著者

Yusuke Kono Hitomi Jinzai Yota Kotera Takuya Fujita

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

pp.b17-00563, (Released:2017-09-30)

参考文献数

48

被引用文献数

10

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The present study aimed to investigate the effect of particle size (100 and 500 nm), surface charge (cationic, neutral and anionic) and polyethylene glycol (PEG) modification of magnetic liposomes on their interaction with the human intestinal epithelial cell line, Caco-2. The cellular associated amount of all the magnetic liposomes was significantly increased by the presence of a magnetic field. The highest association and internalization into Caco-2 cells was observed with magnetic cationic liposomes. Moreover, small magnetic liposomes were more efficiently associated and taken up into the cells, than large ones. In contrast, PEG modification significantly attenuated the enhancing effect of the magnetic field on the cellular association of magnetic liposomes. We also found that magnetic cationic liposomes had the highest retention properties to Caco-2 cells. Moreover, the retention of large magnetic liposomes to the cells was much longer than that of small ones. In addition, magnetic cationic and neutral liposomes had relatively high stability in Caco-2 cells, whereas magnetic anionic liposomes rapidly degraded. These results indicate that the physicochemical properties and PEG modification of magnetic liposomes greatly influences their intestinal epithelial transport.

著者

Shuichi Mori Ryohei Takagaki Shinya Fujii Ko Urushibara Aya Tanatani Hiroyuki Kagechika

出版者

公益社団法人日本薬学会

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.65, no.11, pp.1051-1057, 2017-11-01 (Released:2017-11-01)

参考文献数

39

被引用文献数

3

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The progesterone receptor (PR) controls various physiological processes, including the female reproductive system, and nonsteroidal PR ligands are considered to be drug candidates for treatment of various diseases without significant adverse effects. Here, we designed and synthesized m-carborane-based secondary alcohols and investigated their PR-ligand activity. All the synthesized alcohols exhibited PR-antagonistic activity at subnanomolar concentration. Among them, alcohols having a small alkyl side chain and a 4-cyanophenyl group also exhibited PR-agonistic activity in a relatively high concentration range. Optical resolution of secondary alcohols having a methyl side chain was performed, and the PR-ligand activity and PR-binding affinity of the purified enantiomers were examined. The chirality of the secondary alcohol appears to have a more significant influence on PR-agonistic activity than on antagonistic activity.

著者

Ryo Iketani Yohei Kawasaki Hiroshi Yamada

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.40, no.11, pp.1976-1982, 2017-11-01 (Released:2017-11-01)

参考文献数

43

被引用文献数

12

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We performed a systematic review and Bayesian network meta-analysis to determine atypical antipsychotics that are effective and safe for the treatment of psychosis in Parkinson’s disease (PD). We conducted a comprehensive literature search using PubMed/MEDLINE, Cochrane Library, and Japana Centra Revuo Medicina (Ichu-shi Web). We used randomized controlled trials evaluating the utility of atypical antipsychotics for the treatment of psychosis in PD using the Brief Psychiatric Rating Scale (BPRS) and the Unified PD rating Scale parts III (UPDRS-III) as the endpoints. Posterior distributions of mean differences between each treatment and placebo were estimated using Bayesian network meta-analysis. The distributions describing each treatment effect were expressed as means (95% credible intervals). Ten trials involving any two treatment arms using clozapine (64 subjects in four trials), olanzapine (99 subjects in three trials), quetiapine (79 subjects in five trials), risperidone (five subjects in one trial), or placebo (156 subjects in seven trials) were finally included in the present study. Pooled estimates of each posterior distribution based on the BPRS were as follows: clozapine, −2.0 (−6.7 to 2.7); olanzapine, 0.5 (−2.3 to 3.4); quetiapine, 0.3 (−3.9 to 4.5); and risperidone, −4.7 (−57.4 to 53.3). Based on the UPDRS-III, the pooled estimates were clozapine, 0.7 (−3.8 to 4.3); olanzapine, 2.8 (0.8 to 5.1); quetiapine, 3.3 (−0.7 to 5.8); and risperidone, 4.5 (−57.7 to 63.4). Although clozapine had an effective and relatively safe profile, all atypical antipsychotics included in the present study may be unsafe, as they may worsen motor function when compared to placebo.

著者

世取山守 岡田 安雄 鈴木 邦夫

出版者

公益社団法人日本薬学会

雑誌

衛生化学 (ISSN:0013273X)

巻号頁・発行日

vol.38, pp.471-475, 1992

被引用文献数

2

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Cannabis oil (1 g) was extracted with n-hexane-saturated acetonitrile, and 91% of oil was removed by this method. Cannabinoids in extracted cannabis oil were identified by high performance thin layer chromatography (HPTLC) and capillary gas chromatography-mass spectrometry (GC-MS). The cannabinoid contents were determined by capillary gas chromatography (GC) using 5α-cholestane as an internal standard. Contents of CBD in the cannabis oil were 121±17 μg/g. However, other cannabinoids (THC and CBN) were not detected in this cannabis oil by HPTLC, GC-MS or GC.

著者

Kosuke Chiba Yuichi Hashimoto Takao Yamaguchi

出版者

公益社団法人日本薬学会

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.65, no.10, pp.994-996, 2017-10-01 (Released:2017-10-01)

参考文献数

16

被引用文献数

3

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We recently developed 4-azidophthalimide (AzPI) as a compact fluorogenic photoreactive tag that can be attached to ligands to achieve selective fluorescence labeling of target proteins even in the presence of a large excess of non-target proteins. To further establish the utility of the AzPI tag, we focused here on streptavidin labeling with biotin–AzPI conjugates, and evaluated the relation between the amount of covalently labeled streptavidin (labeling rate) and fluorescence intensity. The labeling rate was proportional to the fluorescence intensity under standardized photo-irradiation conditions. Prolongation of the photo-irradiation time led to a marked increase in the labeling rate, but this was accompanied by a gradual decrease in the fluorescence intensity, which appeared to be due at least in part to photo-induced degradation of the target streptavidin. These findings should be helpful for achieving sensitive fluorescence detection of target proteins by using the AzPI tag.

著者

Charith UB Wijerathne Hee-Seon Park Hye-Yun Jeong Ji-Won Song Og-Sung Moon Young-Won Seo Young-Suk Won Hwa-Young Son Jong-Hwan Lim Sung-Hum Yeon Hyo-Jung Kwun

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

pp.b17-00468, (Released:2017-09-22)

参考文献数

46

被引用文献数

24

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Quisqualis indica (QI) has been used for treating disorders such as stomach pain, constipation, and digestion problem. This study was aimed to evaluate the therapeutic efficacy of QI extract on treating benign prostatic hyperplasia (BPH) in LNCaP human prostate cancer cell line and a testosterone-induced BPH rat model. LNCaP cells were treated with QI plus testosterone propionate (TP), and androgen receptor (AR) and prostate specific antigen (PSA) expression levels were assessed by Western blotting. To induce BPH, the rats were subjected to a daily subcutaneous injection of TP (3 mg/kg) for 4 wk. The rats in treatment group were orally gavaged with QI (150mg/kg) together with the TP injection. In-vitro studies showed that TP-induced increases in AR and PSA expression in LNCaP cells were reduced by QI treatment. In BPH-model rats, the prostate weight, testosterone in serum, DHT concentration and 5α-reductase mRNA expression in prostate tissue were significantly reduced following the treatment with QI. TP-induced prostatic hyperplasia and the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 were significantly attenuated in QI-treated rats. In addition, QI induced apoptosis by up-regulating caspase-3 and -9 activity and decreasing the B-cell lymphoma 2 (Bcl-2)/Bcl-2-associated X protein (Bax) ratio in prostate tissues of BPH rats. Further investigation showed that TP-induced activation of AKT and glycogen synthase kinase 3β (GSK3β) was reduced by QI administration. Therefore, our findings suggest that QI attenuates the BPH state in rats through anti-proliferative and pro-apoptotic activities and might be useful in the clinical treatment of BPH.

著者

Akihiko Ikoma

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.36, no.8, pp.1235-1240, 2013-08-01 (Released:2013-08-01)

参考文献数

70

被引用文献数

8 20

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The unique physiological features of histamine-sensitive C-fibers and spinothalamic tract neurons support the hypothesis of itch specific pathway, whereas subsequent studies on cowhage-induced itch have provided evidence against it, suggesting the presence of multiple neural pathways for itch. Not only peripheral pruritogens but also spinal neural receptors are involved in the control of itch, and will be the target of treatment. Itch sensitization in chronic pruritus is another crucial factor that needs to be considered in the treatment. Neuropathic itch is the type of itch that occurs when nerve fibers are damaged or injured and spontaneous firing of nerves takes place, and plays a major role in itch accompanying some pathological conditions such as herpes zoster. The complexity of itch is due to the broad range of mediators involved and the large variety of neural mechanisms behind.

著者

津島 己幸 真岡 孝至 勝山 政明 小塚 睦夫 松野 隆男 徳田 春邦 西野 輔翼 岩島 昭夫

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.18, no.2, pp.227-233, 1995-02-15 (Released:2008-04-10)

参考文献数

26

被引用文献数

43 77

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As a screening study for anti-tumor promoters, 51 carotenoids with diverse structures were examined for their inhibitory effects on the Epstein-Barr virus activation activity of 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. The results showed that most of the carotenoids exhibited inhibitory activity, and in general, no cytotoxicity on Raji cells was observed in the assay. Among the carotenoids, β-cryptoxanthin, lutein, and lactucaxanthin showed the strongest inhibitory activity, superior to the well known anti-tumor promoter, β-carotene. Heteroxanthin, peridinin, and halocynthiaxanthin showed cytotoxicity at the high concentration (1000 molar ratio per TPA), but indicated a strong inhibitory effect at the lower concentrations, which were only weakly toxic (500 and 100 molar ratios). Based on these results, the essential moiety for the activity of carotenoids was considered to be the 3-hydroxy-ε-end group.

著者

Hitomi Ozawa Atsushi Imaizumi Yoshihiko Sumi Tadashi Hashimoto Masashi Kanai Yuji Makino Takanori Tsuda Nobuaki Takahashi Hideaki Kakeya

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.40, no.9, pp.1515-1524, 2017-09-01 (Released:2017-09-01)

参考文献数

50

被引用文献数

35

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Curcumin, a polyphenol derived from the rhizome of the naturally occurring plant Curcuma longa, has various pharmacological actions such as antioxidant and anti-inflammatory effects. In this paper, we evaluated the role of its internal metabolite, curcumin β-D-glucuronide (curcumin monoglucuronide, CMG), by investigating curcumin kinetics and metabolism in the blood. Firstly, we orally administered highly bioavailable curcumin to rats to elucidate its kinetics, and observed not only the free-form of curcumin, but also, curcumin in a conjugated form, within the portal vein. We confirmed that curcumin is conjugated when it passes through the intestinal wall. CMG, one of the metabolites, was then orally administered to rats. Despite its high aqueous solubility compared to free-form curcumin, it was not well absorbed. In addition, CMG was injected intravenously into rats in order to assess its metabolic behavior in the blood. Interestingly, high levels of free-form curcumin, thought to be sufficiently high to be pharmacologically active, were observed. The in vivo antitumor effects of CMG following intravenous injection were then evaluated in tumor-bearing mice with the HCT116 human colon cancer cell line. The tumor volume within the CMG group was significantly less than that of the control group. Moreover, there was no significant loss of body weight in the CMG group compared to the control group. These results suggest that CMG could be used as an anticancer agent without the serious side effects that most anticancer agents have.

著者

水柿道直 大山 良治 木村 勝彦 石橋 正兀 大野 曜吉 内間 栄行 永盛 肇 鈴木 康男

出版者

公益社団法人日本薬学会

雑誌

衛生学 (ISSN:0013273X)

巻号頁・発行日

vol.34, pp.359-365, 1988

被引用文献数

2

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A gas chromatography/selected ion monitoring (GC/SIM) method for the simultaneous determination of aconitum alkaloids such as aconitine, mesaconitine and hypaconitine has been developed. Aconitum alkaloids were converted to their TMS ether derivatives by treatment with N, O-bis (trimethylsilyl) trifluoroacetamide in pyridine at room temperature. The gas chromatograms of reaction products showed in each case a well-resolved doublet consisting of a major (>70%) and a minor components, when analyzed using a 5%-phenylmethylsilicone cross-linked fused silica capillary column. These alkaloid derivatives gave simplified mass spectra with a base peak at m/z 698 for aconitine, m/z 684 for mesaconitine and m/z 596 for hypaconitine. When GC/SIM of aconitine was carried out under monitoring of the ion at m/z 698,detection limit was 10 picograms with signal-to-noise ratio of greater than 10. Linearity was obtained over a range from at least 10 to 1000pg. Similar results were obtained with another alkaloids. The use of this method for the measurement of aconitum alkaloids in biological fluids is described.

著者

小村 弘 茂本 友貴枝 河原 亥一郎 松田 健一 阿野 理恵子 村山 洋子 森脇 俊哉 吉田 長弘

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 = Journal of the Pharmaceutical Society of Japan (ISSN:00316903)

巻号頁・発行日

vol.125, no.1, pp.141-147, 2005-01-01

参考文献数

27

被引用文献数

1 2

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コンビナトリアルケミストリーの発展により化合物ライブラリーの数は百万を越え, 週に何十万もの化合物が多くの生物学的ターゲットに対してスクリーニングされている. これに伴い多くのリード化合物が見出されている. さらに開発候補品のディベロッパビリティにおいて動態代謝特性が重要な要因の1つであるとの認識が深まり,優れた薬物動態プロファイルを伴った開発候補品を見出すため探索動態グループに対する要求が年々高まってきている.このような状況下において, 溶解性, Caco-2膜透過性及び代謝安定性試験などについてハイスループットスクリーニング(HTS)への取り組みが行われてきた. しかしながら, 探索動態試験におけるHTSは時間と労力を必要とし, 評価できる化合物の数は最大でも生物学的ターゲットに対するHTSの1/100から1/10000と限られている. 近年, 合成化合物の体内動態特性を予測するためのin silicoモデルが検討されている.特にpolar surface area(PSA), molecular weight(MW), 脂溶性(logP)及びhydrogen bonding(HB)の数などの種々のパラメータが用いられ, 薬物の膜透過性又は経口吸収性の予測が試みられている.

著者

小村 弘 松田 健一 茂本 友貴枝 河原 亥一郎 阿野 理恵子 村山 洋子 森脇 俊哉 吉田 長弘

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 = Journal of the Pharmaceutical Society of Japan (ISSN:00316903)

巻号頁・発行日

vol.125, no.1, pp.131-139, 2005-01-01

参考文献数

25

被引用文献数

1 3

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肝臓での代謝安定性は経口吸収性とともに生体内利用率に影響する重要な因子であり, その最適化は多くのプロジェクトにおける最重要課題の1つである. 一般に代謝試験には肝ミクロソーム系又は単離肝細胞系が用いられている. 肝細胞系はphaseI及びII代謝活性, さらに肝取り込みや胆汁排泄に関与する膜輸送系を有しており, 開発候補品を初め薬物の詳細な代謝検討に使用されている.しかし非凍結及び凍結ヒト肝細胞の場合コストが高く付くこと, またロット間の代謝活性の個体差が大きいこと, そしてロボットへの適応が難しいことから, 創薬の初期スクリーニングには適していないものと考えられる. 一方, 肝ミクロソーム系では細胞質の酵素によるphaseI及び硫酸抱合活性などのphaseII代謝を測定することができないが, 主代謝酵素であるcytochromeP450(CYP)活性が存在し,いずれの種についてもミクロソームを容易に入手できる. 特にヒトではハイスループットスクリーニング用として多くのドナーから調製されたミクロソームが市販されている.

著者

小村 弘 河原 亥一郎 茂本 友貴枝 松田 健一 阿野 理恵子 村山 洋子 森脇 俊哉 吉田 長弘

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 = Journal of the Pharmaceutical Society of Japan (ISSN:00316903)

巻号頁・発行日

vol.125, no.1, pp.121-130, 2005-01-01

参考文献数

27

被引用文献数

2 5

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経口吸収性は生体内利用率に影響する重要なファクターの1つであり, ヒトでの低い吸収率さらにはその個体間の大きなバラツキは, 開発候補品のディベロッパビリティーを大きく低下させる. 近年コンビナトリアルケミストリー及びハイスループットスクリーニング(HTS)の導入は幅広い生物学的ターゲットに対して効率的にリード化合物の創出を可能にしてきたが, リード化合物の経口吸収性を初め体内動態に関わる物性を悪化させた. したがって, 創薬において吸収性に優れた開発候補品を創製するためにはリード化合物の最適化が必要となる. 吸収性は主に水に対する溶解性と膜透過性が大きく関わっており, これらのスクリーニング系が開発されてきた.近年その処理能力を上げるため, より簡便な比濁分析法や溶液沈殿法を用いた溶解性試験, さらにはCaco-2細胞の短期間培養法, N in one 及び96 well formatを用いた透過性試験系が採用されている.

著者

朝比 奈泰彦 上野 周

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

no.408, pp.146-159, 1916-02-26

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著者等は甘茶の甘味成分たる結晶性物質の化學的研究を行ひ之をフヰロヅルチンと命名し各種誘導體及分解成績物の檢査によりて一種の構造式を提出せり

著者

岩村 武勇

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.8, no.4, pp.217-220, 1972-04-15

著者

Mitsuyoshi Okita Yuki Yayoshi Kousuke Ohara Akio Negishi Hayato Akimoto Naoko Inoue Sachihiko Numajiri Shigeru Ohshima Seiichi Honma Shinji Oshima Daisuke Kobayashi

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

pp.b17-00340, (Released:2017-08-04)

参考文献数

21

被引用文献数

3

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Kakkonto (KK), a traditional Japanese Kampo formulation for cold and flu, is generally sold as an over-the-counter (OTC) pharmaceuticals used for self-medication. Kampo formulations should be used according to the Sho-symptoms of Kampo medicine. These symptoms refer to the subjective symptoms themselves. Although with OTC pharmaceuticals, this is often not the case. We surveyed the relationship of agreement of Sho with the benefit feeling rate (BFR) of patients who took KK (n = 555), cold remedies with KK (CK, n = 315), and general cold remedies (GC, n = 539) using internet research. BFR of a faster recovery was greater in participants who took the medication early and who had confidence in their physical strength in all treatment groups. BFR was significantly higher in the GC group than in the KK group for patients with headache, runny nose, blocked nose, sneezing, and cough. BFR was also significantly higher in the GC group than in the CK group for headache (males) and cough (females). BFR was the highest in the KK group for stiff shoulders. All cold remedies were more effective when taken early, and the larger the number of Sho that a patient had, the greater the BFR increased. Therefore, a cold remedy is expected to be most effective when there are many cold symptoms and when it is taken at an early stage of the common cold.

著者

Mina Thon Toru Hosoi Chanbora Chea Koichiro Ozawa

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.40, no.8, pp.1161-1164, 2017-08-01 (Released:2017-08-01)

参考文献数

37

被引用文献数

6

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The lack of response to leptin’s actions in the brain, “leptin resistance,” is one of the main causes of the pathogenesis of obesity. However, although high-fat diets affect sensitivity to leptin, the underlying mechanisms of leptin resistance are still an enigma. Here we examined the effect of excess saturated fatty acids (SFAs) on leptin signaling in human neuronal cells. Palmitate, the principle source of SFAs in diet, induced leptin resistance in a human neuroblastoma cell line stably transfected with the Ob-Rb leptin receptor (SH-SY5Y-ObRb). We next investigated the function of stearoyl-CoA desaturase-1 (SCD1), an enzyme which converts SFAs into monounsaturated fatty acids (MUFAs), on leptin-induced signaling. We found that reduction of SCD1 activity, through SCD1 inhibition and knockdown, impairs leptin-induced signal transducer and activator of transcription 3 (STAT3) phosphorylation in human neuronal cells. Our findings suggested that SCD1 plays a key role in the pathophysiology of leptin resistance in neuronal cells associated with obesity.

著者

Ryota Tanaka Yuhki Sato Koji Goto Norihisa Yasuda Yoshifumi Ohchi Yosuke Suzuki Tamio Ueno Kentaro Ito Tetsuya Kaneko Shusaku Kurogi Ko Nonoshita Hiroki Itoh

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.40, no.8, pp.1226-1231, 2017-08-01 (Released:2017-08-01)

参考文献数

28

被引用文献数

6

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Doripenem (DRPM) is a broad-spectrum antibacterial agent often used as empirical therapy for critically ill patients, although there is a lack of studies validating the recommended dosage regimen for patients admitted to intensive care unit (ICU), based on pharmacokinetic (PK)/pharmacodynamic (PD) index. In this study, we estimated the free time above minimum inhibitory concentration (fT>MIC (%)) of DRPM using population PK analysis of 12 patients in ICU, and evaluated the validity of the dosage regimen stratified by creatinine clearance. Using a 2-compartment population PK model reported previously, the mean total clearance or distribution volume of DRPM estimated by Bayesian estimation was significantly lower or higher than that of based on population PK model. The estimated fT>MIC (%) of the recommended standard (normal renal function: 0.5 g every 8 h, moderate: 0.25 g every 8 h, severe renal impairment: 0.25 g every 12 h) and higher doses (normal: 1.0 g every 8 h, moderate: 0.5 g every 8 h, severe: 0.25 g every 8 h) against MICs of 0.5, 1 and 2 µg/mL exceeded 40% in all patients. When stratified by creatinine clearance, the PK/PD breakpoints estimated by Monte Carlo simulation in three grades of renal function tended to be higher than the previously reported PK/PD breakpoints for patients with urinary tract infection, an infection of lesser severity than ICU patients. These results suggest that the dosage regimen stratified by renal function derived from Japanese package insert may be sufficient to achieve effective treatment in ICU patients.

著者

山田 耕史

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 = Journal of the Pharmaceutical Society of Japan (ISSN:00316903)

巻号頁・発行日

vol.122, no.12, pp.1133-1143, 2002-12-01

参考文献数

67

被引用文献数

4 17

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Glycosphingolipids (GSLs), together with glycopeptides, are typical constituents of various cell membranes in a wide variety of organisms. In particular, it is known that GSLs have numerous physiological functions due to variations in the sugar chain, in spite of the very small quantity of constituents. Those are classified into cerebrosides, sulfatides, ceramide oligohexosides, globosides, and gangliosides based on the constituent sugars. Gangliosides, sialic acid-containing GSLs, are especially enriched in the brain and nervous tissues and are involved in the regulation of many cellular events. Recently, a number of GSLs have been isolated from marine invertebrates such as echinoderms, poriferans, and mollusks. We have also been researching biologically active GSLs from echinoderms to elucidate the structure-function relationships of GSLs and to develop novel medicinal resources. This review summarizes the structures and biological activities of GSLs from sea cucumbers. This study showed that the characteristics of GSLs and structure-activity relationships had neuritogenic activity toward the rat pheochromocytoma cell line PC12. That is, most of the cerebroside constituents of the sea cucumber are same glucocerebrosides as in other animals, except for some constituents, while the ganglioside constituents were unique in that a sialic acid directly binds to the glucose of cerebroside, they are mutually connected in tandem, and some are located in the internal parts of the sugar chain. It also became apparent that sialic acid is indispensable for the neuritogenic activities.<br>

著者

Renata Grespan Marcia Paludo Henrique de Paula Lemos Carmem Patrícia Barbosa Ciomar Aparecida Bersani-Amado Marcia Machado de Oliveira Dalalio Roberto Kenji Nakamura Cuman

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.35, no.10, pp.1818-1820, 2012-10-01 (Released:2012-10-01)

参考文献数

11

被引用文献数

8 37

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This study was designed to test the efficacy of eugenol, a compound obtained from the essential oil of cloves (Syzygium aromaticum) in collagen-induced arthritis (CIA), a well characterized murine model of rheumatoid arthritis. Macroscopic clinical evidence of CIA manifests first as periarticular erythema and edema in the hind paws. Treatment with eugenol starting at the onset of arthritis (day 25) ameliorated these clinical signs of CIA. Furthermore, eugenol inhibited mononuclear cell infiltration into the knee joints of arthritic mice and also lowered the levels of cytokines (tumor necrosis factor (TNF)-α, interferon (IFN)-γ and tumor growth factor (TGF)-β) within the ankle joints. Eugenol treatment did not affect the in vitro cell viability as assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Therefore, eugenol ameliorates experimental arthritis and could be useful as a beneficial supplement in treating human arthritis.