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Erythromycin thiocyanate

(Synonyms: 红霉素硫氰酸盐) 目录号 : GC67842

Erythromycin thiocyanate 是由放线菌产生的大环内酯类抗生素 (Antibiotic),具有广泛的抗菌活性。Erythromycin thiocyanate 通过结合细菌的 50S 核糖体亚基而起作用,并通过阻断转肽和/或易位反应来抑制 RNA 依赖性蛋白 (RNA-dependent protein synthesis) 的合成,而不会影响核酸的合成。Erythromycin thiocyanate 在不同领域的研究中显示出抗肿瘤特性和保护神经的作用。

Erythromycin thiocyanate Chemical Structure

Cas No.:7704-67-8

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Sample solution is provided at 25 µL, 10mM.

Description

Erythromycin thiocyanate is a macrolide Antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin thiocyanate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin thiocyanate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].

Erythromycin thiocyanate inhibits growth of P. falciparum with IC50 and IC90 values of 58.2 μM and 104.0 μM, respectively[1].
Erythromycin thiocyanate (10 μM, 100 μM; 24 h, 72 h) shows antioxidant and anti-inflammatory effects and suppresses the accumulation of 4-HNE (p<0.01) and 8-OHdG (p<0.01), reduces Iba-1 (p<0.01) and TNF-α (p<0.01) expression significantly[4].

Cell Viability Assay[4]

Cell Line: Embryos primary cortical neuron (from the cerebral cortices of 17-day-old Sprague-Dawley rat)
Concentration: 10, 100 μM
Incubation Time: 24, 72 hours
Result: Improved the viability of cultured neuronal cells in vitro after 3 hours oxygen-glucose deprivation (OGD).

Erythromycin thiocyanate (gastric intubation; 0.1-50 mg/kg; 30-120 days) decreases tumor growth and prolong the survival time of mice from dose of 5 mg/kg in mice[3].
Erythromycin thiocyanate (gastric intubation; 5 mg/kg) protects mice alive even at 120 days after inoculation, but shortens mean survival time in tumor-bearing mice by 4-5 days with dose of 50 mg/kg[3].
Erythromycin thiocyanate (i.h.; single injection; 50 mg/kg) has a protective effect on the rat model with cerebral ischemia reperfusion-injury[4].

Animal Model: Female ddY mice (6-week-old) with EAC cells or CDF mice (6-week-old) with P388 cells[3]
Dosage: 0.1 mg/kg; 0.5 mg/kg; 10 mg/kg; 30 mg/kg; 50 mg/kg
Administration: Gastric intubation; 30-120 days
Result: Decreased tumor growth and prolonged the mean survival time of mice from the dose of 5 mg/kg, however, the 50 mg/kg dosage shortened the MST in tumorbearing mice.
Animal Model: Male Sprague-Dawley rats (8-week-old, 250-300 g)[4]
Dosage: 50 mg/kg
Administration: Subcutaneous single injection
Result: Reduced infarct volume and edema volume, improved neurological deficit.

[1]. Gribble MJ, et al. Erythromycin. Med Clin North Am. 1982 Jan;66(1):79-89.
[2]. Nakornchai S, et al. Activity of azithromycin or erythromycin in combination with antimalarial drugs against multidrug-resistant Plasmodium falciparum in vitro. Acta Trop. 2006 Dec;100(3):185-91. Epub 2006 Nov 28.
[3]. Hamada K, et al. Antitumor effect of erythromycin in mice. Chemotherapy. 1995 Jan-Feb. 41(1):59-69.
[4]. Katayama Y, et al. Neuroprotective effects of erythromycin on cerebral ischemia reperfusion-injury and cell viability after oxygen-glucose deprivation in cultured neuronal cells. Brain Res. 2014 Nov 7. 1588:159-67.

化学性质

Cas No. 7704-67-8 SDF Download SDF
别名 红霉素硫氰酸盐
分子式 C38H68N2O13S 分子量 793.02
溶解度 DMSO : 100 mg/mL (126.10 mM; Need ultrasonic) 储存条件 Store at -20°C, away from moisture
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1 mg 5 mg 10 mg
1 mM 1.261 mL 6.305 mL 12.61 mL
5 mM 0.2522 mL 1.261 mL 2.522 mL
10 mM 0.1261 mL 0.6305 mL 1.261 mL
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