Jie Zhao, R. Meng, Q. Yao, Hui Wang, J. Niu, Y. Cui, Songlin Chen, Yin-Shan Bai
{"title":"Long non-coding RNA HEIH promotes breast cancer development via negative modulation of microRNA-200b.","authors":"Jie Zhao, R. Meng, Q. Yao, Hui Wang, J. Niu, Y. Cui, Songlin Chen, Yin-Shan Bai","doi":"10.1691/ph.2019.9428","DOIUrl":"https://doi.org/10.1691/ph.2019.9428","url":null,"abstract":"This study aimed to investigate the effects and regulatory mechanism of long non-coding RNA HEIH in the development of breast cancer. The expression of HEIH in breast tumor tissues and breast cancer cells was determined, followed by investigating the effects and regulatory mechanism of HEIH dysregulation on breast cancer cell viability, apoptosis, migration and invasion. The expression of HEIH was upregulated in breast cancer tissue samples and cell lines. Suppression of HEIH inhibited cell viability, promoted cell apoptosis, and decreased migration and invasion in MDA-MB-231 cells. Moreover, a negative relationship existed between HEIH and miR-200b, and HEIH regulated breast cancer development via regulating miR-200b. Pre-leukemia transcription factor 3 (PBX3) was verified as a functional target of miR-200b, and miR-200b regulated the malignant behaviors of breast cancer cells through targeting PBX3. Furthermore, suppression of HEIH inhibited the activation of Wnt/β-catenin pathway, which was remarkably reversed after suppression of HEIH and inhibition of miR-200b synchronously. Our results reveal that HEIH may contribute to breast cancer development via modulation of microRNA-200b/axis and inducing the activation of Wnt/β-catenin pathway. Further studies are still required to confirm our findings.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"43 1","pages":"471-476"},"PeriodicalIF":0.0,"publicationDate":"2019-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87446044","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}
Pang Tao, Z. Jing, Gao Shou-Hong, Piao Shu-juan, Jiao Jian-peng, Lu Wen-Quan, Chen Wan-sheng
{"title":"Effects of leptin on norepinephrine in acute ischemic stroke.","authors":"Pang Tao, Z. Jing, Gao Shou-Hong, Piao Shu-juan, Jiao Jian-peng, Lu Wen-Quan, Chen Wan-sheng","doi":"10.1691/ph.2019.9379","DOIUrl":"https://doi.org/10.1691/ph.2019.9379","url":null,"abstract":"Stroke is a multifactorial disease and a consequence of morbidities of diabetes, obesity, hypertension, and heart diseases. Leptin is a major adipokine that regulates weight balance and energy homeostasis, the level of which has been considered as an indicator of acute ischemic stroke. In the present study, we confirmed the high level of leptin and noradrenaline in stroke patients and mouse models as well as oxygen-glucose deprivation (OGD) primary cerebral neurons. Leptin administration increased noradrenaline concentration and dopamine β-monooxygenase (DBH) but decreased noradrenaline transporter (NET) expression in primary cerebral neurons. Moreover, induced noradrenaline concentration, DBH activity, and inhibited NET were blunted by TG101348 (JAK2 inhibitor). JAK2 silencing also abolished the effects of leptin on noradrenaline metabolism.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"6 1","pages":"477-480"},"PeriodicalIF":0.0,"publicationDate":"2019-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80786131","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}
M. Uchida, M. Hada, M. Yamada, D. Inma, S. Ariyoshi, K. Aoki, S. Inoue, T. Shimazoe, K. Mitsuiki, T. Haraguchi
{"title":"Impact of a systematic education model for palliative care in cancer.","authors":"M. Uchida, M. Hada, M. Yamada, D. Inma, S. Ariyoshi, K. Aoki, S. Inoue, T. Shimazoe, K. Mitsuiki, T. Haraguchi","doi":"10.1691/ph.2019.9417","DOIUrl":"https://doi.org/10.1691/ph.2019.9417","url":null,"abstract":"In clinical practice, pharmacists are continually required to improve their knowledge and expertise; however, the postgraduate education system for professional development cannot be confidently stated to be well established. The establishment of a systematic and multifaceted educational curriculum should be useful to improve home care and pharmacists' contribution; therefore, we developed a curriculum in collaboration with the university faculty of pharmaceutical sciences, department of pharmacy in hospital, and the Fukuoka Pharmaceutical Association. Class topics were extracted from the \"Kanwa-Iryou-Yakugaku\", edited by the Japanese Society for Pharmaceutical Palliative Care and Sciences. The items are necessary to perform palliative care as a pharmacist. A class schedule of 6 days (24 classes in total) was formulated. Questionnaires on comprehension degree before and after each class were provided to the participants. Comprehension was assessed on a scale of 1 to 10, where \"I do not understand at all\" was 1 and \"I understand enough\" was 10. The average recovery rates of questionnaires from each class were 92.6 % and 88.9 % before and after class, respectively. The average number of participants who completely answered the questionnaire before and after class was 45.6; therefore, these data were analyzed. Comprehension degree on each topic had significantly increased after attendance of all classes (p < 0.01). The comprehension degree of participants of the medical science of palliative care did greatly improve. Consequently, it is clear that the standard education model constructed was meaningful for the professional development of pharmacists in palliative care medicine.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"88 1","pages":"499-504"},"PeriodicalIF":0.0,"publicationDate":"2019-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88546478","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}
D. Kilian, H. J. Lemmer, M. Gerber, J. D. du Preez, J. du Plessis
{"title":"Exploratory data analysis of the dependencies between skin permeability, molecular weight and log P.","authors":"D. Kilian, H. J. Lemmer, M. Gerber, J. D. du Preez, J. du Plessis","doi":"10.1691/ph.2015.5170","DOIUrl":"https://doi.org/10.1691/ph.2015.5170","url":null,"abstract":"Molecular weight and log P remain the most frequently used physicochemical properties in models that predict skin permeability. However, several reports over the past two decades have suggested that predictions made by these models may not be sufficiently accurate. In this study, exploratory data analysis of the probabilistic dependencies between molecular weight, log P and log Kp was performed on a dataset constructed from the combination of several popular datasets. The results suggest that, in general, molecular weight and log P are poorly correlated to log Kp. However, after employing several exploratory data analysis techniques, regions within the dataset of statistically significant dependence were identified. As an example of the applicability of the information extracted from the exploratory data analyses, a multiple linear regression model was constructed, bounded by the ranges of dependence. This model gave reasonable approximations to log Kp values obtained from skin permeability studies of selected non-steroidal ant-inflammatory drugs (NSAIDs) administered from a buffer solution and a lipid-based drug delivery system. A method of testing whether a given drug falls within the regions of statistical dependence was also presented. Knowing the ranges within which molecular weight and log P are statistically related to log Kp can supplement existing methods of screening, risk analysis or early drug development decision making to add confidence to predictions made regarding skin permeability.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"28 1","pages":"311-9"},"PeriodicalIF":0.0,"publicationDate":"2016-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87991150","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}
Chen Shi, Ping Liu, Xianzhe Liu, Xiaobo Feng, Dehao Fu
{"title":"The effects of mPEG proportion and LA/GA ratio on degradation and drug release behaviors of PLGA-mPEG microparticles.","authors":"Chen Shi, Ping Liu, Xianzhe Liu, Xiaobo Feng, Dehao Fu","doi":"10.1691/PH.2016.5179","DOIUrl":"https://doi.org/10.1691/PH.2016.5179","url":null,"abstract":"The purpose of this research was to evaluate the effects of mPEG proportion and LA/GA ratio on degradation and release behavior of PLGA-mPEG microparticles prepared by the emulsion evaporation method. Mometasone furoate was employed as model drug and encapsulated into five types of PLGA-mPEG microparticles in the same molecular weight (Mw), but different in mPEG proportion or LA/GA ratio. All types of PLGA-mPEG microparticles showed similar drug encapsulation efficiency and particle mean size, but PLGA-mPEG microparticles with higher mPEG proportion showed a faster Mw reduction rate, mass loss rate and size decrease rate according to the in vitro degradation experiment, and also, a faster drug release rate according to the in vitro release experiment. On the other hand, higher LA/GA ratio in PLGA chain of PLGA-mPEG causes a slower Mw reduction rate, mass loss rate, size decrease rate, and thus, a slower drug release rate.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"29 1","pages":"243-6"},"PeriodicalIF":0.0,"publicationDate":"2016-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87385805","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}
{"title":"Anti-tumor activity of benzylideneacetophenone derivatives via proteasomal inhibition in prostate cancer cells.","authors":"Yun-Hee Lee, Jaesuk Yun, Jae-chul Jung, Seikwan Oh, Young-Suk Jung","doi":"10.1691/PH.2016.5845","DOIUrl":"https://doi.org/10.1691/PH.2016.5845","url":null,"abstract":"A number of some chalcone derivatives possess promising biological properties including anti-inflammation, anti-oxidant, and anti-tumor activity. Although it has been shown that some derivatives of chalcone induce apoptosis in different kinds of cancer cells, the involved mechanism of action is not well defined. The purpose of this study is to investigate the primary target of a benzylideneacetophenone derivative (JC3), which is a synthetic compound derived from the chalcone family, in human cancer, using prostate cancer cells as a working model. Herein, we show that JC3 inhibits proteasomal activity as indicated by both in vitro and in cell-based assays. Especially, the JC3-dimer was more potent than monomer in the aspect of proteasome inhibition, which induced apoptosis significantly in the prostate cancer cells. Owing to the critical roles of the proteasome in the biology of human tumor progression, invasion, and metastasis, these findings give an important clue for the development of novel anti-tumor agents.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"4 1","pages":"274-9"},"PeriodicalIF":0.0,"publicationDate":"2016-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90358814","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}
{"title":"A novel RP-HPLC method for the detection and quantification of roxithromycin in topical delivery studies.","authors":"M. Aucamp, C. Csongradi, M. Gerber, J. du Plessis","doi":"10.1691/PH.2016.5165","DOIUrl":"https://doi.org/10.1691/PH.2016.5165","url":null,"abstract":"A novel HPLC method with UV detection for the identification and quantification of roxithromycin (ROX) during in vitro skin penetration studies has been developed and validated. The method proved to be simple and rapid with isocratic elution (flow rate: 1.0 mL/min) of ROX, using a C18 column and UV detection at 205 nm. The mobile phase consisted of 0.06 M potassium di-hydrogen orthophosphate buffer (pH adjusted to 7.4 with sodium hydroxide) and acetonitrile in a 50:50 (v/v) ratio. This method showed linearity across the concentration range of 5 - 1000 μg/mL with a correlation coefficient of 0.9999. An average recovery of 101.78% was obtained. Limit of detection (LOD) and lower limit of quantification (LLOQ) values proved that ROX can still be detected at a concentration level of 0.3 μg/mL and accurately quantified at a concentration of 0.5 μg/mL. The specificity testing during method validation proved that this method is suitable for the accurate detection and quantification of ROX even when combined with different compounds typically used during the formulation of topical delivery systems.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"149 1","pages":"175-6"},"PeriodicalIF":0.0,"publicationDate":"2016-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74258903","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}
Die Pharmazie. BeiheftePub Date : 2016-02-01DOI: 10.26226/morressier.57d6b2bbd462b8028d88d10c
A. Popielec, É. Fenyvesi, K. Yannakopoulou, T. Loftsson
{"title":"Effect of cyclodextrins on the degradation rate of benzylpenicillin.","authors":"A. Popielec, É. Fenyvesi, K. Yannakopoulou, T. Loftsson","doi":"10.26226/morressier.57d6b2bbd462b8028d88d10c","DOIUrl":"https://doi.org/10.26226/morressier.57d6b2bbd462b8028d88d10c","url":null,"abstract":"The effect of cyclodextrin (CD) inclusion complexes on the degradation of benzylpenicillin in aqueous solutions was investigated at several different pH values and 37°C. The effects of neutral as well as both positively and negatively charged CDs were evaluated; all together 13 different CDs. Kinetic studies with HPβCD and RMβCD at pH ranging from 1.2 to 9.6 showed that CDs have stabilizing effect on the β-lactam ring in aqueous acidic media but generally accelerated the hydrolytic cleavage of the β-lactam ring in neutral and basic media. At physiologic pH (pH 7.4) quaternary ammonium CD derivatives (i.e., positively charged CD derivatives) have the highest catalytic effect, resulting in 6- to 18-fold enhancement of hydrolysis rate, while both the neutral methylated CDs had much less effect, resulting in 2- to 3-fold enhancement, and the negatively charged CD derivatives, resulting in only about 1.1- to 1.2-fold enhancement in the hydrolytic cleavage of the β-lactam ring. Addition of water-soluble polymers to the aqueous reaction media containing CDs was shown to decrease the catalyzing effects of CDs on the β-lactam hydrolysis.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"13 1","pages":"68-75"},"PeriodicalIF":0.0,"publicationDate":"2016-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79646389","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}
{"title":"Therapeutic delivery of RNA effectors: diseases affecting the respiratory system.","authors":"Rima Kandil, M. Merkel","doi":"10.1691/PH.2016.5740","DOIUrl":"https://doi.org/10.1691/PH.2016.5740","url":null,"abstract":"Although there are several hurdles to overcome on the way to the lung, this target organ provides several advantages for successful drug absorption. Recent findings in this field of research give reason to assume that the pulmonary delivery of RNA effector molecules holds a promising potential for the treatment of numerous severe respiratory diseases.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"84 1","pages":"21-6"},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73432989","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}
{"title":"The influence of passage number for Caco2 cell models when evaluating P-gp mediated drug transport.","authors":"S. Senarathna, A. Crowe","doi":"10.1691/PH.2015.5106","DOIUrl":"https://doi.org/10.1691/PH.2015.5106","url":null,"abstract":"Caco2 cells are a human adenocarcinoma cell line that forms tight junctions and are widely used to examine bidirectional drug transport as well as P-glycoprotein mediated efflux. Unfortunately Caco2 cell lines can be very heterogeneous in nature. Our aim was to improve the Caco2 cell model for determination of P-glycoprotein mediated drug transport. Young passage Caco2 from ATCC had inadequate expression of P-glycoprotein, therefore three approaches were adopted to upregulate Caco2 P-glycoprotein expression to mimic that in vivo; a) incubation of mature Caco2 monolayer with rifampicin, b) prolonged exposure of Caco2 cells to vinblastine (generating the Caco2 VIN line), and c) splitting cells every 7 to 9 days until late passage numbers (over P80) were available. Upon development of the models, P-gp expression and activity was determined using western blotting and bidirectional transport studies of rhodamine123. All four models exhibited P-gp mediated efflux transport for rhodamine123. Incubation with rifampicin did not alter bidirectional transport compared to passage 44 cells. Increased passage number altered P-glycoprotein expression and the efflux ratio increased to 4.7 for passage 80 from 1.4 of passage 44. The highest basolateral to apical transport was observed for both passage 89 Caco2 and the Caco2 VIN model with an efflux ratio of 13 to 14. Western blot images confirmed the increased P-glycoprotein expression of late passage and Caco2 VIN. Caco2 cells are not ready for P-gp related research when first acquired from ATCC (Passage 18). Late passage Caco2 cell monolayers or Caco2 VIN models are needed to determine P-gp mediated efflux transport.","PeriodicalId":86039,"journal":{"name":"Die Pharmazie. Beihefte","volume":"34 1","pages":"798-803"},"PeriodicalIF":0.0,"publicationDate":"2015-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84535119","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}