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Role of inositol 1,4,5-trisphosphate receptors in α1-adrenergic receptorinduced cardiomyocyte hypertrophy

Acta Pharmacologica Sinica 2006年第7期27卷 895-900页

作者： Da-li LUO~(2,3.5) Jian GAO~2 Xiao-mei LAN~3.Gang WANG~4 Sheng WEI~4 Rui-ping XIAO~4 Qi-de HAN~3. Department of Pharmacology,School of Chemical Biology & pharmaceutical Sciences,capital university of Medical Sciences,Beijing 100069,china 3.{3. of Cardiovascular Science at Health Science Center,Peking university Beijing 100083.china 4 {3. of Molecular Medicine and College of Life Science,Peking university,Beijing 100871,china Department of Pharmacology School of Chemical Biology & Pharmaceutical Sciences Capital University of Medical Sciences Beijing 100069 China institute of Cardiovascular Science at Health Science Center Peking University Beijing 100083 China institute of Molecular Medicine and College of Life Science Peking University Beijing 100871 China

Aim:Intracellular Ca2+plays pivotal roles in diverse cellular functions,includinggene transcription that underlies cardiac remodeling during stress ***,the role of inositol 1,4,5-trisphosphate receptors（IP3.s）in the media-tion of cardiac intracellular Ca2+and hypertrophic growth remains *** with neonatal rat ventricular myocytes suggests that activation of IP3.smay be linked to α1adrenergic receptor（α1AR）increased stereotyped Ca2+sparkoccurrence and global Ca2+***,we hypothesized that Ca2+releasethrough IP3.s was necessary for α1AR-stimulated cardiac ***:We used myoinositol 1,4,5-trisphosphate hexakis（butyryloxymethyl）ester（IP3.M）,a membrane-permeant ester of IP3.to activate IP3.s directly,and Fluo 4/AM tomeasure intracellular Ca2+***:IP3.M(10μmol·L-1)mimicked theeffects of phenylephrine,a selective agonist of α1AR,in increments in local Ca2+spark release（especially in the perinuclear area）and global Ca2+*** importantly,IP3. inhibitors,2-aminoethoxydiphenyl borateand Xestospongin C,abolished the IP3.M-induced Ca2+responses,and signifi-cantly suppressed α1AR-induced cardiomyocyte hypertrophy assayed by cellsize,[3.]leucine incorporation and atrial natriuretic factor gene expression,dur-ing sustained（48 h）phenylephrine ***:These results,therefore,provide cellular mechanisms that link IP3. signaling to α1AR-stimulatedgene expression and cardiomyocyte hypertrophy.

关键词： inositol 1,4,5-trisphosphate receptors Ca2+sparks α1 adrenergic stimulation cardiac hypertrophy

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Transcervical Approach for Resection of Lateral Skull Base Tumors

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Journal of Otology 2007年第2期2卷 102-108页

作者： LIU Jian-feng1, ZHANG Qiu-hang1, 2, YANG Da-zhang1, QU Qiu-yi2 1 Department of Otorhinolaryngology, china Japan Friendship hospital, Beijing, china 2 Department of Otorhinolaryngology Head & Neck Surgery, {3., capital university of Medical Science, Beijing, 100053, china Department of Otorhinolaryngology China Japan Friendship Hospital Beijing China Department of Otorhinolaryngology Head & Neck Surgery Xuanwu Hospital Capital University of Medical Science Beijing 100053 China

Objectives Conventional approaches for removal of lateral skull base tumors, including transmandibular, infratemporal fossa, preauricular transzygmatic subtemporal approaches, are major invasive procedures that often sacrifice hearing and cause abnormal occlusion and cosmetic defects. Reports of the transcervical approach for resection of skull base tumors are rare, although it was described for resection of clival chordomas in as early as 1966. The purpose of this study is to review our experiences in management of lateral skull base tumors using the transcervical approach. Study Design Retrospective chart review. Methods Six lateral skull base tumor cases treated with transcervical approach procedures were reviewed, including the medical records. Results There were 4 males and 2 females. Age ranged from 12 through 52 years. Histopathological diagnoses included malignant schwannoma(n = 1), malignant carotid body tumor(n = 1), heamangioma(n=1), schwannoma (n=2) and pleomorphic adenoma (n = 1). Transcervical techniques were used in all cases with the use of microscope in the lateral skull base area. Complete tumor removal was achieved in all cases. Postoperative radiotherapy was implemented in 1 case of malignant schwannoma and 1 case of malignant carotid body tumor. Jugular foramen syndrome occurred as a surgical complication in 1 case of malignant Schwannoma of the vagus nerve. There was no tumor recurrence during the 10 - 42 month follow-up period. Conclusion Compared with conventional approaches, the transcervical approach provides a easy, safe, minimal invasive and effective procedure for removal of selected lateral skull base tumors.

关键词： skull base tumor transcervical approach excision

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Population pharmacokinetics of valproate in Chinese children with epilepsy

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Acta Pharmacologica Sinica 2007年第10期28卷 1677-1684页

作者： De-chun JIANG~(2,3.,Li WANG~4,Yu-qin WANG~(2,6),Lin LI~3.Wei LU~5,Xiang-rong BAI~2~2 Department of Pharmacy,Xuan-wu hospital of capital Medical university,Beijing {3. ~4 Department of Pediatrics,Peking universityFirst hospital,Beijing 10003.,china ~3.Department of Pharmacology,Xuan-wu hospital of capital Medical university,Education Ministry KeyLaboratory for Neurodegenerative Diseases,Beijing {3. ~5 School of pharmaceutical Science,Peking university,Beijing 100083.china ment of Pharmacy Xuan-wu Hospital of Capital Medical University Beijing 100053 China. wangyuqin8682@***.

Aim:The aim of the present study is to establish a population pharmacokinetic（PPK） model of valproate （VPA） in Chinese epileptic children to promote thereasonable use of anti-epileptic ***:Sparse data of VPA serumconcentrations from 417 epileptic children were *** patients weredivided into 2 groups:the PPK model group （n=3.7） and the PPK valid group（n=100）.The PPK parameter values of VPA were calculated by NONMEM soft-ware using the data of the PPK model group.A basic model and a final modelwere set *** validate the 2 models,the concentrations of PPK valid groupwere predicted by each model,*** mean prediction error （MPE）,mean squared prediction error （MSPE）,root mean squared prediction error（RMSPE）,weight residues （WRES）,and the 95% confidence intervals （95%CI） were also ***,the values between the 2 models were ***:The PPK of VPA was determined by a 1-compartment model with afirst-order absorption *** basic model was:Ka=3.09 (h-1),V/F=20.4（L）,CL/F=0.296 （L/h）.The final model was:Ka=0.251+2.24·（1-HS）(h-1),V/F=2.88+0.157·WT （L）,CL/F=0.1060.98·CO+0.0157·AGE （L/h）.For thebasic model,the MPE,MSPE,RMSPE,WRES,and the 95% CI were-23.53.-3..3.,-16.70）,3.28.96 （2872.72,4585.20）,3..62 （3..3.,44.90）,and-0.06 （-0.14,0.02）,*** the final model,the MPE,MSPE,RMSPE,WRES,and the95% CI were-1.16 （-4.85,2.53.,1002.83.（1050.64,1143.61）,23.04 （21.12,24.96）,and0.08 （-0.04,0.20）,*** final model was more optimal than the ***:The PPK model of VPA in Chinese epileptic children wassuccessfully *** will be valuable to facilitate individualized dosageregimens.

关键词： population pharmacokinetics valproic acid epilepsy children Bayesian method NONMEM software individualized dosage regimens

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Resolution of α-cyclohexyl-mandelic acid enantiomers by two-phase (O/W) recognition chiral extraction

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Science china Chemistry 2007年第6期50卷 764-769页

作者： TANG KeWen1,2, ZHANG GuoLi2, HUANG KeLong2, LI Yuanjian3.& YI JianMin1,2 1 Department of Chemistry and Chemical Engineering, Hunan institute of Science and Technology, Yueyang 414000, china 2 College of Chemistry and Chemical Engineering, Central South university, Changsha 410083. china 3.College of pharmaceutical Science, Central South university, Changsha 410078, china Department of Chemistry and Chemical Engineering Hunan Institute of Science and TechnologyYueyang 414000China College of Chemistry and Chemical Engineering Central South UniversityChangsha 410083China

This paper presents a new chiral separation technology:two-phase(O/W)recognition chiral *** behavior of alpha-cyclohexyl-mandelic acid enantiomers was studied in the extraction system with D(L)-isobutyl tartrate in 1,2-dichloroethane organic phase and beta-CD derivatives in aqueous phase,and the influence of the kind and concentration of extractant and pH on extraction performance was *** experimental results indicate that two-phase(O/W)recognition chiral extraction is of strong chiral separation ***-^-CD,HE-beta-CD and Me-beta-CD have higher recognition ability for S-CHMA than that for R-CHMA,among which HP-beta-CD has the strongest ability;whereas,D-isobutyl tartrate has reversed recognition ability for *** the extraction system containing HP-beta-CD and D-isobutyl tartrate,e.e.% of S-CHMA in aqueous phase reached 27.6% by one stage extraction,and the distribution ratio for R-CHMA(k_R)and for S-CHMA(k_S)and separation factor(alpha)are 2.44,0.89 and 2.49,***,pH and concentration of extractant have great effects on chiral separation ***-phase(O/W)recognition chiral extraction has great significance for preparative separation of racemic compounds.

关键词： two-phase(W/0)recognition chiral extraction alpha-cyclohexyl-mandelic acid enantiomers

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Propranolol and verapamil inhibit mRNA expression of RyR2 and SERCA in L-thyroxin-induced rat ventricular hypertrophy

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Acta Pharmacologica Sinica 2004年第03期25卷 93-97页

作者： rat ventricular hypertrophy1 Xiao-dong WU2,De-zai DAI2,Qiu-pin ZHANG3.Feng GAO3.Research Division of Pharmacology,china pharmaceutical university 3.aboratorial Center ofMedicine,Southeast university,Nanjing 210009,china Research Division of Pharmacology China Pharmaceutical University Laboratorial Center of Medicine Southeast University

AIM: To study the alteration in the mRNA level of cardiac ryanodine receptor 2 (RyR2) and sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) in L-thyroxin-induced hypertrophy. METHODS: L-thyroxin (500 g/kg) daily was injected for 10 d. RT-PCR was used to determine mRNA expression. RESULTS: An increase in the relative amount of RyR2 (111 %) and SERCA mRNA (65 %) expression was observed in the hypertrophied rats (RyR2: 77±11; SERCA: 87±10, n=9) compared with the normal rats (RyR2: 3.±10; SERCA: 53.10, n=9). Propranolol was effective to inhibit the increase in RyR2 (51±7) and SERCA (63.13. mRNA expression in hypertrophied rats, respectively. Verapamil also reduced RyR2 (62±5) and SERCA (75±8) mRNA expression. CONCLUSION: Both RyR2 and SERCA mRNA level in L-thyroxin-induced cardiac hypertrophy was over-expressed and propranolol or verapamil inhibited the alteration.

关键词： heart hypertrophy arrhythmia ryanodine receptors Ca2+-transporting ATPase L-thyroxin propranolol verapamil reversed transcriptase polymerase chain reaction

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A New Oxoaporphine Alkaloid from Alphonsea Mollis Dun.

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Chinese Chemical Letters 1999年第8期10卷 675-676页

作者： Ning XIE Zhi Hua CHENG Xiao Gan YU (Department of Phytochemistry china pharmaceutical university, Nanjing 210009)(Zhongkun {3. of Pharmaceutics, china pharmaceutical university, Nanjing 210009)(Jiangxi Provincial Children’s hospital, Nanchang 3 china Pharmaceut Univ Dept Phytochem Nanjing 210009 Peoples R China china Pharmaceut Univ Zhongkun Inst Pharmaceut Nanjing 210009 Peoples R China Jiangxi Prov Childrens Hosp Nanchang 330006 Peoples R China

A new oxoaporphine alkaloid, 1,2-methylene-dioxy-8-hydroxy-5- oxoaporphine, was isolated from the stem barks of Alphonsea mollis . Its structure was established on the basis of spectral analysis and chemical correlation.

关键词： Alphonsea mollis oxoaporphine 1.2-methylenedioxy-8-hydroxy-5-methoxy oxoaporphine

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复方碘口腔喷雾原位膜的制备及促口腔溃疡修复评价

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中国药科大学学报 2024年

作者：张小军黄山芩郭潇涵季梦菲沈雁陈大全许颖 1.江苏大学药学院 2.中国药科大学药学院 3.烟台大学药学院江苏大学药学院中国药科大学药学院烟台大学药学院

采用原位凝胶技术，制备了新型复方碘口腔喷雾原位膜，用于发挥缓释作用，并促进口腔溃疡创面修复。首先以喷雾状态和成膜时间为指标，对喷雾药液的处方和工艺进行优化。以成膜时间和药膜黏附性为评价指标对药液混合比例进行考察。并对... 详细信息

采用原位凝胶技术，制备了新型复方碘口腔喷雾原位膜，用于发挥缓释作用，并促进口腔溃疡创面修复。首先以喷雾状态和成膜时间为指标，对喷雾药液的处方和工艺进行优化。以成膜时间和药膜黏附性为评价指标对药液混合比例进行考察。并对最优处方制备的复方碘口腔喷雾药液的药物含量、稳定性、pH、喷雾效果，及原位膜的成膜时间、溶解性、吸湿性、保湿性、体外释放等理化性质进行考察；此外，通过细胞实验考察了成膜材料的生物相容性及复方碘口腔喷雾原位膜的促迁移效果；采用兔口腔溃疡模型，对复方碘口腔喷雾在体成膜效果及促修复效果进行评价。实验结果显示，最优处方制备的药液A和药液B的pH分别为6.21 ± 0.02和 6.42 ± 0.03.符合正常口腔黏膜pH范围；稳定性好，具有良好的喷雾状态；药液B中碘含量为（1.96 ± 0.01）mg/mL；原位膜体外成膜时间为（118.3.± 3.6）s，口腔内成膜时间为（13..3.± 4.6）s；24 h溶解率为（87.3. ± 1.74）%，吸湿率为（124.17 ± 7.13.%，保湿率为（26.85 ± 2.50）%；复方碘口腔喷雾原位膜中碘含量为（47.42 ± 0.3.）mg/g；具有良好的柔韧性和黏附性，并具有一定的缓释效果。细胞实验中，原位膜表现出良好的促成纤维细胞迁移作用。兔口腔溃疡实验表明，复方碘口腔喷雾在体可快速成膜，并可显著促进口腔溃疡修复。本研究所开发的复方碘口腔喷雾原位膜，制备工艺稳定，并可有效促进口腔溃疡创面修复，为口腔黏膜制剂的研究和开发提供了新思路，并具有良好的转化前景。

关键词：口腔喷雾原位膜复方碘口腔溃疡缓释促修复

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Phase II metabolites of etofesalamide in filamentous fungi

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Acta Pharmacologica Sinica 2005年第7期26卷 893-896页

作者： Hai-hua HUANG Gui-lei MA Yu-ming SUN~2 Qiang LI~2 Da-fang ZHONG~(2,3. Department of pharmaceutical Microbiology 2 Laboratory of Drug Metabolism and Pharmacokinetics,Shenyang pharmaceutical university,Shenyang 110016,{3. Department of pharmaceutical Microbiology Shenyang Pharmaceutical University Shenyang 110016 China

Aim:To study phase Ⅱ metabolites of etofesalamide in filamentous ***:Seven fungi were screened to transform *** metabolites ofetofesalamide were assayed using liquid chromatography coupled to *** major metabolite was subject to enzymatic hydrolysis to con-firm its ***:Etofesalamide was converted into two phase Ⅱmetabolites:glucoside and riboside *** conjugate was themajor product with a yield greater than 90%;no phase I metabolites were ***:Glucoside and riboside conjugations of etofesalamide in filamentousfungi differ from the phase Ⅱ metabolism of glucuronidation in mammals.

关键词： etofesalamide Cunninghamella metabolite transformation: mass spectrum analysis

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Immunoenhancing activity of protopanaxatriol-type ginsenoside-F3.in murine spleen cells

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Acta Pharmacologica Sinica 2004年第12期25卷 105-110页

作者： Jun-li YU, De-qiang DOU2, Xiao-hong CHEN, Hong-zhen YANG, Na GUO2,Gui-fang CHENG3. Department of Pharmacology, institute of Materia Medica, Chinese Academy of MedicalSciences, Peking Union MedicalCollege, Beijing 100050 Departmentof Natural ProductsChemistry, Shenyang pharmaceutical university, Shenyang 110001, {3. 2 Department of Pharmacology Institute of Materia Medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

AIM: To investigate the immunoenhancing activity of ginsenoside-F3.inmurine spleen cells andexplore itsmechanism. METHODS: The enhancing effect of ginsenoside-F3.on murine spleen cell proliferation was studied using [3.] thymidine incorporation assay. Effects of ginsenoside-F3.on the production of type 1 cytokines IL-2, IFN-γ, and type 2 cytokines IL-4 and IL-10 from murine spleen cells were detected by ELISA method. Effects of ginsenoside- F3.on mRNA level of cytokines IL-4, IFN-γ, and transcription factors T-bet and GATA-3.were evaluated by RT- PCR analysis. Effect of ginsenoside-F3.on NF-κB DNA binding activity in murine spleen cells was investigated by electrophoretic mobility shift assays (EMSA). RESULTS: Ginsenoside-F3.at 0.1-100 μmol/L not only promoted the murine spleen cell proliferation, but also increased the production of IL-2 and IFN-γ, while decreased the production of IL-4 and IL-10 from murine spleen cells with the maximal effect at 10 μmol/L. RT-PCR analysis displayed that ginsenoside-F3.enhanced the IFN-γ and T-bet gene expression and decreased IL-4 and GATA-3.gene expression. EMSA experiment showed that ginsenoside-F3.10 μmol/L enhanced the NF-κB DNA binding activity induced by ConA in murine spleen cells. CONCLUSION: Ginsenoside-F3.has immunoenhancing activity by regu- lating production and gene expression of type 1 cytokines and type 2 cytokines in murine spleen cells.

关键词： ginsenoside F3 immunity cytokines transcription factors

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The microbial metallogeny of weathering crust REE deposits in South china

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Chinese Science Bulletin 1999年第S2期44卷 71-73页

作者： CHEN Binghui~(1,2), WANG Zhimei~3. HUANG Limei~3. WU Fuhai~3. CHEN Jingde~2 and XU Wenlie~2 1. Department of Earth Sciences, Nanjing university, Nanjing 210093. china 2. Department of Earth Sciences, Zhongshan university, Guangzhou 510275, china 3. Guangdong pharmaceutical College, Guangzhou 510244, china Department of Earth Sciences Nanjing University Nanjing 210093 China Department of Earth Sciences Zhongshan University Guangzhou 510275 China Guangdong pharmaceutical College Guangzhou 510244 China

VERY little is known about the roles of microorganisms in the metallogeny of weathering crust REE deposits, although there has been much literature on REE behavior in weathering conditions. The present note deals with the microorganisms in 4 weathering profiles of an REE deposit and their roles in migration and accumulation of REE in weathering conditions. 1 Cultivation and identification of microorganisms Under strict sterilization, samples were collected from various parts of 4 weathering profiles of granites in a weathering crust REE deposit in South china. The samples were then cultivated for microorganisms with ordinary agars as culture media and then the cultivated microorganisms were dyed and identifiedunder a microscope. The sampled positions and cultivated numbers of microbial colonies are shown

关键词： microbial metallogeny weathering crust REE deposit South china.

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