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Protective effects of ursodeoxycholic acid on chenodeoxycholic acid-induced liver injury in hamsters

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World Journal of Gastroenterology 2007年第37期13卷 5003-5008页

作者： Tomomichi Iwaki Kaoru Ishizaki Shuji Kinoshita Hideki Tanaka Atsushi Fukunari Makoto Tsurufuji Teruaki Imada Research Laboratory Ⅲ (Immunology) Pharmaceuticals Research Division Mitsubishi Pharma Corporation Yokohama Japan Pharmacokinetics Laboratory Pharmaceuticals Research Division Mitsubishi Pharma Corporation Chiba Japan Discovery Technology Laboratory Pharmaceuticals Research Division Mitsubishi Pharma Corporation Yokohama Japan

AIM： TO investigate the effects of ursodeoxycholic acid （UDCA） on chenodeoxycholic acid （CDCA）-induced liver injury in hamsters, and to elucidate a correlation between liver injury and bile acid profiles in the liver.METHODS： Liver injury was induced in hamsters by administration of 0.5% （w/w） CDCA in their feed for 7 d. UDCA （50 mg/kg and 150 mg/kg） was administered for the last 3 d of the experiment.RESULTS： At the end of the experiment, serum alanine aminotransferase （ALl） increased more than 10 times and the presence of liver injury was confirmed histologically. Marked increase in bile acids was observed in the liver. The amount of total bile acids increased approximately three-fold and was accompanied by the increase in hydrophobic bile acids, CDCA and lithocholic acid （LCA）. UDCA （50 mg/kg and 150 mg/kg） improved liver histology, with a significant decrease （679.3 ±77.5 U/L vs 333.6 ± 50.4 U/L and 254.3 ±35.5 U/ L, respectively, P 〈 0.01） in serum ALT level. UDCA decreased the concentrations of the hydrophobic bile acids, and as a result, a decrease in the total bile acid level in the liver was achieved.CONCLUSION： The results show that UDCA improves oral CDCA-induced liver damage in hamsters. The protective effects of UDCA appear to result from a decrease in the concentration of hydrophobic bile acids, CDCA and LCA, which accumulate and show the cytotoxicity in the liver.

关键词： Chenodeoxycholic acid Hamster Liver bileacids Ursodeoxycholic acid

Quality of compounded topical 2% diltiazem hydrochloride formulations for anal fissure

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World Journal of Gastroenterology 2013年第34期19卷 5645-5650页

作者： Monil Shah Laura Sandler Vishwas Rai Charu Sharma Lakshmi Raghavan Ventrus Biosciences Inc. DermPathe pharmaceuticals

AIM:To investigate the quality of topical 2%diltiazem formulations extemporaneously compounded by retail pharmacies openly offering drug-compounding ***:A participating healthcare professional wrote 12 prescriptions for compounded 2%diltiazem cream,with 2 refills allowed per *** 12sets of prescriptions were filled,at intervals of 1-2 wk between refills,at 12 different independent retail pharmacies that openly offer drug-compounding services in a major metropolitan *** 36 resultant preparations,provided as jars or tubes,were shipped,as soon as each was filled,at ambient temperature to the study core laboratory for high-performance liquid chromatography(HPLC)analysis,within 10 d of *** the HPLC analysis,8 different samples of the topical diltiazem,each approximately 1 g in weight,were taken from prespecified locations within each *** initiate the HPLC analysis,each sample was transferredto a 100 mL volumetric flask,to which methanol was *** HPLC analysis was conducted in accordance with the laboratory-validated method for diltiazem in cream,ointment,and gel *** main outcome measures were potency(percentage of label claim)and content uniformity of the compounded topical 2%diltiazem ***:Of the 36 prescriptions filled,30 were packaged in jars and 6 were packaged as *** prescriptions were specifically for cream formulations,but6 of the 12 pharmacies compounded 2%diltiazem as an ointment;for another pharmacy,which had inadequate labeling,the dosage form was *** United States Pharmacopoeia(USP)standard for potency is 90%-115%of label *** the 36 preparations,5(13.89%)were suprapotent and 13(36.11%)were *** suprapotent prescriptions ranged in potency from 117.2%to 128.5%of label claim,and the subpotent prescriptions ranged in potency from34.8%to 89.8%of label ***(38.9%)preparations lacked content uniformity according to the USP standard of 90%-110%pote

关键词： Anal fissure Pharmacy compounding Topical diltiazem Formulation potency Content uniformity

Synthesis, Crystal structure and Antioxidant of 3,5-Dihydroxy-N′-(5-bro-2-hydroxybenzylidene)benzohydrazide Hydrate

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Chinese Journal of Structural Chemistry 2012年第9期31卷 1309-1314页

作者：孙振高连方张建伟孙金龙郭颖张宁刁云鹏 Affiliated Hospital of Shandong University of Traditional Chinese Medicine&pharmaceuticals Shandong University of Traditional Chinese Medicine&pharmaceuticals College of Pharmacy Dalian Medical University

A new compound, 3,5-dihydroxy-N′-（5-bro-2-hydroxybenzylidene）benzohydrazide hydrate, has been synthesized and characterized by single-crystal X-ray diffraction. The title compound crystallizes in a monoclinic system, space group P21/c with a = 14.267（6）, b = 8.079（4）, c = 13.157（6） , β = 108.114（4）, Z = 4, V = 1441.4（11） 3, Dc = 1.701 g/cm3, F（000） = 744.0, μ = 2.878 and S = 1.021. The final R = 0.0457 and wR = 0.1149 for 3500 observed reflections with I 〉 2 （I）. The ability with which the compound scavenges free radicals of ABTS and DPPH, IC50, is 34.13 and 101.6 μM, respectively.

关键词： Schiff base compound crystal structure antioxidant activity

Cancer-specific metabolism:Promising approaches for colorectal cancer treatment

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World Journal of Gastrointestinal Oncology 2019年第10期11卷 768-772页

作者： Keun-Yeong Jeong The Research Center Metimedi Pharmaceuticals

Investigation of cancer-specific metabolism has made it possible to establish the principle that atypically reconstituted metabolism is considered a hallmark of cancer due to changes in physiological ***,a variety of targets depending on the prompted aerobic glycolysis process,starting from the abnormal uptake of glucose,and cancer-specific metabolism due to impaired mitochondrial function and abnormal expression of drug-metabolizing enzymes have been investigated and *** that most solid cancers rely on cancer-specific metabolism to support their growth,it is necessary to examine closely the specific processes of cancer metabolism and have a detailed understanding of how cellular metabolism is altered in colorectal cancer(CRC)related to CRC survival and *** development of key methods to regulate efficiently cancer-specific metabolism in CRC is still in the initial ***,targeting cancer-specific metabolism will yield treatable methods that are critical as a new area of development strategies for CRC treatment.

关键词： Colorectal cancer Cancer metabolism Warburg effect Aerobic glycolysis Mitochondria metabolism

The RAF family: an expanding network of post-translational controls and protein-protein interactions

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Cell Research 1998年第2期8卷 81-98页

作者： YURYEV ANTON LAWRENCE P WENNOGLE (Novartis pharmaceuticals Corporation, Summit, NJ, USA ) Novartis pharmaceuticals Corporation Summit USA

Protein kinase RAF is strategically located in the "Ras - MAP-kinase signal transduction pathway". a principle system which transmits signals from growth factor receptors to the nucleus, resulting in cell *** factor responses are mediated in part by activation of Ras, which in turn activates RAF to phosphorylate MEK, its downstream substrate. MEK activates MAPkinase to influence nuclear events. It is clear, however,that a network of signals other than those carried by Ras plays a role in RAF regulation. These orthogonal influences are mediated by: serine/threonifle kinases, tyrosine kinases, and protein - protein interactions. As a further complication to the RAF network, three isoforms of RAF have been established which have divergent N-terminal regulatory domains. Whereas these divergent regulatory domains implicate isoform-specific functions, no clear evidence or hypothesis for distinct functions for individual isoforms has been presented. Recently, "isoform-specific protein interactions" have been identified among numerous proteins interacting with RAF. These studies may serve to delineate independent functions for RAF isoforms.

关键词： an expanding network of post-translational controls and protein-protein interactions The RAF family Cell

Biorelevant test for supersaturable formulation

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Asian Journal of Pharmaceutical Sciences 2017年第1期12卷 9-20页

作者： Enxian Lu Shoufeng Li Zhongqin Wang Shanghai Aucta pharmaceuticals Co. Ltd.

Supersaturable formulation can generate supersaturation after dissolution, providing kinetic advantage in vivo. However, the supersaturation may precipitate before being absorbed, which makes it difficult to ensure and predict its in vivo performance. The traditional USP method is typically for Quality Control(QC) purpose and cannot be used to predict the formulation in vivo performance. Therefore, there is generally a lack of a predictive biorelevant testing method. In this review, different types of supersaturable formulations are described, including amorphous dispersions, polymorphs, salts/co-crystals, weak base and supersaturable solubilized formulations. Different kinds of in vitro dissolution methods for supersaturable formulations are also reviewed and discussed. Most of the methods take the physiology of gastrointestinal(GI) track into consideration, allowing reasonable prediction of the in vivo performance of supersaturable formulation. However, absorbing drug from GI track into blood stream is a complicate process, which can be affected by different in vivo processes such as transporter and metabolism. These factors cannot be captured by the in vitro testing. Thus,combining in vitro biorelevant dissolution methods with physiology-based pharmacokinetic modeling is a better way for the product development of supersaturable formulation.

关键词： Biorelevant Dissolution Supersaturable Formulation Bioavailability

Skeletal phenotypes in secreted frizzled-related protein 4 gene knockout mice mimic skeletal architectural abnormalities in subjects with Pyle's disease from SFRP4 mutations

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Bone Research 2023年第1期11卷 193-200页

作者： Robert Brommage Jeff Liu David R.Powell Department of Metabolism Research Lexicon PharmaceuticalsThe WoodlandsTX77381USA

Mutations in SFRP4 cause Pyle’s bone disease with wide metaphyses and increased skeletal *** WNT signaling pathway plays important roles in determining skeletal architecture and SFRP4 is a secreted Frizzled decoy receptor that inhibits WNT *** cohorts of male and female Sfrp4 gene knockout mice,examined through 2 years of age,had a normal lifespan but showed cortical and trabecular bone *** human Erlenmeyer flask deformities,bone cross-sectional areas were elevated 2-fold in the distal femur and proximal tibia but only 30%in femur and tibia *** cortical bone thickness was observed in the vertebral body,midshaft femur and distal *** trabecular bone mass and numbers were observed in the vertebral body,distal femur metaphysis and proximal tibia *** femurs retained extensive trabecular bone through 2 years of *** bodies had increased compressive strength,but femur shafts had reduced bending ***,but not cortical,bone parameters in heterozygous Sfrp4mice were modestly *** resulted in similar declines in both cortical and trabecular bone mass in wild-type and Sfrp4 KO ***4 is critical for metaphyseal bone modeling involved in determining bone ***4 KO mice show similar skeletal architecture and bone fragility deficits observed in patients with Pyle’s disease with SFRP4 mutations.

关键词： SFRP4 skeletal elevated

Potential Applications of Polymer Microchips in pharmaceuticals

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材料科学与工程学报 2000年第Z2期20卷 993-1000页

作者： James J. Bao Prcoter & Gamble pharmaceuticals P.O.Box 8006 MasonOH 45040USA

Some of the most recent development in polymer based microchips have been reviewed. Different methods used in fabricating ploymer microchips are introduced. The inportance and applications of the ploymer microchip in pharmaceutical and other areas are discussed. Finally, the potential problems and development areas in polymer microchip technology are also addressed.

关键词： used in

Design and synthesis of DPP-4 inhibitor for the treatment of type 2 diabetes

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Chinese Chemical Letters 2010年第3期21卷 253-256页

作者： Peng Cho Tang Shanghai Hengrui pharmaceuticals Co.Ltd. 279 Wenjing Road

An efficient stereoselective synthesis of the rigid aza-bicyclo[3.2.0]heptane scaffold has been developed to provide 2-cyano-pyrrolidine alpha-amino amide 1 as DPP-4 inhibitor.

关键词： DPP-4 inhibitor Aza-bicyclo[3.2.0]heptane scaffold 2-Cyanopyrrolidine alpha-amino amide derivative Synthesis Type 2 diabetes