著者

加藤 信太郎 齋藤 佳敬 小野田 紘子 熊井 正貴 今井 俊吾 敦賀 健吉 武隈 洋 菅原 満

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.7, pp.755-760, 2022-07-01 (Released:2022-07-01)

参考文献数

19

被引用文献数

1

---

Naldemedine (Nal) is widely used as a therapeutic drug against opioid-induced constipation. However, patients in phase III trials are limited to those with good performance status (PS). Cancer patients may have inferior PS owing to progression of symptoms and adverse events from chemotherapy. Therefore, it is important to survey the efficacy of Nal in patients with poor PS. This study aimed to evaluate Nal efficacy in patients with poor PS. We retrospectively investigated patients from July 2017 to June 2019 and compared Nal efficacy between patients with good and poor PS. The efficacy of Nal was evaluated using changes in the number of spontaneous bowel movements 7 days before and after the introduction of Nal with reference to previous reports. Multivariate analysis was performed to reveal whether poor PS affects Nal efficacy. In total, 141 patients at the Hokkaido University Hospital were analyzed. The effective rate of Nal from day 1 to day 7 of administration was 71.7% and 71.4% in the patients with good and poor PS, respectively, that from day 1 to day 2 of administration was 61.1% and 57.1%, respectively, and that from day 3 to day 7 of administration was 60.2% and 71.4%, respectively, suggesting an absence of significant differences. Furthermore, results of multivariate analysis showed that “best supportive care” and “body weight (55 kg and above)” reduced Nal efficacy. In conclusion, Nal showed similar effectiveness in patients with poor PS as that in those with good PS.

著者

内山 奈穂子 花尻(木倉) 瑠理 正田 卓司 福原 潔 合田 幸広

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.7, pp.1141-1147, 2011-07-01 (Released:2011-07-01)

参考文献数

12

被引用文献数

11 12

---

Recently, many psychotropic herbal products, named such as “Spice”, were distributed worldwide via the Internet. In our previous study, several synthetic cannabinoids were identified as adulterants in herbal products being available in Japan due to their expected narcotic effects. Among those, two derivatives of Δ9-tetrahydrocannabinol (Δ9-THC), which is major psychotropic cannabinoid of marijuana, cannabicyclohexanol (CCH, 3-[2-hydroxy-4-(2-methylnonan-2-yl)phenyl]cyclohexan-1-ol) and CP-47,497 (3-[2-hydroxy-4-(2-methyloctan-2-yl)phenyl]cyclohexan-1-ol), have been controlled as designated substances (Shitei-Yakubutsu) under the Pharmaceutical Affairs Law since November 2009. CCH was detected together with its trans-form (1-epimer) in many herbal products, and CCH and CP-47,497 have two chiral centers in the structures. However, the pharmaceutical activities of the isomers of CCH have not been reported. This study presents chiral separations of CCH, its trans-form and CP-47,497 in the products using LC-circular dichroism (CD) and LC-MS analyses. The enantiomeric pairs of CCH, its trans-form and CP-47,497 were separated, respectively. Subsequently, the analyses of the herbal products showed that CCH and its trans-form existed as mixtures of enantiomers and the relative ratios of CCH and the trans-form enantiomers ranged from 42/58% to 53/47% and from 33/67% to 52/48%, respectively.

著者

鈴木 啓司 児玉 靖司 渡邉 正己

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.10, pp.859-867, 2006-10-01 (Released:2006-10-01)

参考文献数

48

被引用文献数

6 6

---

Accumulated evidence has shown that exposure to low-dose radiation, especially doses less than 0.1 Gy, induces observable effects on mammalian cells. However, the underlying molecular mechanisms have not yet been clarified. Recently, it has been shown that low-dose radiation stimulates growth factor receptor, which results in a sequential activation of the mitogen-activated protein kinase pathway. In addition to the activation of the membrane-bound pathways, it is becoming evident that nuclear pathways are also activated by low-dose radiation. Ionizing radiation has detrimental effects on chromatin structure, since radiation-induced DNA double-strand breaks result in discontinuity of nucleosomes. Recently, it has been shown that ATM protein, the product of the ATM gene mutated in ataxia-telangiectasia, recognizes alteration in the chromatin structure, and it is activated through intermolecular autophosphorylation at serine 1981. Using antibodies against phosphorylated ATM, we found that the activated and phosphorylated ATM protein is detected as discrete foci in the nucleus between doses of 10 mGy and 1 Gy. Interestingly, the size of the foci induced by low-dose radiation was equivalent to the foci induced by high-dose radiation. These results indicate that the initial signal is amplified through foci growth, and cells evolve a system by which they can respond to a small number of DNA double-strand breaks. From these results, it can be concluded that low-dose radiation is sensed both in the membrane and in the nucleus, and activation of multiple signal transduction pathways could be involved in manifestations of low-dose effects.

著者

横山 晴子 山田 安彦 山村 喜一 中村 均 伊賀 立二

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.121, no.3, pp.233-237, 2001-03-01 (Released:2002-09-27)

参考文献数

7

被引用文献数

13 11

---

The effect of mouth wash on the removal of drug residues in both mouth and pharynx after the use of fluticasone propionate dry powder inhaler (FP-DPI) was studied. The concentration of FP in mouth wash after sprinkle and inhalation of Flutide® 50, 100, 200 Rotadisk® was determined by HPLC-UV. The total amount of the removed FP was measured by the sum of the concentration of FP in 5 times of mouth washes. The mouth wash procedures removed totally 79.3±4.4% (50 μg), 68.5±3.6% (100 μg), 69.3±3.4% (200 μg) of sprinkled amount of FP and 29.5±11.1% (50 μg), 35.6±6.6% (100 μg), 31.6±8.3% (200 μg) of inhaled, respectively. It was required for the removal of 90% of the totally recovered FP to do two times of mouth washes in each case. These data suggest that the mouth wash is an effective precaution for candidiasis induced by FP delivered by DPI.

著者

此村 恵子 森井 康博 赤沢 学

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.4, pp.413-420, 2022-04-01 (Released:2022-04-01)

参考文献数

17

---

Pharmacists play a key role in optimizing the safe and effective use of medicines in the super-aged society in Japan. Recently, community pharmacists' role has been transformed and expanded to provide patient-centered care. This study aimed to simulate a change in the demand for community pharmacists resulting from this shift in their role, from 2019 to 2035. The change in demand was estimated by the number of prescriptions obtained from publicly available sources of information. The number of required community pharmacists was calculated separately for full-time and part-time pharmacists and the pharmacists engaged in home medical care. This number was calculated using the estimated demand, the number of prescriptions dispensed per day, and annual working days. We evaluated the effect of changes in the working conditions, which include changes in the dispensing process time, rate of part-time staff and their work time, and number of home medical care per day, on the number of community pharmacists. When the number of prescriptions dispensed per day was set at 19.8, the demand for community pharmacists was estimated as 188,314 in 2035. Furthermore, due to the changes in the working conditions, the demand is expected to change from 153,362 to 266,944. Although the increasing provision of drug information time leads to an increasing number of pharmacists, combining it with work efficiency services could prevent or decrease it. The optimal supply and demand balance of community pharmacists should be determined by both, promoting pharmaceutical care services and improving work efficiency.

著者

佐野 和憲

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.7, pp.999-1005, 2019-07-01 (Released:2019-07-01)

参考文献数

14

---

Pathological α-synuclein (αSyn) has been shown to retain the ability to propagate as prions in humans and animals. However, the molecular basis underlying the prion-like properties of αSyn remains poorly understood. We examined whether brain tissues from cases of dementia with Lewy bodies (DLB), which contain serine 129 (Ser129)-phosphorylated insoluble aggregates of αSyn, exhibit prion-like seeding activity in vitro using the real-time quaking-induced conversion (RT-QuIC) seeding assay. Brain tissues from cases of diffuse neocortical DLB yielded a 50% seeding dose of 107.3-109.8/g brain. The RT-QuIC assay could discriminate between DLB and other neurological and neurodegenerative disorders, suggesting its potential applicability for differential diagnosis. Insoluble aggregates of αSyn>250 kDa detected only in DLB brain tissues by Western blotting analysis were specifically phosphorylated at Ser129. Therefore, we postulated that Ser129-phosphorylated insoluble aggregates of αSyn have prion-like seeding activity. However, insoluble aggregates of recombinant human αSyn (rSyn) with increased β-sheet structures showed little seeding activity in either the phosphorylated or nonphosphorylated state. In contrast, prefibrillar oligomers of rSyn showed seeding activity both with and without phosphorylation. The findings of the present study suggested that soluble oligomeric αSyn, but not the fully fibrillary form, is a seeding species in vitro.

著者

青木 良子 佐井 君江 勝田 由紀子 鈴木 美佳 鈴木 康夫 石井 明子 斎藤 嘉朗

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.547-560, 2022-05-01 (Released:2022-05-01)

参考文献数

19

被引用文献数

1

---

Biosimilars are less expensive than their originators, and Japanese government policies call for their development and promotion. However, the adoption and prescription of some biosimilars, especially antibody/its-related ones, have been delayed for use in Japan, possibly due to concerns on the differences in quality attributes such as glycan structures between the originators and their biosimilars, and that clinical efficacy/safety studies are conducted for usually one disease and its results extrapolated to other indications. We conducted a questionnaire survey among physicians in four disease areas (hematology, medical oncology, rheumatoid arthritis, and inflammatory bowel disease), where biosimilars of antibody/its-related drugs have been approved, regarding their thoughts on the adoption and prescription of biosimilars in Japan from January to April 2020. We received totally 1024 responses. When adopting biosimilars and explaining them to patients, physicians requested specific information including the comparative results of phase III clinical trials and quality characteristics between biosimilars and their originators; the results of clinical studies on switching from originators to their biosimilars; and a comparison of the estimated cost on patients in consideration of the high medical cost payment system. Priority differed depending on the studied disease areas. In terms of post-marketing information, physicians requested a variety of information. When explaining biosimilars to the patients, physicians would like to use general material from government describing the comparability between originators and their biosimilars. These results suggest that physicians sought more comparative information on the quality, efficacy, and patients' cost between originators and their biosimilars when adopting or prescribing biosimilars.

著者

金尾 清造

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.1927, no.540, pp.102-120, 1927-02-26 (Released:2010-11-30)

参考文献数

33

被引用文献数

1

著者

岡田 浩

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.3, pp.211-214, 2022-03-01 (Released:2022-03-01)

参考文献数

8

---

Evidence-based medicine (EBM) has led to the development of evidence-based guidelines. The quality of guidelines has been improved by measuring their quality with The Appraisal of Guidelines for Research and Evaluation II (AGREE II) and Grading of Recommendations, Assessment, Development and Evaluation (GRADE). However, evidenced by guidelines not implemented in clinical practice or society, the evidence-practice gap has become apparent. The dissemination and implementation research, which studies methods to solve this problem, has attracted the attention of both clinicians and clinical researchers in recent years. In hypertension and diabetes, it is possible to prevent complications by maintaining good blood pressure and blood glucose levels. However, it is difficult for patients to maintain good laboratory values over the long term, and there has been no solution to this problem. Recently, it has been reported that pharmacists in the U.S. and Canada can improve patient outcomes over the long term by using pharmacies to treat these diseases. This review describes the results of the COMPASS study (diabetes) and the COMPASS-BP study (hypertension), which are the first cluster randomized controlled trials conducted in pharmacies in Japan. In addition, it discusses the possibility of implementation in pharmacies in Japan.

著者

松尾 和哉

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.513-519, 2022-05-01 (Released:2022-05-01)

参考文献数

14

---

Genetic information is replicated and transmitted from a parent cell to two identical daughter cells through mitotic cell division. To accomplish this dynamic process with high accuracy and precision, various motor proteins work in a concerted manner. Especially in the metaphase, mitotic chromosomes are delivered by the motor protein of centromere-associated protein E (CENP-E) to the cell equatorial plane (metaphase plate) along mitotic spindles. However, the critical functional failure of CENP-E can activate the spindle assembly checkpoint through the misalignment of chromosomes at the metaphase plate. In this symposium review, the reversibly photoswitchable CENP-E inhibitor PCEI-HU (5) is reported. Compound 5 exhibited almost quantitative trans-cis photoisomerization of the arylazopyrazole photoswitch by illuminating light at 365 nm and 510 nm. Depending on the photoisomerization, CENP-E activity was regulated not only in vitro but also in cells. We successfully established a novel technique using 5 to dynamically photocontrol the CENP-E-dependent chromosome movement and mitotic progression in a living cell.

著者

栗原 藤三郎 菊地 正雄

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.98, no.4, pp.541-544, 1978-04-25 (Released:2008-05-30)

参考文献数

5

被引用文献数

1 2

---

In order to examine fragrant components, the essential oil of the flowers of Paulownia tomentosa STEUDEL was examined and, as the odor substances, hydroquinone dimethyl ether, 1-octen-3-ol, cis-3-hexen-1-ol, l-linalool, benzyl alcohol, phenethyl alcohol, benzaldehyde, anisaldehyde, ethyl palmitate, phenol, cresol (o-, m-, p-), 3, 4-dimethoxyphenol, and 12 kinds of volatile acid were identified. Apigenin, ursolic acid, β-sitosterol, campesterol, stigmasterol, β-sitosterol-β-D-glucoside, caffeic acid, p-hydroxybenzoic acid, p-coumaric acid, 3 kinds of fatty acid, and 17 kinds of normal paraffine were isolated from the steam distillation residue, as odorless components.

著者

水上 進

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.503-511, 2022-05-01 (Released:2022-05-01)

参考文献数

41

---

Technologies for the optical control of biomolecular functions have recently attracted considerable attention because they can be combined with advanced laser and microscopic techniques for diverse applications at the cellular and intravital levels. In this account, I review the summary of optical control technologies for biomolecular functions based on organic chemistry or protein science, and then introduce our recent studies on the development of small molecule-based photoregulation techniques. The first is the development of a photoactivatable protein labeling method based on a caged ligand. This method was applied to the photocontrol of intracellular protein dimerization and localization. The second is the development of a reversibly photoswitchable enzyme inhibitor, which was designed from the conformation of the inhibitor in the crystal structure of the enzyme-inhibitor complex. Based on our research strategies and results, I have also outlined the respective advantages and disadvantages of these two technologies: caged compounds and photoswitchable compounds.

著者

大久保 聡子 中畑 則道

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.1, pp.27-40, 2007-01-01 (Released:2007-01-01)

参考文献数

53

被引用文献数

14 15

---

Lipid rafts and caveolae are microdomains in the cell membranes, which contain cholesterol, glycolipids, and sphingomyelin. While caveolae are relatively stable because caveolin, an integral protein, supports the structure, lipid rafts are considered to be unstable, being dynamically produced and degraded. Recent studies have reported that lipid rafts contain many signaling molecules, such as glycosylphosphatidylinositol-anchored proteins, acylated proteins, G-protein-coupled receptors (GPCRs), trimeric and small G-proteins and their effectors, suggesting that the lipid rafts have an important role in receptor-mediated signal transduction. Therefore drugs that modify the composition of lipid rafts might influence the efficacy of cellular signal transduction. In this review, we demonstrate the role of lipid rafts in GPCR-G-protein signaling and also present our recent results showing that the wasp toxin mastoparan modifies Gq/11-mediated phospholipase C activation through the interaction with gangliosides in lipid rafts.

著者

浅井 禎吾

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.142, no.5, pp.439-446, 2022-05-01 (Released:2022-05-01)

参考文献数

36

---

Discovery of natural products that possess novel chemical structures and pharmaceutical activities increases opportunities of drug development. Filamentous fungi have been recognized as an attractive source for pharmaceutically beneficial natural products. Genome sequencing innovation represented by Next-generation sequencer opened fungal genomes one after another, suggesting that one fungal strain has far more biosynthetic gene clusters than that are estimated from the number of previously isolated natural products. In addition, bioinformatics analyses have indicated that most biosynthetic gene clusters are silent under laboratory culture conditions and there are a huge number of natural products hidden in the fungal genome. Therefore, we focused on those silent biosynthetic gene clusters as a potential source for novel natural products and developed methods to activate silent biosynthetic gene clusters by using low molecular weight molecules. In this review, we describe on discovery of novel natural products through activating fungal silent biosynthesis by addition of epigenetic modifiers and plant hormones.

著者

山本 緑

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.521-526, 2022-05-01 (Released:2022-05-01)

参考文献数

29

被引用文献数

1

---

Pharmacological cognitive enhancement (PCE) refers to the use of biochemical enhancers for achieving improved mental performance in healthy individuals. One particular use of PCE prevalence is the misuse of these enhancers among university students for academic performance enhancement. The prevalence rates demonstrate the use of a broad spectrum of substances for PCE that can be classified as OTC, prescription, and illegal drugs. Given that certain substances have been widely used for years, their long-term effectiveness and side effects in the healthy population are essential to know. The question of safety and efficacy or benefit versus risk is not only of individual and societal interest but also bears implications for regulatory and policy decision-making. As far as safety is concerned, there is a particular problem with healthy children, whose brains are still in development. Soft enhancers, such as energy drinks, might be commonly used worldwide. Performance pressure, stress, and psychiatric disorders may be associated with PCE use and need to be considered when planning anti-PCE-themed educational activities. In an increasingly complex information society, demands for cognitive functioning are growing; however, it is doubtful whether we should welcome the use of PCEs for the support of work productivity or the improvement of our life quality. Societal discussions on PCE might give an opportunity to consider a meaningful life in all aspects.

著者

入谷 信彦 滝野 吉雄 谷沢 久之

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.87, no.9, pp.1128-1131, 1967-09-25 (Released:2008-05-30)

参考文献数

11

---

4-Iodothymol was reduced with zinc dust in acetic acid and iodide ion produced was titrated with potassium iodate standard solution in the presence of hydrogen cyanide. By the visual titration, 20∼100 mg. of 4-iodothymol was determined using chloroform as an indicator and 2∼20 mg. was determined by the dead stop end point titration. Results obtained show that both methods are found to be enough accurate and precise for the determination. The determination had no interference by thymol and surface active agents contained in anthelminthic preparations of 4-iodothymol.

著者

矢島 領 今岡 楓太 輪湖 哲也 黒田 裕子 松元 一明 木津 純子 片山 志郎

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.135, no.12, pp.1397-1402, 2015-12-01 (Released:2015-12-01)

参考文献数

18

---

Stomatitis frequently occurs during chemotherapy and radiotherapy for cancer. Because of its pharmacological properties including anti-inflammatory activity and stimulatory effects on endogenous prostaglandin synthesis, rebamipide has been suggested as a potentially effective treatment against stomatitis. In the present study we tested the stability of oral rebamipide solutions prepared in our hospital pharmacy using sodium alginate as a thickener to increase retention of this agent in the oral cavity, and the addition of different flavoring mixtures intended for use in enteral diets to reduce the bitterness of rebamipide and sodium alginate. Samples of oral rebamipide solution prepared with 13 kinds of flavoring and sodium alginate were evaluated in terms of their appearance, redispersibility, pH, viscosity, and rebamipide content immediately after preparation and 1, 3, 7, and 10 days after storage at room temperature under ambient light or in a cool, dark place. After 10 days of storage, favorable stability was observed in four sample solutions supplemented with green apple, pineapple, yogurt, and tomato flavoring mixtures intended for use in Elental® diets. These oral solutions may have potential clinical application.

著者

鴻海 俊太郎 末丸 克矢 川崎 博己 町支 臣成 日比野 俐 荒木 博陽

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.197-201, 2009-02-01 (Released:2009-02-01)

参考文献数

12

被引用文献数

2 2

---

The rate of smoking in patients with schizophrenia is higher than that in the general population. Nicotinic acetylcholine receptors (nAChR) are involved in the sensorimotor gating deficits in schizophrenia. We have revealed that nicotine ameliorates the disruption of the PPI, a model of sensorimotor gating, which is induced by apomorphine, a dopamine receptor agonist, but is not effective for the disruption of the PPI induced by phencyclidine, a glutamine NMDA receptor antagonist, in rats. Furthermore, the ameliorating effect of nicotine is antagonized by methyllycaconitine, a selective α7 nAChR antagonist. The effect of nocitine was also investigated in the stereotyped behavior induced by apomorphine, however, nicotine was found to have no significant effect. Considering these results, the ameliorating effect of the disruption of the PPI via α7 nAChR is therefore thought to be involved in dopaminergic systems. The dopaminergic systems involved in α7 nAChR may be different from the systems involved in stereotypy. In addition, this review describes the effects of the α7 nicotinic receptor agonists.

著者

藤田 勇三郎 上原 郁恵 森本 泰子 中嶋 真由美 波多野 力 奥田 拓男

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.108, no.2, pp.129-135, 1988

被引用文献数

38

---

Inhibitory effects of caffeoylquinic acids isolated from leaves of Artemisia species and other related compounds on the lipoxygenase dependent peroxidation of linoleic acid were studied by kinetic and electron spin resonance(ESR) measurements. The order of inhibition activity was as follows : 3, 5-dicaffeoylquinic acid (ID<SUB>5</SUB>0=2.0&times;10<SUP>-</SUP>5 M)=rosmarinic acid > geraniin (2.8&times;10<SUP>-</SUP>5 M)>&alpha;-tocopherol (3.7&times;10<SUP>-</SUP>5 M)>chlorogenic acid (7.5&times;10<SUP>-</SUP>5 M)=caffeic acid>ferulic acid (2.5&times;10<SUP>-</SUP>4 M). This order coincided well with that obtained from the measurement of radical scavenging activities of these compounds against 1, 1-diphenyl-2-picryl hydrazyl. The inhibition profile of these compounds on lipid peroxidation in the lipoxygenase system was quite similar to those obtained previously in the biological systems of rat liver mitochondria and microsomes. In the separate ESR measurements in alkaline dimethyl sulfoxide solution, all caffeoyl-quinic acids exhibited relatively stable ESR signals assigned as a radical derived from the one-electron oxidation of dihydroxyphenyl group. From these results, it was concluded that the radical scavenging mechanism is commonly operative in both chemical and biological peroxidation systems.

著者

藤田 勇三郎 上原 郁恵 森本 泰子 中嶋 真由美 波多野 力 奥田 拓男

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.108, no.2, pp.p129-135, 1988-02

被引用文献数

7

---

Inhibitory effects of caffeoylquinic acids isolated from leaves of Artemisia species and other related compounds on the lipoxygenase dependent peroxidation of linoleic acid were studied by kinetic and electron spin resonance(ESR) measurements. The order of inhibition activity was as follows : 3,5-dicaffeoylquinic acid (ID_50=2.0×10^-5 M)=rosmarinic acid > geraniin (2.8×10^-5 M)>α-tocopherol (3.7×10^-5 M)>chlorogenic acid (7.5×10^-5 M)=caffeic acid>ferulic acid (2.5×10^-4 M). This order coincided well with that obtained from the measurement of radical scavenging activities of these compounds against 1,1-diphenyl-2-picryl hydrazyl. The inhibition profile of these compounds on lipid peroxidation in the lipoxygenase system was quite similar to those obtained previously in the biological systems of rat liver mitochondria and microsomes. In the separate ESR measurements in alkaline dimethyl sulfoxide solution, all caffeoyl-quinic acids exhibited relatively stable ESR signals assigned as a radical derived from the one-electron oxidation of dihydroxyphenyl group. From these results, it was concluded that the radical scavenging mechanism is commonly operative in both chemical and biological peroxidation systems.