著者

池田 浩人 森脇 英恵 松原 友規 湯川 美穂 岩瀬 由紀子 湯川 栄二 安藝 初美

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.132, no.1, pp.145-153, 2012-01-01 (Released:2012-01-01)

参考文献数

8

被引用文献数

4 4

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The influence of the presence of a galloyl group in catechin on complexation with risperidone (RISP) was examined using (−)-epigallocatechin gallate (EGCg) and (−)-epigallocatechin (EGC), which are present in green tea as tea catechins. By quantitative analysis using HPLC, it was found that EGCg formed an insoluble complex with RISP for concentration dependence, whereas EGC did not. The large contribution of the galloyl group of catechin to form an insoluble complex with RISP was recognized in this study. In a molecular modeling study, it was found that the EGCg-R complex (EGCg with RISP) formed three hydrogen bonds between the hydroxyl groups of EGCg and the two N atoms and an O atom of RISP. The hydrogen bond between the hydroxyl group of the galloyl ring in EGCg and the N atom of the piperidine ring in RISP stabilized EGCg-R more energetically. The EGC-R complex (EGC with RISP) also formed three hydrogen bonds, but the N atom of the piperidine ring in RISP did not participate in hydrogen bond formation. According to the calculation using the COSMO-RS method, the water solubility of the EGCg-R complex was 1/26 that of the EGC-R complex. Therefore, the EGCg-R complex was difficult to dissolve in water. In the 1H-NMR spectra of RISP in DMSO-d6, although chemical shifts of protons near the N atom on the piperidine ring moved downfield on the addition of EGCg, no change in chemical shifts of these protons was observed on the addition of EGC. Therefore, based on these results, the galloyl group of EGCg contributes to the formation of an insoluble complex between tea catechin and RISP, and this insoluble complex is stabilized by the hydrogen bond between the hydroxyl group of the galloyl ring in EGCg and the N atom of the piperidine ring in RISP.

著者

堀川 俊二 梶谷 真也 川上 恵子 只佐 宣子 伊東 明彦

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.133, no.4, pp.473-478, 2013 (Released:2013-04-01)

参考文献数

7

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In recent years there has been a rise in the number of diabetic patients in Japan, with the increase in elderly diabetic patients becoming a serious problem. This study looked at 488 elderly type 2 diabetes patients who were admitted as emergency cases to the Department of Internal Medicine, JA Yoshida General Hospital, Akitakada City, Japan. All patients were classified by age into three groups: <70, 70-80 and >80. The most common cause of emergency hospitalization in each of the three age groups was infection. This was significantly higher in the >80 group in comparison with<70 (p<0.05). The most common infection among the three groups was respiratory infection, followed by urinary tract infection. The number of emergency hospitalization cases due to hypoglycemia was much higher in the over 80 group, particularly in comparison with<70-80 (p<0.05). The incidence of hypoglycemia in our patients could be explained mainly by reduced energy intake. Most cases were treated with oral administration of hypoglycemic drugs. As elderly diabetic patients have a number of underlying illnesses that are prone to aggravation and may lead to unfavorable prognosis, early medical examination and disease detection are considered to be important. Pharmacists are required to educate patients, home-visit nursing care personnel on sick-day rule, and provide diabetes care.

著者

笠師 久美子

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.132, no.12, pp.1325-1328, 2012 (Released:2012-12-01)

被引用文献数

1

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When athletes consult sports outpatient or orthopedic clinics it is possible to undergo drug treatment with the medical staff having prior knowledge of that patient being an athlete. However, if athletes seek any other diagnosis and treatment as an ordinary patient, the possibility of medical staff realizing the potential for imposing a doping issue on the athlete is extremely low. As a result, if the athlete fails to provide medical staff with information regarding anti-doping regulations when receiving clinical treatment, drug treatment administered as part of medical practices could be viewed as doping, resulting in the athlete being disciplined. In order to avoid this, pharmacist should participate in training in order to be able to provide information for anti-doping purposes. It is my personal opinion that knowledge regarding anti-doping is something that should be shared by all pharmacists, as pharmacists are educated in the fields of pharmacology and pharmacokinetics during the pharmacy education process, and sports pharmacology is a part of this. However, in order for pharmacists to understand sports pharmacology, it is necessary to provide education not only on the benefits and adverse effects of pharmaceutical products, but also on the concept of banned substances. It can be considered one of the pharmacist's duties to protect athletes who purchase drugs at a pharmacy or consult medical institutions as patients. With this, I would like to propose considering the potential for introducing sports pharmacology to pharmaceutical education, and specialist pharmacist training in the sports spectrum.

著者

冨田 隆志 佐伯 康之 鴫田 江理嘉 河田 麻美 木村 康浩 木平 健治

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.129, no.4, pp.451-457, 2009 (Released:2009-04-01)

参考文献数

16

被引用文献数

1 1 1

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We conducted a survey on the immunization requirements of the students in the fourth year of the 4-year-course departments of pharmacy in Japan by using a self-administered questionnaire, which was mailed to the directors of the institutes. Of the 61 departments invited, 54 responded. Program of seroprevalence examination or vaccination was not in place against measles, rubella, mumps and varicella, and hepatitis B in 31.5% (17/54), 53.7% (29/54), 57.4% (31/54), and 68.5% (37/54), respectively. Surveillance of the history of infection and vaccination was carried out in 21 departments, but only 5 departments insisted on documented evidence of immunity. Students who were proven to be susceptible to these diseases were required to receive immunization in most departments that performed seroprevalence examination. Seroprevalence examination was carried out in colleges in 83.3% (25/30), and the expenses were born by department in 70.0% (21/30). On the other hand, vaccination was carried out in colleges in 30.0% (9/30), and the expenses were born by department in 6.7% (2/30). Of the 54 departments, 29, 11, and 3 departments executed these programs in the 3rd year, 4th year, and at the time of admission, respectively. Influenza vaccination during the year of clinical clerkship and tuberculosis skin test was required in 20.4% (11/54) and 37.0% (20/54), respectively; these were carried out in the colleges in 8 and 19 departments and the expenses were born by department in 1 and 18 departments, respectively. Countermeasures against these infectious diseases were found to be insufficient in most departments of pharmacy.

著者

西田 圭吾

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.131, no.1, pp.85-92, 2011-01-01 (Released:2011-01-01)

参考文献数

26

被引用文献数

3 3

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Zinc (Zn) is an essential nutrient and its deficiency causes growth retardation, immunodeficiency, and neuronal degeneration. Zn homeostasis is tightly controlled by transporting through Zn transporters and by buffering via metallothioneins, all of which are involved in the intricate regulation of Zn concentration and distribution in individual cells. Research in understanding of these molecules has progressed with application of genetic techniques, which allow us to clarify the diverse role of Zn in vivo and in vitro. However, the precise roles and molecular mechanism(s) of Zn's function in allergic response have not been clarified. Mast cells are granulated cells that play a pivotal role in allergic reactions. The granules of mast cells contain various chemical mediators and inflammatory cytokines that are released upon FcεRI crosslinking. In this article, I will describe a role of Zn/Zn transporter in FcεRI-mediated mast cell degranulation and cytokine production. Furthermore, Zn acts as an intracellular signaling molecule, that is, a molecule whose intracellular status is altered in response to an extracellular stimulus in mast cell, and that is capable of transducing the extracellular stimulus into an intracellular signaling event, like Ca2+. I have proposed that there are two classes of Zn signaling: “Early” and “Late” Zn signaling. In this review, I discussed how Zn and its homeostasis affect biological events especially for mast cell-mediated allergy response.

著者

草野 源次郎 芝野 真喜雄 渡辺 斉 尾崎 和男

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.123, no.8, pp.619-631, 2003-08-01 (Released:2003-08-01)

参考文献数

38

被引用文献数

9 9

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Some Glycyrrhiza species grown in several domestic research gardens of medicinal plants were collected by the Osaka University of Pharmaceutical Sciences and were cultivated to compare their morphological properties. HPLC profile analysis was performed and index compounds of MeOH extracts of aerial parts and EtOAc extracts of subterranean parts were determined. Glycyrrhizin contents and growth rates of the underground parts of some types of Glycyrrhiza uralensis and Glycyrrhiza glabra were compared and four excellent types were selected as candidates for cultivation. One of them was due to Kanzo-Yashiki (Enzan, Yamanashi prefecture), where G. uralensis was cultivated in the Edo period. Alkaloidal constituents of G. uralensis and G. glabra were also investigated and anabasine (an insecticide) and a new tricyclic alkaloid were obtained.

著者

中山 貢一

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.126, no.8, pp.565-577, 2006-08-01 (Released:2006-08-01)

参考文献数

54

被引用文献数

1 1

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Mechanoreception and subsequent cellular/molecular mechanisms of signal transduction pathways in response to mechanical stresses, including hemodynamic factors, passive stretching, and exercise, are ubiquitous in living organisms. Of these, the cardiovascular system involving the heart and blood vessels is known to be particularly sensitive to mechanical stimuli, for example, stretching and intraluminal pressurization, which might mimic an acute and/or chronic change in blood pressure and flow, induce a variety of responses including contraction, activation of various kinases and ionic channels, production of vasoactive substances, gene expression, and phenotype changes. We have started to clarify the mechanisms underlying this basic principle in the cardiovascular system as it is now generally considered that obesity and a lack of exercise are serious risk factors for cardiovascular diseases such as hypertension, atherosclerosis, and type 2 diabetes. We further extended our research field of mechanotransduction into adipocytes, skeletal muscle cells, and pancreatic beta cells, all of which are related to the core concerns in cardiovascular disease, including the so-called metabolic syndrome. In the present article, we discuss briefly the prologue to our study of mechanotransduction and several topics in the recent progress in this interesting area. We also emphasize that it is important to recognize biomechanical factors and control them not only for improvement in our knowledge of health and disease but also for the development of new drugs.

著者

村上 怜子

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.59, no.11, pp.1041, 2023 (Released:2023-11-01)

参考文献数

4

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現代社会において,砂糖の摂りすぎによる肥満および,それに伴う様々な疾患は大きな問題となっている.そのため,ゼロもしくは低カロリーの人工甘味料は,砂糖の摂取量を減らし,減量や血糖値をコントロールするために,広く使われている.様々な人工甘味料の短期の安全性は評価されているが,長期的に大量に摂取した場合の影響の評価は不十分であり,近年,長期の大量摂取が循環器系の病態に影響する可能性が指摘されている.人工甘味料の1つであるエリスリトール(C4H10O4)は,果物など自然界にも含まれる物質で,砂糖の60~70%の甘みを持ち,生体内でほとんど代謝されない「ゼロカロリー」の糖アルコールである.エリスリトールは,食べ物や飲み物において広く使用されてきた.本論文4)では,食生活の聞き取り調査等ではなく,血液中に含まれるエリスリトールの濃度を質量分析計(mass spectrometry: MS)によって実際に測定し,心疾患リスクとの相関関係を検証している.なお,本稿は下記の文献に基づいて,その研究成果を紹介するものである.1) Janzi S. et al., Front. Nutr., 7, 603653(2020).2) Debras C. et al., BMI, 378, e071204(2022).3) Vyas A. et al., J. Gen. Intern. Med., 30, 462–468(2015).4) Witkowski M. et al., Nat. Med., 29, 710–718(2023).

著者

野上 寿

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.1, no.4, pp.17-18, 1965-04-05 (Released:2018-08-26)

著者

竹内 孝輔 国本 亮

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.60, no.2, pp.106-110, 2024 (Released:2024-02-01)

参考文献数

21

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医薬品研究開発には多額の費用と10年以上の期間を要する。創薬研究の成功確率向上および効率化を図るため、データおよびAI利活用の取り組みが注目されている。第一三共創薬化学研究所では、データサイエンス専門チームを作り創薬化学にデータサイエンスを融合させるとともに、2つの研究領域のシナジーを生むための循環型の人材育成策を実施した。本施策によって20%の研究業務効率化を達成し、さらに生産性向上に向けた前向きな変化を確認することができた。

著者

関 淳

出版者

公益社団法人 日本薬学会

雑誌

MEDCHEM NEWS (ISSN:24328618)

巻号頁・発行日

vol.22, no.3, pp.46, 2012-08-01 (Released:2020-08-01)

著者

小池 敦資

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.56, no.12, pp.1134, 2020 (Released:2020-12-01)

参考文献数

4

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飲食物中へのスクロースや異性化糖の使用により,フルクトースの摂取はここ数十年で顕著に増加している.フルクトースの過剰な摂取は肥満や非アルコール性脂肪肝疾患,糖尿病などの発症と強く相関している.フルクトースの摂取は,肝臓における脂質生合成を誘発し,アセチルCoAから脂肪酸の合成を促進する.さらにフルクトースは,腸内細菌によって短鎖脂肪酸に代謝される.しかし,食餌中のフルクトースから肝臓のアセチルCoAや脂質生合成に至る経路や短鎖脂肪酸の脂質生合成への影響については未解明な点が多い.ATPクエン酸リアーゼ(ACLY)はクエン酸からアセチルCoAに変換する酵素であり,糖代謝と脂肪酸生合成を結ぶ重要な酵素として知られている.本稿では,肝臓特異的にACLYをノックアウトしたマウス(LAKOマウス)を用いて,同位体標識したフルクトース(13Cフルクトース)による追跡実験を行うことによって,肝臓でのフルクトースからの脂質生合成に腸内細菌が関与することを明らかにした報告を紹介する.なお,本稿は下記の文献に基づいて,その研究成果を紹介するものである.1) Jegatheesan P., De Bandt J. -P., Nutrients, 9, 230(2017).2) Jang C. et al., Cell Metab., 27, 351-361.e3(2018).3) Zhao S. et al., Nature, 579, 586-591(2020).4) Zagelbaum N. K. et al., Caldiol. Rev., 27, 49-56(2019).

著者

宮田(古谷) 聡美 河野 惠三 森元 崇史 原島 哲 岩田 裕子 有安 利夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.142, no.5, pp.535-546, 2022-05-01 (Released:2022-05-01)

参考文献数

29

被引用文献数

1

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Transient receptor potential vanilloid 2 (TRPV2) channels are expressed and play functional roles in various immune cells. Physical stimuli leading to TRPV2 activation causes mast cell degranulation. Besides their roles in immune cells, it has been shown that TRPV2 channels are pathophysiologically relevant to degenerative muscular diseases such as dilated cardiomyopathy and muscular dystrophy. Hence, development of drug candidates that inhibit human TRPV2 activation is an urgent matter. NK-4, a cryptocyanine dye, inhibited agonist-induced TRPV2 activity in mouse TRPV2-transfected HEK293 cells. However, it remains unclear whether NK-4 exerts regulatory effects on the activation of human TRPV2 channels. In this study, we show that NK-4 inhibits intracellular Ca2+ increase in human TRPV2-transfected HEK293 cells preactivated with a TRPV2 agonist. The inhibitory effect of NK-4 (IC50=0.27 μM) on human TRPV2 activation was 74-fold stronger than that on mouse TRPV2 activation (IC50=20 μM). NK-4 also inhibited the agonist-induced TRPV2 expression at the plasma membrane, when the human TRPV2-expressing cells were stimulated with the agonist in the presence of NK-4. These results suggest that NK-4 abrogates the agonist-induced signaling events leading to human TRPV2 activation. Furthermore, TRPV2 agonist caused degranulation of RBL-2H3 cells, which represents a phenomenon related to physical urticarias. NK-4 suppressed the release of β-hexosaminidases upon degradation with IC50 of 1.9 μM, 35-fold lower than that determined with an anti-allergic drug, Epinastine. Our results suggest that NK-4 would be a potential therapeutic strategy to resolve dilated cardiomyopathy and its associated heart failure as well as physical urticarias.

著者

平山 文俊

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.57, no.6, pp.525_3, 2021 (Released:2021-06-01)

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結晶多形を有する化合物が溶液から晶析する時,熱力学的安定性の低い準安定形が先に晶析し,その後安定形が出現する現象をオストワルドの段階則(Ostwald’s step rule,Ostwald’s rule of stages)といい,Whilhelm Ostwald(1909年ノーベル化学賞受賞)により提唱された理論である.結晶化の第1段階である1次核発生速度は,溶液の過飽和度と結晶核の界面エネルギーに依存するが,核発生では後者の影響が大きくなるため,高過飽和度では界面エネルギーが小さい準安定形の晶析が優勢となる.なお,オストワルド・ライプニング(Ostwald ripening)は,同一多形でも結晶の大きさに不均一性がある場合,小さい結晶が溶解し,大きい結晶が成長する現象をいう.

著者

大林 幹彦

出版者

公益社団法人 日本薬学会

雑誌

MEDCHEM NEWS (ISSN:24328618)

巻号頁・発行日

vol.10, no.3, pp.7-9, 2000-08-01 (Released:2021-06-19)

著者

木村 優花 川上 和宜 中村 匡志 横川 貴志 清水 久範 小林 一男 青山 剛 鈴木 亘 羽鳥 正浩 鈴木 賢一 高張 大亮 小倉 真理子 陳 勁松 中山 厳馬 若槻 尊 山口 研成 山口 正和

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.143, no.12, pp.1075-1081, 2023-12-01 (Released:2023-12-01)

参考文献数

21

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Since it is important that patients take their oral anticancer therapy as prescribed, pharmacists need to assess adherence. In addition, oral anticancer drugs are expensive, and reuse of leftover drugs at outpatient pharmacy clinics is useful in reducing drug costs. The present study aimed to clarify when and why patients have leftover capecitabine tablets, and the cost of leftover capecitabine tablets reused at an outpatient pharmacy clinic, focusing on adjuvant capecitabine plus oxaliplatin (CAPOX) chemotherapy for gastric cancer. We retrospectively studied patients who received adjuvant CAPOX chemotherapy for gastric cancer between November 1, 2015, and April 30, 2021, at the Cancer Institute Hospital of the Japanese Foundation for Cancer Research. The cost of leftover capecitabine reused by pharmacists was calculated based on the National Health Insurance drug price standard for the study period. This study included 64 patients who received adjuvant CAPOX chemotherapy. Thirty-seven patients had 152 leftover capecitabine tablets. The most common reasons for leftover capecitabine tablets were nausea and vomiting (21.7%), missed doses (18.4%), and diarrhea (13.2%). The leftover capecitabine tablets for 25 patients were reused at the outpatient pharmacy clinic at a cost of JPY 604142.8 (JPY 24165.7 per patient). The study results suggest that evaluating capecitabine adherence and the reasons for leftover capecitabine tablets at outpatient pharmacy clinics as well as reusing leftover medication can contribute to reducing drug costs.

著者

今町 憲貴

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.56, no.9, pp.843-845, 2020 (Released:2020-09-01)

参考文献数

22

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最近の基礎研究により脊髄レベルでの痒みの機序やその制御についての知見が明らかとなってきた。また、オピオイドによる痒みの機序の一部がガストリン放出ペプチド受容体を介することにより生じることも解明されてきた。臨床においてオピオイドよる痒みは頻度の高い副作用であるが、現状では予防や治療に関するガイドラインがない状態である。本稿では、オピオイドによる痒みの機序、及びさまざまな薬物による鎮痒効果に関する臨床研究について概説する。

著者

大野 清隆 西尾 伸太郎

出版者

公益社団法人 日本薬学会

雑誌

MEDCHEM NEWS (ISSN:24328618)

巻号頁・発行日

vol.3, no.2, pp.37-42, 1993-04-15 (Released:2021-10-13)

参考文献数

9

著者

武村 俊之

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.28, no.1, pp.61-65, 1992-01-01 (Released:2018-08-26)

被引用文献数

2

著者

田中 大輔

出版者

公益社団法人 日本薬学会

雑誌

MEDCHEM NEWS (ISSN:24328618)

巻号頁・発行日

vol.30, no.4, pp.171-176, 2020-11-01 (Released:2021-05-01)

参考文献数

5

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2012年英国で誕生したExscientiaは、人工知能(AI)創薬における世界のフロントランナーである。本年1月には大日本住友製薬との共同研究で生み出された化合物が臨床試験入りし、世界で最初のAIがデザインした治験薬として多くのメディアに採り上げられるなど、その実力と実績を「成果物」として世に知らしめた。その結果、ExscientiaはAIによるドラッグデザインをする企業であると理解されがちであるが、それは主要であるものの一部に過ぎない。Exscientiaではドラッグデザインに止まらず、これから注目される新規標的分子の提案にもAIを活用している。筆者らのAI創薬プラットフォームを紹介するとともに、世界のAI創薬の最前線に身を置く立場からこれからの創薬化学者のあり方についても私見を述べてみたい。