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Journal of Pharmaceutical Analysis 2016年第4期6卷 268-275页

作者： Emilia Sawicki Michel J.Hillebrand hilde rosing Jan H.M.Schellens Bastiaan Nuijen Jos H.Beijnen Department of Pharmacy & Pharmacology The Netherlands Cancer Institute/Antoni van Leeuwenhoek Hospital Division of Clinical Pharmacology Department of Medical OncologyThe Netherlands Cancer Institute/Antoni van Leeuwenhoek Hospital Division of Pharmacoepidemiology & Clinical Pharmacology.Department of Pharmaceutical Sciences Faculty of Science.Utrecht University

Many anticancer drugs have an impaired bioavailability and poor brain penetration because they are substrates to drug efflux pumps such as P-glycoprotein and Breast Cancer Resistance *** is a strong inhibitor of these two drug efflux pumps and therefore has great potential to improve oral absorption and brain penetration of many anticancer ***,a clinical formulation of elacridar is unavailable and therefore the pharmaceutical development of a drug product is highly *** also necessitates the availability of an analytical method for its quality control.A reverse-phase high-performance liquid chromatographic method with ultraviolet detection was developed for the pharmaceutical quality control of products containing elacridar as the active pharmaceutical *** analytical method was validated for linearity,accuracy,precision,selectivity,carry-over,stability of stock and reference solutions,stability of the final extract,stability-indicating capability and impurity *** found that elacridar is unstable in aqueous solutions that are exposed to light because a hydroxylation product of elacridar is ***,sample solutions with elacridar must be protected from light.

关键词： GF120918 Solid dispersion Dissolution Hydroxylation HPLC-UV

Carboxylesterase 1 family knockout alters drug disposition and lipid metabolism

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Acta Pharmaceutica Sinica B 2023年第2期13卷 618-631页

作者： Changpei Gan Jing Wang Alejandra Martínez-Chávez Michel Hillebrand Niels de Vries Joke Beukers Els Wagenaar Yaogeng Wang Maria C.Lebre hilde rosing Sjoerd Klarenbeek Rahmen Bin Ali Colin Pritchard Ivo Huijbers Jos H.Beijnen Alfred H.Schinkel Division of Pharmacology the Netherlands Cancer InstituteAmsterdam 1066 CXthe Netherlands Department of Pharmacy&Pharmacology the Netherlands Cancer InstituteAmsterdam 1066 CXthe Netherlands Division of Pharmacoepidemiology and Clinical Pharmacology Utrecht Institute for Pharmaceutical SciencesUtrecht UniversityUtrecht 3584 CSthe Netherlands Experimental Animal Pathology Facility the Netherlands Cancer InstituteAmsterdam 1066 CXthe Netherlands Mouse Clinic for Cancer and Aging(MCCA)Transgenic Facility the Netherlands Cancer InstituteAmsterdam 1066 CXthe Netherlands

The mammalian carboxylesterase 1(Ces1/CES1)family comprises several enzymes that hydrolyze many xenobiotic chemicals and endogenous *** investigate the pharmacological and physiological roles of Ces1/CES1,we generated Ces1 cluster knockout(Ces1^(-/-))mice,and a hepatic human CES1 transgenic model in the Ces1^(-/-)background(TgCES1).Ces1^(-/-)mice displayed profoundly decreased conversion of the anticancer prodrug irinotecan to SN-38 in plasma and ***1 mice exhibited enhanced metabolism of irinotecan to SN-38 in liver and ***1 and hCES1 activity increased irinotecan toxicity,likely by enhancing the formation of pharmacodynamically active ***1^(-/-)mice also showed markedly increased capecitabine plasma exposure,which was moderately decreased in TgCES1 ***1^(-/-)mice were overweight with increased adipose tissue,white adipose tissue inflammation(in males),a higher lipid load in brown adipose tissue,and impaired blood glucose tolerance(in males).These phenotypes were mostly reversed in TgCES1 ***1 mice displayed increased triglyceride secretion from liver to plasma,together with higher triglyceride levels in the male *** results indicate that the carboxylesterase 1 family plays essential roles in drug and lipid metabolism and ***1^(-/-)and TgCES1 mice will provide excellent tools for further study of the in vivo functions of Ces1/CES1 enzymes.

关键词： Ces1/CES1 enzymes Irinotecan Capecitabine Adipose tissue Lipid homeostasis Inflammation Triglyceride mobilization Mouse models

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北极熊的小跟班

小哥白尼（野生动物） 2007年第12期 2-5页

作者：小丽 Norbert rosing

冰封雪盖的北极。如果有只大乌鸦,从空中扔下一根骨头到冰上,或者某个猎人的帐篷里飘出烹煮野味的香味,这时候,就会不知从哪突然冒出个小白点,屁颠屁颠地跑过来搞一番调查。这个小白点,就是北极狐。而更多的时候,北极狐爱跟在北极熊的后... 详细信息

冰封雪盖的北极。如果有只大乌鸦,从空中扔下一根骨头到冰上,或者某个猎人的帐篷里飘出烹煮野味的香味,这时候,就会不知从哪突然冒出个小白点,屁颠屁颠地跑过来搞一番调查。这个小白点,就是北极狐。而更多的时候,北极狐爱跟在北极熊的后面,属于那种不请自来的机灵小跟班。

关键词：北极狐北极熊海豹旅鼠捕食岩石坡风雪兴奋睡觉海鸟

变质作用中流体控制元素的活动性对全岩同位素体系的影响、某些理论和实例

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国外前寒武纪地质 1990年第3期 80-92页

作者： D.Bridgwater M.rosing 杨春亮

Rb、Sr、Sm、Nd、U和Pb等元素在与区域变质作用相伴的流体活动中均出现重新分配。对于一般用作鉴定年代的同位素系统,这种重新分配作用对测年系统的影响取决于几种因素。某一地区在适变质到麻粒岩相的过程中Rb、U和Pb发生丢失,而在退变... 详细信息

Rb、Sr、Sm、Nd、U和Pb等元素在与区域变质作用相伴的流体活动中均出现重新分配。对于一般用作鉴定年代的同位素系统,这种重新分配作用对测年系统的影响取决于几种因素。某一地区在适变质到麻粒岩相的过程中Rb、U和Pb发生丢失,而在退变质中又重新获得。Sr在进变质作用和退变质作用中其重新分配的活动范围有几厘米,而在有剪切相伴的退变质作用中其活动范围就有几十米。由于Rb的活动性比Sr要大得多,在露头上没有Sr均一化作用的各个样品的Rb/Sf比值是变化的。在一组样品中有Rb加入,

关键词：岩石元素活动性同位素体

Relationship between vascular endothelium and periodontal disease in atherosclerotic lesions: Review article

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World Journal of Cardiology 2015年第1期7卷 26-30页

作者： Marco Aurélio Lumertz Saffi Mariana Vargas Furtado Carisi Anne Polanczyk Márlon Munhoz Montenegro Ingrid Webb Josephson Ribeiro Cassio Kampits Alex Nogueira Haas Cassiano Kuchenbecker rosing Eneida Rejane Rabelo-Silva Cardiovascular Division Hospital de Clínicas de Porto Alegre Porto Alegre 90035-003 Brazil Federal University of Rio Grande do Sul Faculty of Dentistry Periodontology Porto Alegre 90030-035 Brazil School of Nursing Federal University of Rio Grande do Sul Porto Alegre 90620-110 Brazil

Inflammation and endothelial dysfunction are linked to the pathogenesis of atherosclerotic disease. Recent studies suggest that periodontal infection and the ensuing increase in the levels of inflammatory markers may be associated with myocardial infarction, peripheral vascular disease and cerebrovascular disease. The present article aimed at reviewing contemporary data on the pathophysiology of vascular endothelium and its association with periodontitis in the scenario of cardiovascular disease.

关键词： Endothelium Vascular Atherosclerosis Periodontal diseases Nitric oxide Cardiovascular diseases

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矿物包裹体中发现早太古代的生命遗迹

矿物岩石地球化学通报 2017年第5期36卷 735-735页

作者： Hassenkam T Andersson1 M P Dalby1 K N Mackenzie2 D M A rosing M T 袁超

西格陵兰Lsua地区37亿年的表壳岩带中富铁的变泥质岩的弱变形区域保存有较好的原始沉积层理,以亚毫米级的成分层为特征。其所含的石榴子石-绿帘石-黑云母-白云母-石英-石墨矿物组合反映了角闪岩相的变质作用。

关键词：矿物包裹体太古代遗迹生命变质作用角闪岩相矿物组合石榴子石