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强力霉素

强力霉素用途

Doxycycline 是一种四环素抗生素,口服有效的,广谱的金属蛋白酶 (MMP) 抑制剂,具有抗菌活性。

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强力霉素名称

[ CAS 号 ]:
564-25-0

[ 中文名 ]:
强力霉素

[ 英文名 ]:
Doxycycline

[中文别名 ]:

脱氧土霉素

[英文别名 ]:

Monodox
azudoxat
Doxycen
MFCD02682958
gs-3065
Ronaxan
doxocycline
doryx
Unidox
doxitard

强力霉素生物活性

[ 描述 ]:

Doxycycline 是一种四环素抗生素,口服有效的,广谱的金属蛋白酶 (MMP) 抑制剂,具有抗菌活性。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 代谢酶/蛋白酶 >> MMP

[体外研究]

多西环素仅在高浓度下影响胶质瘤细胞的生长[2]。多西环素降低SVG细胞中MT-CO1蛋白含量,浓度为1μg/mL或更高[2]。细胞增殖测定[2]细胞系：LNT-229、G55和U343胶质瘤细胞浓度：0.01、0.1、1或10μg/mL培养时间：4天结果：仅在高浓度下影响胶质瘤细胞的生长。Western Blot分析[2]细胞系：SVG细胞浓度：0.01,0.1,1或10μg/mL培养时间：24小时结果：浓度为1μg/mL或更高的MT-CO1蛋白含量降低。

[体内研究]

多西环素(口服；200或800mg/kg/天；3个月)以剂量依赖性方式降低未治疗HT小鼠中的活性MMP-9[1]。动物模型：6个月大的雌性杂合子Col3a1缺陷(HT)小鼠[1]剂量：200或800 mg/kg给药：口服；每天；持续3个月结果：活性MMP-9以剂量依赖性方式降低。

[参考文献]

[1]. Briest W, et al. Doxycycline ameliorates the susceptibility to aortic lesions in a mouse model for the vascular type of Ehlers-Danlos syndrome. J Pharmacol Exp Ther. 2011 Jun;337(3):621-7.

[2]. Luger AL, et al. Doxycycline Impairs Mitochondrial Function and Protects Human Glioma Cells from Hypoxia-Induced Cell Death: Implications of Using Tet-Inducible Systems. Int J Mol Sci. 2018 May 17;19(5).

强力霉素物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
685.2±55.0 °C at 760 mmHg

[ 熔点 ]:
206-209ºC

[ 分子式 ]:
C₂₂H₂₄N₂O₈

[ 分子量 ]:
444.435

[ 闪点 ]:
368.2±31.5 °C

[ 精确质量 ]:
444.153259

[ PSA ]:
181.62000

[ LogP ]:
1.36

[ 外观性状 ]:
黄色晶体粉末

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.737

[ 储存条件 ]:
2-8C

强力霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QI8650000

CHEMICAL NAME :: 2-Naphthacenecarboxamide, 4-alpha-S-(dimethylamino)-1,4,4a-alpha-5,5a-alpha,6,1 1,12a- octahydro-3,5-alpha,10,12,12a-alpha-pentahydroxy-6-al pha-methyl-1,11-dioxo-

CAS REGISTRY NUMBER :: 564-25-0

LAST UPDATED :: 199609

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C22-H24-N2-O8

MOLECULAR WEIGHT :: 444.48

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

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 68 mg/kg/24D-I

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 378 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 :: 228 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 :: 1870 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 410 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 :: 241 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 :: Mammal - dog

DOSE/DURATION :: >500 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 :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 750 mg/kg

SEX/DURATION :: female 2 day(s) after conception

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

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 3750 ug/L

REFERENCE :: BCPHBM British Journal of Clinical Pharmacology. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1974- Volume(issue)/page/year: 16,127,1983 *** REVIEWS *** TOXICOLOGY REVIEW PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,305,1979 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84744 No. of Facilities: 641 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1281 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 84744 No. of Facilities: 450 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 22055 (estimated) No. of Female Employees: 18813 (estimated)

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强力霉素安全信息

[ 海关编码 ]:
3004909090

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强力霉素海关

[ 海关编码 ]: 3004909090