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	1. Cardioprotective effects of a novel hydrogen sulfide donor in diabetes mellitus rat models with acute myocardial infarction
	Wei Guo,Zhijun Wang,Yizhun Zhu
	Pharmacy 10 May 2016
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	Abstract:Although many studies have been performed to elucidate the molecular mechanisms of heart failure, an effective pharmacological therapy to protect cardiac tissues from severe loss of contractile function associated with heart failure after acute Myocardial Infarction(MI)has yet to be developed. We examined the cardioprotective effects of S-Propargyl-L-cysteine (SPRC, also named as ZYZ-802), a novel hydrogen sulfide donor with potent antioxidant and anti-apoptotic activities in diabetes mellitus (DM) rat models of heart failure.SPRC was systemically delivered to rats 7 days before MI and 6 weeks after MI at different doses (15, 30, 60mg/kg). Cardiac function was assessed by hemodynamic measurements. The expression of proinflammatory cytokines, apoptosis-related molecules and the markers of adverse ventricular remodeling were measured using RT-PCR and Western blot. Treatment with SPRC significantly improved cardiac function, in particular by increasing dP/dt. Simultaneously, the expression of the pro-inflammatory cytokines TNF-α and IL-1 was markedly reduced in the treatment group compared with the MI group. In addition， SPRC-treated tissues displayed decreased expression of Bax, caspase-3, and caspase-9 and increased expression of Bcl-2, which was in part due to the promotion of Akt phosphorylation. These data demonstrated that SPRC possesses potent cardioprotective effects against cardiac injury in DM rat modelsof heart failure, which is mediated, at least in part, by suppression of the inflammatory and cell apoptosis responses.
	TO cite this article:Wei Guo,Zhijun Wang,Yizhun Zhu. Cardioprotective effects of a novel hydrogen sulfide donor in diabetes mellitus rat models with acute myocardial infarction[OL].[10 May 2016] http://en.paper.edu.cn/en_releasepaper/content/4687929


	2. The influence of C-terminal residue N-methylation on opioid activities of endomorphin-2
	DIAO Yuxiang,WANG Changlin
	Pharmacy 21 January 2014
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	Abstract:In the present study, the endomorphin-2 (EM-2) analogs with N-methylated modifications at C-terminal residue were investigated. Evaluating the opioid affinity, guinea pig ileum (GPI) / mouse vas deferens (MVD) potency and in vitro colonic contraction of these analogs, our results demonstrated that all analogs exerted lower μ-opioid receptor affinities and GPI/MVD potencies. The μ-opioid affinity of analog 3 was qualitatively similar to that of analog 1, but lower than that of EM-2. However, this analog showed a δ-opioid receptor affinity approximately 2-fold higher than that of EM-2. Moreover, the EC50 values on contractions of the longitudinal muscle of distal colon induced by analogs 1 and 3 were about 1.5 and 4-fold higher than that of EM-2, respectively, and the contractile effects induced by analogs 2 and 4 were deeply attenuated. Our recent results gave the evidence that N-methylated modifications of the C-terminal residue was crucial for opioid pharmacological activities of EM-2 analogs.
	TO cite this article:DIAO Yuxiang,WANG Changlin. The influence of C-terminal residue N-methylation on opioid activities of endomorphin-2[OL].[21 January 2014] http://en.paper.edu.cn/en_releasepaper/content/4583402


	3. Subcellular Quantification of Doxorubicin and its Metabolite in Cultured Human Leukemia Cells using Liquid Chromatography-Tandem Mass Spectrometry
	Xu Jinhui,Chen Yun
	Pharmacy 03 December 2012
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	Abstract:Doxorubicin (DOX) is widely used in the world as an anti-cancer agent for the treatment of leukemia and solid tumors. However, its clinic use is largely limited by the emergence of cardiotoxicity. One of the most frequently proposed mechanisms for DOX induced cardiotoxicity is the formation of metabolites. However, the enzymatic pathways involved in DOX intracellular metabolism have not been fully elucidated thus far. To provide a more detailed description of DOX metabolism, an assay using liquid chromatography-tandem mass spectrometry (LC/MS/MS) was developed in our lab to simultaneously determine DOX and its primary metabolite doxorubicinol (DOXol) in subcellular compartments. Good accuracy and precision were achieved. Using this assay, the accumulation of DOX and DOXol in whole cells, nuclear enriched fraction (NEF) and organelle-enriched fraction (OEF) were compared between two human T leukemia cell lines (i.e., Jurkat and CCRF-CEM). A time-course analysis was also carried out. The resulting varieties of DOX and DOXol subcellular distributions and concentration-time profiles might be attributed to the differential expression, activities and localization of reductive enzymes within these cell lines. More importantly, this work demonstrated that simultaneous determination of drug and its metabolite in subcellular compartments could be achieved using LC/MS/MS.
	TO cite this article:Xu Jinhui,Chen Yun. Subcellular Quantification of Doxorubicin and its Metabolite in Cultured Human Leukemia Cells using Liquid Chromatography-Tandem Mass Spectrometry[OL].[ 3 December 2012] http://en.paper.edu.cn/en_releasepaper/content/4500290


	4. Effects of catalpol against Aβ1-42-induced Alzheimer’s disease in rats brain
	Zhang Huan,Jiang Bo,Bao Yongming,Zhang Xiuli
	Pharmacy 15 May 2008
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	Abstract:Amyloid beta-peptide (Aβ) has been proposed as a model of Alzheimer’s disease (AD) as it has neurotoxicity and induces neuronal loss and cognitive decline similar to the features of AD. Catalpol, an iridoid glycoside richly in the roots of Rehmannia glutinosa, was found to have protective effects on neurodegenerative diseases in our previous experiment. The aim of this study was to assess the neuroprotective effects of catalpol against Aβ induced neurotoxicity and learning impairment in rats. The rats were divided into control group, AD-model group, sham-operated group, therapy group and prevention group. Except control and sham-operated group, Aβ1-42 was injected into the rat hippocampus to establish AD model after or before subcutaneous injection of catalpol (10 mg/kg, 5 days). The rats of therapy and prevention group showed significantly improved learning and memory ability in Morris water maze test compared with those of AD-model group. Further study showed that catalpol increased the activities of acetylcholinesterase (AChE), Na+-K+-ATPase and Ca2+ -ATPase in the hippocampus of Aβ treated rats. Simultaneously, catalpol remarkably increased ChAT positive neurons by immunohistochemical staining and reduced the histological lesions by hematoxylin and eosin (HE) staining in the hippocampus of therapy and prevention group rats. All the data indicated that catalpol might prevent and treat Aβ1-42 –induced damage in rat model and be worth studying for further preclinical study aimed for AD.
	TO cite this article:Zhang Huan,Jiang Bo,Bao Yongming, et al. Effects of catalpol against Aβ1-42-induced Alzheimer’s disease in rats brain[OL].[15 May 2008] http://en.paper.edu.cn/en_releasepaper/content/21419


	5. Anti-Angiogenesis and Anti-Tumor Activity of Modified Endostatin by Polyethylene Glycol and Low Molecular Weight Heparin
	Yang Shenglin,Tan Haining,Wang Fengshan
	Pharmacy 28 January 2008
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	Abstract:Endostatin (ES), a potent endogenous angiogenesis inhibitor, was found in 1997 by O’Reilly. In our research we chemically modified ES by polyethylene glycol (PEG) and low molecular weight heparin (LMWH). Then we studied the change of its biological activity of the modified products so as to obtain better ES derivatives. ES and its modified products could significantly inhibit the multiplication of HUVEC, angiogenesis of CAM, CNV and growth of tumor in mice. The inhibitory effects of PEG-ES and LMWH-ES were better than that of ES.
	TO cite this article:Yang Shenglin,Tan Haining,Wang Fengshan. Anti-Angiogenesis and Anti-Tumor Activity of Modified Endostatin by Polyethylene Glycol and Low Molecular Weight Heparin[OL].[28 January 2008] http://en.paper.edu.cn/en_releasepaper/content/18434


	6. Characterization and Secondary Structure Analysis of Endostatin Covalently Modified by Polyethylene Glycol and Low Molecular Weight Heparin
	Haining Tan,Shenglin Yang,You Feng,Liu Chunhui,Cao Jichao,Mou Guoying,Fengshan Wang
	Pharmacy 09 January 2008
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	Abstract:Endostatin (ES), as an angiogenesis inhibitor, has been approved by the State Food and Drug Administration (SFDA) in China for the treatment of patients with non-small-cell lung cancer. However, as a protein drug, there are a lots of obstacles on its clinical application, such as need of high dose to maintain its efficacy, expensive, poor stability, and immunogenicity, etc and limits its clinical use. In order to overcome these shortcomings, we chemically modified ES by polyethylene glycol (PEG) and low molecular weight heparin (LMWH), respectively. The changes of the secondary structure of the modified products were studied by Fourier transform infrared spectroscopy (FTIR) to obtain better ES derivatives. Our study demonstrated that the modified products have a better heat tolerance than ES towards. The result of secondary-structure analysis suggests the percentage of β-turn in whole protein is an important factor on the activity and heat stability and ES modified by LMWH can maintain higher activity and its secondary structure.
	TO cite this article:Haining Tan,Shenglin Yang,You Feng, et al. Characterization and Secondary Structure Analysis of Endostatin Covalently Modified by Polyethylene Glycol and Low Molecular Weight Heparin[OL].[ 9 January 2008] http://en.paper.edu.cn/en_releasepaper/content/17884


	7. Research Advances of Endostatin and its Short Internal Fragments
	XU HuanLi ,WANG FengShan ,TANG Wei
	Pharmacy 08 January 2008
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	Abstract:Endostatin, the C-terminal fragment of collagen XVIII, is a potent angiogenesis inhibitor. At present, there are a great deal of research papers on endostatin. However, the action mechanism of endostatin is still a matter of ongoing discussion. The objective of this review is to elucidate its origin and elementary structure, and to discuss its structure basis of activity and action mechanisms based on the latest research. Furthermore, some published studies reporting the antiangiogenic effects of endostatin-derived peptides were also reviewed. It is proposed that the amino acid sequence of endostatin contains both angiosuppressive and angiostimulatory domains. Short endostatin fragments may be exploited as a new angiogenesis inhibitor for therapeutic applications, in substitution of the full length endostatin. These studies on endostatin fragments also shed light on our understanding of the molecular action mechanisms of endostatin.
	TO cite this article:XU HuanLi ,WANG FengShan ,TANG Wei . Research Advances of Endostatin and its Short Internal Fragments[OL].[ 8 January 2008] http://en.paper.edu.cn/en_releasepaper/content/17845

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