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短杆菌素

短杆菌素用途

Tyrothricin 是一种从短小芽孢杆菌中分离的多肽抗生素混合物,由酪氨酸和短杆菌肽组成。Tyrothricin 可抑制细菌,真菌和某些病毒的活性。含 Tyrothricin 的制剂可用于治愈咽喉痛或浅表及小面积伤口的感染。

短杆菌素名称

[ CAS 号 ]:
1404-88-2

[ 中文名 ]:
短杆菌素

[ 英文名 ]:
TYROTHRICIN

短杆菌素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 抗感染 >> 流感病毒

研究领域 >> 感染

信号通路 >> 抗感染 >> 真菌

信号通路 >> 抗感染 >> 细菌

[体外研究]

酪氨酸是一种多肽的混合物,由50%-70%的酪氨酸和25%-50%的禾本科植物苷组成。酪氨酸是碱性的环肽,而类胰蛋白酶是中性的线性肽。除生理性和必需的L-氨基酸外,酪氨酸还含有D-氨基酸[1]。酪氨酸是由革兰氏阳性需氧芽孢杆菌(Bacillus brevis,菌株ATCC 8185)在产孢阶段通过非核糖体途径产生的。酪氨酸酶的作用谱主要包括革兰氏阳性菌和几种革兰氏阴性菌。棒状杆菌和葡萄球菌对酪氨酸酶的抑制作用范围更广(2-256μg/mL)。与单用胍组分相比,酪氨酸酶在最大浓度为128μg/mL时能抑制所有葡萄球菌。在革兰氏阴性菌中,淋球菌和脑膜炎球菌是最敏感的细菌(96μg/mL)[1]。酪氨酸酶对多种念珠菌的杀菌作用种酪氨酸酶显示了对副流感病毒(仙台型)的抗感染活性[1]。

[体内研究]

在使用HSV-1型的动物模型中,用酪氨酸酶对病毒悬浮液进行预孵育可显著降低小鼠的致死率。这种效果只有在酪氨酸酶和病毒直接接触后才能显现出来[1]。然而,在体外高浓度的酪氨酸酶可以破坏真核细胞膜的完整性。这一效应在体外研究和应用于静脉注射的动物中被证实为酪氨酸酶的溶血活性。。与静脉注射(LD50小鼠：3,7 mg/kg)和腹腔注射(LD50小鼠：20-45 mg/kg)相比,口服给药具有很好的耐受性,因为酪氨酸在胃肠道中被破坏[1]。

[参考文献]

[1]. Lang C, et al. Tyrothricin--An underrated agent for the treatment of bacterial skin infections and superficial wounds? Pharmazie. 2016 Jun;71(6):299-305.

短杆菌素物理化学性质

[ 密度 ]:
1.32g/cm3

[ 沸点 ]:
1516.6ºC at 760mmHg

[ 分子式 ]:
C₆₅H₈₅N₁₁O₁₃

[ 分子量 ]:
1228.44000

[ 闪点 ]:
871ºC

[ 精确质量 ]:
1227.63000

[ PSA ]:
379.75000

[ LogP ]:
5.10700

[ 蒸汽压 ]:
0mmHg at 25°C

[ 折射率 ]:
1.635

[ 水溶解性 ]:
Practically insoluble in water, soluble in ethanol (96 per cent) and in methanol.

短杆菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YP2975000

CHEMICAL NAME :: Tyrothricin

CAS REGISTRY NUMBER :: 1404-88-2

LAST UPDATED :: 199503

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 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 - mouse

DOSE/DURATION :: 100 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 :: >1500 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 :: Rodent - mouse

DOSE/DURATION :: 1200 ug/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 20 mg/kg/10D-I

TOXIC EFFECTS :: Blood - changes in cell count (unspecified) Blood - changes in spleen Related to Chronic Data - death

MUTATION DATA

TYPE OF TEST :: DNA adduct

TEST SYSTEM :: Bacteria - Escherichia coli

DOSE/DURATION :: 25 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 89,95,1981 *** REVIEWS *** TOXICOLOGY REVIEW ADENAE Advances in Enzymology and Related Subjects of Biochemistry. (New York, NY) V.1-28, 1941-66. For publisher information, see AERAAD. Volume(issue)/page/year: 4,153,1944

短杆菌素安全信息

[ 安全声明 (欧洲) ]:
22-24/25

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

[ WGK德国 ]:
2

[ RTECS号 ]:
YP2975000

短杆菌素文献

Salivary levels of gramicidin after use of a tyrothricin-containing gargle/mouth-wash and tyrothricin lozenges.

Int. J. Clin. Pharmacol. Res. 8(4) , 259-61, (1988)

Three pharmaceutical preparations for the disinfection of the oropharynx were tested with regard to the gramicidin concentration obtained in the saliva after their appropriate application. Peak values...

Tyrocidine-induced modulation of the DNA conformation in Bacillus brevis.

Eur. J. Biochem. 170(1-2) , 253-8, (1987)

Using the [3H]trimethylpsoralen photobinding method [Sinden, R.R., Carlson, J.O. & Pettijohn, D.E. (1980) Cell 21, 773-783], a decrease in unrestrained torsional tension of DNA was detected in Bacillu...

Fungicidal effect of tyrothricin on Candida albicans.

Mycoses 39(1-2) , 45-50, (1996)

Tyrothricin, a polypeptide antibiotic, is active against yeast cells. Tyrothricin was rapidly fungicidal towards Candida albicans. Concentration of four times the minimum inhibitory (25 mg l-1) reduce...

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