Erythromycin 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 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 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 is amacrolideantibioticproduced byactinomycete Streptomyceserythreus with a broad spectrum of antimicrobial activity. Erythromycin 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 also exhibits antitumor and neuroprotective effect in different fields of research[3][4]. |
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体外研究
(In Vitro) | Erythromycin inhibits growth ofP. falciparumwith IC50and IC90values of 58.2 μM and 104.0 μM, respectively[1].
Erythromycin (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 (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 (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 (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 at the age of 6 weeks with EAC cells or CDF mice at the age of 6 weeks 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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(136.25 mM) H2O : 1 mg/mL(1.36 mM;ultrasonic and warming and heat to 80℃) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.3625 mL | 6.8126 mL | 13.6253 mL | | 5 mM | 0.2725 mL | 1.3625 mL | 2.7251 mL | | 10 mM | 0.1363 mL | 0.6813 mL | 1.3625 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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (2.83 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.83 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (2.83 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.83 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (2.83 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (2.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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