著者
大橋 一智 里中 勝人 山本 哲郎 山崎 正利 木村 貞夫 安部 茂 山口 英世
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.113, no.5, pp.396-399, 1993-05-25
被引用文献数
10

The antitumor activity of a preparation of heat-killed cells of Enterococcus faecalis, FK-23. Intraperitoneal injection of the preparation prolonged the lifespan of C3H/He N mice which were intraperitoneally inoculated with MM46 mammary carcinoma. Not only intraperitoneal but also oral administration of the FK-23 preparation inhibited the growth of these carcinomas inoculated intradermally. The tumor-bearing mice produced tumor necrosis factor (TNF) in their sera 2 h after intravenous injection of OK432. This TNF level increased after the mice were fed with food supplemented with the FK-23 preparation. Additionally, the FK-23 preparation inhibited the growth of Meth A fibrosarcoma in cyclophosphamide-treated BALB/c mice.
著者
亀岡 弘 鄭 玉珍 宮沢 三雄
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.96, no.3, pp.p293-298, 1976-03

An essential oil was obtained in 0.11% yield by steam distillation from the fresh fruit of Canarium album RAEUSCH The oil was treated successively with 5% sodium carbonate and 5% sodium hydroxide solution, and separated into neutral, sodium carbonate-soluble, and sodium hydroxide-soluble fractions. α-Pinene, camphene, β-pinene, myrcene, limonene, 1,8-cineole, p-cymene, linalool, α-copaene, linalyl acetate, cis-p-2-menthen-1-ol, 1-terpinen-4-ol, trans-p-2-menthen-1-ol, β-caryophylene, citronellyl acetate, β-terpineol, α-terpineol, terpinyl acetate, neryl acetate, geranyl acetate, nerol, δ-cadinene, geraniol, δ-cadinol, elemol, 14 kinds of carboxylic acid, 6 kinds of phenolic compound, and alkane of C_<10> to C_<32> were identified from their infrared, mass, and nuclear magnetic resonance spectra, and by chemical methods.
著者
山口 幸洋 任張 幸子 小幡 博子 大河原 知水 江口 裕伸 黒津 敏嗣 鈴木 敬一郎
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.122, no.7, pp.495-498, 2002-07-01
参考文献数
5
被引用文献数
1

The direct sequencing of PCR products, a bacterial colony (plasmid DNA), or a phage plaque (λDNA) is a very powerful technique in several molecular biological applications. Recently, we reported the successful application of this direct sequencing methodology, called recyclesequencing. Occasionally, however, our sequencing efforts failed due to the presence of agarose gel containing Luria-Bertani (LB) medium. Consequently, we pursued a semiquantitative investigation of the inhibitory effects of agarose and LB medium on the direct sequencing reaction. We found that LB medium concentrations greater than 26.7% inhibited the sequencing reaction. Furthermore, agarose concentrations greater than 0.20% in a reaction mixture also inhibited the sequencing reaction.
著者
酒井 一夫
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.126, no.10, pp.827-831, 2006 (Released:2006-10-01)
参考文献数
8
被引用文献数
10 18

“Hormesis” is defined, originally in the field of toxicology, as a phenomenon in which a harmful substance gives stimulating effects to living organisms when the quantity is small. The concept was extended and applied to ionizing radiation, high doses of which are harmful. Although radiation has been thought to be, based on findings in high dose ranges, harmful no matter low the dose is, recent investigation revealed that living organisms possess the ability to respond to low-dose radiation in very sophisticated ways. A good example of such responses is the so-called radiation adaptive response, a process in which acquired radioresistance is induced by low-dose radiation given in advance. The stimulation of certain bioprotective functions, including antioxidative capacity, DNA repair functions, apoptosis, and immune functions are thought to underly the adaptive response. The adaptive response is effective for chromosome induction, acute death, and tumorigenesis induced by high doses of radiation. Radiation hormesis and adaptive response provide a new scope in the risk assessment and medical application of ionizing radiation.
著者
国分 秀也 的場 元弘 山田 安彦 矢後 和夫
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.131, no.1, pp.113-127, 2011-01-01 (Released:2011-01-01)
参考文献数
89
被引用文献数
1 1

The pain experienced by cancer patients can be managed in 70-90% of cases by the World Health Organisation protocol for cancer pain. However, cancer pain treatment in Japan is not sufficiently effective. To use medicine safely and effectively, various problems must be solved. Therefore, in this study, appropriate usage of cancer pain treatment was examined. We were able to use acetaminophen suppositories (800 mg each) in cancer pain patients. It was suggested that high serum concentrations of oxycodone and hydrocotarnine might be observed in geriatric patients or in the state of decreased hepatic blood flow, making dose adjustment is necessary for such patients. We also clarified that the conversion ratio from oral oxycodone to intravenous ocycodone/hydrocotarnine was 0.71±0.12. In addition, we clarified the pharmacokinetics of controlled-release oxycodone in patients with cancer pain. Moreover, the findings of our study indicate that in the steady state, the serum concentrations of fentanyl are not maintained at a constant level for 3 days following the use of transdermal fentanyl. We established a method of appropriately passing a nasal duct for sustained release of fine granules of morphine sulfate. Resolution of the clinical problems associated with cancer pain treatments is anticipated to allow the proper use of cancer pain treatments in Japan.
著者
辻 彰
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.122, no.12, pp.1037-1058, 2002 (Released:2003-02-18)
参考文献数
148
被引用文献数
11 11

By incorporating the transporter-mediated or receptor-mediated transport process in physiologically based pharmacokinetic models, we succeeded in the quantitative prediction of plasma and tissue concentrations of β-lactam antibiotics, insulin, pentazocine, quinolone antibacterial agents, and inaperizone and digoxin. The author's research on transporter-mediated pharmacokinetics focuses on the molecular and functional characteristics of drug transporters such as oligopeptide transporter, monocarboxylic acid transporter, anion antiporter, organic anion transporters, organic cation/carnitine transporters (OCTNs), and the ATP-binding cassette transporters P-glycoprotein and MRP2. We have successfully demonstrated that these transporters play important roles in the influxes and/or effluxes of drugs in intestinal and renal epithelial cells, hepatocytes, and brain capillary endothelial cells that form the blood-brain barrier. In the systemic carnitine deficiency (SCD) phenotype mouse model, juvenile visceral steatosis (jvs) mouse, a mutation in the OCTN2 gene was found. Furthermore, several types of mutation in human SCD patients were found, demonstrating that OCTN2 is a physiologically important carnitine transporter. Interestingly, OCTNs transport carnitine in a sodium-dependent manner and various cationic drugs transport it in a sodium-independent manner. OCTNs are thought to be multifunctional transporters for the uptake of carnitine into tissue cells and for the elimination of intracellular organic cationic drugs.
著者
長島 弘明 増保 安彦
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.130, no.1, pp.49-54, 2010-01-01 (Released:2010-01-01)
参考文献数
19
被引用文献数
1 1

Monoclonal antibodies are being used as therapeutics for a number of cancers, such as leukemia, breast and colon cancers, and a lot of monoclonal antibodies specific for tumor-related antigens have been on clinical trials. Antibody-dependent cellular cytotoxicity (ADCC) is one of the major mechanisms by which antibodies exert anti-tumor effects. ADCC occurs through interaction between the Fc domains of IgG antibodies bound to target cells and Fcγ receptors on the surface of effector cells. In our study, a chimeric antibody, designated M-Ab, was constructed with the V regions from mouse anti-CD20 mAb 1F5 and the C regions from human IgG1 and κ chain. Two or three Fc domains were tandemly repeated downstream of the C-terminus of the M-Ab to give D0-Ab (Fc dimer Ab without a linker), T0-Ab (Fc trimer Ab without a linker), and T3-Ab (Fc trimer Ab with a (GGGGS)3 linker in front of the second and third hinge regions). Here, we show that Fc tandem repeat antibodies bind to all the low-affinity Fcγ receptors with very potent avidities and have greatly enhanced ADCC activity. T3-Ab is about 100 times more potent than the parental 1F5 chimeric antibody in terms of both Fcγ receptor binding and exerted ADCC activity at a 50-100 times less concentration as compared with the parental antibody. Thus, Fc tandem repeat antibodies are anticipated to be candidates for anti-tumor therapeutics and useful tools to elucidate the biological roles of Fcγ receptors.
著者
西村 信弘 土井 教雄 上村 智哉 竹谷 健 林 丈二 葛西 武司 金井 理恵 山口 清次 岩本 喜久生 直良 浩司
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.6, pp.759-766, 2009 (Released:2009-06-01)
参考文献数
21
被引用文献数
4 5

A traditional Chinese herbal medicine, Kampo medicine, maoto, has been widely used in the treatment of febrile symptoms caused by viral infection. This herbal extract granule for oral use, however, is not well accepted by infants or young children due to its unpleasant taste and odor. Therefore, we prepared Kampo medicine, maoto, suppository and investigated the pharmaceutical and clinical efficacy of the suppository. Kampo medicine, maoto, granules were micro-pulverized and homogeneously dispersed into Hosco-H15 to prepare suppositories containing 0.25 to 1.0 g herbal extract by the conventional fusion method. Content of l-ephedrine, an index compound of Kampo medicine, maoto, in the extract granules and suppositories was determined by using a high performance liquid chromatographic method. Physicochemical experiments revealed that the suppository containing 0.5 g herbal extract had the most suitable melting point of 34°C. Contents of l-ephedrine in the suppository were constant, 93-96% of those in the same amount of the extract granules in different three lots. Upper and lower portions of the suppository had the same content of l-ephedrine. The suppository maintained more than 95% of l-ephedrine content through 6 months at 4°C, room temperature and 40°C, although maldistribution of the extract constituent was observed after storage at 40°C. The suppository was administered to 21 pediatric febrile patients at a dose of 1/3 to 2 full pieces depending on their body weight and physical status. Significant reduction (p<0.001) of body temperature from 39.5 to 37.5°C without serious adverse effects was observed in 17 patients who were monitored the clinical effects on the febrile symptoms. In conclusion, Kampo medicine, maoto, suppository was found to satisfy the physicochemical quality and quantity standards as well as to be clinically applicable to neonates, infants and children with viral febrile symptoms without any adverse effects.
著者
佐藤 かな子 長井 二三子 青木 直人 西島 基弘
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.120, no.12, pp.1429-1433, 2000-12-01
被引用文献数
5

Alkyl p-hydroxybenzoates such as isobutyl p-hydroxybenzoate (PHBA-iBu), butyl p-hydroxybenzoate (PHBA-nBu), isopropyl p-hydroxybenzoate (PHBA-iPr), propyl p-hydroxybenzoate (PHBA-nPr), ethyl p-hydroxybenzoate (PHBA-Et), and methyl p-hydroxybenzoate (PHBA-Me) are widely used as preservatives, stabilizers and antiseptics for medical supplies, cosmetics, foodstuffs etc. We determined the binding affinity of alkyl p-hydroxybenzoates to human estrogen receptor α (ERα) and β (ERβ) by non-RI receptor binding assays. PHBA-iBu had a high binding affinity for ERα (IC_<50> : 6.0×10^<-6>M, the relative binding affinity (RBA) : 0.267) and ERβ (IC_<50> : 5.0×10^<-6>M, RBA : 0.340). These IC_<50> values and RBA were almost the same as those of bisphenol A. The ranking of the estrogenic potency of alkyl p-hydroxybenzoates for both ERs is different; that is, PHBA-iBu>PHBA-nBu≒PHBA-iPr≒PHBA-nPr>PHBA-Et≫PHBA-Me. Alkyl p-hydroxybenzoates bound with equal relative affinity to both ERα and β proteins. Alkyl p-hydroxybenzoate having a long alkyl side-chain showed a high affinity for ERα and β. These findings suggest that p-hydroxybenzoates may be endocrine disruptors.
著者
西岡 五夫 松尾 律子 大倉 洋甫 百瀬 勉
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.88, no.10, pp.1281-1285, 1968-10

A new colorimetric method for microdetermination of isothiocyanates was established, using 3,6-dinitrophthalic acid as a color developing agent in a potassium carbonatesodium thiosulfate solution. The reaction conditions were examined with allyl isothiocyanate as a model compound. The outline of the procedure is as follows : To 2.0 ml of allyl isothiocyanate solution (10-150 μg/ml), (dissolved in 50% ethylene glycol solution, 1.0 ml of 3,6-dinitrophthalic acid monopyridinium salt solution (0.1%), and 1.0 ml of alkaline solution (40% potassium carbonate and 30% sodium thiosulfate) are added and mixed well. The mixture is heated in a boiling water bath for exactly 10 minutes, cooled in running water, and diluted to 20.0 ml with water. The absorbance of the developed color is read at 400 mμ against the reagent blank. In this color reaction, 3,6-dinitrophthalic acid was assumed to be reduced to 3-amino-6-nitrophthalic acid by S^<2->, which was liberated from allyl isothiocyanate in the alkaline medium.
著者
石井 康子 谷澤 久之 滝野 吉雄
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.9, pp.904-910, 1988-09-25
被引用文献数
4

The mechanism of cathartic effect of barbaloin, representative of Aloe, was investigated by using male rats. Barbaloin administered orally was demonstrated to decompose to aloe-emodin-9-anthrone and aloe-emodin in the rat large intestine. And, these decomposed compounds were likely to change each other in the large intestine. Any compound of barbaloin, aloe-emodin-9-anthrone and aloe-emodin administered orally to rats was found to cause an obvious increase of water content in the large intestine, and only aloe-emodin-9-anthrone administered orally caused a significant increase of water content in the small intestine. Furthermore, the clear increase of water content and abnormality of electrolytes (Na^+, K^+) in the colon segment of rat were observed only by aloe-emodin-9-anthrone when compounds tested were injected directly into the colon segment. Therefore, it seemed that aloe-emodin-9-anthrone, a decomposition product of babaloin in the rat large intestine, caused an increase of water content in the large intestine by a different mechanism from the stimulation of peristalsis and this played an important role in cathartic activity of barbaloin.
著者
竹本 常松 醍醐 皓二 近藤 嘉和 近藤 一恵
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.86, no.10, pp.874-877, 1966-10-25

The NMR spectrum of domoic acid (in CF_3COOH) indicates signals for a methyl at 1.43 p.p.m. (d;J=6.6 c.p.s.) and at 1.94 p.p.m. (a broad singlet), and no signal for an ethyl group. The methyl signal at 1.94 p.p.m. shows a long-range I-I coupling due to spin decoupling. The NMR spectrum of trimethyl domoate (in CDCl_3) shows a doublet methyl (J=7.0 c.p.s.) at 1.29 p.p.m., a methyl signal which indicates an allylic coupling at 1.79 p.p.m., and an olefinic proton signal corresponding to 3H at 5.5〜6.6 p.p.m. From its first-order analysis, the configuration of the 1,3-hexadienyl side chain was determined as trans : trans : S-trans. The infrared spectra of both domoic acid and trimethyl domoate show absorption due to the trans-double bond. The NMR spectrum of tetrahydrodomoic acid (in CF_3COOH) shows signals for a methyl bonded to a secondary carbon at 1.12 p.p.m. (d;J=6.0 c.p.s.) and at 1.22 p.p.m. (d;J=6.6 c.p.s.). It was concluded from these observations that the structure of domoic acid would be more appropriately represented as L_s-arabo-2-carboxy-4-(1-methyl-5-carboxy-trans : trans : S-trans-1,3-hexadienyl)-3-pyrrolidineacetic acid (VIII) rather than the previously proposed L_s-arabo-2-carboxy-4-(1-methyl-2-carboxy-1,3-hexadieny1)-3-pyrrolidineacetic acid (I).
著者
北村 二朗 嶋 みな子 平塚 京子 浅野 進吾
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.6, pp.732-736, 1976-06-25

Examinations were made on the action of anhydromevalonic acid lactone, which inhibits incorporation of mevalonic acid into cholesterol in the cell-free system of rat liver, on microorganisms was studied. Microorganisms examined were mevalonic acid-requiring Lactobacillus acidphilus ATCC 4963 and L. heterohiochii H-1,and Saccharomyces cerevisiae and S. carlsbergensis ATCC 9080 which do not require mevalonic acid and have the ability to synthesize sterol. In the presence of 0.1 μg/ml of mevalonic acid, L. acidophilus required ca. 15 mg/ml of anhydromevalonic acid lactone for 50% suppression and 25 mg/ml for 100% suppression. In the presence of 1.0 or 4.0 μg/ml of mevalonic acid, L. heterohiochii required 0.5 and 20 mg/ml, respectively, of anhydromevalonic acid lactone. In the presence of 15 and 20 mg/ml of anhydromevalonic acid lactone the growth of S. cerevisiae and S. carlsbergensis was completely inhibited. However, there was hardly any effect on the sterol content per unit cell weight.
著者
原野 一誠
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.6, pp.469-489, 2005-06-01
被引用文献数
7

一昔前までは大型計算機センターの汎用計算機で実行していた科学技術計算がパーソナルコンピュータで実行できる時代を迎えた. 化学領域における分子軌道計算も例外ではなく, 非経験的分子軌道計算(ab initio)を実験室の片隅で実行している有り様である. 計算"器"化学と呼ばれるようになった所以である. 筆者らは, 長年合成反応において, 反応基質の反応性や生成物予測あるいは反応機構解析に分子軌道法を利用してきたが, 半経験的分子軌道計算法におけるパラメータの改善, さらには1998年ノーベル化学賞を授賞した密度汎関数法プログラムパッケージの開発により分子軌道計算が本格的実用化の段階に入ったと実感するに至った. 本稿では, thione-to-thiol転位反応を機軸として, ペリ環状反応を連続的に配置したカスケード反応を例に, 計算機化学の有用性を紹介したい. 2. チオン炭酸エステル類の熱反応 有機合成における著名な反応を集めた人名反応集にChugaev反応と呼ばれる反応がある. 本来オレフィン合成反応であるが, 最近ではほとんど利用されることはない.
著者
向後 麻里 斉藤 有深 柏原 由佳 小市 佳代子 市川 幾重 堀地 直也 今井 俊道 足立 満 村山 純一郎 木内 祐二
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.124, no.12, pp.973-981, 2004-12-01
被引用文献数
1 2

日本における肺癌罹患者数は増加傾向にあり, 男性では悪性腫瘍の中で死亡原因の1位となっている. 非小細胞肺癌(non-small-cell lung cancer:NSCLC)は早期診断, 早期切除が原則となってくるが, 進行性肺癌や小細胞肺癌(small-cell lung cancer:SCLC)に対しては外科的切除の適応は少なく, 強力な化学療法や放射線療法が実施されるものの, 5年生存率は1%未満である. 近年, 肺癌の化学療法は, cisplatin(CDDP)と他剤との併用療法が主流でありSCLCではetoposide(VP-16), irinotecan hydrochloride(CPT-11), NSCLCではvinorelbin tartarate(VNR), gemcitabin hydrochloride(GEM)などと併用されている. こうした併用化学療法を安全かつ効率的に実施するためのクリニカル, パス(パス)を用いることは有用と考えられるが, 国内ではいまだ十分には活用されていない. パスとは, 病棟でのチーム医療の「質」と「効率」を同時に保障するために考え出されたマネージメントツールであり, パス導入により, 医療の標準化, チーム医療の推進, 情報の共有などの効果が期待される.