链霉溶菌素

链霉溶菌素用途

Streptolydigin (Portamycin) 是一种 3-乙酰基四酸抗生素,是一种有效的细菌 RNA 聚合酶 (bacterial RNA polymerase) 抑制剂,Ki 为 18 μM,Kd 为 15 μM。Streptolydigin 通过与 RNA 聚合酶结合来抑制 RNA 合成 (RNA synthesis),但不抑制真核生物 RNA 聚合酶。Streptolydigin 具有强大的抗菌活性,特别是对厌氧菌和一些革兰氏阳性需氧菌。

链霉溶菌素名称

[ CAS 号 ]:
7229-50-7

[ 中文名 ]:
链菌碱

[ 英文名 ]:
Streptolydigin

[中文别名 ]:

門黴素

[英文别名 ]:

Antibiotic D-45
portamycin
Streptolydigin

链霉溶菌素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Ki: 18 μM (Bacterial RNA polymerase)[3] Kd: 15 μM (Bacterial RNA polymerase)[3]

[体外研究]

抗生素链霉素(Stl)是3-乙酰四胺酸的衍生物。链霉素与RNA聚合酶的结合严格依赖于非催化镁离子,该镁离子可能被活性中心桥螺旋的天冬氨酸螯合[1]。链霉素以1.8μM的Ki抑制嗜热链球菌RNA聚合酶[3]。链霉素(Stl)抑制细菌RNA聚合酶的起始、延伸和热释磷。链霉素与RNAP中的三个结构元素相互作用：Stl腔、桥螺旋和触发环区域。链霉素-链霉素部分与链霉素囊和桥螺旋相互作用,链霉素-四价酸部分与触发环区域相互作用[3]。

[参考文献]

[1]. Zorov S, et al. Antibiotic streptolydigin requires noncatalytic Mg2+ for binding to RNA polymerase. Antimicrob Agents Chemother. 2014;58(3):1420-4.

[2]. Temiakov D, et al. Structural basis of transcription inhibition by antibiotic streptolydigin. Mol Cell. 2005 Sep 2;19(5):655-66.

[3]. Tuske S, et al. Inhibition of bacterial RNA polymerase by streptolydigin: stabilization of a straight-bridge-helix active-center conformation. Cell. 2005 Aug 26;122(4):541-52.

[4]. Rosen T, et al. Aromatic dienoyl tetramic acids. Novel antibacterial agents with activity against anaerobes and staphylococci. J Med Chem. 1989 May;32(5):1062-9.

链霉溶菌素物理化学性质

[ 密度 ]:
1.3 g/cm3

[ 沸点 ]:
826.6ºC at 760 mmHg

[ 分子式 ]:
C₃₂H₄₄N₂O₉

[ 分子量 ]:
600.70000

[ 闪点 ]:
453.7ºC

[ 精确质量 ]:
600.30500

[ PSA ]:
147.16000

[ LogP ]:
2.78890

[ 折射率 ]:
1.598

[ 储存条件 ]:
-20°C，干燥，密封

链霉溶菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WK4250000

CHEMICAL NAME :: Streptolydigin

CAS REGISTRY NUMBER :: 7229-50-7

LAST UPDATED :: 199403

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C32-H44-N2-O9

MOLECULAR WEIGHT :: 600.78

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 533 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 :: Subcutaneous

SPECIES OBSERVED :: Bird - chicken

DOSE/DURATION :: 10 mg/kg

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

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Bacteria - Bacillus subtilis

DOSE/DURATION :: 288 mg/L

REFERENCE :: FOMIAZ Folia Microbiologica (Prague). (Academia, Vodickova 40, 112 29 Prague 1, Czechoslavakia) V.4- 1959- Volume(issue)/page/year: 22,329,1977

链霉溶菌素安全信息

[ 危害码 (欧洲) ]:
Xi