S. Verbeeck, A. Yadav, B. Maes, K. Augustyns, P. Van der Veken, P. Cos, L. Maes, L. Pieters
The antiprotozoal properties of a series of amino substituted 1-methyl-1 H-alpha-carbolines were investigated in a broad panel of parasites. Various substituents were systematically introduced at various positions on the carbocyclic ring of the parent 1-methyl-1 H-alpha-carboline. Most compounds showed a potent antiprotozoal activity, although mostly accompanied by cytotoxicity on MRC-5 cells. One compound, containing the same amino-substitution as chloroquine, showed an IC50 against Plasmodium falciparum of 2.37 microM and was reasonably selective.
研究了一系列氨基取代的1-甲基-1 h - α -碳卡啉在寄生虫中的抗原性。在母体1-甲基-1 h -羰基碳环的不同位置系统地引入了不同的取代基。大多数化合物显示出有效的抗原虫活性，尽管大多数化合物对MRC-5细胞具有细胞毒性。其中一种化合物与氯喹含有相同的氨基取代，对恶性疟原虫的IC50为2.37微米，具有合理的选择性。
{"title":"Antiprotozoal activity of synthetic amino substituted 1-methyl-1 H-alpha-carbolines.","authors":"S. Verbeeck, A. Yadav, B. Maes, K. Augustyns, P. Van der Veken, P. Cos, L. Maes, L. Pieters","doi":"10.1691/PH.2014.3748","DOIUrl":"https://doi.org/10.1691/PH.2014.3748","url":null,"abstract":"The antiprotozoal properties of a series of amino substituted 1-methyl-1 H-alpha-carbolines were investigated in a broad panel of parasites. Various substituents were systematically introduced at various positions on the carbocyclic ring of the parent 1-methyl-1 H-alpha-carboline. Most compounds showed a potent antiprotozoal activity, although mostly accompanied by cytotoxicity on MRC-5 cells. One compound, containing the same amino-substitution as chloroquine, showed an IC50 against Plasmodium falciparum of 2.37 microM and was reasonably selective.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"195 1","pages":"83-5"},"PeriodicalIF":0.0,"publicationDate":"2014-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72871562","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The first study of pharmacy on Croatian territory was founded in the early 19th century (1806-1813). Vicencio Dandolo (1758-1819), a pharmacist from Venice who was Napoleon's governor of Dalmatia, established a lyceum in Zadar in 1806. It included education for pharmacists. The Lyceum (later the Central School) was closed in 1811. The founding of the modern University of Zagreb (1874) and its Department of Mathematics and Natural Sciences (1876) created the conditions for the development of university education for pharmacists. The study of pharmacy was introduced at the University of Zagreb in 1882 through the efforts of the Croatian-Slavonian Pharmaceutical Association and the professors of the Faculty of Philosophy. The study went through a series of reforms. The most significant one came with the introduction of the four-year study of pharmacy and the establishment of the Pharmacy Department of the Faculty of Philosophy (1928). The independent Faculty of Pharmacy (today's Faculty of Pharmacy and Biochemistry) was founded at the University of Zagreb in 1942. Since 1989, it has had two separate studies (Pharmacy and Medical Biochemistry).
{"title":"The history of pharmacy studies in Croatia.","authors":"N. Kujundẑić, S. Inić","doi":"10.1691/PH.2014.3127","DOIUrl":"https://doi.org/10.1691/PH.2014.3127","url":null,"abstract":"The first study of pharmacy on Croatian territory was founded in the early 19th century (1806-1813). Vicencio Dandolo (1758-1819), a pharmacist from Venice who was Napoleon's governor of Dalmatia, established a lyceum in Zadar in 1806. It included education for pharmacists. The Lyceum (later the Central School) was closed in 1811. The founding of the modern University of Zagreb (1874) and its Department of Mathematics and Natural Sciences (1876) created the conditions for the development of university education for pharmacists. The study of pharmacy was introduced at the University of Zagreb in 1882 through the efforts of the Croatian-Slavonian Pharmaceutical Association and the professors of the Faculty of Philosophy. The study went through a series of reforms. The most significant one came with the introduction of the four-year study of pharmacy and the establishment of the Pharmacy Department of the Faculty of Philosophy (1928). The independent Faculty of Pharmacy (today's Faculty of Pharmacy and Biochemistry) was founded at the University of Zagreb in 1942. Since 1989, it has had two separate studies (Pharmacy and Medical Biochemistry).","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"26 2 1","pages":"154-60"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82701212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hailan Li, H. Yun, K. Baek, N. Kwon, Kyoung-Chan Park, Dong-Seok Kim
The purpose of this study was to investigate effects of myriocin, an inhibitor of serine palmitoyltransferase, on melanogenesis. It was found that myriocin increased melanin synthesis in a concentration-dependent manner. Moreover, myriocin up-regulated microphthalmia-associated transcription factor (MITF) and tyrosinase expression via phosphorylation of CREB, but it did not directly activate tyrosinase, a rate-limiting melanogenic enzyme. Furthermore, we demonstrated increased melanin synthesis with myriocin on a pigmented skin equivalent model established using Cervi cornus Colla (deer antler glue). One and 5 microM of myriocin darkened the color of the skin equivalent. These results suggest that myriocin may have potential effects for the treatment of hypopigmentary skin diseases like vitiligo or for sunless tanning.
{"title":"Myriocin, a serine palmitoyltransferase inhibitor, increases melanin synthesis in Mel-Ab cells and a skin equivalent model.","authors":"Hailan Li, H. Yun, K. Baek, N. Kwon, Kyoung-Chan Park, Dong-Seok Kim","doi":"10.1691/PH.2014.3835","DOIUrl":"https://doi.org/10.1691/PH.2014.3835","url":null,"abstract":"The purpose of this study was to investigate effects of myriocin, an inhibitor of serine palmitoyltransferase, on melanogenesis. It was found that myriocin increased melanin synthesis in a concentration-dependent manner. Moreover, myriocin up-regulated microphthalmia-associated transcription factor (MITF) and tyrosinase expression via phosphorylation of CREB, but it did not directly activate tyrosinase, a rate-limiting melanogenic enzyme. Furthermore, we demonstrated increased melanin synthesis with myriocin on a pigmented skin equivalent model established using Cervi cornus Colla (deer antler glue). One and 5 microM of myriocin darkened the color of the skin equivalent. These results suggest that myriocin may have potential effects for the treatment of hypopigmentary skin diseases like vitiligo or for sunless tanning.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"72 1","pages":"187-91"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75137487","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
K. Hermans, D. van den Plas, E. Schreurs, W. Weyenberg, A. Ludwig
Cyclosporine A loaded poly(lactide-co-glycolide) nanoparticles were prepared using the o/w emulsification solvent evaporation method and the effect of four preparation parameters on particle size and zeta potential was investigated. Release properties of the nanoparticles were examined and in vitro experiments were performed in order to evaluate the cytotoxicity and anti-inflammatory activity of the nanoparticles developed. Particle sizes varied between 191 and 303 nm depending on the different preparation parameters and all nanoparticle dispersions were monodisperse. The nanoparticles showed negative zeta potential values varying between -16 and -35 mV and 57 to 70 % of the amount of loaded cyclosporine A was released after 24 h. None of the nanoparticle formulations showed significant cytotoxicity compared to the negative control using human epithelial cells (HaCaT). Cyclosporine A incorporated in the various nanoparticle formulations retained its anti-inflammatory activity as significant suppression of interleukine-2 secretion in concanavalin A stimulated Jurkat T cells was measured. As the overall influence of the freeze-drying process on the characteristics of nanoparticles was limited, trehalose and carnitine should be preferred as cryoprotectants in ocular formulations for treatment of dry eye disease.
{"title":"Cytotoxicity and anti-inflammatory activity of cyclosporine A loaded PLGA nanoparticles for ocular use.","authors":"K. Hermans, D. van den Plas, E. Schreurs, W. Weyenberg, A. Ludwig","doi":"10.1691/PH.2014.2206","DOIUrl":"https://doi.org/10.1691/PH.2014.2206","url":null,"abstract":"Cyclosporine A loaded poly(lactide-co-glycolide) nanoparticles were prepared using the o/w emulsification solvent evaporation method and the effect of four preparation parameters on particle size and zeta potential was investigated. Release properties of the nanoparticles were examined and in vitro experiments were performed in order to evaluate the cytotoxicity and anti-inflammatory activity of the nanoparticles developed. Particle sizes varied between 191 and 303 nm depending on the different preparation parameters and all nanoparticle dispersions were monodisperse. The nanoparticles showed negative zeta potential values varying between -16 and -35 mV and 57 to 70 % of the amount of loaded cyclosporine A was released after 24 h. None of the nanoparticle formulations showed significant cytotoxicity compared to the negative control using human epithelial cells (HaCaT). Cyclosporine A incorporated in the various nanoparticle formulations retained its anti-inflammatory activity as significant suppression of interleukine-2 secretion in concanavalin A stimulated Jurkat T cells was measured. As the overall influence of the freeze-drying process on the characteristics of nanoparticles was limited, trehalose and carnitine should be preferred as cryoprotectants in ocular formulations for treatment of dry eye disease.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"228 1","pages":"32-7"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77081406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug (NSAID) widely used in humans and animals. There are limited published studies evaluating diclofenac's skin permeation following topical administration. The aim of our study was to evaluate and compare the in vitro permeation of three different diclofenac-containing formulations (patch, gel, solution) over 24 hours. These formulations were applied (n = 6 per formulation) to pig skin sandwiched between the two chambers in a static Franz diffusion cell and aliquots from the receptor medium were sampled at pre-defined time points. An HPLC method with UV detection was developed and validated with the aim of characterizing the transepidermal penetration in the in vitro system. Using this assay to determine the permeation parameters, results at 24 hours showed that the Flector patch released the highest drug amount (54.6%), whereas a lower drug amount was delivered with the Voltaren Emulgel (38.2%) and the solution (34.4%). The commercial gel showed the highest flux (39.9 +/- 0.9 microg/cm2/h) and the shortest lag-time (1.97 +/- 0.02 h). Based on these in vitro results using pig skin, the transdermal patch resulted in a long-lasting controlled release of diclofenac, while the gel had the shortest lag-time.
{"title":"Comparison of skin permeability for three diclofenac topical formulations: an in vitro study.","authors":"E. Folzer, D. Gonzalez, R. Singh, H. Derendorf","doi":"10.1691/PH.2014.3087","DOIUrl":"https://doi.org/10.1691/PH.2014.3087","url":null,"abstract":"Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug (NSAID) widely used in humans and animals. There are limited published studies evaluating diclofenac's skin permeation following topical administration. The aim of our study was to evaluate and compare the in vitro permeation of three different diclofenac-containing formulations (patch, gel, solution) over 24 hours. These formulations were applied (n = 6 per formulation) to pig skin sandwiched between the two chambers in a static Franz diffusion cell and aliquots from the receptor medium were sampled at pre-defined time points. An HPLC method with UV detection was developed and validated with the aim of characterizing the transepidermal penetration in the in vitro system. Using this assay to determine the permeation parameters, results at 24 hours showed that the Flector patch released the highest drug amount (54.6%), whereas a lower drug amount was delivered with the Voltaren Emulgel (38.2%) and the solution (34.4%). The commercial gel showed the highest flux (39.9 +/- 0.9 microg/cm2/h) and the shortest lag-time (1.97 +/- 0.02 h). Based on these in vitro results using pig skin, the transdermal patch resulted in a long-lasting controlled release of diclofenac, while the gel had the shortest lag-time.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"12 1","pages":"27-31"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72719269","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Z. Liu, W. Li, K. Qin, K. Wen, C. J. Zhu, N. Li, H. Bian, H. Wen, L. Chen
Liguzinediol (LZDO) could mediate the positive inotropic effects through sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism without the risk of arrhythmia. However, the pharmacophore of LZDO contributed to the activities was not clear. The aim of this work was to explore the relationship between positive inotropic effect and scaffold of LZDO as well as to check whether the pharmacophore of LZDO on anti-heart failure activity was located at the pyrazine ring. A series of LZDO analogs (3a-b, 4a-b, 9-19) were designed and synthesised, and their activities were evaluated on isolated heart contractility by Langendorff perfusion. The results showed that the efficacy of LZDO was reduced when the hydroxyl, carboxyl or ester moieties at the side chain position of LZDO were induced, and the para-dihydroxy in LZDO was necessary for its activity. Thus, the pharmacophore of the positive inotropic effect might be located at the whole scaffold of LZDO, but not at the pyrazine ring. The finding may provide an important clue of the pharmacophore for the development of novel cardiotonic agents.
{"title":"Scaffold evaluation of liguzinediol analogs as novel cardiotonic agents.","authors":"Z. Liu, W. Li, K. Qin, K. Wen, C. J. Zhu, N. Li, H. Bian, H. Wen, L. Chen","doi":"10.1691/PH.2013.3597","DOIUrl":"https://doi.org/10.1691/PH.2013.3597","url":null,"abstract":"Liguzinediol (LZDO) could mediate the positive inotropic effects through sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism without the risk of arrhythmia. However, the pharmacophore of LZDO contributed to the activities was not clear. The aim of this work was to explore the relationship between positive inotropic effect and scaffold of LZDO as well as to check whether the pharmacophore of LZDO on anti-heart failure activity was located at the pyrazine ring. A series of LZDO analogs (3a-b, 4a-b, 9-19) were designed and synthesised, and their activities were evaluated on isolated heart contractility by Langendorff perfusion. The results showed that the efficacy of LZDO was reduced when the hydroxyl, carboxyl or ester moieties at the side chain position of LZDO were induced, and the para-dihydroxy in LZDO was necessary for its activity. Thus, the pharmacophore of the positive inotropic effect might be located at the whole scaffold of LZDO, but not at the pyrazine ring. The finding may provide an important clue of the pharmacophore for the development of novel cardiotonic agents.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"82 1","pages":"926-32"},"PeriodicalIF":0.0,"publicationDate":"2013-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83884166","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Chaoxiang Liu, Zhongxiang Lin, Xing Yu, Zhou Lu, Ai-min Zhou, Y. Bao
A series of novel dehydroabietylamine derivatives containing tricyclic diterpene structures were synthesized. The antitumor activities of these compounds against L02, Hey-1B and HepG2 cells were investigated. Significant activity was discovered forfourteen analogs. Meanwhile these compounds exhibit DNA cleavage activities on plasmid DNA (Escherichia coli), which depend on the Schiff base structure and the substituent of the aromatic moiety. Our findings present further information on the relationship between the chemical structure, biological function and DNA cleavage characteristics.
{"title":"A comparative study of antitumor activities and DNA cleavage on a class of dehydroabietylamine derivatives.","authors":"Chaoxiang Liu, Zhongxiang Lin, Xing Yu, Zhou Lu, Ai-min Zhou, Y. Bao","doi":"10.1691/PH.2013.3575","DOIUrl":"https://doi.org/10.1691/PH.2013.3575","url":null,"abstract":"A series of novel dehydroabietylamine derivatives containing tricyclic diterpene structures were synthesized. The antitumor activities of these compounds against L02, Hey-1B and HepG2 cells were investigated. Significant activity was discovered forfourteen analogs. Meanwhile these compounds exhibit DNA cleavage activities on plasmid DNA (Escherichia coli), which depend on the Schiff base structure and the substituent of the aromatic moiety. Our findings present further information on the relationship between the chemical structure, biological function and DNA cleavage characteristics.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"64 1","pages":"861-5"},"PeriodicalIF":0.0,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85748913","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Atherosclerosis is an inflammatory disease characterized by extensive lipid deposition and atherosclerotic plaque formation in the intima. Interleukin (IL)-37 is anti-inflammatory cytokine in the IL-1 ligand family. Given that IL-37 plays an important function in the development and progression of inflammatory and autoimmune diseases, it may be associated with the development of atherosclerosis. IL-37, which is normally expressed at low levels in peripheral blood mononuclear cells (PBMC), mainly monocytes, and dendritic cells (DC), is rapidly up-regulated in the inflammatory context, and therefore IL-37 conversely inhibits the production of inflammatory cytokines in PBMC and DC. In addition, IL-37 effectively suppresses the activation of macrophage and DC. It is not controversial that the activation of macrophage and DC and the over-expression of inflammatory cytokines are critical component elements in inflammatory process of atherosclerosis. Therefore, IL-37 may play a protective role in atherosclerosis through inhibition of inflammatory cytokines production and suppression of macrophage and DC activation.
{"title":"The potential role of IL-37 in atherosclerosis.","authors":"Bang-wei Wu, Q. Zeng, K. Meng, Qingwei Ji","doi":"10.1691/PH.2013.3590","DOIUrl":"https://doi.org/10.1691/PH.2013.3590","url":null,"abstract":"Atherosclerosis is an inflammatory disease characterized by extensive lipid deposition and atherosclerotic plaque formation in the intima. Interleukin (IL)-37 is anti-inflammatory cytokine in the IL-1 ligand family. Given that IL-37 plays an important function in the development and progression of inflammatory and autoimmune diseases, it may be associated with the development of atherosclerosis. IL-37, which is normally expressed at low levels in peripheral blood mononuclear cells (PBMC), mainly monocytes, and dendritic cells (DC), is rapidly up-regulated in the inflammatory context, and therefore IL-37 conversely inhibits the production of inflammatory cytokines in PBMC and DC. In addition, IL-37 effectively suppresses the activation of macrophage and DC. It is not controversial that the activation of macrophage and DC and the over-expression of inflammatory cytokines are critical component elements in inflammatory process of atherosclerosis. Therefore, IL-37 may play a protective role in atherosclerosis through inhibition of inflammatory cytokines production and suppression of macrophage and DC activation.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"9 1","pages":"857-60"},"PeriodicalIF":0.0,"publicationDate":"2013-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81590098","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The imbalance of anti- inflammatory/pro-inflammatory cytokines plays an important role in the process of atherosclerosis. IL-35 is an anti-inflammatory cytokine comprising the p35 subunit of IL-12 and the subunit Epstein-Barr virus (EBV) -induced gene 3(EBI3). Accumulating evidence showed that IL-35 up-regulates the expression of anti-inflammatory cytokines, induces the generation of CD4 + regulatory T cells, inhibits CD4 + effector T cells response and other target cells activity, and reduces the progression of inflammatory and autoimmune diseases. In addition, it has been found that Ebi3 and p35 strongly coexpressed in human advanced lesions. Therefore, we hypothesize that IL-35 may become a novel target for the treatment of atherosclerosis. Further studies are required to investigate the precise effect and the signaling pathway of IL-35 in atherosclerosis process.
{"title":"IL-35: a potential target for the treatment of atherosclerosis.","authors":"Ying Huang, Ying-zhong Lin, Ying Shi, Qingwei Ji","doi":"10.1691/PH.2013.2928","DOIUrl":"https://doi.org/10.1691/PH.2013.2928","url":null,"abstract":"The imbalance of anti- inflammatory/pro-inflammatory cytokines plays an important role in the process of atherosclerosis. IL-35 is an anti-inflammatory cytokine comprising the p35 subunit of IL-12 and the subunit Epstein-Barr virus (EBV) -induced gene 3(EBI3). Accumulating evidence showed that IL-35 up-regulates the expression of anti-inflammatory cytokines, induces the generation of CD4 + regulatory T cells, inhibits CD4 + effector T cells response and other target cells activity, and reduces the progression of inflammatory and autoimmune diseases. In addition, it has been found that Ebi3 and p35 strongly coexpressed in human advanced lesions. Therefore, we hypothesize that IL-35 may become a novel target for the treatment of atherosclerosis. Further studies are required to investigate the precise effect and the signaling pathway of IL-35 in atherosclerosis process.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"20 1","pages":"793-5"},"PeriodicalIF":0.0,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80100884","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xiuwen Wu, Ru-Feng Wang, Ming Yuan, W. Xu, Xiu-wei Yang
The Caco-2 cell monolayer model is widely used in drug absorption studies. Dulbecco's Modified Eagle's Medium (DMEM) and Minimum Essential Medium (MEM) have been used alternatively in the development of this model, although they are different in composition which may affect the differentiation and junction formation of the Caco-2 cell monolayer. Two Caco-2 cell monolayers cultured in both media were compared herein in order to underlay the standardization of this model. These two monolayers were comparatively evaluated regarding reliability and stability by morphology, transepithelial electrical resistance (TEER), alkaline phosphatase (AKPase) activity and transport experiments. Although the results showed that characteristic microvilli were present at the apical side of both monolayers, the dynamic change of TEER of the monolayer cultured in DMEM was more stable than that cultured in MEM, and AKPase activity of the former was stronger than that of the latter. Furthermore, the quantity of atenolol, a key indicator usually used for assessment of this model, across the monolayer cultured in MEM was significantly more than that cultured in DMEM. Therefore, the Caco-2 monolayer cultured in DMEM was more reliable and stable than that cultured in MEM, and thus the former was preferred for drug absorption investigation in vitro.
Caco-2细胞单层模型广泛应用于药物吸收研究。Dulbecco's Modified Eagle's Medium (DMEM)和Minimum Essential Medium (MEM)在该模型的开发中被交替使用，尽管它们的成分不同，可能会影响Caco-2细胞单层的分化和连接形成。本文比较了两种培养基中培养的Caco-2细胞单层，以奠定该模型的标准化基础。通过形态学、经上皮电阻(TEER)、碱性磷酸酶(AKPase)活性和转运实验，比较评价了这两种单层膜的可靠性和稳定性。虽然结果显示，两种单分子膜的顶端侧均存在特征微绒毛，但DMEM培养的单分子膜TEER的动态变化比MEM培养的更稳定，且前者的AKPase活性强于后者。此外，通常用于评估该模型的关键指标阿替洛尔(atenolol)在MEM培养的单层中的数量明显多于DMEM培养的单层。因此，DMEM培养的Caco-2单层膜比MEM培养的Caco-2单层膜更可靠、更稳定，因此DMEM培养的Caco-2单层膜更适合体外药物吸收研究。
{"title":"Dulbecco's modified eagle's medium and minimum essential medium--which one is more preferred for establishment of Caco-2 cell monolayer model used in evaluation of drug absorption?","authors":"Xiuwen Wu, Ru-Feng Wang, Ming Yuan, W. Xu, Xiu-wei Yang","doi":"10.1691/PH.2013.2225","DOIUrl":"https://doi.org/10.1691/PH.2013.2225","url":null,"abstract":"The Caco-2 cell monolayer model is widely used in drug absorption studies. Dulbecco's Modified Eagle's Medium (DMEM) and Minimum Essential Medium (MEM) have been used alternatively in the development of this model, although they are different in composition which may affect the differentiation and junction formation of the Caco-2 cell monolayer. Two Caco-2 cell monolayers cultured in both media were compared herein in order to underlay the standardization of this model. These two monolayers were comparatively evaluated regarding reliability and stability by morphology, transepithelial electrical resistance (TEER), alkaline phosphatase (AKPase) activity and transport experiments. Although the results showed that characteristic microvilli were present at the apical side of both monolayers, the dynamic change of TEER of the monolayer cultured in DMEM was more stable than that cultured in MEM, and AKPase activity of the former was stronger than that of the latter. Furthermore, the quantity of atenolol, a key indicator usually used for assessment of this model, across the monolayer cultured in MEM was significantly more than that cultured in DMEM. Therefore, the Caco-2 monolayer cultured in DMEM was more reliable and stable than that cultured in MEM, and thus the former was preferred for drug absorption investigation in vitro.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"109 1","pages":"805-10"},"PeriodicalIF":0.0,"publicationDate":"2013-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80560824","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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