著者

野曽原 紗綾 Saaya Nosohara

出版者

東京音楽大学

雑誌

東京音楽大学大学院博士後期課程 2019年度博士共同研究A報告書 : 《オリンピックと音楽》 = Class Essays from Doctoral Cooperative Research Seminar A, 2019 : The Olympics and music

巻号頁・発行日

pp.61-74, 2020-03-31

著者

Kazunori Miwa Yan Guo Masayuki Hata Norio Yamamoto Tyuji Hoshino

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.71, no.5, pp.360-367, 2023-05-01 (Released:2023-05-01)

参考文献数

39

被引用文献数

4

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Computational screening is one of the fundamental techniques in drug discovery. Each compound in a chemical database is bound to the target protein in virtual, and candidate compounds are selected from the binding scores. In this work, we carried out combinational computation of docking simulation to generate binding poses and molecular mechanics calculation to estimate binding scores. The coronavirus infectious disease has spread worldwide, and effective chemotherapy is strongly required. The viral 3-chymotrypsin-like (3CL) protease is a good target of low molecular-weight inhibitors. Hence, computational screening was performed to search for inhibitory compounds acting on the 3CL protease. As a preliminary assessment of the performance of this approach, we used 51 compounds for which inhibitory activity had already been confirmed. Docking simulations and molecular mechanics calculations were performed to evaluate binding scores. The preliminary evaluation suggested that our approach successfully selected the inhibitory compounds identified by the experiments. The same approach was applied to 8820 compounds in a database consisting of approved and investigational chemicals. Hence, docking simulations, molecular mechanics calculations, and re-evaluation of binding scores including solvation effects were performed, and the top 200 poses were selected as candidates for experimental assays. Consequently, 25 compounds were chosen for in vitro measurement of the enzymatic inhibitory activity. From the enzymatic assay, 5 compounds were identified to have inhibitory activities against the 3CL protease. The present work demonstrated the feasibility of a combination of docking simulation and molecular mechanics calculation for practical use in computational virtual screening.

著者

戸田巌

雑誌

情報処理

巻号頁・発行日

vol.51, no.2, pp.219-220, 2010-02-15

著者

Stella Amarachi Ihim Yukiko K. Kaneko Moe Yamamoto Momoka Yamaguchi Toshihide Kimura Tomohisa Ishikawa

出版者

The Pharmaceutical Society of Japan

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.46, no.4, pp.630-635, 2023-04-01 (Released:2023-04-01)

参考文献数

31

被引用文献数

2

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The improvement of type 2 diabetes mellitus induced by naturally occurring polyphenols, known as flavonoids, has received considerable attention. However, there is a dearth of information regarding the effect of the trihydroxyflavone apigenin on pancreatic β-cell function. In the present study, the anti-diabetic effect of apigenin on pancreatic β-cell insulin secretion, apoptosis, and the mechanism underlying its anti-diabetic effects, were investigated in the INS-ID β-cell line. The results showed that apigenin concentration-dependently facilitated 11.1-mM glucose-induced insulin secretion, which peaked at 30 µM. Apigenin also concentration-dependently inhibited the expression of endoplasmic reticulum (ER) stress signaling proteins, CCAAT/enhancer binding protein (C/EBP) homologous protein (CHOP) and cleaved caspase-3, which was elevated by thapsigargin in INS-1D cells, with peak suppression at 30 µM. This was strongly correlated with the results of flow cytometric analysis of annexin V/propidium iodide (PI) staining and DNA fragmentation analysis. Moreover, the increased expression of thioredoxin-interacting protein (TXNIP) induced by thapsigargin was remarkably reduced by apigenin in a concentration-dependent manner. These results suggest that apigenin is an attractive candidate with remarkable and potent anti-diabetic effects on β-cells, which are mediated by facilitating glucose-stimulated insulin secretion and preventing ER stress-mediated β-cell apoptosis, the latter of which may be possibly mediated by reduced expression of CHOP and TXNIP, thereby promoting β-cell survival and function.

著者

Hiroko Shibata Kazuko Nishimura Yoshiro Saito Akiko Ishii-Watabe

出版者

The Pharmaceutical Society of Japan

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.46, no.4, pp.621-629, 2023-04-01 (Released:2023-04-01)

参考文献数

13

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Monitoring serum infliximab (INF) concentrations is crucial for designing appropriate doses for patients with rheumatoid arthritis. It is recommended to maintain the serum trough INF level at least 1.0 µg/mL. In Japan, an in vitro diagnostic kit using immunochromatography has been approved to determine whether the serum INF concentration is over 1.0 µg/mL or not, and to support the determination of the necessity of increasing the dose or switching to another drug. Biosimilars (BS) of INF may have immunochemical properties different from those of its innovator product, which may show different reactivities on the diagnostic kit. In this study, the responses of the innovator and five BS products on the kit were compared. Based on visually comparing the intensity of color development between the test and control samples, differences were found in the judgment results depending on the analyst. In particular, 1.0 µg/mL was not determined as positive in some cases, whereas 2.0 µg/mL was reliably determined as positive. Overall, no significant difference in reactivity was found between the innovator and five BS products. To further compare the differences in immunochemical properties, the reactivity of these products with three enzyme-linked immunosorbent assay (ELISA) kits was compared. The results confirmed that there were no significant differences among the innovator and BS products in reactivity with the examined kits. When using that diagnostic kit, the users need to be aware that the judgement around 1.0 µg/mL INF may differ depending on the test conditions, including the analyst.

著者

上市 秀雄 関沢 洋一

出版者

公益社団法人 日本心理学会

雑誌

日本心理学会大会発表論文集 日本心理学会第78回大会 (ISSN:24337609)

巻号頁・発行日

pp.2AM-1-097, 2014-09-10 (Released:2021-03-30)

出版者

一般社団法人電子情報通信学会

雑誌

情報・システムソサイエティ誌 (ISSN:21899797)

巻号頁・発行日

vol.28, no.1, pp.1, 2023-05-01 (Released:2023-05-01)

著者

井宮 淳

出版者

一般社団法人電子情報通信学会

雑誌

情報・システムソサイエティ誌 (ISSN:21899797)

巻号頁・発行日

vol.28, no.1, pp.3-4, 2023-05-01 (Released:2023-05-01)

著者

井上 一稔

雑誌

美術研究 = The bijutsu kenkyu : the journal of art studies

巻号頁・発行日

no.343, pp.1-18, 1989-02-28

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Among various iconographical forms of Amitābhā, crowned Amitābhā images are classified into 1) the main image of Jōgyōdō hall at an Esoteric Buddhist temple, 2) Amitābhā of guhari colour and 3) others. The second type was painted and sculpted. While the painted images hold a crown on dressed hair, the carved ones hold a crown on curled hair, the latter being the theme of the present paper. Painted examples are all later than the Kamakura Period and the carved examples are almost exclusively from the mid-Heian Period (the tenth and eleventh centuries). Thus, it seems unnatural to the author to include both painted and carved works in the single category of “Amitābhā of guhari colour”. This is the starting point of his discussion. The author tried to find the Esoteric Buddhist significance of the carved images of “Amitābhā of guhari colour” in their iconographical characteristics, namely, the existence of the crown and their mudrā known as jōin. He was led to an idea that Chin-kang-ting-ching-kuan-tzü-tsai-wang-ju-lai-hsiuhsing-fa translated into Chinese by Amoghavajra, Chin-kang-ting-ching-yü-ch'ieh-kuan-tzŭ-tasi-wang-ju-laihsiu-hsing-fa translated by Vajrabodhi and Chingkang-ting-yü-ch’ieh-ch'ing-ching-ta-pei-wang-kuantzŭ-tsai-nien-sung-i-kuei by the same translator are the basis of the notion. These writings describe the process that perfected Buddhist devotees who perform a certain kind of meditation with the aim of spiritual incorporation with Amitābhā are finally given a crown in the vision. The author theorizes that the iconography is the sculptur tion of the imagery of Amitābhā thus considered to be attained by this kind of meditation.

著者

Wei HAN Muhan LI Mengyi YANG Si CHEN Yuanyuan LU Tiantian TANG Rui WANG Chenguang ZHANG Kemin QI

出版者

Center for Academic Publications Japan

雑誌

Journal of Nutritional Science and Vitaminology (ISSN:03014800)

巻号頁・発行日

vol.69, no.2, pp.105-120, 2023-04-30 (Released:2023-04-30)

参考文献数

66

被引用文献数

4

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The effects of folic acid on body weight gain in obesity and gut microbiota-associated branched-chain amino acids (BCAAs) and mitochondrial function were investigated. Three- to four-wk-old male C57BL/6J conventional (CV) and germ-free (GF) mice were fed a high-fat diet (HD), folic acid-supplemented HD (FSHD) and a normal-fat diet (ND) for 25 wk. In CV mice, the HD-induced increases in body weight and plasma BCAA concentrations, downregulated expression of genes related to BCAA catabolism (Bcat2, Bckdha, or Ppm1k), mitochondrial biogenesis (Pgc-1α, Cox1, Nd1 or Nd6), fusion (Mfn1, Mfn2 or Opa1) and mitophagy (Pink1 or Park2), and upregulated expression of the fission-associated gene Drp1 in epididymal fat were reversely corrected with FSHD feeding. In contrast, the expression of these genes in the liver was the opposite under HD feeding or folic acid supplementation. In GF mice, plasma BCAA concentrations were much less affected by HD feeding and were reduced by FSHD feeding, with almost no alterations in the expression of genes associated with BCAA catabolism and mitochondrial function. Further analysis indicated a correlation between adipose and hepatic Mt C/N and plasma BCAA concentrations, and the latter had a close association with specific gut bacteria. Therefore, dietary folic acid supplementation differentially affected body weight gain, BCAA catabolism, and mitochondrial dynamics and metabolism under HD feeding between CV and GF mice, suggesting that gut bacteria-altered BCAAs and mitochondria might partially share the responsibility for the beneficial effects of dietary folic acid on obesity.

著者

Seiya Ohki Shingo Ogawa Hiroki Takano Hayato Shimazaki Momoka Fukae Tomomi Furihata Hiromi Shibasaki Akitomo Yokokawa

出版者

The Pharmaceutical Society of Japan

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.46, no.5, pp.736-740, 2023-05-01 (Released:2023-05-01)

参考文献数

22

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The method of administering caffeine as a probe to evaluate the phenotypic activity of the CYP1A2, has not yet been applied clinically. In contrast, if endogenous melatonin (MEL) metabolism can be used to assess CYP1A2 activity, it could be a simple method that does not require substance administration. The study aim was to calculate the MEL partial metabolic clearance (CLm(MEL)) from plasma MEL and its urinary metabolites and to test the potential of this approach as a novel CYP1A2 phenotyping method. Nine subjects were included in the study; 3 had 6 blood and 4 urine samples collected between 10:00 and 18:00 (collectively, the intraday sample). Nine subjects had 3 blood samples and 2-h urine samples collected between 10:00 and 12:00 once a week for 3 weeks (interday sample). The CLm(MEL) was calculated from the plasma area under the curve (AUC) of MEL (AUCMEL) and urinary MEL metabolites excretion (X6MEL). Among the intraday samples, the AUCMEL ranged from 6.45–13.17 pmol·h/L and X6MEL ranged from 0.204–0.899 nmol/2 h, showing a decrease in concentration over time. In contrast, the CLm(MEL) ranged from 30.52–69.57 L/h (within-individual percent relative standard deviation: 9.2–20.1%), showing no time-dependent variation. Large interindividual variability was observed in AUCMEL and X6MEL in the interday sample, but CLm(MEL) showed small interindividual variabilities. The CLm(MEL) was 1.8-fold higher for smokers than for nonsmokers. The results obtained in this study may be valuable in future studies of evaluating novel CYP1A2 phenotyping method.

著者

金 京南

出版者

Japanese Association of Indian and Buddhist Studies

雑誌

印度學佛教學研究 (ISSN:00194344)

巻号頁・発行日

vol.55, no.2, pp.945-942,1280, 2007-03-20 (Released:2010-07-01)

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As is well-known, the Six Characteristics (六相), originating from the Dasabhumika-sutra (DBh), are used as the method of annotation in the DBhV. The purpose of this paper is to clarify the interpretation of the Six Characteristics in the DBhV, specifically focusing on the Fifth Characteristic (vivarta,成相) and the Sixth Characteristic (samvarta, 壊相)by comparing a Tibetan version with a Chinese version.We can find a transfiguration between the equivalent Tibetan and Chinese versions. That is, vivarta and samvarta are translated as 'du ba (to assemble) and rgyas pa (to spread) in the Tibetan version, whereas vivarta translates as evolution(成相) and samvarta translates as destruction (壊相)in the Chinese version. This transfiguration brings a difference in interpretation of vivarta and samvarta in commentaries of the DBhV. Furthermore, misinterpretations of vivarta and samvarta can be seen in current studies of the Six Characteristics due to a use of both versions but a lack of consideration regarding the aforementioned transfiguration.

著者

Yoji Kyotani Jing Zhao Kiichi Nakahira Masanori Yoshizumi

出版者

The Pharmaceutical Society of Japan

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.46, no.5, pp.655-660, 2023-05-01 (Released:2023-05-01)

参考文献数

36

被引用文献数

1

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Appendicitis is one of the most common abdominal surgical emergencies worldwide; however, its causes remain poorly understood. The Japanese Adverse Drug Event Report (JADER) database is a spontaneous reporting system (SRS) that can be utilized to analyze the safety signals of adverse events. In this study, we investigated the association between drug use and the onset of appendicitis using the JADER database. We first used the reporting odds ratio (ROR) as the signal and found signals for appendicitis, perforated appendicitis, and complicated appendicitis for 23, 9, and 1 drug, respectively. To investigate the level of hazard over time in drug-associated appendicitis, the Weibull shape parameter β was calculated using a Weibull plot, which revealed drug-dependent patterns for changes in the risk of appendicitis over time for the eight drugs. Furthermore, logistic regression analysis was performed to account for the influence of age, sex, and primary disease, and a significant association was detected between two drugs and appendicitis. Several types of drugs, such as antitumor, antirheumatic, and anti-inflammatory drugs, were included in our analyses; however, only clozapine, which is used for patients with schizophrenia, was commonly identified in these analyses. The resulting data suggest that certain drugs may be associated with appendicitis and may require adequate attention.

著者

Masahiko Imai Tomohiro Izumisawa Daisuke Saito Shinya Hasegawa Masahiro Yamasaki Noriko Takahashi

出版者

The Pharmaceutical Society of Japan

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.46, no.5, pp.661-671, 2023-05-01 (Released:2023-05-01)

参考文献数

21

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Myelosuppression, a side effect of anticancer drugs, makes people more susceptible to infectious diseases by compromising the immune system. When a cancer patient develops a contagious disease, treatment with an anticancer drug is suspended or postponed to treat the infectious disease. If there was a drug that suppresses the growth of cancer cells among antibacterial agents, it would be possible to treat both infectious diseases and cancer. Therefore, this study investigated the effect of antibacterial agents on cancer cell development. Vancomycin (VAN) had little effect on cell proliferation against the breast cancer cell, MCF-7, prostate cancer cell, PC-3, and gallbladder cancer cell, NOZ C-1. Alternatively, Teicoplanin (TEIC) and Daptomycin (DAP) promoted the growth of some cancer cells. In contrast, Linezolid (LZD) suppressed the proliferation of MCF-7, PC-3, and NOZ C-1 cells. Therefore, we found a drug that affects the growth of cancer cells among antibacterial agents. Next, when we examined the effects of the combined use of existing anticancer and antibacterial agents, we found VAN did not affect the growth suppression by anticancer agents. However, TEIC and DAP attenuated the growth suppression of anticancer agents. In contrast, LZD additively enhanced the growth suppression by Docetaxel in PC-3 cells. Furthermore, we showed that LZD inhibits cancer cell growth by mechanisms that involve phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) pathway suppression. Therefore, LZD might simultaneously treat cancer and infectious diseases.

著者

久内清孝

出版者

植物研究雑誌編集委員会

雑誌

植物研究雑誌 (ISSN:00222062)

巻号頁・発行日

vol.10, no.4, pp.250-251, 1934-04-25 (Released:2023-04-05)

著者

中島 利博 川原 幸一 西 順一郎 三浦 直樹

出版者

東京医科大学

雑誌

基盤研究(B)

巻号頁・発行日

2016

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キルギスではRheumatic fever : (以下、RF)が未だに猛威を奮っている。さらに、顕在化しないRFの後遺症も含めたRheumatic heart diseases(以下、RHD)が食生活(肉食、ウオッカ)、環境因子(低酸素)と併せて当該地域での死因の過半数を占める60歳までの心不全の潜在的リスクファクターであることを報告していた。10年を超える継続的な医療支援によりキルギスのほぼ全土を網羅する詳細なフィールド調査を行い、RF/RHDの有無、心エコーなど理学的所見、溶連菌など細菌感染症の頻度、家族歴など2000人を超える住民から100を超える項目に関する調査を完遂していた。その結果より、溶連菌以外の細菌感染の陽性率も高く、その一因に未だに主流であるバイオマス燃料による粘膜免疫の低下が考えられることを見出した。呼吸器分野の専門家を加え、感染の遷延化・慢性化に対する宿主因子の探索を行った。さらに細菌感染に対する啓蒙活動を行いその効果を検討した。キルギスの食生活について循環器疾患や免疫に対する影響を検討するため生理活性を測定した。その結果キルギスの特産として知られるある食物が本国のものと比較して血管内皮細胞に対して高い抗酸化作用を有していることが示唆された。上記の成分を分析しRF/RHDの予防として活用できるのではないかと期待できる。啓蒙活動についてはロシア語に加えてもう一つの公用語であるキルギス語の母子手帳を作成し、現地JICAを通して国民に配布を開始した。また名誉領事会議において本活動の重要性をキルギス政府に対しても働きかけを行った。既に配布済みであるロシア語が広く使われている都市部においてはRF/RHDの減少が認められることからその効果が期待される。

著者

Yukiko K. Kaneko

出版者

The Pharmaceutical Society of Japan

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.46, no.5, pp.640-646, 2023-05-01 (Released:2023-05-01)

参考文献数

47

被引用文献数

1

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Although diabetes is associated with an increased risk of various diseases, including cancer and infectious diseases, no definitive cure has yet been found. Long-term treatment for blood glucose control significantly reduces the QOL. Pancreatic β-cells are the only cells that can lower blood glucose levels by secreting insulin. Therefore, maintaining insulin-secreting β-cells is crucial in preventing the progression of diabetes and improving the QOL. We have investigated the mechanisms for the regulation of insulin secretion, the prevention of β-cell apoptosis, and the increase in β-cell mass. In particular, we have elucidated the involvement of type I diacylglycerol kinase (DGK) in the regulation of insulin secretion and the effects of nitric oxide (NO) signaling and natural products in suppressing β-cell death. In addition, we have elucidated the function of DGKδ as a suppressor of β-cell proliferation. This review introduces the findings of our study leading to development of novel anti-diabetic therapeutics that targets pancreatic β-cells.

著者

関根 禎嘉

出版者

一般社団法人 情報科学技術協会

雑誌

情報の科学と技術 (ISSN:09133801)

巻号頁・発行日

vol.73, no.5, pp.169-175, 2023-05-01 (Released:2023-05-01)

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テレビ放送番組のアーカイブ利用のためのメタデータモデル構築を行う。「番組」は放送されるコンテンツを指す基礎的な用語でありながら,その範囲について明確な定義が存在しない。本研究では放送ライブラリー公開番組データベースを例にして,「番組」の階層構造や放送番組を特徴づける各実体を定義し,メタデータモデルを汎用的な記述言語であるRDFを用いて構築する。構築したメタデータモデルは,放送番組を構成する要素をContents,Agent,Eventの3つのドメインに分類した。その上で,必要に応じて独自語彙を用いてクラスおよびプロパティを設定した。

著者

佐藤 久美子

出版者

一般社団法人 情報科学技術協会

雑誌

情報の科学と技術 (ISSN:09133801)

巻号頁・発行日

vol.73, no.5, pp.168, 2023-05-01 (Released:2023-05-01)

出版者

一般社団法人 情報科学技術協会

雑誌

情報の科学と技術 (ISSN:09133801)

巻号頁・発行日

vol.73, no.5, pp.195-198, 2023-05-01 (Released:2023-05-01)