper/content/39224


	8. A Rapid and Reliable Method for Pharmacokinetics Study of tilidine and its metabolite
	Li Sun,Jin Ouyang,LiYang Shen,GuoZhu Xu,YanPing Deng
	Pharmacy 13 April 2009
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	Abstract:In this article, we established a rapid and feasible gas chromatography method for the detection of tilidine and its active metabolite nortilidine in human plasma, and investigated the pharmacokinetics of tilidine in Chinese healthy subjects. The drug concentration of plasma sample from the 9 volunteers was determined by GC method and ketamine was used as internal standard. The method has been validated over a liner range from 2.5 to 160 ng/ml for tilidine, and from 5 to 160 ng/ml for nortilidine. After validation, the method was used to study the pharmacokinetic profile of tilidine and its active metabolite nortilidine in 9 Chinese healthy volunteers following administration of a single oral dose 50mg tilidine hydrochloride oral solution, the main pharmacokinetics data (mean±SD) for tilidine and nortilidine were Cmax 63.39±28.99 and 122.53±23.23 ng/ml; Tmax 0.37±0.07 and 0.64±0.30 h; t1/2 2.83±135 and 5.72±1.37 h; AUC0-∞101.59±41.85 and 577.13±189.77 ng•h•ml-1, respectively. The method is simple, sensitive, accurate and can be used for pharmacokinetics studies of tilidine and its active metabolite nortilidine.
	TO cite this article:Li Sun,Jin Ouyang,LiYang Shen, et al. A Rapid and Reliable Method for Pharmacokinetics Study of tilidine and its metabolite[OL].[13 April 2009] http://en.paper.edu.cn/en_releasepaper/content/31344


	9. Screening an anti-angiogenesis component from Tupistra Cinensis Bak. using cell membrane chromatography combined with chicken chorioallantoic membrane assay
	Langchong He,Cuiqin Li,,Sicen Wang
	Pharmacy 13 January 2009
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	Abstract:We tried to find an anti-angiogenesis component from Tupistra Cinensis Bak., a natural medicinal herb in China, using the ECV304 cell membrane chromatography (CMC) combined with chicken chorioallantoic membrane (CAM) assay. Samples were obtained using ethanol extraction, a resin column and a normal-phase column separation from Tupistra Cinensis Bak. Samples were screened by an ECV304 CMC model with the anti-flt-1 antibody as the control molecule. An active component that acted on the ECV304 cell membrane receptor (e.g., VEGFR) was found. The structure of this component was determined by UV, IR, MS and NMR and named as (5?-oleandrigenin-3-(?L-rhamnopyranoside) or ODGR. The pharmacological effect of ODGR was tested by a chicken CAM neovascularization model in vivo. ODGR significantly inhibited CAM angiogenesis within 0.94?5 礸/egg. CAM histomorphological results indicated that ODGR could inhibit sprouting of blood vessels and proliferation of vascular endothelial cells. These findings suggest that ODGR is a promising inhibitor of angiogenesis. The method of ECV304 CMC combined with chicken CAM assay can be used for discovering compounds with anti-angiogenesis actions from natural medicinal herbs.
	TO cite this article:Langchong He,Cuiqin Li,,Sicen Wang. Screening an anti-angiogenesis component from Tupistra Cinensis Bak. using cell membrane chromatography combined with chicken chorioallantoic membrane assay[OL].[13 January 2009] http://en.paper.edu.cn/en_releasepaper/content/27719

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