著者

税所 篤行 高砂 美和子 若林 和貴 秋山 真里 幸田 恭治 髙崎 彰久 松永 和人 石田 博 北原 隆志

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.141, no.7, pp.971-978, 2021-07-01 (Released:2021-07-01)

参考文献数

14

---

To reduce the number of falls caused by hypnotic agents, the standardization of insomnia treatment was carried out at Yamaguchi University Hospital from April 2019. There were concerns that medical costs would increase due to the selected medicines―suvorexant and eszopiclone―being more expensive than conventional benzodiazepines. In this study, the standardization of insomnia treatment was evaluated by pharmacoeconomics. The costs of the hypnotic agents was considered, as was the cost of examination/treatment following falls. Effectiveness was evaluated as the incidence of falls within 24 hours of taking hypnotic agents. This analysis took the public healthcare payer's perspective. Propensity score matching based on patient background, showed that, per hospitalization the medicine costs of the recommended group increased by 1,020 yen, however, the examination/treatment costs following falls decreased by 487 yen when compared with the non-recommended group. Overall, the recommended group incurred costs of 533 yen more per hospitalization for patients prescribed hypnotic agents compared to the non-recommended group, but the incidence of falls for the recommended group was significantly lower than that in the non-recommended group (1.9% vs. 6.3%; p<0.01). These results suggest that in order to prevent the incidence of falls by 1 case, it is necessary to increase costs by 12,086 yen which is the subthreshold cost for switching to the recommended medicine as standardization. The selection of recommended medicines may be a cost-effectiveness option compared with non-recommended medicines.

著者

宮村 充彦 横田 淳子 西原 利治

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.136, no.4, pp.579-582, 2016-04-01 (Released:2016-04-01)

参考文献数

9

被引用文献数

2 5

---

Nonalcoholic steatohepatitis (NASH) is a chronic progressive liver disease characterized by intense liver steatosis accompanied by hepatocyte destruction, inflammation and fibrous, despite little or no history of alcoholic consumption. There are also cases of drug-induced secondary steatohepatitis. Drug-induced steatohepatitis is a relatively rare type of drug-induced liver disease, but close attention to the possible onset of steatohepatitis is needed when drugs with the potential to induce fatty liver are prescribed for long term use. Estrogen is a factor indispensable to smooth fatty acid β-oxidation in hepatocytes. However, treatment with Tamoxifen markedly suppresses fatty acid β-oxidation in the liver. As free fatty acids are toxic, their accumulation results in the activation of alternative fatty acid oxidation pathways mediated by CYP2E1 in cytosol and lipid peroxidases in peroxisomes in hepatocytes. CYP2E1 enhances lipid peroxidation and dicarboxylic acid synthesis via the activation of fatty acid ω-oxidation that injures mitochondria and results in the emergence of ballooned hepatocytes. In such cases, the attenuation of alternative fatty acid oxidation pathways could have some beneficial effects on mitochondrial injury, since fibrates (PPAR-α ligands) are potent enough to stimulate neutral fat consumption through the activation of peroxisomal fatty acid β-oxidation. Fortunately, fibrates attenuate serum estrogen levels by affecting estrogen receptor expression, so the co-administration of fibrates with Tamoxifen is expected to exert higher efficacy in breast cancer patients with Tamoxifen-induced hepatic steatosis.

著者

小田 真隆

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.10, pp.1233-1238, 2009-10-01 (Released:2009-10-01)

参考文献数

11

被引用文献数

1 1

---

Bacillus cereus is one that causes of opportunistic human infections. Sphingomyelinase produced by B. cereus is assumed a virulence factor for the infection. Sphingomyelinase from Bacillus cereus (Bc-SMase) is Mg2+-containing metalloenzyme. Bc-SMase is a family of neutral SMase (nSMase) and mimics the actions of the endogenous mammalian nSMase in causing differentiation, development, and apoptosis. Bc-SMase may be a good model for the poorly characterized mammalian nSMase. Activation of Bc-SMase by divalent metal ions was in the order Co2+>Mn2+>Mg2+≫Ca2+>Sr2+. Crystal structure analysis of Bc-SMase bound to Co2+, Mg2+, or Ca2+ revealed that the water-bridged double divalent metal ions at the center of the cleft in both the Co2+- and Mg2+-bound forms is the catalytic architecture required for sphingomyelinase activity. In contrast, the architecture of Ca2+ binding at the site showed only one binding site. A further single metal-binding site existed at one side edge of the cleft. Based on the highly conserved nature of amino acid residues of the binding sites, the crystal structure of Bc-SMase with Mg2+ or Co2+ provided a common structural framework applicable to phosphohydrolases belonging to the DNase I-like folding superfamily. In addition, our analysis provided evidence that β-hairpin containing the aromatic amino acid residues and the metal ion of the side-edge participate in binding to sphinogmyelin and membranes containing sphingomyelin. This article summarized current knowledge of characteristics and mode of action of Bc-SMase.

著者

髙鳥 悠記

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.141, no.6, pp.851-856, 2021-06-01 (Released:2021-06-01)

参考文献数

33

被引用文献数

2

---

Donepezil, the most widely used drug for the treatment of Alzheimer's disease (AD), is an acetylcholinesterase (AChE) inhibitor and is thought to improve cognition by stimulating cholinergic neurotransmission. However, no correlation has yet been established between the inhibitory role of AChE inhibitors and their therapeutic effects when used in AD patients. The cleavage pathway of amyloid precursor protein (APP) includes amyloidgenic (β, γ-cleavage) and non-amyloidgenic (α-cleavage) pathways. The intracellular transportation of APP is important in determining these cleavage pathways. It has been suggested that sorting nexin (SNX) family proteins regulates the intracellular transport of APP, thereby enhancing α-cleavage. In this study, we examined the effects of donepezil on SNX33 expression changes and APP processing in primary cultures of fetal rat cortical neurons. While donepezil treatment increased the levels of SNX33 expression and soluble APPα (sAPPα) in culture media, no changes were observed regarding full-length APP expression in the cell lysate. Donepezil also reduced the release of amyloid β (Aβ) into culture media in a concentration- and time-dependent manner. This reduction was not affected by acetylcholine receptor antagonists. The membrane surface expression of APP was elevated by donepezil. Furthermore, SNX knockdown by antisense morpholino oligos prevented the effects of donepezil. These results indicated that donepezil increased APP expression at the surface of the plasma membrane by decreasing APP endocytosis through upregulation of SNX33, suggesting donepezil might stimulate the non-amyloidogenic pathway. This new mechanism of action for the currently used anti-AD drug may provide a valuable basis for future drug discovery.

著者

林 輝明

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.96, no.3, pp.356-361, 1976-03-25

被引用文献数

1

---

Two new methods for the determination of gentiopicroside in gentian radix and Gentiana scabra radix were developed by the combination of thin-layer chromatography (TLC) and spectrophotometry. In the preparative TLC-ultraviolet (UV) method, gentiopicroside contained in the methanol extract ofsamples is quantitatively separated by preparative TLC (detection by a PAN UV lamp) and the amount is determined from the absorbance at 270 nm by using a calibration graph. In the TLC-densitometer (DM) method, the methanol extract containing gentiopicroside is developed on the TLC plate, and the amount of gentiopicroside (Rf=ca. 0.4) is measured by TLC densitometry using a dual-wavelength TLC scanner. By these two methods, the content of gentiopicroside vras determined as 1-2% in gentian idix (Osaka market product), 1-3% in Gentiana scabra radix (Osaka market product), and 7-10% in the fresh root of Gentiana scabra BUNGE.

著者

内田 英二

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.2, pp.213-221, 2009-02-01 (Released:2009-02-01)

参考文献数

8

被引用文献数

3 4

---

This paper describes the history of discussions on ethnic differences at the International Conference on Harmonization of technical requirements for registration of pharmaceuticals for human use (ICH). The first part of this paper gives a short outline of the purpose, organization, history, decision making process of the ICH. The ICH process consists of five steps. Step 1: Consensus building by Expert Working Group (EWG); Step 2: Confirmation of six-party consensus; Step 3: Regulatory consultation and discussion; Step 4: Adoption of an ICH harmonized tripartite guideline and Step 5: Implementation. Ethnic factors in the acceptability of foreign clinical data (“Ethnic Difference”) was one of the 14 topics on Efficacy. The author being one of the members of ICH-E5 EWG took part in the discussion of Ethnic Difference. The second part of this paper, describes the history of the discussion on this topic (from its inception to the finalization of the guideline) focusing on Step 2. A retrospective survey on individual pharmacokinetic data of around 80 drugs approved or under development in the 3 regions was conducted. In drafts 2 and 3, acceptance of phase 1 study only was discussed. But the proposal was opposed by industry members from US and EU. In drafts 4 and 5, the concept of “triage” was introduced and several algorithms were proposed, but finally a consensus could not be reached because the proposal was not so pragmatic. In drafts 7 and 8, the concept of “bridging study” was discussed to solve the problem of conducting phase II and III studies. Again, a consensus could not be reached. After the discussion of the “complete clinical data package” as proposed in drafts 9-12, the bridging study was once again discussed in drafts 13-19. Finally, draft 20 was confirmed and the discussion then moved to Step 3.

著者

高石 清和

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.88, no.11, pp.1467-1471, 1968-11-25 (Released:2008-05-30)

参考文献数

12

被引用文献数

7 7

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Coumarin (1) and coumaric acid glucoside (2) were isolated from the leaves of Prunus yedoensis MATSUM. (cherry tree). The structure of (2) was proved as o-coumaric acid β-D-glucoside which had been isolated from Melilotus altissima TEUIL. and named melilotoside by C. Charaux. Comparative determination of (1) and (2) in the leaves of cherry tree was made, and it was thereby found that red leaves in autumn contained much more o-coumaric acid glucoside than green leaves in spring, with a very small amount of coumarin in free state throughout the year. It is noteworthy that the deeper the red color of the leaves, the higher the content of o-coumaric acid glucoside. It is also interesting from biosynthetic point of view that both coumarin and anthocyan are synthesized through shikimic acid pathway. It was suggested that the leaves of cherry tree contain a fairly high amount of coumarin in the form of o-coumaric acid glucoside with a very small amount of free coumarin, although Kosuge, Brown, and Soine, have reported that o-coumaric acid glucoside in Melilotus spp. is finally converted into free coumarin.

著者

志摩 典明 佐々木 啓子 鎌田 徹 三木 昭宏 片木 宗弘

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.139, no.5, pp.705-713, 2019-05-01 (Released:2019-05-01)

参考文献数

27

被引用文献数

2 2

---

Hair testing for drugs has been used extensively in the field of forensics since the 1990s as a means of obtaining firm evidence of drug ingestion. In addition to its longer detection windows, hair is the only specimen that can provide chronological information on individual drug use. Illicit drugs and hypnotics account for the majority of substances involved in crimes; they are usually analyzed to prove an addictive use or an exposure to drugs in drug-facilitated crimes. The mechanism of drug incorporation into hair has been intensively investigated to properly interpret the results of hair analysis. However, the exact mechanism remains under much discussion, despite the growing application of hair tests. Recently, the authors have applied matrix-assisted laser desorption/ionization-mass spectrometry (MALDI-MS) imaging and sectional hair analysis of 1-mm segments using liquid chromatography-tandem mass spectrometry (LC-MS/MS) for single-strand hair, to investigate the incorporation pathways of drugs into hair. Time-course changes in drug distribution along single-strand hair suggest that the incorporation of drugs occurs in two regions of the hair root, the hair bulb and the upper part of hair root, and suggest that incorporation from the hair bulb continues for about 2 weeks. Distribution profiles of different drugs in hair additionally revealed that the main incorporation pathway varies (i.e., via the hair bulb or the upper part of hair root) depending on the properties of the drug/metabolite. These findings should be taken into account upon discussing individual drug-use history based on the results of hair analysis.

著者

小合 由起 砂金 信義 太田 隆文 宇留野 強

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.125, no.12, pp.1009-1011, 2005-12-01

被引用文献数

7

---

This study aimed to examine the effects of banana juice on levodopa bioavailability in rats. When a levodopa preparation (EC-Doparl tablets) was orally administered with banana juice made by mixing with a fresh banana and water, there were significant decreases in C_<max>(17.4±2.5vs.8.6±3.1μg/ml;α=0.05) and AUC(1882.8±49.2vs.933.5±286.6μg・min/ml;α=0.05) for levodopa. On the other hand, administration of the levodopa preparation with a commercial beverage containing 10% banana juice resulted in no significant change in C_<max> or AUC. These results indicate that concomitant intake of levodopa preparations with banana juice, but not with a commercial banana beverage, may cause a drug-food interaction reducing levodopa bioavailability, and we should pay attention to such interactions during levodopa therapy for patients with Parkinson's disease.

著者

江頭 かの子 北原 隆志 柏木 香 樋口 則英 中嶋 幹郎 一川 暢宏 佐々木 均

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.11, pp.1155-1161, 2006-11-01 (Released:2006-11-01)

参考文献数

13

被引用文献数

5 5

---

Antimicrobial agents sometimes cause the adverse effects of diarrhea and loose stool. Antibiotic-resistant lactic acid bacteria are used to prevent these adverse effects. The bacteria are not resistant to several antimicrobial agents, although the bacterium preparations are sometimes prescribed the antimicrobial agents concomitantly. Therefore this paper reports that the minimal inhibitory concentration of three new antimicrobial agents against antibiotic-resistant lactic acid bacteria were determined using a microdilution method with cation-adjusted Mueller-Hinton broth. Furthermore, we investigated antimicrobial agents that are prescribed concomitantly with antibiotic-resistant lactic acid bacterium preparations or a clostridium butyricum preparation. The bacteria were susceptible to the three new antimicrobial agents. Approximately 50% of the bacterium preparations were prescribed alone, and 30% were prescribed concomitantly with antimicrobial agents that show antimicrobial activity against the bacteria. Consequently, we suggest that pharmacists need to confirm prescriptions and to provide more drug information on antibiotic-resistant lactic acid bacterium preparations.

著者

下村 裕子 指田 豊 大島 行雄 我妻 禎 斎藤 昌彦

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.100, no.11, pp.1164-1166, 1980-11-25 (Released:2008-05-30)

参考文献数

8

被引用文献数

5 5

---

Scopoletin, protocatechualdehyde, ethyl and methyl caffeate and phytosterols were isolated from stems and leaves of Artemisia apiacea HANCE (Compositae).

著者

中垣 正幸 嶋林 三郎 早川 栄治 小槻 節

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.99, no.6, pp.618-627, 1979-06-25 (Released:2008-05-30)

参考文献数

11

被引用文献数

5 3

---

The amounts of both Ca2+ and Na+, x and y, respectively, bound to C-type chondroitin sulfate (Chs) from an aqueous solution of CaCl2 mixed with NaCl were obtained by the membrane equilibrium method. To estimate x and y under the effect of the Donnan equilibrium, [Ca2+] and [Cl-] for both sides of the dialysing tube and [Chs] for the inner side were analysed. The binding isotherm for Ca2+ was of the Langmuir type, and both x and kCa2+, the binding constant for Ca2+, decreased with ionic strength, J. On the other hand, the binding isotherm for Na+ was not of the Langmuir type but its shape was explained as the competitive adsorption of the two components, Na+ and Ca2+, because Ca2+ binds more strongly to Chs than Na+ and, therefore, the effect of coexistence of Ca2+ with Na+ cannot be neglected when the Na+ binding is examined. It was also suggested that y and kNa+ decreases with J when the amount of the occupied site by the Ca2+ is kept constant at x. The degree of the ionization, z, of Chs was found to be 0.40-0.41 for Na2Chs and 0.20-0.21 for CaChs by this membrane equilibrium method assuming x+y+z=1. These values coincide with those obtained from the vapour pressure osmometry by the authors and with the literature values calculated with considering the Manning theory.

著者

木村 和子

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.134, no.2, pp.195-196, 2014 (Released:2014-02-01)

被引用文献数

1 1

著者

輪島 丈明 中南 秀将 青木 沙恵 瀨山 翔史 野口 雅久

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.141, no.1, pp.135-142, 2021-01-01 (Released:2021-01-01)

参考文献数

19

被引用文献数

1

---

Environmental microorganisms can cause several infections in humans, especially in compromised hosts. Since there are many compromised hosts in a hospital setting, it is important to control environmental pathogens in such scenarios. To disinfect the environment, photocatalysts that produce reactive oxygen in response to light have attracted attention. In the present study, the effects of a visible-light-driven antimicrobial photocatalyst, silver (I) iodide and benzalkonium complex, on bacteria, viruses, and fungi were evaluated in vitro. In addition, uncoated panels and panels coated with the photocatalyst were set up at 11 points in a university campus for 6 months, and the adherent bacteria and fungi were measured. Bacteria, bacterial spores, viruses, and fungi were completely inactivated within 45 min on the photocatalyst-coated surface exposed to approximately 700-lux fluorescent light. In the university setting, there were fewer viable adherent bacteria and fungi on the coated plates. Our findings indicate that the silver (I) iodide and benzalkonium complex photocatalyst can decrease environmental bacteria in vitro and in actual environmental settings, and thus highlight its potential in controlling and disinfecting environmental pathogens.

著者

石丸 博雅 津田 泰正 景 秀典 河野 友昭 高山 慎司 森元 能仁 後藤 一美 渡部 一宏

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.141, no.1, pp.143-150, 2021-01-01 (Released:2021-01-01)

参考文献数

28

被引用文献数

1

---

Occupational exposure to anticancer drugs may increase the risk of cancer and the risk of miscarriage and stillbirth, and cause other adverse events such as hypersensitivity reactions, skin/mucous reactions, and digestive symptoms. Several studies have investigated the use of closed-system drug-transfer devices (CSTDs) to reduce the environmental pollution by hazardous drugs. However, few reports have verified whether CSTDs contain the hazardous drugs within the vials. The BD PhaSealTM System is a CSTD that is frequently used in Japan. However, the fit of each anti-cancer drug vial has not been investigated. We investigated the fit of 71 major anti-cancer drug vials and protectors released and frequently used in Japan by means of a pressure compatibility test that we developed. The pressure compatibility test involved attaching a three-way stopcock to a Luer lock syringe and attaching an injector in line with the syringe. The pressure tubing was connected to the other side of the three-way stopcock and connected to the pressure inlet of the pressure gauge. The pressure in the anti-cancer drug vial was raised to 100 kPa and connected/disconnected repeatedly. If the pressure fluctuation during the 10th connection was within 6%, it was defined as “no change”, and the compatibility of the protector and the vial was evaluated. The median pressure reduction rates at the 10th connection ranged from −1.98% to −4.95%. All drugs surveyed had an error rate within 6%. The BD PhaSealTM Protector was shown to be compatible with the 71 anti-cancer drugs we surveyed.

著者

松居 隆 大塚 幸 酒井 浄

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.120, no.10, pp.825-837, 2000-10-01 (Released:2008-05-30)

参考文献数

36

被引用文献数

4 11

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One century has passed since fugu toxin was named tetrodotoxin (TTX) by Tahara. Chemical problems such as crystallization of tetrodotoxin and subsequent structure determination were solved by research groups headed by Tsuda, Hirata, Woodward, and Mosher. The International Symposium on the Chemistry of Natural Products in Kyoto (1964) was well known as symposium which the structure of TTX was internationally clarified. Since the first isolation of toxin from taricha torosa (imori) as natural source except for fugu fishes, distribution of toxin in nature has been widely investigated. And, it was proved that toxin is not produced by fugu fishes, but rather is formed by sea bacteria (30 sp.) such as Alteromonas sp, Vibrio sp, Shewanella. However, it seems to be difficult to explain the tetrodotoxin accumulation at high concentration in fugu by only toxin production by bacteria. TTX analogues were isolated from natural origins such as crabs, fish, annelids, and algae. Based on the structure of these toxin analogues, the biosynthesis of toxin and the structure-activity relationship (Na+ channel) were proposed by Yasumoto-Yamashita. The findings of wide distribution of toxin in nature may be attributed to development of highly sensitive detection method for toxin. The interesting proposal for the biosynthesis and the structure activity, and the detection method for toxin are outlined in this review.

著者

原 宏和

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.127, no.8, pp.1199-1205, 2007-08-01 (Released:2007-08-01)

参考文献数

27

被引用文献数

4 4

---

NF-E2-related factor-2 (Nrf2), a basic leucine zipper transcription factor, is involved in the expression of numerous detoxifying and antioxidant genes via the antioxidant response element (ARE). Keap1, a cytoplasmic protein, sequesters Nrf2 in the cytoplasm under normal conditions. Various stimuli, including electrophiles and oxidative stress, liberate Nrf2 from Keap1, allowing Nrf2 to translocate into the nucleus and to bind to the ARE. Recently, there is increasing evidence that compounds that stimulate the activation of the Nrf2-ARE pathway may become useful therapeutic drugs for neurodegenerative diseases associated with oxidative stress. Apomorphine (Apo), a dopamine D1/D2 receptor agonist, is used for clinical therapy of Parkinson's disease. On the other hand, Apo is a potent radical scavenger and has protective effects on oxidative stress-induced cell death. We previously reported that pretreatment of human neuroblastoma SH-SY5Y cells with Apo enhanced the protective effects. In addition, we have recently demonstrated that Apo stimulates the translocation of Nrf2 into the nucleus and the transactivation of the ARE. Our findings suggest that not only the function as a radical scavenger, but also the function as an Nrf2-ARE pathway activator may be involved in the neuroprotective effects of Apo on oxidative stress-induced neuronal cell death. In this review, our recent studies on the mechanism underlying Apo-induced neuroprotection are summarized.

著者

涌井 袈裟參 平井 文代

出版者

公益社団法人 日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.61, no.10, pp.401-405, 1941-10-26 (Released:2009-10-21)

参考文献数

5

著者

後藤 佐多良

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.140, no.3, pp.407-410, 2020-03-01 (Released:2020-03-01)

参考文献数

6

---

As a teacher of biochemistry in a school of pharmacy, a basic subject in pharmacist education, I try to include applied topics such as the biochemical mechanisms of diseases and side effects of medicines in relation to basic knowledge of biochemistry for advanced subjects that students will learn in later years. In aging societies, many people visiting community pharmacies are elderly who tend to have health concerns other than diseases diagnosed by physicians. If asked, community pharmacists should be able to give advice on potential problems patients might have, in addition to giving explanations of medicines prescribed. Basic subjects covered in university pharmacy courses should be the most useful in such community settings.

著者

榊 利之 安田 佳織 西川 美宇 生城 真一

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.138, no.3, pp.357-363, 2018-03-01 (Released:2018-03-01)

参考文献数

22

被引用文献数

2 9

---

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 mediated by CYP2C9 in human liver, sesamin causes a mechanism-based inhibition (MBI) of CYP2C9. However, we found that the metabolite-intermediate complex between CYP2C9 and sesamin was unstable, and the effects of sesamin appeared to be minimal. To confirm this assumption, in vivo studies using rats were conducted. After the administration of sesamin to rats for 3 d, diclofenac (an NSAID) was administered to measure the time course of plasma concentration of diclofenac. No significant differences were observed in the diclofenac Cmax, Tmax, and AUC0-24 h between the group that was administered sesamin and the group that was not. Based on these results, it could be concluded that no significant interaction occurs in people who take sesamin supplements at a standard dose.