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利福布汀

利福布汀用途

Rifabutin (Ansamycin) 是半合成的安莎霉素抗生素,具有抗分枝杆菌特性。

利福布汀名称

[ CAS 号 ]:
72559-06-9

[ 中文名 ]:
利福布丁

[ 英文名 ]:
Rifabutin

[中文别名 ]:

[英文别名 ]:

Rifabutin
Ansamycin
RIFABUTINE
Mycobutin
lm427
Rifabatin
antibioticlm427
Ansatipine

利福布汀生物活性

[ 描述 ]:

Rifabutin (Ansamycin) 是半合成的安莎霉素抗生素,具有抗分枝杆菌特性。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[ 靶点 ]

Antibacterial

[体外研究]

利福布丁主要是用于治疗结核病的杀菌抗生素药物。它对细菌的作用是基于DNA依赖性RNA聚合酶阻断药物利福霉素S.,一种半合成衍生物。例如,它在高抗性分枝杆菌,革兰氏阳性菌(和一些对革兰氏阴性菌有效)中有效,但也对结核分枝杆菌,麻风杆菌和胞内分枝杆菌有效。利福布丁是一种抗生素;抗肿瘤。利福布汀干扰HSP-90分子伴侣,增强泛素化和蛋白质降解,并使细菌RNA聚合酶失活。

[参考文献]

[1]. Review Article: Rifabutin in the Treatment of Refractory Helicobacter pylori Infection J. P. Gisbert, X. Calvet Issue Alimentary Pharmacology & Therapeutics Volume 35, Issue 2, pages 209-221, January 2012

[2]. Vourvahis M, Davis J, Wang R, Layton G, Choo HW, Chong CL, Tawadrous M.Effect of rifampin and rifabutin on the pharmacokinetics of lersivirine and effect of lersivirine on the pharmacokinetics of rifabutin and 25-o-desacetyl-rifabutin in healthy subjects.Antimicrob Agents Chemother. 2012 Aug;56(8):4303-9.

[3]. Gisbert JP, Castro-Fernandez M, Perez-Aisa A, Cosme A, Molina-Infante J, Rodrigo L, Modolell I, Cabriada JL, Gisbert JL, Lamas E, Marcos E, Calvet X.Fourth-line rescue therapy with rifabutin in patients with three Helicobacter pylori eradication failures.Aliment Pharmacol Ther. 2012 Apr;35(8):941-7. doi: 10.1111/j.1365-2036.2012.05053.x.

[4]. Gisbert JP, Calvet X.Review article: rifabutin in the treatment of refractory Helicobacter pylori infection.Aliment Pharmacol Ther. 2012 Jan;35(2):209-21. doi: 10.1111/j.1365-2036.2011.04937.x.

[5]. Horne DJ, Spitters C, Narita M.Experience with rifabutin replacing rifampin in the treatment of tuberculosis.Int J Tuberc Lung Dis. 2011 Nov;15(11):1485-9, i.

[相关活性小分子]

利福布汀物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
969.6±65.0 °C at 760 mmHg

[ 熔点 ]:
169-171ºC

[ 分子式 ]:
C₄₆H₆₂N₄O₁₁

[ 分子量 ]:
847.005

[ 闪点 ]:
540.2±34.3 °C

[ 精确质量 ]:
846.441528

[ PSA ]:
205.55000

[ LogP ]:
3.45

[ 外观性状 ]:
红色-紫罗兰色结晶粉末

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.623

[ 储存条件 ]:
Amber Vial, -20°C Freezer, Under Inert Atmosphere

[ 水溶解性 ]:
DMSO: >5mg/mL

利福布汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VJ6700000

CHEMICAL NAME :: Rifamycin XIV, 1,4-dihydro-1-deoxy-1',4-didehydro-5'-(2-methylpropyl )-1-oxo-

CAS REGISTRY NUMBER :: 72559-06-9

LAST UPDATED :: 199709

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C46-H62-N4-O11

MOLECULAR WEIGHT :: 847.12

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 60 mg/kg/14D-I

TOXIC EFFECTS :: Blood - agranulocytosis

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 348,685,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 84 mg/kg/14D-I

TOXIC EFFECTS :: Blood - agranulocytosis

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 348,685,1996

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 51 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3322 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 266 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9100 mg/kg/13W-C

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Blood - changes in spleen

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 29120 mg/kg/1Y-I

TOXIC EFFECTS :: Blood - normocytic anemia Endocrine - changes in spleen weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 47 mg/kg/1Y-C

TOXIC EFFECTS :: Blood - normocytic anemia Blood - changes in spleen Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: ETPAEK Experimental and Toxicologic Pathology. (Gustav Fischer Verlag Jena, Postfach 100537, D-07705 Jena, Germany) V.44- 1992- Volume(issue)/page/year: 47,1,1995

利福布汀安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
VJ6700000

[ 海关编码 ]:
2941903000

利福布汀制备

【方法1】
以1，4-二氢利福霉素S为原料，经溴化，亚硝基取代，氢化，氨化，再和N-异丁基哌啶酮反应，即可得到利福布汀。

利福布汀海关

[ 海关编码 ]: 2941903000

利福布汀文献

Simple and accurate quantitative analysis of 20 anti-tuberculosis drugs in human plasma using liquid chromatography-electrospray ionization-tandem mass spectrometry.

J. Pharm. Biomed. Anal. 102 , 9-16, (2014)

A simple and accurate liquid chromatography (LC)-tandem mass spectrometry (MS/MS) method for the quantitation of 20 anti-tuberculosis (anti-TB) drugs in human plasma, was developed as a tool for thera...

Different antibiotic susceptibility between antrum and corpus of the stomach, a possible reason for treatment failure of Helicobacter pylori infection.

World J. Gastroenterol. 20(43) , 16245-51, (2014)

To assess whether antibiotic resistance varies between the antrum and corpus of the stomach of patients that are either Helicobacter pylori (H. pylori) therapy-naive or pre-treated.H. pylori strains w...

Genipin crosslinked ethyl cellulose-chitosan complex microspheres for anti-tuberculosis delivery.

Colloids Surf. B Biointerfaces 103 , 530-7, (2013)

Genipin-crosslinked complex microspheres made of the combination of two polymers, ethyl cellulose and chitosan, were prepared by spray drying method. Rifabutin, an anti-tuberculosis agent was used as ...

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