[Metabolism of Sesamin and Drug-Sesamin Interaction].
Abstract  Sesamin, derived from sesame seeds, is known to have various biological effects. Since some of these effects appear to be derived from its metabolites, the elucidation of sesamin metabolism is essential to understanding the molecular mechanism of its effects. In addition, it is important to clarify drug-sesamin interactions in order to address safety concerns, as some food factors are known to affect drug metabolism. Our previous studies revealed that sesamin was sequentially metabolized by cytochrome P450 (CYP) and UDP-glucuronosyltransferase or sulfotransferase. Whereas sesamin metabolism is mainly m...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Sakaki T, Yasuda K, Nishikawa M, Ikushiro S Tags: Yakugaku Zasshi Source Type: research

[Drug-Drug Interactions with Consideration of Pharmacogenetics].
Abstract  Elderly patients often suffer from a variety of diseases and therefore may be prescribed several kinds of drugs. Interactions between these drugs may cause problems in some patients. Guidelines for drug interactions were released on July 8, 2014 "Drug Interaction Guideline for Drug Development and Labeling Recommendations (Final Draft)". These guidelines include the theoretical basis for evaluating the mechanisms of drug interaction, the possible extent of drug interactions, and take into consideration special populations (e.g., infants, children, elderly patients, patients with hepatic or re...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Ozawa S Tags: Yakugaku Zasshi Source Type: research

[Bioinorganic Chemistry of Iron].
Abstract  The X-ray crystallographic analysis of the single-crystal mugineic acid-Cu(II) complex showed that mugineic acid acts as a hexadentate ligand. Mugineic acid, a typical phytosiderophore, shows a marked stimulating effect on 59Fe-uptake and chlorophyll synthesis in rice plants. A salient feature is the higher reduction potential of the mugineic acid-Fe(III) complex than those of bacterial siderophores. X-ray diffraction study of the structurally analogous Co(III) complex of the mugineic acid-Fe(III) complex demonstrates that the azetidine nitrogen and secondary amine nitrogen, and both terminal carboxyla...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Mino Y Tags: Yakugaku Zasshi Source Type: research

[Pharmacological Mechanisms of Boiogito and Bofutsushosan in Diabetes and Obesity Models].
Abstract  The antihyperglycemic activities of extracts of boiogito (BOT) and bofutsushosan (BTS) were investigated in streptozotocin-induced (STZ)-diabetic mice. BOT extract containing Stephania tetrandra S. MOORE root (stephania), has more potent antihyperglycemic activity than BOT extract containing sinomenium stem (sinomenium). Extracts of stephania and astragalus root (astragalus) exert combined effects in the antihyperglycemic and insulinotropic activities of BOT extract. Fangchinoline, but not tetrandrine, in stephania plays a role in its activity. Formononetin in astragalus potentiates the actions of fang...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Kobayashi S Tags: Yakugaku Zasshi Source Type: research

[Enzymological Studies on the Mechanisms of Pathogenesis of Diabetic Complications].
In this study, the enzymatic properties of AR isolated from various sources and a recombinant human AR (rh-AR) were analyzed in detail. The sensitivity of different forms of AR to several AR inhibitors (ARIs) was compared. Our findings enabled us to propose that human AR should be used as the target enzyme in the development of ARIs. An enzyme-linked immunosorbent assay (ELISA) for human AR which employed monoclonal antibodies against rh-AR was created, and this method was used to demonstrate the distribution of AR in human tissues. AR was widely distributed in various organs and blood cell components. The levels of erythr...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Tanimoto T Tags: Yakugaku Zasshi Source Type: research

[A Questionnaire Survey on Cooperation between Community Pharmacies and Hospitals in Outpatient Chemotherapy-Comparison of Roles of Pharmacists in Community Pharmacy and Hospitals].
Abstract  Previous reports suggested that sharing outpatient information during chemotherapy is very important for managing pharmaceutical usage between community pharmacies and hospitals. We herein examined using a questionnaire survey whether pharmaceutical management for outpatient chemotherapy is desired by community and hospital pharmacists. The response rates were 44.3% (133/300) for pharmacists in community pharmacies and 53.7% (161/300) for pharmacists in hospitals. Prescriptions for outpatients during chemotherapy were issued at 88.2% of the hospitals. Currently, 28.9% of hospital pharmacists rarely pro...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Ishibashi M, Ishii M, Nagano M, Kiuchi Y, Iwamoto S Tags: Yakugaku Zasshi Source Type: research

[Role of Pharmacists in Completion of Adjuvant Cisplatin-Vinorelbine Chemotherapy in Japanese Patients with Non-small Cell Lung Cancer].
Abstract  Adjuvant cisplatin-vinorelbine chemotherapy has been shown to be effective in patients with completely resected non-small cell lung cancer (NSCLC) in several Phase III trials, but not yet in the Japanese population. Pharmacists are expected to assist patients with completion of adjuvant chemotherapy. The aim of this retrospective study was to evaluate the compliance with and safety of adjuvant cisplatin-vinorelbine chemotherapy in Japanese patients and to evaluate the contribution of pharmacists to completion of treatment. Thirty-four patients with NSCLC who received adjuvant cisplatin-vinorelbine chem...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 7, 2018 Category: Drugs & Pharmacology Authors: Morimoto Y, Takei H, Tachibana K, Nakazato Y, Tanaka R, Nagashima Y, Watanabe K, Seki R, Shinohara T, Kondo H Tags: Yakugaku Zasshi Source Type: research

[The Immunosuppressive Function of Myeloid-derived Suppressor Cells Is Regulated by the HMGB1-TLR4 Axis].
Abstract  Myeloid-derived suppressor cells (MDSCs) accumulate under pathological conditions, including cancer and chronic inflammation, and they suppress various immune responses such as T cell proliferation. Although several inflammatory signals enhance the differentiation and/or function of MDSCs, it is not clear which factors regulate their differentiation and immunosuppressive function. It has been highlighted that damage-associated molecular patterns (DAMPs) play important roles in the induction of inflammation. One of the DAMPs, the high mobility group box 1 (HMGB1), is released from necrotic cells and sec...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Tachibana M Tags: Yakugaku Zasshi Source Type: research

[Role of Pharmacy in the Promotion of Drug Safety in Pharmacotherapy].
PMID: 29386428 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Satoh M Tags: Yakugaku Zasshi Source Type: research

[Pathogenic Mechanism and Diagnostic Testing for Drug Allergies].
Abstract  Three stages of the pathogenic mechanism of drug allergies can be considered: antigen formation, immune reaction and inflammation/disorder reaction. Drugs are thought to form 4 types of antigens: drug only, polymers, drug-carrier conjugates, and metabolite-carrier complexes. Antigens are recognized by B cell receptors and T cell receptors. Helper T cells (Th) are differentiated into four subsets, namely, Th1, Th2, Th17 and regulatory T cells (Treg). Th1 produces interleukin (IL)-2 and interferon (IFN)-γ, and activates macrophages and cytotoxic T cells (Tc). Macrophages induce type IV allergies, a...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Uno K Tags: Yakugaku Zasshi Source Type: research

[Development of "Patient Friendly Formulations" to Counter the Side Effects of Cancer Chemotherapy].
[Development of "Patient Friendly Formulations" to Counter the Side Effects of Cancer Chemotherapy]. Yakugaku Zasshi. 2018;138(2):169-175 Authors: Hanawa T, Kawano Y, Satoh M Abstract  Anticancer drug-induced stomatitis develops in 30% to 40% of cancer patients undergoing chemotherapy. However, medications for this condition are not commercially available in Japan. The "hospital formulation" is a customized medicine which hospital pharmacists prepare when doctors cannot carry out the medical therapy most suitable for a patient using commercial medicines. However, as the duties of...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Hanawa T, Kawano Y, Satoh M Tags: Yakugaku Zasshi Source Type: research

[Safe Use of Recent New Drugs-Current Status and Challenges].
Abstract  In Japan and overseas, Chugai Pharmaceutical Company handles numerous biopharmaceuticals, molecular targeted therapies and other pharmaceuticals with innovative modes of action. Expert safety evaluation is essential for promoting the appropriate use of these pharmaceuticals around the world and in gaining acceptance from patients and healthcare professionals (HCPs), while speedy decision-making is crucial for the timely collection and provision of safety information and thus ensuring safety. In 2015, we collected safety information on more than 180000 cases and evaluated it from a medical standpoint. W...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Ohashi Y Tags: Yakugaku Zasshi Source Type: research

[Adverse Effect Predictions Based on Computational Toxicology Techniques and Large-scale Databases].
Abstract  Understanding the features of chemical structures related to the adverse effects of drugs is useful for identifying potential adverse effects of new drugs. This can be based on the limited information available from post-marketing surveillance, assessment of the potential toxicities of metabolites and illegal drugs with unclear characteristics, screening of lead compounds at the drug discovery stage, and identification of leads for the discovery of new pharmacological mechanisms. This present paper describes techniques used in computational toxicology to investigate the content of large-scale spontaneo...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Uesawa Y Tags: Yakugaku Zasshi Source Type: research

[Stereocontrolled Total Synthesis of Biologically Active Natural Products].
Abstract  This review article describes the total syntheses of englerin A, ophiodilactones A and B, marinomycin A, N-methylwelwitindolinone C isothiocyanate, tirandamycins A-D, and tirandalydigin, which possess intriguing biological activities and challenging structures with characteristic ring systems. The focus is on the synthetic methodologies that lead to the highly stereocontrolled assembly of these natural products. PMID: 29386433 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Hatakeyama S Tags: Yakugaku Zasshi Source Type: research

[From a Ph.D. Thesis: Understanding the Past, Predicting the Future].
Abstract  Posey et al. have reported multiple molecular diagnoses in 4.5% of cases (101/2076) in which whole-exome sequencing was informative. Distinct disease phenotypes affect different organ systems, whereas overlapping disease phenotypes are more likely to be caused by two genes encoding proteins that interact within the same pathway. My research projects at the Niigata University of Pharmacy have investigated underlying mechanisms involved in human disease, including fatty acid metabolism, diabetic cardiomyopathy, atopic dermatitis, colitis, hepatitis, etc. Three students from abroad graduated this year fro...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Watanabe K Tags: Yakugaku Zasshi Source Type: research

[Modification of the Insulin Pen Assistive Device to Improve the Usability and Its Evaluation].
In this study, we prepared 4 assistive devices (A-D) for Miriopen® to improve the "ease of holding" and "ease of pushing" and compared their usability with that of a device provided by the pharmaceutical company (S). Fifty-five healthy volunteers in their 20s performed the self-injection maneuver using all 5 assistive devices and ranked them regarding 3 items, i.e., the "ease of holding", "ease of pushing", and "overall ease of administration". In all evaluation items, C was ranked first by the largest number of subjects, and the ranking by the subjects was shown by Ken...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Murakami M, Toraishi K, Koinuma M, Amano M Tags: Yakugaku Zasshi Source Type: research

[Analysis of Time-to-onset of Interstitial Lung Disease after the Administration of Small Molecule Molecularly-targeted Drugs].
Abstract  The aim of this study was to investigate the time-to-onset of drug-induced interstitial lung disease (DILD) following the administration of small molecule molecularly-targeted drugs via the use of the spontaneous adverse reaction reporting system of the Japanese Adverse Drug Event Report database. DILD datasets for afatinib, alectinib, bortezomib, crizotinib, dasatinib, erlotinib, everolimus, gefitinib, imatinib, lapatinib, nilotinib, osimertinib, sorafenib, sunitinib, temsirolimus, and tofacitinib were used to calculate the median onset times of DILD and the Weibull distribution parameters, and to per...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Komada F Tags: Yakugaku Zasshi Source Type: research

[Comparative Study of the Efficacy and Safety of Caffeine and Aminophylline for the Treatment of Apnea in Preterm Infants].
Abstract  Methylxanthine is widely administered for the treatment of apnea of prematurity in many countries, and previous reports have clearly established that caffeine is effective for the treatment of apnea of prematurity. In Japan, caffeine has been available since December 2014. Thus, we compared the efficacy and safety of caffeine with that of aminophylline in our hospital. There was no significant difference between the caffeine group and aminophylline group regarding the characteristics of the study patients. The mean efficacy rate from day 1 to day 10 was 89.5% in the caffeine group, and 81.9% in the ami...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Nagasato A, Nakamura M, Kamimura H Tags: Yakugaku Zasshi Source Type: research

[The Present Implementation Status and Problems of Vital-signs Measurement by Community Pharmacists in Home Medical Care in Osaka].
Abstract  While the community-based integrated care systems are in the process of being structured currently, more and more community pharmacists want to learn physical assessment skills. However, no large-scale survey focusing on present implementation status and problems of physical assessment by community pharmacists has been conducted yet. Osaka has the 2nd highest number of community pharmacies in Japan now, and the population aged ≥65 years will be expected to become the 3rd highest in 2025. Thus, Osaka can become a national leading model case for community pharmacists' activity in future home medical c...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Niki K, Takemura M, Kitagawa K, Shimizu R, Takahashi Y, Hatabu A, Uejima E Tags: Yakugaku Zasshi Source Type: research

[Survey of Description on Package Inserts of OTC Drugs].
In this study, we first checked whether the items, as required in the notifications of the Japanese Ministry of Health, Labour and Welfare, are described in the package inserts of cold remedies and analgesic antipyretics in OTC drugs. The descriptions of almost all packages checked in this study were based on the notifications, but those of a small number of them were not. Next, we examined the description of the items, unrequired in the notification, but worthy for proper use of drugs; e.g., the description of prohibition for use by "patients with severe hypertension" in case of ibuprofen-containing products, an...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - February 3, 2018 Category: Drugs & Pharmacology Authors: Shimauchi A, Naganuma M, Sasaoka S, Hatahira H, Motooka Y, Hasegawa S, Fukuda A, Nakao S, Sakai C, Yokoyama S, Ino Y, Nakamura M, Iguchi K Tags: Yakugaku Zasshi Source Type: research

[Quality evaluation of Saposhnikoviae Radix (Differences between wild-type and cultivated products)].
In this study, we compared the contents of the extract and the quantitative values of characteristic constituents obtained from wild-type and cultivated plants, and found a remarkable difference. Therefore, it is considered that these indicators play an important role in the establishment of better cultivation technology. PMID: 29386422 [PubMed - as supplied by publisher] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 30, 2018 Category: Drugs & Pharmacology Authors: Nishihara M, Nukui K, Osumi Y, Shiota H Tags: Yakugaku Zasshi Source Type: research

[Development of Plant Metabolomics and Medicinal Plant Genomics].
Abstract  A variety of chemicals produced by plants, often referred to as 'phytochemicals', have been used as medicines, food, fuels and industrial raw materials. Recent advances in the study of genomics and metabolomics in plant science have accelerated our understanding of the mechanisms, regulation and evolution of the biosynthesis of specialized plant products. We can now address such questions as how the metabolomic diversity of plants is originated at the levels of genome, and how we should apply this knowledge to drug discovery, industry and agriculture. Our research group has focused on metabolomics-b...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Saito K Tags: Yakugaku Zasshi Source Type: research

[Evaluation of the Safety of 2.0% Ganciclovir Eye Drops for Hospital Preparation].
Abstract  The concentration of ganciclovir eye drops for hospital preparation was changed from 0.5% to 2.0% at the Nagasaki University Hospital from March 2015. We investigated the incidence of side effects in 12 patients using 2.0% ganciclovir eye drops and evaluated the cytotoxicity of 2.0% ganciclovir eye drops using cultured rabbit corneal cells in vitro. As a side effect of 2.0% ganciclovir eye drops, three patients exhibited an early feeling of transient stimulation. The 2.0% ganciclovir eye drops did not demonstrate cell cytotoxicity for cultured corneal cells after 5 min, but did after 10 min. These f...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Nakagawa H, Matsumaru Y, Nose S, Sasaki H, Kitahara T Tags: Yakugaku Zasshi Source Type: research

[A Survey of the Adverse Effects and Influence of Concomitant Drugs for Methotrexate Intrathecal Administration].
We examined the patients who received MTX intrathecal administration at Fukuoka University Hospital from January 2013 to December 2014 with respect to the onset of side effects and combination therapy. MTX intrathecal administration was performed a total of 79 times in 27 patients. In five of these 27 patients, MTX intrathecal administration was performed twice a week, and hematotoxicity and non-hematotoxicity developed in two patients in whom ST was also administered. On the other hand, even if ST and/or PPI was administered, no side effects were observed in the patients administered levofolinate. PMID: 29311456 [Pub...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Uchiyama M, Ueno M, Takamatsu Y, Matsuo K, Imakyure O, Kamimura H Tags: Yakugaku Zasshi Source Type: research

[Intestinal Microbiota in Migrating Barn Swallows around Osaka].
In this study, we characterized the fecal bacterial community in barn swallow. Using 16S rRNA gene metagenomic sequencing analysis, we examined the presence and composition of potentially pathogenic bacteria in the fecal samples, which were collected during spring season from Osaka. The number (±S.D.) of total bacteria was approximately 2.1(±3.4)×108 per gram of feces. In most samples, the bacterial community composition was dominated by families, such as Enterobacteriaceae, Pseudomonadaceae, Mycoplasmataceae, Enterococcaceae, Streptococcaceae, and Alcaligenaceae. However, no relationship was found betw...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Kenzaka T, Kataoka K, Fujimitsu T, Tani K Tags: Yakugaku Zasshi Source Type: research

[Adverse Event Trends Associated with Over-the-counter Combination Cold Remedy: Data Mining of the Japanese Adverse Drug Event Report Database].
Abstract  OTC combination cold remedies are widely used in Japan. In the present study, we aimed to evaluate the adverse event profiles of OTC combination cold remedy based on the components using the Japanese Adverse Drug Event Report (JADER) database. The JADER database contained 430587 reports between April 2004 and November 2016. 1084 adverse events associated with the use of OTC combination cold remedy were reported. Reporting odds ratio (ROR) was used to detect safety signals. The ROR values for "skin and subcutaneous tissue disorders", "hepatobiliary disorders", and "immune sys...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Sasaoka S, Hatahira H, Hasegawa S, Motooka Y, Fukuda A, Naganuma M, Umetsu R, Nakao S, Shimauchi A, Ueda N, Hirade K, Iguchi K, Nakamura M Tags: Yakugaku Zasshi Source Type: research

[Low Continuity Rate of Sucroferric Oxyhydroxide among Japanese Hemodialysis Patients with High Phosphate Binder Pill Burden].
Abstract  This prospective observational study was conducted to evaluate the continuity, efficacy, and tolerability of sucroferric oxyhydroxide (SO) among hemodialysis (HD) patients who switched to SO from sevelamer hydrochloride (SH) or bixalomer (BX). Participants were 9 HD patients in Kaetsu Hospital who had been receiving more than 9 tablets/d of SH or BX and were switched to SO 750 mg/d. All the participants were men. Over a 6-month observational period, 6 of the 9 patients (67%) discontinued SO because of adverse events, including diarrhea, atheroma, and polycythemia. Although the diarrhea and atheroma ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Mitsuboshi S, Yamada H, Nagai K, Okajima H Tags: Yakugaku Zasshi Source Type: research

[Errata: Roles and Educational Effects of Clinical Case Studies in Home Medical Care].
PMID: 29311460 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Ohsawa T, Shimazoe T Tags: Yakugaku Zasshi Source Type: research

[Novel Methods for the Synthesis of Heterocycles Using Highly Reactive Spirocyclopropanes].
Abstract  This review describes our recent efforts to develop efficient methods for the synthesis of heterocyclic compounds, such as indoles and benzofurans, employing ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes, which were prepared by the reaction of 1,3-cyclohexanediones with sulfonium salts. Ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes with primary amines proceeded at room temperature to provide 2-substituted tetrahydroindol-4(5H)-ones in good to excellent yield. The obtained product was readily converted into a 2-substituted 4-hydroxyindole derivative. ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Nambu H Tags: Yakugaku Zasshi Source Type: research

[Development of Efficient Methods for Benzyne Generation].
Abstract  2-[(Neopentyl glycolato)boryl]phenyl triflates, readily synthesized from 2-iodophenol derivatives via halogen-magnesium exchange or Miyaura borylation, were developed as new benzyne precursors. Benzynes were generated under fluoride-ion-mediated conditions and reacted immediately with various arynophiles. Herein, we describe the generation of benzynes having reactive functional groups, such as methoxycarbonyl, acetyl, bromo, and amino groups, as well as their [4+2], (3+2), and [2+2] cycloaddition reactions which produce corresponding benzo-fused compounds. PMID: 29311462 [PubMed - in process] (...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Takagi A Tags: Yakugaku Zasshi Source Type: research

[Chemical Biology for Pharmaceutical Sciences (Development of Practical Chemical Biotechnology)].
PMID: 29311463 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Inokuma T, Sato S Tags: Yakugaku Zasshi Source Type: research

[Development and Application of Catalytic Tyrosine Modification].
Abstract  The chemical labeling of proteins with synthetic probes is a key technique used in chemical biology, protein-based therapy, and material science. Much of the chemical labeling of native proteins, however, depends on the labeling of lysine and cysteine residues. While those methods have significantly contributed to native protein labeling, alternative methods that can modify different amino acid residues are still required. Herein we report the development of a novel methodology of tyrosine labeling, inspired by the luminol chemiluminescence reaction. Tyrosine residues are often exposed on a protein'...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Sato S, Tsushima M, Nakamura K, Nakamura H Tags: Yakugaku Zasshi Source Type: research

[Amyloid-selective Photooxygenation toward Treatment for Amyloid Diseases].
Abstract  Amyloid proteins and peptides form aggregates which lead to amyloid diseases. For example, Alzheimer's disease-related amyloid β (Aβ) forms oligomers, protofibrils, and amyloid fibrils, which exhibit neurotoxicity. Controlling the aggregation and toxicity of Aβ would be a therapeutic strategy for the treatment of Alzheimer's disease. Recently, we have investigated an artificial oxygenative modification (chemical introduction of oxygen atoms) of amyloid proteins using a photocatalyst, which attenuated the aggregation potency and toxicity of these proteins. The oxygenation of Aβ1-4...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Taniguchi A Tags: Yakugaku Zasshi Source Type: research

[Elaboration of Pseudo-natural Products Using Artificial In Vitro Biosynthesis Systems].
Abstract  Peptidic natural products often consist of not only proteinogenic building blocks but also unique non-proteinogenic structures such as macrocyclic scaffolds and N-methylated backbones. Since such non-proteinogenic structures are important structural motifs that contribute to diverse bioactivity, we have proposed that peptides with non-proteinogenic structures should be attractive candidates as artificial bioactive peptides mimicking natural products, or so-called pseudo-natural products. We previously devised an engineered translation system for pseudo-natural peptides, referred to as the flexible i...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Goto Y Tags: Yakugaku Zasshi Source Type: research

[Linezolid-induced Apoptosis through Mitochondrial Damage and Role of Superoxide Dismutase-1 in Human Monocytic Cell Line U937].
The objective of this study was to examine whether the cytotoxicity of linezolid to eukaryotic cells was associated with mitochondrial dysfunction and apoptosis-like cell death in human leukemic monocyte lymphoma cell line U937. Apoptosis-like cell death was clearly observed when cells were incubated with linezolid, depending on the duration and linezolid concentration. Mitochondrial membrane potential of cells treated with linezolid collapsed in a short period of time, but the number of mitochondria did not decrease. Cytotoxicity of linezolid was relieved by the knockdown of superoxide dismutase-1 in U937 cells. On the ot...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Fujii S, Muraoka S, Miyamoto A, Sakurai K Tags: Yakugaku Zasshi Source Type: research

[Economic Evaluation of mFOLFOX6-based First-line Regimens for Unresectable Advanced or Recurrent Colorectal Cancer Using Clinical Decision Analysis].
Abstract  We evaluated four representative chemotherapy regimens for unresectable advanced or recurrent KRAS-wild type colorectal cancer: mFOLFOX6, mFOLFOX6+bevacizumab (Bmab), cetuximab (Cmab), or panitumumab (Pmab). We employed a decision analysis method in combination with clinical and economic evidence. The health outcomes of the regimens were analyzed on the basis of overall and progression-free survival. The data were drawn from the literature on randomized controlled clinical trials of the above-mentioned drugs. The total costs of the regimens were calculated on the basis of direct costs obtained from ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Shida T, Endo Y, Shiraishi T, Yoshioka T, Suzuki K, Kobayashi Y, Ono Y, Ito T, Inoue T Tags: Yakugaku Zasshi Source Type: research

[Sex Differences of the Inflammatory Mediator Level at the Time of Itch Onset in Patients with Chronic Venous Disease].
This study investigated the sex differences of the inflammatory mediator level at the time of itch onset in patients with chronic venous disease (CVD). Twenty-seven CVD patients (nineteen women, eight men) and nine healthy controls (five women, four men) participated. CVD-associated itching was observed in both men and women. Before sclerotherapy, both sexes had elevations in several itch-related mediators. Among these, women had significantly higher tryptase, whereas men had significantly higher β-endorphin and adrenocorticotropic hormone. After sclerotherapy, all levels normalized in both sexes. In this study, itchi...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - January 11, 2018 Category: Drugs & Pharmacology Authors: Takai Y, Hiramoto K, Nishimura Y, Ooi K Tags: Yakugaku Zasshi Source Type: research

[Rotational Isomers of Diphenhydramine].
Abstract   Diphenhydramine(DP), an antihistaminic agent, may become colored and daker or more fluorescent during storage. Herein, we spectroscopically examined the causes of this phenomenon under various DP storage conditions and durations. The infrared vibration-rotation spectrum shows multiple Gauche (G )-type conformers with different intramolecular n→π* interaction strengths. The splitting pattern of the dimethylamino group protons in the 1H-NMR spectrum indicates that DP is mainly in the G-type with a small portion in the Trans(T)-type. The correlation between the red-shifted peak intensity ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 27, 2017 Category: Drugs & Pharmacology Authors: Ebitani M, Ebitani T Tags: Yakugaku Zasshi Source Type: research

[Change Emergency Intensive Care!!Create and Disseminate Evidence That Contributes to Improving the Treatment of Critically Ill Patients].
PMID: 29199251 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Ishizawa K, Irie T Tags: Yakugaku Zasshi Source Type: research

[Evaluation of Pharmacotherapy on Emergency and Intensive Care Medicine: The Influence of Intensity and Duration of Invasion].
Abstract  Critically ill patients who receive high-level invasion show physiological changes different from those under more normal conditions, along with variable therapeutic effects and pharmacokinetics. The concept of systemic inflammatory response syndrome (SIRS) has been introduced to describe the clinical state resulting from invasive actions taken under acute circumstances, resulting in an acute-phase systemic response. In particular, dosages of vancomycin (VCM) and phenytoin (PHT) need to be adjusted by therapeutic drug monitoring (TDM) because of their narrow therapeutic concentration windows. Howeve...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Imai T Tags: Yakugaku Zasshi Source Type: research

[Effects of Pharmacist Intervention on the Treatment of Infectious Diseases in Critically Ill Patients].
Abstract  The pathological conditions of patients who require intensive care are usually complex and extremely severe; their health and life are in a critical state. Therefore, correct, rapid treatment of these conditions is indispensable. Furthermore, the selection of drugs and adjustment of their dosage for an immediate effect are important. Moreover, most patients are immunocompromised and present an extremely high level of risk for complications involving infectious diseases. Since such complications may lead to life-threatening outcomes, a rational dosage regimen to achieve sufficient antimicrobial activ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Imaura M Tags: Yakugaku Zasshi Source Type: research

[Drug Repositioning Research Utilizing a Large-scale Medical Claims Database to Improve Survival Rates after Cardiopulmonary Arrest].
Abstract  Approximately 100000 people suffer cardiopulmonary arrest in Japan every year, and the aging of society means that this number is expected to increase. Worldwide, approximately 100 million develop cardiac arrest annually, making it an international issue. Although survival has improved thanks to advances in cardiopulmonary resuscitation, there is a high rate of postresuscitation encephalopathy after the return of spontaneous circulation, and the proportion of patients who can return to normal life is extremely low. Treatment for postresuscitation encephalopathy is long term, and if sequelae persist ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Zamami Y, Niimura T, Takechi K, Imanishi M, Koyama T, Ishizawa K Tags: Yakugaku Zasshi Source Type: research

[Diversity of Secondary Metabolites from Some Medicinal Plants and Cultivated Lichen Mycobionts].
Abstract  Studies on the structural determination, biosynthesis, and biological activities of secondary metabolites from natural sources are significant in the field of natural products chemistry. This review focuses on diverse secondary metabolites isolated from medicinal plants and cultivated mycobionts of lichens in our laboratory. Monoterpene-tetrahydroisoquinoline glycosides and alkaloids isolated from Cephaelis acuminata and Alangium lamarckii gave important information on the biosynthesis of ipecac alkaloids. A variety of glycosides linked with a secologanin unit and indole alkaloids were obtained from...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Tanahashi T Tags: Yakugaku Zasshi Source Type: research

[Synthesis, Aggregation, Self-assembly, and Dynamic Properties of Helicene Oligomers].
Abstract  Biological systems exhibit dynamic phenomena at the macroscopic level as a result of the hierarchical integration of phenomena at the molecular level. For example, a number of amino acids compose actin proteins, which form three-dimensional structures determined by the sequence of amino acids. They form fibers by self-assembly, which then form ordered structures such as meshes, lyotropic liquid crystals (LCs), and bundles. The dynamic and reversible polymorphism between these nano- to centimeter-sized ordered structures is essential for biological functions such as cell division, contraction, and lo...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Saito N Tags: Yakugaku Zasshi Source Type: research

[Retinoic Acid Prevents Dendritic Cells from Inducing Novel Inflammatory T Cells That Produce Abundant Interleukin-13].
Abstract  Vitamin A (VA) plays critical roles in gut homeostasis. Dendritic cells in mesenteric lymph nodes (MLN-DCs) can metabolize VA to retinoic acid (RA), thereby inducing gut-tropic lymphocytes and enhancing peripheral differentiation of regulatory T cells expressing forkhead box P3. We found that MLN-DCs from VA-deficient mice induced a distinct inflammatory T helper type 2 (Th2)-cell subset that produced abundant interleukin-13 (IL-13) and expressed receptors for homing to skin and inflammatory sites but not to the intestine. IL-6-neutralizing antibodies or RA abrogated the induction of this subset. On...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Yokota-Nakatsuma A Tags: Yakugaku Zasshi Source Type: research

[Research on Insufficient Information for Pharmaceutical Products].
Abstract  Several issues concerning medicines remain unclear, including the availability of known, but not easily recognizable information. This review evaluates the mechanisms of side effects and the various risk indications included in package inserts. The results can be summarized as follows. 1) Short-term exposure to gatifloxacin significantly induced insulin secretion and increased the cytosolic Ca2+ concentration of islet cells by augmenting extracellular Ca2+ influx and its release from the endoplasmic reticulum. Alternatively, there was a decline in the cellular insulin level and reactivity to sulfony...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Tomita T Tags: Yakugaku Zasshi Source Type: research

[Development of Novel Functional Molecules Based on the Molecular Structure Characteristics of Diketopiperazines].
This article focuses on our investigation of the molecular structure characteristics of diketopiperazines (DKPs), and application of these findings to the development of novel functional molecules. DKPs bearing a benzyl moiety are known to adopt a folded conformation, in which the benzyl moiety is folded over the DKP ring. In order to investigate the driving force behind the folded conformation, we synthesized DKPs bearing a benzyl moiety with different para-substituents, and demonstrated that the folded conformation likely arose from intramolecular CH/π interactions, based on the electronic effects of para-substituents...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Nakao M Tags: Yakugaku Zasshi Source Type: research

[Implementation and Evaluation of Genetic Testing Seminars about Lifestyle-related Disease Prevention in Pharmacy Insurance-The Need for Cooperation between the Pharmacy and the University in Genetic Testing].
Abstract  A seminar titled "Implementation and evaluation of genetic testing of lifestyle-related disease genes" was held for pharmacists, medical clerks, and clerks of pharmacy insurance, with the aim of holding seminars led by pharmacists for the general public (including patients) in the future. The subject of the seminar was single nucleotide polymorphisms in obesity-related genes and alcohol metabolism-related genes. The purpose of the seminar was to contribute to the prevention of lifestyle-related diseases of the general public. We evaluated it by administering a questionnaire to the particip...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - December 5, 2017 Category: Drugs & Pharmacology Authors: Ikeda K, Kasuga M, Hosoi T, Yoshii M, Sugiyama M, Wako A, Ozawa K Tags: Yakugaku Zasshi Source Type: research

[Outcomes of Pharmaceutical Faculty-focused Introduction to Nursing Education for Pharmacy Students: A Questionnaire Survey].
In this study, we examined the effect of incorporating certain aspects of introductory nursing education into pharmaceutical education on the self-efficacy of pharmaceutical students. We thus ran an introduction to nursing education course for fourth-year pharmaceutical students (n=86). After the course had finished, we surveyed students about the course. Approximately 94.2% of the students became more interested in team medical care and nearly all (98.8%) thought that what they had learned in the course would be useful in their career. The results indicated that the introduction to nursing education course offered student...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 9, 2017 Category: Drugs & Pharmacology Authors: Majima T, Ohara H Tags: Yakugaku Zasshi Source Type: research

[Novel Anticancer Strategy Targeting Switch Mechanisms in Two Types of Cell Death: Necrosis and Apoptosis].
Abstract  Two types of cell death, necrosis and apoptosis, are defined in terms of cell death morphological features. We have been studying the mechanisms by which cell death processes are switched during the treatment of mouse tumor FM3A with anticancer, 5-fluoro-2'-deoxyuridine (FUdR): it induces original clone F28-7 to necrosis, but its sub-clone F28-7-A to apoptosis. We identified several such switch regulators of cell death: heat shock protein 90 (HSP90), lamin-B1, cytokeratin-19, and activating transcription factor 3 (ATF3), by using transcriptomic, proteomic analyses and siRNA screening. For example, t...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 4, 2017 Category: Drugs & Pharmacology Authors: Sato A Tags: Yakugaku Zasshi Source Type: research