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Sisomicin

(Synonyms: 紫苏霉素) 目录号 : GC44894

Sisomicin是一种由伊诺单孢菌(Micromonospora inyoensis)产生的天然氨基糖苷类抗生素,对革兰氏阳性菌具有很强的活性。

Sisomicin Chemical Structure

Cas No.:32385-11-8

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Sample solution is provided at 25 µL, 10mM.

Description

Sisomicin is a naturally occurring aminoglycoside antibiotic produced by Micromonospora inyoensis and has strong activity against Gram-positive bacteria[1].

In vitro, Compared to the wild-type Mycobacterium smegmatis, the PdtaS gene deletion (ΔpdtaS) mutant shows increased sensitivity to sisomicin (2.3μg/ml; 3, 6, 9 and 24h)[2]. Sisomicin (20μg/mL; 30min) does not interfere with the function of polymorphonuclear neutrophils (PMN)[3].

In vivo, Hypertonic Sisomicin (20mg/ml) can be used for intracochlear perfusion to construct an inner ear injury model in mice[4]. Sisomicin (20mg/kg; i.p.) caused a decrease in neuromuscular twitch tension in rabbits[5].

References:
[1] Noone P. Sisomicin, netilmicin and dibekacin. A review of their antibacterial activity and therapeutic use. Drugs. 1984 Jun;27(6):548-78.
[2] Dadura K, Płocińska R, Rumijowska-Galewicz A, et al. PdtaS Deficiency Affects Resistance of Mycobacteria to Ribosome Targeting Antibiotics. Front Microbiol. 2017 Nov 3;8:2145.
[3] Le Moli S, Seminara R, D'Amelio R, et al. In vitro and in vivo effect of sisomicin and gentamycin on polymorphonuclear chemotaxis and phagocytosis. Int J Immunopharmacol. 1983;5(1):49-54.
[4] Maraslioglu-Sperber A, Blanc F, Heller S, et al. Hyperosmotic sisomicin infusion: a mouse model for hearing loss. Sci Rep. 2024 Jul 10;14(1):15903.
[5] Matsukawa S, Suh JH, Hashimoto Y, et al. Neuromuscular blocking actions of the aminoglycoside antibiotics sisomicin and micronomicin in the rabbit. Tohoku J Exp Med. 1997 Apr;181(4):471-3.

Sisomicin是一种由伊诺单孢菌(Micromonospora inyoensis)产生的天然氨基糖苷类抗生素,对革兰氏阳性菌具有很强的活性[1]

在体外实验中,与野生型分枝杆菌(Mycobacterium smegmatis)相比,PdtaS基因敲除(ΔpdtaS)突变株对Sisomicin(2.3µg/ml; 3, 6, 9和24h)的敏感性增加[2]。Sisomicin (20μg/mL; 30min) 不会干扰多形核中性粒细胞(PMN) 功能[3]

在体内实验中,高渗Sisomicin(20mg/ml; 耳内灌注)可用于构建小鼠内耳损伤模型[4]。Sisomicin(20mg/kg; i.p.)导致兔子神经肌肉抽搐张力降低[5]

实验参考方法

Cell experiment [1]:

Cell lines

Mycobacterium smegmatis

Preparation Method

The survival of M. smegmatis ΔpdtaS mutant cells grown in liquid medium with the addition of selected antibiotics was studied using standard colony-forming unit (CFU) methodology. Actively growing cells from the logarithmic stage of growth were diluted in 7H9 medium supplemented with OADC and Tween-80 to an OD600 of 0.1. Sisomicin at a final concentration of 2.3μg/ml was used. The kinetics of growth was measured by recording OD600 at 3, 6, 9 and 24h after the addition of antibiotics. At the 9 and 24h time points, 10-fold serial dilutions of cells were spread on 7H10 agar containing OADC. Plates were incubated at 37°C for 3-5 days, colonies were counted, and data were plotted using Excel. A Student's t-test was performed to determine the statistical significance between the test and control values.

Reaction Conditions

2.3μg/ml; 3, 6, 9 and 24h

Applications

Compared to the wild-type Mycobacterium smegmatis, the PdtaS gene deletion (ΔpdtaS) mutant shows increased sensitivity to sisomicin.
Animal experiment [2]:

Animal models

Rabbits

Preparation Method

Twenty rabbits weighing 2.2-4.4kg were subjected to tracheotomy after anesthesia induction. Mechanical ventilation was controlled to maintain arterial carbon dioxide pressure (PaCO₂) between 35-45mmHg. Blood pressure and arterial blood gas analysis were monitored through a catheterized carotid artery. The external jugular vein was cannulated for fluid (5%D/W, at a rate of 10ml/kg/hr) and drug administration. The left gastrocnemius tendon was cut and secured to a U-type force-displacement transducer. A heating pad was used to maintain body temperature above 36°C, and the muscle was housed in a clear enclosure warmed by a heat lamp. A thermometer in contact with the muscle surface measured muscle temperature. The left tibial nerve was cut after dissection from the sciatic nerve and covered with mineral oil. The cut tibial nerve was directly stimulated using a stimulator and 27 gauge thin-walled steel-needle electrodes. Maximal square-wave pulses (0.1ms duration) were delivered at a rate of 0.1Hz. The resultant isometric force of muscle twitch tension and arterial blood pressure were continuously recorded on a Nihon Kohden polygraph.

When a stable twitch was obtained, an initial dose of Sisomicin (20mg/kg, n=7) was administered intravenously, and the initial dose and maximum percentage of twitch inhibition were determined. Additional Sisomicin (10mg/kg) was given to study the response to twitch inhibition exceeding 90%.

Dosage form

20mg/kg; i.p.

Applications

Sisomicin caused a decrease in neuromuscular twitch tension in rabbits.

References:
[1] Dadura K, P?oci?ska R, Rumijowska-Galewicz A, et al. PdtaS Deficiency Affects Resistance of Mycobacteria to Ribosome Targeting Antibiotics. Front Microbiol. 2017 Nov 3;8:2145.
[2] Matsukawa S, Suh JH, Hashimoto Y, et al. Neuromuscular blocking actions of the aminoglycoside antibiotics sisomicin and micronomicin in the rabbit. Tohoku J Exp Med. 1997 Apr;181(4):471-3.

化学性质

Cas No. 32385-11-8 SDF
别名 紫苏霉素
Canonical SMILES N[C@H]1[C@](O[C@@H]2[C@@H](N)C[C@@H](N)[C@H](O[C@@]3([H])OC[C@](C)(O)[C@H](NC)[C@H]3O)[C@H]2O)([H])OC(CN)=CC1
分子式 C19H37N5O7 分子量 447.5
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1 mM 2.2346 mL 11.1732 mL 22.3464 mL
5 mM 446.9 μL 2.2346 mL 4.4693 mL
10 mM 223.5 μL 1.1173 mL 2.2346 mL
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