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交沙霉素

交沙霉素用途

交沙霉素是一种大环内酯类抗生素，对多种病原体，比如细菌 (bacteria) 具有抗菌活性。交沙霉素对核糖体的解离常数 K_d 为 5.5 nM。

交沙霉素名称

[ CAS 号 ]:
16846-24-5

[ 中文名 ]:
交沙霉素

[ 英文名 ]:
Josamycin

[中文别名 ]:

角沙霉素

[英文别名 ]:

Iosalide
Vilprafen
Leucomycin V 3-Acetate 4B-(3-Methylbutanoate)
MFCD00211043
Leucomycin A3
EN 141
Josamina
EINECS 240-871-6
JOSAMYCIN
carbomycin B

交沙霉素生物活性

[ 描述 ]:

Josamycin (EN-141) 是一种大环内酯类抗生素,对多种病原体, 比如细菌 (bacteria) 具有抗菌活性。 Josamycin (EN-141) 对核糖体的解离常数 Kd 为 5.5 nM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[ 靶点 ]

Kd: 5.5 nM (ribosome)[1]

[体外研究]

研究表明,对于交沙霉素,核糖体的平均寿命为3小时,并且Josamycin与核糖体结合的解离常数为5.5nM。交沙霉素以氨基酸依赖性方式减慢新生肽的第一个肽键的形成,并完全抑制第二个或第三个肽键的形成,这取决于饱和药物浓度下的肽序列,全长蛋白质的合成完全关闭由Josamycin提供。在饱和药物浓度下,全长蛋白质的合成被Josamycin完全关闭[1]。

[体内研究]

口服给药后交沙霉素的血液和组织水平为兔子200mg/kg。组织水平通常远高于血液水平,并且在给药后3小时,当血液水平非常低时,组织水平相当高于给药后1小时的组织水平。服药一小时后,肺部水平是所有组织水平中最高的[2]。

[激酶实验]

在多晶缓冲液中制备交沙霉素，其含有5mM乙酸镁，5mM氯化铵，95mM氯化钾，0.5mM氯化钙，8mM腐胺，1mM亚精胺，5mM磷酸钾和1mM二硫赤藓糖醇。将不同浓度（2,3,4和6μM）的交沙霉素加入到初始化的核糖体中以开始培养。在每个培养时间将1体积的延伸混合物加入1体积的反应混合物中，并在10秒后淬灭反应。结合率由三肽形成核糖体的比例估算[1]。

[动物实验]

大鼠：将氚标记的交沙霉素（200mg / kg）口服给予大鼠。通过生物测定在1小时和3小时测定血液和组织水平[2]。小鼠：将氚标记的交沙霉素（200mg / kg）口服给予小鼠。通过生物测定在1小时和3小时测定血液和组织水平[2]。

[参考文献]

[1]. Lovmar M, et al. Kinetics of macrolide action: the Josamycin and erythromycin cases. J Biol Chem. 2004 Dec 17;279(51):53506-15.

[2]. Osono T, et al. Pharmacokinetics of macrolides, lincosamides and streptogramins. J Antimicrob Chemother. 1985 Jul;16 Suppl A:151-66.

[相关活性小分子]

交沙霉素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
877.8±65.0 °C at 760 mmHg

[ 熔点 ]:
131.5℃

[ 分子式 ]:
C₄₂H₆₉NO₁₅

[ 分子量 ]:
827.995

[ 闪点 ]:
484.7±34.3 °C

[ 精确质量 ]:
827.466736

[ PSA ]:
206.05000

[ LogP ]:
3.88

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.535

交沙霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OH4725810

CHEMICAL NAME :: Leucomycin V, 3-acetate 4(sup B)-(3-methylbutanoate)

CAS REGISTRY NUMBER :: 16846-24-5

LAST UPDATED :: 199603

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C42-H69-N-O15

MOLECULAR WEIGHT :: 828.12

WISWESSER LINE NOTATION :: T-16-OV KU MUTJ DOV1 EO1 G1VH I1 JQ P1 FO- BT6OTJ CQ DN1&1 F1 EO- FT6OTJ B1 COV1Y1&1 DQ D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >7 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 390 mg/kg

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

REFERENCE :: NIPDAD Nihon Daigaku No-juigakubu Gakujutsu Kenkyu Hokoku. Research Reports of the College of Agriculture and Veterinary Medicine, Nihon University. (Nihon Daigaku Nojuigakkai, 34-1 Shimouma, 3-chome, Setagaya-ku, Tokyo 154, Japan) No.1- 1953- Volume(issue)/page/year: (35),41,1978

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6400 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 37,1565,1984

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 780 mg/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 2,85,1980

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,364,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 385 mg/kg

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

REFERENCE :: NIPDAD Nihon Daigaku No-juigakubu Gakujutsu Kenkyu Hokoku. Research Reports of the College of Agriculture and Veterinary Medicine, Nihon University. (Nihon Daigaku Nojuigakkai, 34-1 Shimouma, 3-chome, Setagaya-ku, Tokyo 154, Japan) No.1- 1953- Volume(issue)/page/year: (35),41,1978

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 520 mg/kg

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

REFERENCE :: HINAAU Hindustan Antibiotics Bulletin. (Hindustan Antibiotics, Ltd., Pimpri, Poona, India) V.1- 1958- Volume(issue)/page/year: 11,26,1969

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 786 mg/kg

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

REFERENCE :: HINAAU Hindustan Antibiotics Bulletin. (Hindustan Antibiotics, Ltd., Pimpri, Poona, India) V.1- 1958- Volume(issue)/page/year: 11,26,1969

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 385 mg/kg

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

REFERENCE :: HINAAU Hindustan Antibiotics Bulletin. (Hindustan Antibiotics, Ltd., Pimpri, Poona, India) V.1- 1958- Volume(issue)/page/year: 11,26,1969 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9 gm/kg/5W-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 22,219,1969 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 21 gm/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 22,219,1969

交沙霉素安全信息

[ 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

[ WGK德国 ]:
2

[ RTECS号 ]:
OH4725810

交沙霉素文献

Substrate competition studies using whole-cell accumulation assays with the major tripartite multidrug efflux pumps of Escherichia coli.

Antimicrob. Agents Chemother. 51 , 923-9, (2007)

AcrAB-TolC is the major, constitutively expressed tripartite multidrug efflux system in Escherichia coli that recognizes various structurally unrelated molecules, including many antibiotics, dyes, and...

Performance characterization of a quantitative liquid chromatography-tandem mass spectrometric method for 12 macrolide and lincosamide antibiotics in salmon, shrimp and tilapia.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 967 , 203-10, (2014)

This paper describes an extension and performance characterization of a quantitative confirmatory multi-residue liquid chromatography-tandem mass spectrometric method for residues of macrolide and lin...

Multi-residue Determination of Polar Veterinary Drugs in Livestock and Fishery Products by Liquid Chromatography/Tandem Mass Spectrometry.

J. AOAC Int. 98(1) , 230-47, (2015)

Residues of 37 polar veterinary drugs belonging to six families (quinolones, tetracyclines, macrolides, lincosamides, sulfonamides, and others) in livestock and fishery products were determined using ...

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