卡那霉素碱

卡那霉素碱用途

卡那霉素(卡那霉霉素A)是一种口服活性抗菌剂(革兰氏阴性/阳性细菌),通过与70 S核糖体亚单位结合,抑制易位并导致编码错误。卡那霉素对结核分枝杆菌(敏感和耐药)和肺炎克雷伯菌均有良好的抑制活性,可用于结核病和肺炎的研究[1][2][3][4]。

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卡那霉素碱名称

[ CAS 号 ]:
59-01-8

[ 中文名 ]:
卡那霉素碱

[ 英文名 ]:
kanamycin

[中文别名 ]:

[英文别名 ]:

KANAMYCIN
kanamycin from Streptomyces kanamyceticus
d-deoxydi
Kannamycin Monosulfate
d-xydi
kanamicina
KanamycinMonosulfateA
gentamicin A

卡那霉素碱生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 抗感染 >> 细菌

[体外研究]

卡那霉素(0.1-100μg/mL；2周)在体外对各种分枝杆菌菌株表现出良好的抗菌活性(MIC=1-5μg/mL)[1]。细胞活力测定[1]细胞系：分枝杆菌H37Rv、H2、H37RvR PAS、Ravenel、Kirchbergand和BCG。浓度：0.1-100μg/mL孵育时间：2周结果：对各种分枝杆菌(H37Rv、H2、H37RvR PAS、Ravenel和BCG)表现出良好的抗菌活性,Kirchbergand菌株的MIC分别为1μg/mL和5μg/mL。

[体内研究]

卡那霉素(2,4 mg/kg；皮下注射；每日一次,每周6次,共3周)抑制小鼠肺和脾脏中牛结核杆菌的生长[1]。卡那霉素(1.25,5 mg/kg；皮下注射；单次(感染后3小时))抑制小鼠肺、气管和血液中肺炎克雷伯菌DT-s的增殖,并与给药剂量成比例,还增加了小鼠的存活率[2]。动物模型：近交系正常小鼠(14-16g；牛结核杆菌(Ravenel株)感染模型)[1]。剂量：2,4mg/kg给药：皮下注射；每天一次,每周6次,持续3周。结果：对小鼠体内尤其是肺结核的增殖有明显的抑制作用。动物模型：Slc:ICR雄性小鼠(4周龄；18-24克；肺炎克雷伯菌DT-S感染模型(通过气溶胶法))[2]。剂量：1.25,5mg/kg给药：皮下给药；单个(感染后3小时)。结果：与给药剂量成比例地抑制肺炎克雷伯菌DT-S在肺、气管和血液中的生长。在感染后第6天导致90%的存活率(阴性对照组：所有人在4天内死亡),并在48小时内(当剂量为5 mg/kg时)从小鼠的肺、气管和血液中清除肺炎克雷伯菌DT-S。

[参考文献]

[1]. YANAGISAWA K, et al. Studies on kanamycin, a new antibiotic against tubercle bacilli. I. Effect on virulent tubercle bacilli in vitro and in mice. J Antibiot (Tokyo). 1957 Nov;10(6):233-5.

[2]. Nishi T, et al. Experimental respiratory tract infection with Klebsiella pneumoniae DT-S in mice: chemotherapy with kanamycin. Antimicrob Agents Chemother. 1980 Mar;17(3):494-505.

[3]. Misumi M, et al. Interaction of kanamycin and related antibiotics with the large subunit of ribosomes and the inhibition of translocation. Biochem Biophys Res Commun. 1978 Sep 29;84(2):358-65.

[4]. Misumi M, et al. Mechanism of inhibition of translocation by kanamycin and viomycin: a comparative study with fusidic acid. Biochem Biophys Res Commun. 1980 Jan 29;92(2):647-54.

卡那霉素碱物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
809.5±65.0 °C at 760 mmHg

[ 分子式 ]:
C₁₈H₃₆N₄O₁₁

[ 分子量 ]:
484.499

[ 闪点 ]:
443.4±34.3 °C

[ 精确质量 ]:
484.238068

[ PSA ]:
282.61000

[ LogP ]:
-2.58

[ 蒸汽压 ]:
0.0±6.5 mmHg at 25°C

[ 折射率 ]:
1.670

卡那霉素碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WK1962000

CHEMICAL NAME :: D-Streptamine, O-3-amino-3-deoxy-alpha-D-glucopyranosyl-(1-6)-O-(6-a mino-6-deoxy-alpha- D-glucopyranosyl-(1-4))-2-deoxy-

CAS REGISTRY NUMBER :: 59-01-8

BEILSTEIN REFERENCE NO. :: 0061647

LAST UPDATED :: 199706

DATA ITEMS CITED :: 27

MOLECULAR FORMULA :: C18-H36-N4-O11

MOLECULAR WEIGHT :: 484.58

WISWESSER LINE NOTATION :: T6OTJ CQ DZ EQ F1Q BO- BL6TJ AZ CQ EZ DO- BT6OTJ CQ DQ EQ F1Z

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 :: >10 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 :: 1515 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 - rat

DOSE/DURATION :: 4070 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 :: 437 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1014 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - other changes

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20700 ug/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 :: 794 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 :: 1350 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 :: 115 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 :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 54 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 :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 33750 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Cardiac - other changes Lungs, Thorax, or Respiration - respiratory depression

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 150 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 - guinea pig

DOSE/DURATION :: 1385 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 960 mg/kg/4D-I

TOXIC EFFECTS :: Blood - changes in other cell count (unspecified) Blood - changes in leukocyte (WBC) count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 12 gm/kg/30D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - changes in bladder weight Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3600 mg/kg

SEX/DURATION :: female 1-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3600 mg/kg

SEX/DURATION :: female 12-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 3500 mg/kg

SEX/DURATION :: female 12-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear

MUTATION DATA

TYPE OF TEST :: DNA repair

TEST SYSTEM :: Bacteria - Bacillus subtilis

DOSE/DURATION :: 27 ug/L

REFERENCE :: WATRAG Water Research. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 0BW, UK) V.1- 1967- Volume(issue)/page/year: 14,1613,1980 *** REVIEWS *** TOXICOLOGY REVIEW CLANA4 Clinical Anesthesia. (Philadelphia, PA 19103) V.1-11, 1963-76. Volume(issue)/page/year: 10(Pt 1),283,1973 TOXICOLOGY REVIEW MMWOAU Muenchener Medicinische Wochenschrift. (Munich, Fed. Rep. Ger.) V.33-115, 1886-1973. Volume(issue)/page/year: 115,1661,1973 TOXICOLOGY REVIEW INTEAG Internist. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1960- Volume(issue)/page/year: 15,7,1974 TOXICOLOGY REVIEW ARVPAX Annual Review of Pharmacology. (Palo Alto, CA) V.1-15, 1961-75. For publisher information, see ARPTDI. Volume(issue)/page/year: 5,447,1965 TOXICOLOGY REVIEW AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 38,409,1965

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卡那霉素碱安全信息

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