著者
IKUO ADACHI TERUO YAMAMORI YOSHIHARU HIRAMATSU KATSUNORI SAKAI SHIN-ICHI MIHARA MASARU KAWAKAMI MASAO MASUI OSAMU UNO MOTOHIKO UEDA
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.36, no.11, pp.4389-4402, 1988-11-25 (Released:2011-02-08)
参考文献数
19
被引用文献数
31 49

A series of 4-aryl-4, 7-dihydrothieno [2, 3-b] pyridine-5-carboxylate derivatives (I) was synthesized and tested for binding affinity to Ca2+ channels in rat cerebral cortex membranes, coronary vasodilator effect in isolated guinea pig hearts, and antihypertensive activity in spontaneously hypertensive rats.Several compounds had potent coronary vasodilator and antihypertensive activities.The structure-ctivity relationships of the series indicated that a lipophilic 3-alkyl substituent with moderate bulkiness was effective for enhancing the pharmacological potencies.Among them, methyl 4, 7-dihydro-3-isobuty1-6-methy1-4-(3-nitrophenyl) thieno [2, 3-b] pyridine-5-carboxylate (S-312) was selected as a promising cardiovascular agent.The relationship between the absolute configuration of S-312 and its biological activities is also presented.
著者
HASHIGUCHI Masayuki WATANABE Eriko CHIYODA Takeshi IRIE Shin KUROKAWA Tatsuo MOCHIZUKI Mayumi
出版者
The Japanese Society of Clinical Pharmacology and Therapeutics
雑誌
臨床薬理 (ISSN:03881601)
巻号頁・発行日
vol.44, no.1, pp.29-36, 2013
被引用文献数
1

<b>Background:</b> Lifestyle-related diseases are increasing in Japan, and the national medical expenditure is increasing. Converting prescription drugs to over-the-ounter (OTC) drugs would appear to be one solution to cut expenditure. The willingness to pay (WTP) of the Japanese public for OTC imidapril, an angiotensin-converting enzyme (ACE) inhibitor, as a healthcare-related item has not been evaluated.<br><b>Objective:</b> To measure the value of OTC imidapril as a health care-related item by investigating the public's WTP as self-medication for primary prevention of stroke, assuming that ACE inhibitors are switched from prescription-only to OTC status.<br><b>Methods:</b> A questionnaire was distributed among healthy individuals engaged in various jobs in office buildings (including a clinic) in Tokyo and Fukuoka, Japan. For the WTP question format, the double-bound dichotomous choice approach was employed. Participants were randomly assigned to 3 groups. Group A was provided with a starting price per month of ¥6,000, group B with ¥8,000, and group C with ¥10,000. Weibull regression analysis was used to investigate factors affecting WTP.<br><b>Results:</b> The questionnaire survey was completed correctly by 311 individuals (156 men, mean age 50 years), and the mean WTP was ¥7,237 per month. Weibull regression analysis showed that gender significantly affected WTP. The bid acceptance rates differed among the age groups of 20-39 years, 40-64 years, and ≥65 years.<br><b>Conclusion:</b> The public's WTP amount was approximately ¥7,000 per month, and the WTP based on the questionnaire responses was about 20% lower than the present cost for physician visits. (Jpn J Clin Pharmacol Ther 2013; 44(1): 29-36)
著者
Tomoko Otsuka Yosuke Kuroiwa Kazunari Sato Kazunari Yamashita Tadashi Hakomori Shin-ichiro Kimura Yasunori Iwao Shigeru Itai
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.66, no.5, pp.554-561, 2018-05-01 (Released:2018-05-01)
参考文献数
24
被引用文献数
6

The properties of wet mass, which indicate the progress of high shear granulation processes, usually have an effect on final product properties, such as tablet dissolution. The mixer torque rheometer (MTR) is a useful tool for quantitatively measuring the ‘kneading state’ of wet mass and detecting differences in granules. However, there have been no studies of the relationship between the MTR torque and the final product properties to date. In this study, we measured the MTR torque of wet granules at different kneading states, which were prepared by changing the granulation conditions. We then evaluated the relationship between the MTR torque and the dissolution rate of the final product properties. The amperage of the high shear granulator is usually monitored during granulation, but we could not detect a difference in the kneading state through the amperage. However, using MTR torque we were able to quantify the difference of the wet mass. Moreover, MTR torque showed a high correlation with dissolution, compared with the correlations with other intermediate properties, such as granules particle size and tablet hardness. These other properties are affected by following processes and are not properties that directly relate to the kneading state. Thus, MTR torque is a property of wet mass after granulation, and it can be used to directly evaluate differences of the kneading state, and as a result, dissolution. These results indicate the importance of controlling the kneading state, i.e., the progress of granulation, and the utility of MTR for detecting differences in wet mass.
著者
Kwon Hak Cheol Jung Chil Mann Shin Cha Gyun LEE Jong Kyo CHOI Sang Un KIM Sun Yeou LEE Kang Ro
出版者
公益社団法人日本薬学会
雑誌
Chemical & pharmaceutical bulletin (ISSN:00092363)
巻号頁・発行日
vol.48, no.11, pp.1796-1798, 2000-11-01
参考文献数
17
被引用文献数
5

The phytochemical study of the aerial parts of Aster scaber THUNB. (Asteraceae) yielded a new caffeoyl quinic acid, (-) 3,5-dicaffeoyl-muco-quinic acid (2) and three known compounds, (-) 3,5-dicaffeoyl quinic acid (1), (-) 4,5-dicaffeoyl quinic acid (3), (-) 5-caffeoyl quinic acid (4). The structures were established by high resolution spectroscopic methods. The antiviral effects against HIV-1 integrase of the compounds was evaluated. (-) 3,5-Dicaffeoyl-muco-quinic acid (2) exhibited potent antiviral activity with an IC_<50> value of 7.0±1.3 μg/ml.
著者
平島 真一 多田 教浩 三浦 剛 伊藤 彰近 ヒラシマ シンイチ タダ ノリヒロ ミウラ ツヨシ イトウ アキチカ Shin-ichi HIRASHIMA Norihiro TADA Tsuyoshi MIURA Akichika ITOH
雑誌
岐阜薬科大学紀要 = The annual proceedings of Gifu Pharmaceutical University
巻号頁・発行日
vol.60, pp.1-9, 2011-06-30

酸化反応は有機合成における最も重要な柱の一つである。しかしながら、従来の酸化反応は重金属を大量に使用しなければならない、廃棄物が大量に副生するなどの問題点を有しており、いわゆる“グリーンケミストリー”の概念に必ずしもそぐわないものがほとんどであった。一方、最近では安価で原子効率が高い分子状酸素を酸化剤として用いた触媒的酸化反応が報告されている。この方法は適当な触媒を用いた場合に、反応後に副生されるものが理論的に水のみであり、理想の酸化反応として注目を集めている。係る背景において、筆者らは分子状酸素を用いる酸化反応について研究を行い、紫外光照射下(<400 nm)、HBrやBr2のような触媒量の臭素源存在下、芳香環上メチル基やアルコール類から対応するカルボン酸への酸化反応の開発に成功した。また、臭素源として触媒量のMgBr2を用いることにより可視光照射下(>400 nm)でも同様の酸化反応が進行することも見出した。さらに、上記の光酸素酸化反応を連続するエステル化反応へ展開し、芳香環上メチル基から芳香族カルボン酸エステルへの効率的な直接一段階合成法を確立することにも成功した。
著者
Komatsu Yoshito Ishioka Chikashi Shimada Ken Yamada Yasuhide Gamoh Makio Sato Atsushi Yamaguchi Tatsuro Yuki Satoshi Morita Satoshi Takahashi Shin Goto Rei Kurihara Minoru
出版者
BioMed Central Ltd.
雑誌
BMC Cancer (ISSN:14712407)
巻号頁・発行日
vol.15, 2015-09-09
被引用文献数
13

Background: Metastatic colorectal cancer carries a poor prognosis and cannot be cured by currently available therapy. Chemotherapy designed to prolong survival and improve the quality of life (QOL) of patients is the mainstay of treatment. Standard regimens of FOLFOX/bevacizumab and CapeOX/bevacizumab can cause neurotoxicity, potentially disrupting treatment. The results of 3 phase II studies of combination therapy with S-1, irinotecan, and bevacizumab showed comparable efficacy to mFOLFOX6/bevacizumab and CapeOX/bevacizumab, without severe neurotoxicity. Therefore, the establishment and evaluation of S-1-containing irinotecan-based regimens for first-line treatment are expected to become more important. Methods: The TRICOLORE trial is a multicenter, randomized, open-label, controlled phase III study which aims to evaluate the non-inferiority of combination therapy with S-1/irinotecan/bevacizumab (a 3-week regimen [SIRB] or 4-week regimen [IRIS/bevacizumab]) to oxaliplatin-based standard treatment (mFOLFOX6/bevacizumab or CapeOX/bevacizumab) in patients with metastatic colorectal cancer who had not previously received chemotherapy. Patients will be randomly assigned to either the control group (mFOLFOX6/bevacizumab or CapeOX/bevacizumab) or study group (SIRB or IRIS/bevacizumab). The target sample size is 450 patients. The primary endpoint is progression-free survival (PFS), and the secondary endpoints are overall survival (OS), response rate (RR), time to treatment failure (TTF), relative dose intensity (RDI), the incidence and severity of adverse events, quality of life (QOL), quality-adjusted life years (QALY), health care costs, and relations between biomarkers and treatment response (translational research, TR). Discussion: The results of this study will provide important information that will help to improve the therapeutic strategy for metastatic colorectal cancer, and we believe that this study is very meaningful from the perspective of comparative effectiveness research. Trial registration:UMIN000007834
著者
Yukie Narasaki Yumiko Obayashi Sayami Ito Shoko Murakami Jun-Young Song Kei Nakayama Shin-Ichi Kitamura
出版者
The Japanese Society of Fish Pathology
雑誌
魚病研究 (ISSN:0388788X)
巻号頁・発行日
vol.53, no.1, pp.1-9, 2018 (Released:2018-04-03)
参考文献数
36
被引用文献数
3

Miamiensis avidus is the causative agent of scuticociliatosis in various marine fish species. The virulence factors of the parasite have not been identified, so far. In this study, we examined M. avidus extracellular proteinases (ECPs) as potential virulence factors, using culture supernatants as an ECPs source. We investigated the substrate specificity of ECPs using artificial peptides, and the cytotoxicity of the ECPs was examined using CHSE-214 cells. To elucidate the role of ECPs in ciliate growth, M. avidus was cultured on CHSE-214 cells in the presence of proteinase inhibitors. We detected proteinase activities from the supernatant of M. avidus. Viable CHSE-214 cells decreased significantly in number, when incubated in a medium supplemented with the culture supernatant of M. avidus. The growth of ciliates on CHSE-214 cells was delayed in the presence of PMSF (serine proteinase inhibitor) and E-64 (cysteine proteinase inhibitor). These results suggested that the culture supernatant contained ECPs showing cytotoxicity, and the proteinases facilitated nutrient uptake by the ciliates. Thus, ECPs may be responsible for virulence factors of M. avidus.
著者
Suk Pyo Shin Yoon Mi Choi Won Hee Kim Sung Pyo Hong Jong-Min Park Joohee Kim Oran Kwon Eun Hyun Lee Ki Baik Hahm
出版者
SOCIETY FOR FREE RADICAL RESEARCH JAPAN
雑誌
Journal of Clinical Biochemistry and Nutrition (ISSN:09120009)
巻号頁・発行日
vol.62, no.2, pp.179-186, 2018 (Released:2018-03-01)
参考文献数
41
被引用文献数
37

The exact pathogenesis of diarrhea-dominant irritable bowel syndrome (IBS) is not known, but the abnormal microbiota of the gastrointestinal tract is considered to be one of the important contributing factors as in other gastrointestinal diseases such as inflammatory bowel disease, antibiotic-associated diarrhea, and colorectal cancer as well as systemic diseases. Though diverse trials of probiotics had been continued in the treatment of diarrhea-IBS, only a few proved by randomized clinical trial. To prove the efficacy of Lactobacillus gasseri BNR17 isolated from breast milk in patients with diarrhea-IBS, prospective, randomized, placebo controlled clinical trial was done including health related-quality of life analysis, colon transit time, and the changes of fecal microbiota. BNR17 significantly improved the symptoms of diarrhea compared to control group. Health related-QOL analysis showed significant improvement of abdominal pain, distension, disturbed daily life, and mean defecation frequency with BNR17. On comparative CTT before and after BNR17, 6 out of 24 subjects showed significant correction of rapid colon transit pattern, while only 2 out of 24 in placebo (p<0.01). Upon fecal microbiota analysis, BNR17 significantly increased B. fecalis, E. rectale, C. aerofaciens, F. prausnitzil and B. steroris. Conclusively, Lactobacillus gasseri BNR17 can be a potential probiotics to ameliorate diarrhea-IBS.
著者
Ryuichi Suwa Hironori Tajima Shinichi Gima Naoko Uehara Kenta Watanabe Shin Yabuta Jun Tominaga Yoshinobu Kawamitsu
出版者
The Japanese Society for Horticultural Science
雑誌
The Horticulture Journal (ISSN:21890102)
巻号頁・発行日
pp.OKD-069, (Released:2018-03-13)
被引用文献数
8

In Japan, several plant species have high commercial value because of their functional properties. In this study, we aimed to investigate the effects of soil type (red, dark-red, and gray soil) and growth stage (vegetative and reproductive) on the growth and polyphenol production (chlorogenic acid, rutin, hesperidin, and diosmin) of P. japonicum. Plants grown in gray soil had the heaviest dry weight, followed by those grown in dark-red soil. Flowering plants grown in gray soil had a polyphenol concentration lower than those grown in the other two soil types. However, differences in the concentration of polyphenols were even larger between the growth stages. During the flowering period, the concentration of polyphenols sharply increased in the stems. Additionally, the flowers contained relatively similar amounts of polyphenols to stems and leaves, accounting for approximately 1/4–1/2 of the net amount in the plant.
著者
Shin Terada Seiji Sekine Toshiaki Aoyama
出版者
Japan Oil Chemists' Society
雑誌
Journal of Oleo Science (ISSN:13458957)
巻号頁・発行日
vol.64, no.6, pp.683-688, 2015 (Released:2015-06-01)
参考文献数
20
被引用文献数
3 15

We examined the effects of the dietary intake of medium- and long-chain triacylglycerol (MLCT) on hyperglycemia in diabetic ob/ob mice. Six-week-old male ob/ob mice were fed a diet containing longchain triacylglycerol (LCT) or MLCT for 3 wks. During the dietary treatment, we determined the plasma glucose and insulin concentrations in the fed state once a week. Whereas the body weights did not differ between the two groups, the total intra-abdominal fat mass was significantly higher in the MLCT group compared to the LCT group. The plasma glucose levels in the freely fed state gradually increased during the 3-wk dietary treatment in the LCT but not MLCT group, although the daily food intake did not differ between the two groups. In the fed state, the MLCT group’s plasma glucose was significantly lower and their insulin concentrations were significantly higher than those observed in the LCT group (p<0.01). Plasma glucose concentrations at the end of dietary treatment (3rd wk) were negatively correlated with plasma insulin concentrations (p<0.05) and tended to be inversely related to total intra-abdominal fat mass (p=0.08). These results suggest that the dietary intake of MLCT may delay the progression of hyperglycemia in ob/ob mice, possibly through the stimulation of glucose uptake in intra-abdominal fat tissue caused by enhanced insulin secretion.
著者
浦田 悠 槇 姫宰 岩居 弘樹 Shin Heejae Urata Yu Iwai Hiroki
出版者
大阪大学全学教育推進機構
雑誌
大阪大学高等教育研究 = Osaka University higher education studies (ISSN:21876002)
巻号頁・発行日
no.5, pp.87-96, 2017

Attention toward active learning and usage of information and communication technology (ICT) is becoming more substantial in higher education. Hence, a new learning space to realize and establish such education environment is undertaken. The highly flexible spaces are developed to adopt today's diverse learning styles. However, the standard to rate more objective quality needs to be practiced in Japan. In this study, Learning Space Rating System (LSRS), developed for measuring the quality of learning spaces, has been translated into Japanese.
著者
福島 紳 中村 強 Shin FUKUSHIMA Tsuyoshi NAKAMURA
雑誌
南極資料 (ISSN:00857289)
巻号頁・発行日
vol.11, pp.885-893, 1961-01

The third latitude survey in cosmic-ray neutrons has been carried out along the same ship-route and by using the same apparatus as in the preceeding two surveys. Although the observation room was the same as that in the second survey, one additional room was constructed over our room. Thus, as observational conditions in the three latitude surveys are different from one another, the obtained results could not be compared in absolute intensity but in relative. The periods during which each survey was performed are represented with the corresponding sunspot relative numbers in Fig. 1, where a full curve shows the 12 months running average of monthly mean values in sunspot numbers. Fig. 2 shows 12 hour mean values for each latitude curve in the southern hemisphere. It is seen from the figure that the slope of latitude curve becomes gentle at the second survey and then almost recovers at the third. To explain such changes in primary cosmic-rays by terms of changes in solar activity represented by sunspot numbers as shown in Fig. 1, we suppose a hysteresis effect of solar activity upon cosmic-rays. In other words, changes in cosmic-rays do not immediately follow that in solar activity but about half a year later.
著者
福島 紳 小玉 正弘 宮崎 友喜雄 Shin FUKUSHIMA Masahiro KODAMA Yukio MIYAZAKI
雑誌
南極資料 (ISSN:00857289)
巻号頁・発行日
vol.11, pp.894-898, 1961-01

当初,南極観測用に製作された宇宙線中性子観測装置は,IGY用として設計されたもので,全体の重量が6トンを超えるため,ヘリコプター輸送に適さない.そこで重量軽減化の方法として,(1)ニュートロン減速剤として,パラフィンの代りに現地の海水を利用する.(2)真空管方式の増幅,計数装流をすべてトランジスター化する.の2点から,新しい観測装置を製作した.この装置は重量約500kgで,第4次観測隊により無事基地へ空輪された.観測は1960年3月3日より開始された.観測結果の一部として,日平均値の変化及び5月4日の宇宙線異常増加の結果を示した.