cycloserine

サイクロセリン  

WordNet

  1. an antibiotic that is especially active against the tubercle bacillus

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/09/15 22:37:16」(JST)

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English Journal

  • Resveratrol induced ER expansion and ER caspase-mediated apoptosis in human nasopharyngeal carcinoma cells.
  • Chow SE1, Kao CH, Liu YT, Cheng ML, Yang YW, Huang YK, Hsu CC, Wang JS.Author information 1Department of Nature Science Center for General Studies, Chang Gung University, Taoyuan, Taiwan, chowse@mail.cgu.edu.tw.AbstractAutophagy and endoplasmic reticulum (ER) stress response is important for cancer cells to maintain malignancy and resistance to therapy. trans-Resveratrol (RSV), a non-flavonoid agent, has been shown to induce apoptosis in human nasopharyngeal carcinoma (NPC) cells. In this study, the involvements of tumor-specific ER stress and autophagy in the RSV-mediated apoptosis were investigated. In addition to traditional autophagosomes, the images of transmission electron microscopy (TEM) indicated that RSV markedly induced larger, crescent-shaped vacuoles with single-layered membranes whose the expanded cisternae contains multi-lamellar membrane structures. Prolonged exposure to RSV induced a massive accumulation of ER expansion. Using an EGFP-LC3B transfection and confocal laser microscopy approach, we found RSV-induced EGFP-LC3 puncta co-localized with ER-tracker red dye, implicating the involvement of LC3II in ER expansion. The proapoptotic effect of RSV was enhanced after suppression of autophagy by ATG7 siRNA or blocking the autophagic flux by bafilomycin A1, but that was not changed after targeted silence of IRE1 or CHOP by siRNA. Using caspase inhibitors, we demonstrated the upregulation of caspase-12 (casp12) and the activation of casp4 were associated with the proapoptotic induction of RSV through the caspase-9/caspase-3 pathway. Intriguingly, siRNA knockdown of casp12, but not caspase-4, decreased the susceptibility of the NPC cells to RSV-mediated apoptosis. Further, we showed that RSV dose-dependently increased the ceramide accumulation as assessed by LC-MS/MS system. Using serine palmitoyltransferase (SPT, a key enzyme of de novo ceramide biosynthesis) inhibitors (L-cycloserine and myriocin), we found the increased ceramide accumulation was strongly correlated with the proapoptotic potential of RSV. This study revealed the ER expansion and upregulation of ER casp12 together may indicate profound biological effects of RSV and contributed to NPC cell death. Targeting the different status of ER stress may provide a possible strategy for cancer treatments.
  • Apoptosis : an international journal on programmed cell death.Apoptosis.2014 Mar;19(3):527-41. doi: 10.1007/s10495-013-0945-0.
  • Autophagy and endoplasmic reticulum (ER) stress response is important for cancer cells to maintain malignancy and resistance to therapy. trans-Resveratrol (RSV), a non-flavonoid agent, has been shown to induce apoptosis in human nasopharyngeal carcinoma (NPC) cells. In this study, the involvements o
  • PMID 24264887
  • The role of the medial prefrontal cortex in regulating social familiarity-induced anxiolysis.
  • Lungwitz EA1, Stuber GD2, Johnson PL3, Dietrich AD4, Schartz N4, Hanrahan B4, Shekhar A5, Truitt WA3.Author information 11] Graduate Program in Medical Neuroscience, Indiana University School of Medicine, Indianapolis, IN, USA [2] Stark Neurosciences Research Institute, Indiana University School of Medicine, Indianapolis, IN, USA.2Departments of Psychiatry & Cell Biology and Physiology; UNC Neuroscience Center and Bowles Center for Alcohol Studies, University of North Carolina at Chapel Hill, NC, USA.31] Stark Neurosciences Research Institute, Indiana University School of Medicine, Indianapolis, IN, USA [2] Department of Anatomy and Cellular Biology, Indiana University School of Medicine, Indianapolis, IN, USA [3] Department of Psychiatry, Institute of Psychiatric Research, Indiana University School of Medicine, Indianapolis, IN, USA.4Department of Anatomy and Cellular Biology, Indiana University School of Medicine, Indianapolis, IN, USA.51] Stark Neurosciences Research Institute, Indiana University School of Medicine, Indianapolis, IN, USA [2] Department of Psychiatry, Institute of Psychiatric Research, Indiana University School of Medicine, Indianapolis, IN, USA [3] Indiana Clinical and Translational Sciences Institute, Indiana University School of Medicine, Indianapolis, IN, USA.AbstractOvercoming specific fears and subsequent anxiety can be greatly enhanced by the presence of familiar social partners, but the neural circuitry that controls this phenomenon remains unclear. To overcome this, the social interaction (SI) habituation test was developed in this lab to systematically investigate the effects of social familiarity on anxiety-like behavior in rats. Here, we show that social familiarity selectively reduced anxiety-like behaviors induced by an ethological anxiogenic stimulus. The anxiolytic effect of social familiarity could be elicited over multiple training sessions and was specific to both the presence of the anxiogenic stimulus and the familiar social partner. In addition, socially familiar conspecifics served as a safety signal, as anxiety-like responses returned in the absence of the familiar partner. The expression of the social familiarity-induced anxiolysis (SFiA) appears dependent on the prefrontal cortex (PFC), an area associated with cortical regulation of fear and anxiety behaviors. Inhibition of the PFC, with bilateral injections of the GABAA agonist muscimol, selectively blocked the expression of SFiA while having no effect on SI with a novel partner. Finally, the effect of D-cycloserine, a cognitive enhancer that clinically enhances behavioral treatments for anxiety, was investigated with SFiA. D-cycloserine, when paired with familiarity training sessions, selectively enhanced the rate at which SFiA was acquired. Collectively, these outcomes suggest that the PFC has a pivotal role in SFiA, a complex behavior involving the integration of social cues of familiarity with contextual and emotional information to regulate anxiety-like behavior.
  • Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.Neuropsychopharmacology.2014 Mar;39(4):1009-19. doi: 10.1038/npp.2013.302. Epub 2013 Oct 25.
  • Overcoming specific fears and subsequent anxiety can be greatly enhanced by the presence of familiar social partners, but the neural circuitry that controls this phenomenon remains unclear. To overcome this, the social interaction (SI) habituation test was developed in this lab to systematically inv
  • PMID 24157502
  • Design, Synthesis and Antimycobacterial Activity of Some New Pyridazine Derivatives: Bis-Pyridazine. Part IV12-14.
  • Mantu D, Antoci V, Mangalagiu II1.Author information 1Al. I. Cuza" University of Iasi, Faculty of Chemistry, Bd. Carol 11, 700506 Iasi, Romania. ionelm@uaic.ro.AbstractThe design, synthesis, structure and the antimycobacterial activities of a new class of nitrogen heterocycles, namely N1-substituted-diphenyl ether-bis-pyridazine (BP), is presented. An efficient, facile and straight applicable method for preparation of BP derivatives is described. The primary cycle high throughput screening reveals that two BP compounds, 2a and 3b, are potent inhibitors against Mycobacterium tuberculosis (Mtb), their antitubercular activity being superior to the second-line antitubercular drug Pyrimethamine and equal to Cycloserine. The data from cycle-2 screening confirm the results from cycle-1.The MIC, MBC, LORA, intracellular (macrophage) drug screening, and MTT cell proliferation, indicate the intracellular drug effectiveness against Mtb of these compounds, the lack of toxicity, a significant activity against both replicating and non-replicating Mtb and, a bactericidal mechanism of action (for 2b). SAR correlations have been done. Overall, the BP derivatives and especially compound 2b, appeared as a new leading antitubercular structure, which makes it a promising lead for further drug development.
  • Infectious disorders drug targets.Infect Disord Drug Targets.2014 Feb 17. [Epub ahead of print]
  • The design, synthesis, structure and the antimycobacterial activities of a new class of nitrogen heterocycles, namely N1-substituted-diphenyl ether-bis-pyridazine (BP), is presented. An efficient, facile and straight applicable method for preparation of BP derivatives is described. The primary cycle
  • PMID 24552228

Japanese Journal

  • 精神疾患の治療法としての記憶操作 (特集 WFSBP2013シンポジウム)
  • 武田 雅俊
  • 日本生物学的精神医学会誌 = Japanese journal of biological psychiatry 25(3), 149-151, 2014
  • NAID 40020239876
  • 1P-069 O-ウレイド-L-セリン合成酵素DcsDの活性発現に重要なアミノ酸残基の特定(酵素学,酵素工学,一般講演)
  • 宇田 成利,的場 康幸,小田 康祐,熊谷 孝則,野田 正文,杉山 政則
  • 日本生物工学会大会講演要旨集 65, 35, 2013-08-25
  • NAID 110009737449
  • 1P-015 D-サイクロセリンの生合成においてN^ω-ヒドロキシ-L-アルギニンの生成に関与するdcsA遺伝子の解析(遺伝子工学,一般講演)
  • 熊谷 孝則,高木 紀抄,的場 康幸,野田 正文,杉山 政則
  • 日本生物工学会大会講演要旨集 65, 21, 2013-08-25
  • NAID 110009737395

Related Links

These psychotropic responses are related to D-cycloserine's action as a partial agonist of the neuronal NMDA receptor for glutamate and have been examined in implications with sensory-related fear extinction in the amygdala, and extinction ...


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★リンクテーブル★
リンク元抗菌薬」「抗結核薬」「CS」「サイクロセリン

抗菌薬」

  [★]

antibacterial drug, antibacterial
抗生剤薬理学抗菌薬一覧抗細菌薬
first aid step 1 2006 p.165

定義

  • 細菌/微生物に静菌作用、殺菌作用を示す物質。結果として、人において病原性を除去する目的で使用される。
  • このうち、微生物によって産生される物質を抗生物質と呼ぶ


作用機序による分類

first aid step 1 2006 p.165
  Mechanism of action Drugs
1 Block cell wall synthesis by inhibition of peptidoglycan cross-linking penicillin, ampicillin, ticarcillin, piperacillin, imipenem, aztreonam, cephalosporins
2 Block peptidoglycan synthesis bacitracin, vancomycin, cycloserine
3 Disrupt bacterial/fungal cell membranes polymyxins
4 Disrupt fungal cell membranes amphotericin B, nystatin, fluconazole/azoles
5 Block nucleotide synthesis sulfonamides, trimethoprim
6 Block DNA topoisomerases quinolones
7 Block mRNA synthesis rifampin
8 Block protein synthesis at 50S ribosomal subunit chloramphenicol, erythromycin/macrolides, lincomycin, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid
9 Block protein synthesis at 30S ribosomal subunit aminoglycosides, tetracyclines, spectinomycin
 ATuSi → あつし


薬物動態

  • 濃度依存性:アミノグリコシド系抗菌薬、ニューロキノロン系抗菌薬
  • 時間依存性:βラクタム系抗菌薬

治療期間

小児

尾内一信 ; 第 39 回日本小児感染症学会教育講演 2 小児感染症の抗菌薬療法 -耐性菌時代の適正使用-
感染臓器・臨床診断 原因菌 投与期間(抗菌薬)
髄膜炎 インフルエンザ菌 7-10日
肺炎球菌 10-14日
髄膜炎菌 7-10日
GBS,腸内細菌,リステリア 21日
中耳炎 <2 歳 10日
2 歳≦ 5-7日
咽頭炎 A 群連鎖球菌 10日(ペニシリン系薬)
5日(セフェム系薬)
肺炎 肺炎球菌,インフルエンザ菌 解熱後3-4日
黄色ブドウ球菌 3-4週間
マイコプラズマ,クラミジア 10-21日
腎臓、膀胱炎、腎盂腎炎 大腸菌,プロテウス,腸球菌 3日
14日
骨髄炎 黄色ブドウ球菌 21日
連鎖球菌,インフルエンザ菌 14日

主要な感染症の抗菌薬投与期間

感染レジマニュ p.27
骨髄炎 4-6週
耳鼻咽喉 中耳炎 5-7日
副鼻腔炎 5-14日
A群溶連菌咽頭炎 10日
肺炎 肺炎球菌 7-10日 or 解熱後3日間
インフルエンザ菌 10-14日
マイコプラズマ 14日(7-10日)
レジオネラ 21日
肺化膿症 28-42日
心臓 感染性心内膜炎 α連鎖球菌 2-4週
黄色ブドウ球菌 4-6週
消化管 腸炎 赤痢菌 3日
チフス 14日(5-7日)
パラチフス
腹膜炎 特発性 5日
二次性 10-14日
胆肝膵 肝膿瘍 細菌性 4-8週
アメーバ性 10日
尿路 膀胱炎 3日
急性腎盂腎炎 14日(7-10日)
急性腎盂腎炎・再発 6週
慢性前立腺炎 1-3ヶ月
髄腔 髄膜炎 インフルエンザ菌 7-10日
髄膜炎菌
肺炎球菌 10-14日
リステリア 21日
敗血症 敗血症 コアグラーゼ陰性ブドウ球菌 5-7日
黄色ブドウ球菌 28日(14日)
グラム陰性桿菌 14日(7-14日)
カンジダ 血液培養陰性化後, 14日

ソース不明

妊婦に避けるべき抗菌薬

  • Antibiotics to avoid in pregnancy
  • Sulfonamides––kernicterus.
  • Aminoglycosides––ototoxicity.
  • Fluoroquinolones––cartilage damage.
  • Erythromycin––acute cholestatic hepatitis in mom
(and clarithromycin––embryotoxic).
  • Metronidazole––mutagenesis.
  • Tetracyclines––discolored teeth, inhibition of bone growth.
  • Ribavirin (antiviral)––teratogenic.
  • Griseofulvin (antifungal)––teratogenic.
  • Chloramphenicol––“gray baby.”
  • SAFE Moms Take Really Good Care.

使っても良い

YN.H-24
  • βラクタム系
  • エリスロマイシン、アジスロマイシン

参考

  • 抗菌薬インターネットブック
まとまっていてよい
[display]http://www.antibiotic-books.jp

抗菌薬一覧

抗結核薬」

  [★]

antituberculous, antitubercular agent antituberculous agent antitubercular drug antituberculous drug antituberculosis drugs, antituberculotic
抗結核剤
結核
  • first aid step1 2006 p.172

抗結核薬一覧

  • 覚え方:INH-SM-PZA-INH-RFP-EB → INH-SPIRE(inspire)
  • イソニアジドだけは予防薬として用いられる(first aid step1 2006 p.172)
  • 2nd line drugとしてcycloserineがある。

作用点

抗結核薬の副作用

CS」

  [★]

サイクロセリン」

  [★]

cycloserine CS
cycloserinum
抗結核薬