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。
| 生物活性 | Erythromycin thiocyanate is amacrolideantibioticproduced byactinomycete Streptomyceserythreus with a broad spectrum of antimicrobial activity. Erythromycin thiocyanate binds tobacterial50S 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]. |
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体外研究
(In Vitro) | Erythromycin thiocyanate inhibits growth ofP. falciparumwith IC50and IC90values 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). |
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体内研究
(In Vivo) | 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. |
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| 结构分类 | - Antibiotics
- Macrolide Antibiotics
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(126.10 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2610 mL | 6.3050 mL | 12.6100 mL | | 5 mM | 0.2522 mL | 1.2610 mL | 2.5220 mL | | 10 mM | 0.1261 mL | 0.6305 mL | 1.2610 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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