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Pharmaceutical Sciences Advancing Molecular Cancer Therapeutics ~To Improve Rationale and Effectiveness of Molecularly Targeted Drugs~.
Pharmaceutical Sciences Advancing Molecular Cancer Therapeutics~To Improve Rationale and Effectiveness of Molecularly Targeted Drugs~. Yakugaku Zasshi. 2017;137(2):127-128 Authors: Noguchi K, Mashima T PMID: 28154318 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Noguchi K, Mashima T Tags: Yakugaku Zasshi Source Type: research

Cancer Stem Cells (CSCs) as a Rational Therapeutic Cancer Target, and Screening for CSC-targeting Drugs.
Abstract  The emergence of drug resistance is a major obstacle to the successful pharmacological treatment of cancer. Tumor heterogeneity is one of the key factors underlying drug resistance. Cancer cell heterogeneity in tumors is caused by genetic mutation and by the existence of cancer stem cells (CSCs). CSCs are defined as a subpopulation of highly tumorigenic cancer cells with self-renewal activity. It has been reported that various types of cancer involve CSCs, and that CSCs are generally resistant to anticancer drugs. Therefore, CSC-targeting agents could allow for more effective pharmacological treatment ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Mashima T Tags: Yakugaku Zasshi Source Type: research

Screening for Chemical Suppressors of the Wnt/ β-catenin Signaling Pathway.
Screening for Chemical Suppressors of the Wnt/β-catenin Signaling Pathway. Yakugaku Zasshi. 2017;137(2):133-136 Authors: Nishiya N Abstract  Aberrant activation of Wnt/β-catenin canonical signaling is observed in multiple malignant tumors, and is recognized as an attractive therapeutic target for molecular targeted drugs. This signaling pathway is also involved in maintaining pluripotency in adult stem cells. Therefore, lowering potential stem cell toxicity is a key factor for the development of a Wnt/β-catenin signaling inhibitor. Here, we show Wnt/β-catenin pathway inhibitors with low toxicity...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Nishiya N Tags: Yakugaku Zasshi Source Type: research

New Type of Antitumor Agent Targeting the Cell Adhesion Molecule, Integrin.
Abstract  The extracellular matrix (ECM) provides a variety of biological signals for cell regulation. It is apparent that some of these signals are derived from functional sites, which are concealed in the higher structure of ECM protein molecules. Previously, we found that fibronectin, a ubiquitous cell adhesive ECM protein, harbors a cryptic functional site termed FNIII14, which can be exposed through the processing of fibronectin by inflammatory proteinases, including matrix metalloproteinase-2 (MMP-2). FNIII14, once exposed, induces a conformational change in beta1-integrins necessary for their functional i...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Fukai F Tags: Yakugaku Zasshi Source Type: research

Non-canonical Activation of Receptor Tyrosine Kinases in Cancer Progression.
Abstract  Receptor tyrosine kinases (RTKs) are known to be key regulators of cancer cell proliferation, migration, invasion and metastatic spread. Ligand-binding to the extracellular domain triggers canonical activation of the intracellular tyrosine kinase domain. In contrast, it has become evident that RTKs are also regulated by non-canonical tyrosine kinase-independent mechanisms via phosphorylation of their serine/threonine residues. In this review, I mainly introduce our recent findings on the non-canonical regulation of epidermal growth factor receptor (EGFR), ErbB2 and erythropoietin-producing hepatocellul...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Sakurai H Tags: Yakugaku Zasshi Source Type: research

Exploration of Molecular Targets in the Development of New Therapeutics Aimed at Overcoming Multidrug Resistance.
Abstract  Multidrug resistance (MDR) in cancer is a major problem in clinical settings: MDR correlates with a patient's poor prognosis and decreased quality of life. Recently, MDR was found to be involved in various signal pathways, so the inhibition of signal molecules by molecular targeting drugs may help overcome MDR. In addition, the acquisition of MDR is shown to be associated with the overexpression of drug efflux pumps such as P-glycoprotein (MDR1), which in turn affects the regulation of the expression of cell survival factors, B-cell leukemia protein 2 (Bcl-2) family proteins, etc. We analyzed the mecha...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Nishida S, Tsubaki M Tags: Yakugaku Zasshi Source Type: research

Novel Mechanisms of Resistance to Investigational Molecularly Targeted Drugs.
This study suggests that novel mechanisms reduce cytokinetic dysregulation caused by those inhibitors, and anti-apoptotic activities are associated with resistant phenotypes. These observations suggest that the activation of various bypass mechanisms may allow cancer cells to avoid the selective antiproliferative effect of molecularly targeted drugs, and such bypass activation mechanism would thus be a critical target for designing combination chemotherapy to overcome non-genetic drug resistance. PMID: 28154324 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Noguchi K Tags: Yakugaku Zasshi Source Type: research

Our Approaches to the New Drug Application of Ephedrine Alkaloids-free Ephedra Herb Extract (EFE): Toward Breakthrough in Natural Medicines in Japan.
PMID: 28154325 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Goda Y Tags: Yakugaku Zasshi Source Type: research

Marketing Approval of Ethical Kampo Medicines.
Abstract  Kampo medicine is an original traditional medicine in Japan. Currently, 148 ethical Kampo formulations (Kampo prescription drugs) are registered in the National Health Insurance Price List. Kampo medicines can be prescribed under the national insurance system, which shows that they are part of conventional medicine in Japan. Japan has a unified drug approval system that does not distinguish between Western and Kampo medicines, and both are subject to the same regulations. The application for the market approval of ethical Kampo medicines is based on the general notification for drugs, i.e., "Handling o...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Hakamatsuka T Tags: Yakugaku Zasshi Source Type: research

Characterization of Phenolic Constituents from Ephedra Herb Extract.
Abstract  Ephedra Herb (Japanese name: mao) is defined as the terrestrial stem of Ephedra species. It is one of the most important crude drugs in Kampo prescriptions such as maoto, kakkonto, and shoseiryuto. The traditional biological properties of Ephedra Herb are mainly attributable to ephedrine alkaloids. Recently, our research group has found that Ephedra Herb extract also shows alkaloid-independent pharmacological action; therefore, we focused on polyphenols, other active ingredients of Ephedra Herb extract. Reports on the constituents of the extract other than ephedrine alkaloids are limited, although cond...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Amakura Y Tags: Yakugaku Zasshi Source Type: research

Efficient Preparation of Ephedrine Alkaloids-free Ephedra Herb Extract and Its Antitumor Effect and Putative Marker Compound.
Abstract  Ephedra Herb is a crude drug for the treatment of headache, bronchial asthma, nasal inflammation, and the common cold. Although it has been considered that ephedrine alkaloids (EAs) are the principal active ingredients of Ephedra Herb, EAs are known to induce palpitations, hypertension, insomnia, and dysuria as major side effects. Therefore, the administration of EAs-containing drugs to patients with cardiovascular-related diseases is strongly contraindicated. Previously, we isolated herbacetin 7-O-neohesperidoside from Ephedra Herb. In addition, we found that herbacetin, a flavonoid aglycone in Ephedr...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Oshima N Tags: Yakugaku Zasshi Source Type: research

The Pharmacological Actions of Ephedrine Alkaloids-free Ephreda Herb Extract and Preparation for Clinical Application.
Abstract  Ephedra Herb is defined in the 17th edition of the Japanese Pharmacopoeia as the terrestrial stem of Ephedra sinica STAPF., Ephedra intermedia SCHRENK et C.A. MEYER, or Ephedra equisetina BUNGE (Ephedraceae) which contains more than 0.7% ephedrine alkaloids (ephedrine and pseudoephedrine). The primary effects and adverse effects of Ephedra Herb are traditionally believed to be mediated by ephedrine alkaloids. We recently reported that Ephedra Herb extract (EHE) exhibits antimetastatic and antitumor effects by suppressing the hepatocyte growth factor-c-Met signaling pathway through the inhibition of c-M...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Hyuga S Tags: Yakugaku Zasshi Source Type: research

Analgesic Effects and Side Effects of Ephedra Herb Extract and Ephedrine Alkaloids-free Ephedra Herb Extract.
In this study, we demonstrated that Ephedra Herb extract (EHE) shows strong TRPV1 activation, although ephedrine didn't show such effects. Both EHE and ephedrine alkaloids-free EHE (EFE) expressed similar analgesic action following oral administration, suggesting the presence of active components other than ephedrine alkaloids. Furthermore, EFE did not show side effects such as loss of sleep and irregular heartbeat in mice. Caution needs to be exercised while prescribing Ephedra Herb because it contains ephedrine. The application of EFE in Kampo medicine might be a better alternative in some cases. PMID: 28154330 [Pub...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Kobayashi Y Tags: Yakugaku Zasshi Source Type: research

Clinical Research Testing the Usefulness of Ephedrine Alkaloids-free Ephedra Herb Extract.
Abstract  We aimed to test the clinical usefulness of ephedrine alkaloids-free Ephedra Herb extract (EFE), which has been proven to be effective and safe in animal studies. First, we performed a safety trial with 7 healthy volunteers, and increased white blood cell counts were observed in 2. However, it was unknown whether this observation was a result of EFE administration. Then, we implemented a controlled, double-blind, randomized crossover trial as the second safety trial for EFE. The trial was conducted under strict conditions, and the participants were managed in the hospital and monitored using an increas...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Odaguchi H Tags: Yakugaku Zasshi Source Type: research

A New Pain Regulatory System via the Brain Long Chain Fatty Acid Receptor GPR40/FFA1 Signal.
Abstract  An increasingly large number of pharmacological and physiological works on fatty acids have shown that the functional properties of fatty acids are regulated by the amount of individual fatty acid intake and the distribution of fatty acids among organs. Recently, it has been determined that G-protein-coupled receptor 40/free fatty acid receptor 1 (GPR40/FFA1) is activated by long-chain fatty acids, such as docosahexaenoic acid (DHA). GPR40/FFA1 is mainly expressed in the β cell of the pancreas, spinal cord and brain. It is reported that this receptor has a functional role in controlling blood glucose ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Nakamoto K Tags: Yakugaku Zasshi Source Type: research

Structural and Biochemical Analyses on the RNA-dependent RNA Polymerase of Influenza Virus for Development of Novel Anti-influenza Agents.
In this study, we describe a novel Val/Arg/Gly (VRG) site in the PB2 cap-binding domain, which is necessary for interaction with acetyl-CoA found in eukaryotic histone acetyltransferases (HATs). In vitro experiments revealed that the recombinant PB2 cap-binding domain that includes the VRG site interacts with acetyl-CoA; moreover, it was found that this interaction could be blocked by CoA and various HAT inhibitors. Interestingly, m(7)GTP also inhibited this interaction, suggesting that the same active pocket is capable of interacting with acetyl-CoA and m(7)GTP. To elucidate the importance of the VRG site on PB2 function ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Hatakeyama D Tags: Yakugaku Zasshi Source Type: research

The Chemical Constituents of Uninvestigated Plants in Hiroshima Prefecture.
Abstract  Recently, the investigation of bioactive constituents from natural products has been performed extensively around the world, yet many plants remain to be studied, even now. The author is especially interested in saponins, which are included in various natural products and Kampo medicines. Based on these study aims, we isolated the chemical constituents of Dianthus japonicus and Clethra barbinervis. The aerial parts of Dianthus japonicus were isolated into nine new (1-9) and seven known oleanane-type triterpene saponins. The structural elucidation of their chemical constituents was examined by several s...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Sugimoto S Tags: Yakugaku Zasshi Source Type: research

Analysis of the Risk Factors for Severe Oral Mucositis in Head and Neck Cancer after Chemoradiotherapy with S-1.
Abstract  Radiotherapy (RT) and chemoradiotherapy (CRT) is widely accepted as the standard treatment for head and neck cancer (HNC). Oral mucositis (OM) often develops as an adverse reaction in HNC patients that receive RT or CRT involving S-1. However, little is known about the risk factors for OM in HNC patients. We retrospectively evaluated patients' pre-treatment clinical data in order to identify the risk factors for severe OM in HNC patients that are treated with RT or CRT involving S-1. We analyzed the cases of 129 patients who received RT or CRT involving S-1 for HNC. The endpoint of the survey was the o...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Nagatani A, Ogawa Y, Sunaga T, Tomura K, Naito Y, Fujii N, Okabe T, Hashimoto T, Kogo M, Sasaki T Tags: Yakugaku Zasshi Source Type: research

Development and Validation of a Training Program Using a Cognitive Behavioral Therapy Approach with the Purpose of Enabling Community Pharmacists to Provide Empathic Patient Counseling.
Abstract  To enable community pharmacists to provide empathic patient counseling, we developed and validated a training program based on cognitive reframing, which is one of the cognitive behavioral therapies. We divided 24 community pharmacists into two groups, providing training to the intervention group. The duration of the training program was two hours per session, with a total of eight hours. We conducted a survey of the intervention group to evaluate their training experience. In addition, we performed two role-play scenarios on patient counseling using simulated patients, evaluating the patient counselin...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Tanuma K, Watanabe F, Maeda H, Shiina M, Hara K, Kamei M Tags: Yakugaku Zasshi Source Type: research

Investigation of Mental Disorders in Lung Cancer Outpatients: A Retrospective Analysis.
In this study, we performed a retrospective analysis to identify the risk factors for psychiatric disorders in lung cancer survivors. Most lung cancer survivors that were diagnosed with psychiatric disorders had stage 4 disease. In addition, it was found that an increase in disease stage and high doses of opioids are associated with an increased risk of psychiatric disorders in lung cancer survivors. These findings suggest that it is necessary to consider the mental changes experienced by lung cancer patients during disease progression. PMID: 28154337 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pha...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 7, 2017 Category: Drugs & Pharmacology Authors: Nakamura Y, Kanemoto E, Kajizono M, Kitamura Y, Sendo T Tags: Yakugaku Zasshi Source Type: research

Pharmacokinetic Studies of Orally Administered Magnesium Oxide in Rats.
Abstract   Magnesium oxide (MgO) tablets are widely used as laxatives in patients with constipation. Recently, the "Revision of Precautions on the Use of Magnesium Oxide" has been issued by the Japanese Pharmaceuticals and Medical Devices Agency, warning against the risk of hypermagnesemia with the use of MgO. However, the majority of physicians continue to administer MgO for constipation without adequately considering its safe use. In the present study, we performed two analyses using an identical lot of MgO tablets and evaluated the risk of hypermagnesemia. Approximately 90% of the MgO tablets dissolved within...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 26, 2017 Category: Drugs & Pharmacology Authors: Yoshimura Y, Fujisaki K, Yamamoto T, Shinohara Y Tags: Yakugaku Zasshi Source Type: research

Relationship between Physicochemical Properties of Medical Supplies and Serious Adverse Drug Reactions Listed in the Package Inserts.
Abstract <bibitem lang="en">  We sought to clarify the relationship between the physicochemical properties of each medical supply and serious adverse drug reactions listed in the package inserts, by reviewing new information. We investigated 1) 1,078 medicines currently available on the domestic Japanese market by using physicochemical data, such as cLogD, molecular weight (MW), and pKa and 2) the serious adverse drug reactions stated in the package inserts and the presence or absence of serious renal and liver disorders, as well as mental, extrapyramidal, and skin disorders. The renal disorders data showe...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 13, 2017 Category: Drugs & Pharmacology Authors: Yano R, Ohtsu F, Goto N Tags: Yakugaku Zasshi Source Type: research

Reconciling Pharmaceutical Education with Clinical Research, while Maintaining and Enhancing Clinical Ability within the Universities of Clinical Professors.
PMID: 28049886 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Teramachi H, Shigeyama M Tags: Yakugaku Zasshi Source Type: research

Evaluation of the Expression Profile of Extrapyramidal Symptoms Due to Antipsychotics by Data Mining of Japanese Adverse Drug Event Report (JADER) Database.
This study aimed to evaluate the expression profile of EPS in atypical and typical antipsychotics treatment using the Japanese Adverse Drug Event Report (JADER) database. We analyzed reports of EPS in the JADER database and calculated the reporting odds ratio (ROR) of antipsychotics potentially associated with EPS. We applied the Weibull shape parameter to time-to-event data in the JADER database. Consequently, there was little information to distinguish between the ROR of atypical and typical antipsychotics. A significant difference related to the time of onset of EPS in both antipsychotics was not recognized. However, wh...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Kose E, Uno K, Hayashi H Tags: Yakugaku Zasshi Source Type: research

Influence of Memantine on Continuous Treatment with Rivastigmine Patches-Retrospective Study Using the Logistic Regression Analysis.
Abstract  Rivastigmine patches exhibit stable effects when attached once a day, and may reduce Alzheimer's disease (AD) patient's or caregiver's burden. On the other hand, it was reported that adverse events, such as dermal disorder, frequently appeared after the start of rivastigmine administration. We retrospectively investigated medical records in 120 patients with moderate or mild AD in whom rivastigmine administration was started in the Department of Neurology, Fukuoka University Hospital between July 2011 and June 2014 (43 males, 77 females, mean age: 76.9±8.0 years). In 72 patients (60.0%), rivastigmine ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Yasutaka Y, Fujioka S, Terasawa M, Shibaguchi H, Futagami K, Ouma S, Tsuboi Y, Kamimura H Tags: Yakugaku Zasshi Source Type: research

Importance of Pharmaceutical Training and Clinical Research at Medical Facilities.
Abstract  To respond to advancements in medical techniques, and to address the separation of medical and dispensary practices, clinical professors are required to educate human resource staff to become highly-skilled pharmacists. For this purpose, it is extremely important for these professors to learn about cutting-edge practical skills and knowledge, as well as to advance their expertise. In addition, they need to conduct clinical research in cooperation with relevant facilities. As our university does not have its own hospital or pharmacy, it is important to provide training for clinical professors in clinica...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Myotoku M Tags: Yakugaku Zasshi Source Type: research

Nurturing Pharmacists Who Contribute to Clinical Practice through Galenical-pharmaceutical Studies.
Abstract  In clinical environments, difficulty in the uniform preparation of Mohs paste has been noted, due to variations in its physical properties, and despite preparations being based on the same prescriptions. Therefore, studies have been conducted to clarify the physicochemical phenomena influencing such variations, and then to develop a prescription design that will improve the usability of this product through the use of additives with sufficient safety, thereby addressing the above-mentioned demerit. An improved form of Mohs paste, not containing the starch that is responsible for the variations in physi...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Shigeyama M, Taguchi M, Yamamoto H Tags: Yakugaku Zasshi Source Type: research

Development of Cellular and Tissue-based Products for Retinal Regenerative Medicine.
Abstract  Since the discovery of induced pluripotent stem cells (iPSCs) generation, much progress has been made in the fields of medical and pharmaceutical research, such as cell transplantation therapy. We have generated retinal cells and tissues, including retinal pigment epithelia (RPE), from human iPSCs. The ability to produce iPSCs from patients allows for autologous transplantation without causing immune rejection. The autologous transplantation of iPSC-derived retinal pigment epithelial sheets to a patient with age-related macular degeneration was carried out in Japan in 2014 as a first-in-human clinical ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Osakada F Tags: Yakugaku Zasshi Source Type: research

Maintenance of Clinical Expertise and Clinical Research by the Clinical Professors at Gifu Pharmaceutical University.
Abstract  The clinical professors at Gifu Pharmaceutical University (GPU) provide pharmaceutical services at GPU Pharmacy, Gifu University Hospital, and Gifu Municipal Hospital to keep their clinical skills up-to-date; they also perform clinical research in collaboration with many clinical institutes. The Laboratory of Clinical Pharmacy is part of the Department of Pharmacy Practice and Science, to which the clinical professors belong, and is composed of three clinical professors (a professor, an associate professor, and an assistant professor). The professor administers the GPU Pharmacy as its director, while t...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Tachi T, Noguchi Y, Teramachi H Tags: Yakugaku Zasshi Source Type: research

Development of Novel Hydrophobic Pharmacophores Based on Three-dimensional Molecular Architectures and Elements Chemistry.
In this study, we developed various bioactive compounds bearing a boron cluster, silicon-containing or germanium-containing functionalities as novel hydrophobic structures. Regarding the boron cluster-based compounds, we developed highly potent nonsteroidal androgen receptor (AR) antagonists, progesterone receptor (PR) antagonists, and non-secosteroidal vitamin D receptor (VDR) agonists. Regarding the Group 14 elements, we systematically determined hydrophobicity parameters of various trialylmethyl, trialkylsilyl and trialkylgermyl substituents, and revealed that silicon and germanium containing compounds exhibited higher ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Fujii S Tags: Yakugaku Zasshi Source Type: research

Development of New Liposome Targeting Strategies for Application of Disease Therapies.
Abstract  Drug delivery systems (DDS) are based on the concept of providing the optimal amount of a drug to a specific area requiring treatment. Liposomes are lipid-based nanoparticles capable of encapsulating any drug into both their membrane and aqueous phases. They have the potential to be targeted when their surfaces are modified with functional molecules such as antibodies and peptides. Thus, liposomes have strong potential as drug carriers if designed for active targeting. Our research group has recently developed a new concept for liposome targeting called "reverse targeting DDS (RT-DDS)". RT-DDS differs ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Shimizu K Tags: Yakugaku Zasshi Source Type: research

Pathogenesis of Diet-induced Atopic Dermatitis in Hairless Mice.
In this study, we examined whether the deficiency of certain polyunsaturated fatty acids (PUFAs) was involved in the diet-induced AD pathogenesis. In the serum of HR-AD-fed mice, levels of linoleic acid (LA, 18:2n-6) and α-linolenic acid (ALA, 18:3n-3), as well as their metabolites, were markedly decreased. HR-AD-induced AD symptoms were significantly ameliorated by LA supplementation, and to a lesser extent by ALA supplementation. In addition, LA metabolites, such as γ-linolenic acid and arachidonic acid, had effects similar to those of LA. Further, using semi-purified custom diets, we attempted to reproduce HR-AD-induc...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Fujii M Tags: Yakugaku Zasshi Source Type: research

Development of Molecular Probes Based on Iron Oxide Nanoparticles for in Vivo Magnetic Resonance/Photoacoustic Dual Imaging of Target Molecules in Tumors.
Abstract  Molecular imaging probes that enable seamless diagnoses of tumors in the preoperative and intraoperative stages could lead to surgical resection of tumors based on highly accurate diagnoses. Because iron oxide nanoparticles (IONPs) have high proton relaxivity and high molar extinction coefficients suitable for magnetic resonance imaging (MRI) and photoacoustic imaging, respectively, we planned to develop molecular imaging probes applicable to the pre- (MRI) and intraoperative (photoacoustic imaging) stages. Human epidermal growth factor receptor 2 (EGFR2; HER2) was selected as a target molecule, and we...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Sano K Tags: Yakugaku Zasshi Source Type: research

Expression and Regulation of Tal2 during Neuronal Differentiation in P19 Cells.
Abstract  T-cell acute lymphocytic leukemia 2 (Tal2) is a gene encoding a member of the basic helix-loop-helix transcription factor family, which is essential for the normal development of the mouse brain. We found that Tal2 was induced during neural differentiation in P19 cells, which are pluripotent mouse embryonal carcinoma cells that differentiate into the neural lineage upon both exposure to all-trans retinoic acid (atRA) and the formation of cell aggregation. Tal2 expression during neural differentiation in P19 cells was detected within 3 h after induction with atRA and retinoic acid receptor α (RARα). T...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Kobayashi T Tags: Yakugaku Zasshi Source Type: research

Developmental Toxicity of Nanoparticles on the Brain.
Abstract  The toxicity of nanoparticles (nanotoxicology) is being investigated to understand both the health impacts of atmospheric ultrafine particles-the size of which is a fraction (<0.1 μm aerodynamic diameter) of that of PM2.5 (<2.5 μm diameter)-and the safer use of engineered nanomaterials. Developmental toxicity of nanoparticles has been studied since their transfer from pregnant body to fetal circulation and offspring body was first reported. Here we reviewed the developmental toxicity of nanoparticles on the brain, one of the most important organs in maintenance of mental health and high quality...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Umezawa M, Onoda A, Takeda K Tags: Yakugaku Zasshi Source Type: research

The Incidence of Cisplatin-induced Hypomagnesemia in Cervical Cancer Patients Receiving Cisplatin Alone.
Abstract  Hypomagnesemia is one side effect in patients receiving cisplatin. However, there are few reports of cisplatin-induced hypomagnesemia in Japan. We retrospectively investigated the incidence of hypomagnesemia and nephrotoxicity in patients undergoing radiation therapy who were treated with cisplatin alone (dosage: 40 mg/m(2), administration interval: 1 week) for cervical cancer. Thirty-two patients undergoing radiation therapy who received cisplatin alone for cervical cancer between January 2012 and May 2016 at Aichi Medical University Hospital were included. We measured patients' serum magnesium and cr...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Yamamoto Y, Watanabe K, Matsushita H, Tsukiyama I, Matsuura K, Wakatsuki A Tags: Yakugaku Zasshi Source Type: research

Effect of Medical Educational Lectures by Pharmacists for Understanding and Relieving Post-laryngectomy Symptoms.
In conclusion, the participants might not feel relief of four symptoms because of inadequate understanding of the method including medicine use for coping with their symptoms. Grasping the current situation and medication use of patients after TL by pharmacists will be helpful for appropriate medication use. PMID: 28049900 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Hyoguchi N, Kubota T, Kobayashi D, Shimazoe T Tags: Yakugaku Zasshi Source Type: research

Improvement of Clinical Skills through Pharmaceutical Education and Clinical Research.
Abstract  Professors and teaching staff in the field of pharmaceutical sciences should devote themselves to staying abreast of relevant education and research. Similarly those in clinical pharmacies should contribute to the advancement of pharmaceutical research and the development of next generation pharmacists and pharmaceuticals. It is thought that those who work in clinical pharmacies should improve their own skills and expertise in problem-finding and -solving, i.e., "clinical skills". They should be keen to learn new standard treatments based on the latest drug information, and should try to be in a positi...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Ishizaki J Tags: Yakugaku Zasshi Source Type: research

Analysis of Primary Aromatic Amines Derived from Azo Colorants in Textile Products and Determination of Their Source Colorant.
Abstract  Twenty-four primary aromatic amines (PAAs) derived from azo colorants, which are controlled by the Act on Control of Household Products Containing Harmful Substances by the Japan Ministry of Health, Labour and Welfare, aniline and 1,4-phenylendiamine were analyzed in 86 samples of 40 textile products by GC-MS. Even though these PAAs detected in the samples did not exceed the regulation value (30 μg/g), 14 kinds of PAAs were detected that exceeded the limit of quantification. 4,4'-Methylenedianiline, in amounts that exceeded the limit of quantification, was detected in 20 textile samples containing syn...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 5, 2017 Category: Drugs & Pharmacology Authors: Sugaya N, Sato Y, Takahashi M, Sakurai K, Kawakami T Tags: Yakugaku Zasshi Source Type: research

Delay in the provision of medication by a pharmacy outside the respiratory outpatient department.
Abstract   Respiratory medicine physicians prescribe many different kinds of medications depending on the specific patient. To examine an outside pharmacy's ability to meet the demand of our respiratory prescription services, we developed a questionnaire for all the patients who came to our outpatient department from November 1, 2015 to January 31, 2016. A total of 298 of 330 patients answered the questionnaire.   Overall, 169 patients mainly went to the pharmacy near our hospital, whereas 64 patients mainly went to another pharmacy. Specifically, 23 of 219 patients were not immediately given medication by the...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2016 Category: Drugs & Pharmacology Authors: Matsumoto M, Fujita S, Kannen M, Kawase K, Kaneshiro K, Takatsuki K Tags: Yakugaku Zasshi Source Type: research

Development and Biosensor Applications of Novel Functional Electrodes.
This article reviews the voltammetric properties of sugar sensors prepared using dithiobis (4-butyrylamino-m-phenylboronic acid) (DTBA-PBA)-modified electrodes and PBA-appended layer-by-layer film-modified electrodes. In addition, the redox properties of reduced graphene oxide (rGO)-modified glassy carbon electrodes (GCEs) are discussed. The surface of a gold electrode was modified with a monolayer of DTBA-PBA to prepare sugar-sensitive electrodes. The modified electrodes exhibited attenuated cyclic voltammograms for Fe(CN)6(3-/4-) in the presence of sugars at neutral pH as a result of their binding to DTBA-PBA on the elec...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Takahashi S Tags: Yakugaku Zasshi Source Type: research

Nonequilibrium Molecular Switching of Chiral Helicene Oligomers in Double-Helix Formation.
Abstract  Molecular switching is the phenomenon in which a molecular structural change occurs reversibly in response to an external stimulus or energy. It plays an important role in biology, in which it is used for sensing environmental changes. In contrast to well-studied equilibrium molecular switching involving thermodynamically stable states, nonequilibrium molecular switching involving a metastable state is a notable chemical phenomenon and is the theme of this study. Sulfonamido- and aminomethylenehelicene oligomers show a reversible structural change from a double helix to a random coil in dilute solution...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Shigeno M Tags: Yakugaku Zasshi Source Type: research

Design and Synthesis of Functional Molecules Based on Complexation and Their Biological Applications.
Abstract  In this review, we introduce the development of supermolecules, host-guest complexes, and metal complexes formed from the combination of non-covalent interactions and/or coordination bonds, as well as their biological applications. An adenine selective host molecule 1 provides a correctly oriented array of complementary hydrogen bonding sites for the adenine nucleobase. Furthermore, the new DDAA (D: hydrogen bond donor, A: hydrogen bond acceptor) module 4 and ADDA module 7 have been developed as quadruple hydrogen-bonding modules. A quadruple zwitterion 8 forms supramolecular gel in dimethyl sulfoxide,...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Hisamatsu Y Tags: Yakugaku Zasshi Source Type: research

Synthesis of Effective Food Constituents toward the Development of Chemical Biology Investigations.
This article describes the development of various probes and immunogens for chemical-biological investigations of food flavonoids. We accomplished a large (gram)-scale asymmetric synthesis of a key intermediate, 5-aminopentyl deoxy epigallocatechin-3-gallate (APDOEGCg; 3), an analogue of green tea polyphenol EGCg, in which the key step was cationic cyclization utilizing neighboring group participation of the gallate carbonyl group. The synthetic APDOEGCg (3) was efficiently converted to a fluorescent probe 18 and an immunogen 19 by utilizing the high reactivity of the amine functional group. We confirmed the usefulness of ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Asakawa T Tags: Yakugaku Zasshi Source Type: research

Development and Analysis of Novel Therapeutic Targets to Improve Pancreatic β-Cell Function in Type 2 Diabetes.
Abstract  Pancreatic β-cell dysfunction is a major feature of type 2 diabetes. Therefore maintenance of β-cell function is essential to preventing the onset and progression of type 2 diabetes. To elucidate the mechanisms underlying the regulation of insulin secretion and β-cell survival, we particularly focused on the roles of gasotransmitters in pancreatic β-cells. Nitric oxide (NO) and hydrogen sulfide (H2S) are recognized as toxic gases. However, they are also vital physiological and pathophysiological mediators in various cell types. NO, generated from L-arginine by reactions catalyzed by NO synthases, i...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Kaneko YK Tags: Yakugaku Zasshi Source Type: research

Final-stage Site-selective Acylation for the Total Synthesis of Natural Glycosides.
Abstract  The first total syntheses of multifidosides A-C are reported. The prominent feature is an unconventional retrosynthesis based on organocatalytic site-selective acylation of unprotected glycosides at the final stage of synthesis. A notable advantage of this strategy is that it avoids the risks of undesired side reactions during the removal of the protecting groups at the final stage of total synthesis. The proposed synthetic strategy has another advantage in terms of efficient late-stage derivatization of natural products. Due to the predictability and reliability of the catalytic site-selective introdu...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Ueda Y Tags: Yakugaku Zasshi Source Type: research

Relationship between PK/PD of Cefepime and Clinical Outcome in Febrile Neutropenic Patients with Normal Renal Function.
The objective of this study was to clarify the relation between %T>MIC and clinical outcome of CFPM, and to identify the optimal dosage regimen. We investigated the outcome of CFPM treatment for febrile neutropenia (FN) patients with normal renal function. Treatment success was defined as the completion of FN therapy with CFPM only. And we calculated %T>MIC for each case based on population pharmacokinetic parameters. The MIC value for simulation was set as 8 μg/mL. In logistic regression analysis, treatment success was significantly associated with the elevation of %T>MIC in the group with persistent neutropenia...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Yamashita Y, Kamiyama H, Yamamoto A, Kanoh H, Yuhki Y, Ueda A, Kawamoto Y, Gotoh Y, Yamamoto S Tags: Yakugaku Zasshi Source Type: research

Effects of Reinforcement Method of Dissection Physiology Education on the Achievement in Pharmacology.
In this study, we evaluated the effects of the reinforcement method of physiology education on achievement in pharmacology that was not conducted in the proficiency-dependent teaching method. The students in the basic class in physiology education were chosen based on achievement levels in anatomy. Achievement levels of pharmacology students in the basic class of physiology improved compared with those of students who had the same achievement levels in physiology but were not taught according to proficiency-dependent teaching in the 2013 academic year. These results suggest that the reinforcement method for education in ba...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Kitayama T, Kagota S, Yoshikawa N, Kawai N, Nishimura K, Miura T, Yasui N, Shinozuka K, Nakabayashi T Tags: Yakugaku Zasshi Source Type: research

Usefulness of Oral Care-related Information Provision at Drugstores to Prevent Pneumonia.
This study examined the usefulness of oral care-related information provision for the elderly by pharmacists working at drugstores. A questionnaire survey was conducted, involving 387 pharmacists working at drugstores and 51 elderly individuals who visited such stores. Oral care-related information had been actively provided by 14.5% of the pharmacists, and 62.5% of all oral care products were being sold as care products. When focusing on the elderly, 70.6% showed interest in oral care, but the proportion of those who had performed self-care to promote such health was limited to 5.9%. After being provided with oral care-in...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Mizoguchi M, Kuwano S, Suzuki I, Shigeyama M Tags: Yakugaku Zasshi Source Type: research

Probable Serotonin Syndrome and Withdrawal Symptoms Caused by Milnacipran.
Abstract  A 70-year-old woman, residing in a nursing home, was admitted to our hospital because of cerebral hemorrhage. She had excessive sweating, a temperature above 37°C, and intermittent muscle spasm such as myoclonus, since the time of admission. We suspected that these symptoms were related to side effects caused by the milnacipran she was taking for depression, prior to hospitalization. After we discontinued milnacipran, the patient began exhibiting withdrawal symptoms such as excitement and insomnia. When we substituted milnacipran with mianserin, the withdrawal symptoms diminished and the excessive swe...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 4, 2016 Category: Drugs & Pharmacology Authors: Koshiishi T, Okuyama K Tags: Yakugaku Zasshi Source Type: research