盐酸土霉素

盐酸土霉素用途

Oxytetracycline hydrochloride 是一种属于四环素类的抗生素。Oxytetracycline hydrochloride 强力抑制革兰氏阴性和革兰氏阳性细菌。Oxytetracycline hydrochloride 是一种蛋白质合成抑制剂,可阻止 aminoacil-tRNA 与复杂的核糖体 RNA 结合。Oxytetracycline hydrochloride 还具有抗 HSV-1 的活性。

盐酸土霉素作用

属广谱抗菌素，其抗菌谱、抗菌原理和应用与四环素基本相同。许多立克次体属、支原体属、衣原体属、螺旋体、阿米巴原虫和某些疟原虫也对本品敏感。肠球菌属对其耐药。其他如放线菌属、炭疽杆菌、单核细胞增多性李斯特菌、梭状芽孢杆菌、奴卡菌属、弧菌、布鲁菌属、弯曲杆菌、耶尔森菌等对本品敏感。本品对淋球菌和脑膜炎球菌具一定抗菌活性，但耐青霉素的淋球菌对土霉素也耐药。多年来由于四环素类的广泛应用,临床常见病原菌对土霉素耐药现象严重，包括葡萄球菌等革兰阳性菌及多数革兰阴性杆菌。四环素类抗生素的不同品种之间存在交叉耐药。本品作用机制为药物能特异性地与细菌核糖体30S亚基的A位置结合，抑制肽链的增长和影响细菌蛋白质的合成。本品对肠道感染，包括阿米巴痢疾，疗效略强于四环素。与四环素有密切的交叉耐药性。

盐酸土霉素名称

[ CAS 号 ]:
2058-46-0

[ 中文名 ]:
水合霉素

[ 英文名 ]:
Oxytetracycline HCl

[中文别名 ]:

[英文别名 ]:

engemycin
mepatar
Oxytetracycline Hydrochloride
MFCD00135815
oxytetracyclin hydrochloride
oxlopar
EINECS 218-161-2
oxytetracycline HCl
Oxycline
terramycin hydrochloride

盐酸土霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 抗感染 >> HSV

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Gram-negative and Gram-positive bacteria[1] HSV-1[3]

[体外研究]

土霉素是细菌芳香族聚酮家族的重要成员,是一类结构多样的天然产物。土霉素由一种II型聚酮合酶合成,该合酶通过丙二酰辅酶a扩链单元的连续脱羧缩合生成聚β酮主链,随后通过环化酶、加氧酶、转移酶和其他裁剪酶进行修饰[2]。

[体内研究]

给药10天的土霉素治疗剂量(82.8 mg/kg体重至1%体重/天)具有种属特异性。土霉素增加了白杨的相对肝重,增加了鸡腿蘑中CYP3A4的酶活性,增加了尼罗罗非鱼中CYP3A4的蛋白表达,减少了后者中CYP3A4的含量[1]。土霉素的限量为肌肉和牛奶100μg/kg,鸡蛋200μg/kg,肝脏300μg/kg,肾脏600μg/kg。将土霉素(OTC)作为药物饲料,以35至75 mg a.i kg-1生物量日-1的浓度投喂鱼7-14天[1]。

[参考文献]

[1]. Elia AC, et al. Transferability of oxytetracycline (OTC) from feed to carp muscle and evaluation of the antibiotic effects on antioxidant systems in liver and kidney. Fish Physiol Biochem. 2014 Aug;40(4):1055-68.

[2]. Pickens LB, et al. Oxytetracycline biosynthesis. J Biol Chem. 2010 Sep 3;285(36):27509-15.

[3]. Oguz Guvenmez, et al. A New Treatment Method for Herpes Simplex Virus Type 1-related Skin Lesions. Scientific & Academic. 2019; 8(1): 6-8.

盐酸土霉素物理化学性质

[ 密度 ]:
1.71 g/cm3

[ 沸点 ]:
839.6ºC at 760 mmHg

[ 熔点 ]:
180°C

[ 分子式 ]:
C₂₂H₂₅ClN₂O₉

[ 分子量 ]:
533.356

[ 闪点 ]:
461.6ºC

[ 精确质量 ]:
532.101563

[ PSA ]:
201.85000

[ LogP ]:
0.25870

[ 外观性状 ]:
黄色结晶固体

[ 蒸汽压 ]:
2.17E-30mmHg at 25°C

[ 储存条件 ]:
0-6°C

[ 水溶解性 ]:
>100 g/L

盐酸土霉素MSDS

详细MSDS(安全技术说明书)

盐酸土霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QI8225000

CHEMICAL NAME :: 2-Naphthacenecarboxamide, 4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,5, 6,10,12,12a- hexahydroxy-6-methyl-1,11-dioxo-, monohydrochloride

CAS REGISTRY NUMBER :: 2058-46-0

LAST UPDATED :: 199701

DATA ITEMS CITED :: 26

MOLECULAR FORMULA :: C22-H24-N2-O9.Cl-H

MOLECULAR WEIGHT :: 496.94

WISWESSER LINE NOTATION :: L E6 C666 BV FV CU GUTTT&J DQ EQ GVZ HQ IN1&1 KQ MQ M1 RQ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 800 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 302 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6696 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 100 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 80 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1802 gm/kg/2Y

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 20 mg/kg

SEX/DURATION :: female 20 week(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11250 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 12 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 21 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 900 mg/kg

SEX/DURATION :: female 10-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TYPE OF TEST :: Unscheduled DNA synthesis

TEST SYSTEM :: Mammal - species unspecified Lymphocyte

DOSE/DURATION :: 20 mg/L

REFERENCE :: BIORAK Biochemistry (English Translation). Translation of BIOHAO. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) V.21- 1956- Volume(issue)/page/year: 39,587,1974 *** U.S. STANDARDS AND REGULATIONS *** EPA FIFRA 1988 PESTICIDE SUBJECT TO REGISTRATION OR RE-REGISTRATION FEREAC Federal Register. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) V.1- 1936- Volume(issue)/page/year: 54,7740,1989 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 83236 No. of Facilities: 49 (estimated) No. of Industries: 2 No. of Occupations: 6 No. of Employees: 9441 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83236 No. of Facilities: 763 (estimated) No. of Industries: 2 No. of Occupations: 10 No. of Employees: 20845 (estimated) No. of Female Employees: 16524 (estimated)

盐酸土霉素安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H361d

[ 警示性声明 ]:
P281

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R36;R63

[ 安全声明 (欧洲) ]:
S36/37/39-S26

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

[ WGK德国 ]:
2

[ RTECS号 ]:
QI8225000

[ 海关编码 ]:
3003209000

盐酸土霉素合成路线

详细合成路线

盐酸土霉素上下游产品

盐酸土霉素上游产品

盐酸土霉素下游产品

盐酸土霉素海关

[ 海关编码 ]: 3003209000

盐酸土霉素文献

Development and validation of a liquid chromatographic/ tandem mass spectrometric method for determination of chlortetracycline, oxytetracycline, tetracycline, and doxycycline in animal feeds.

J. AOAC Int. 95(4) , 1010-5, (2012)

A selective and accurate LC/MS/MS method for the simultaneous determination of chlortetracycline (CTC), oxytetracycline (OTC), tetracycline (TC), and doxycycline (DC) in animal feeds was developed. Sa...

Heterologous expression and manipulation of three tetracycline biosynthetic pathways.

Angew. Chem. Int. Ed. Engl. 51(44) , 11136-40, (2012)

A very accommodating host: Three tetracycline biosynthetic pathways were overexpressed and manipulated in the heterologous host Streptomyces lividans K4-114. Through the inactivation of various genes ...

Topical steroids for chronic wounds displaying abnormal inflammation.

Ann. R. Coll. Surg. Engl. 95(4) , 291-6, (2013)

Chronic, non-healing wounds are often characterised by an excessive, and detrimental, inflammatory response. We review our experience of using a combined topical steroid, antibiotic and antifungal pre...

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