1. Anti-infection
  2. Antibiotic
  3. Amicoumacin A

Amicoumacin A 是一种具有口服活性的抗生素 (Antibiotic)。Amicoumacin A 以细菌核糖体为作用靶点,通过稳定 mRNA 与核糖体的相互作用抑制细菌翻译。Amicoumacin A 通过靶向真核核糖体诱导癌细胞死亡。Amicoumacin A 具有抗炎和抗溃疡活性,抑制角叉菜胶诱导的爪水肿,预防应激诱导的胃溃疡。Amicoumacin A 抑制革兰氏阳性菌、沙门氏菌属、志贺氏菌属、幽门螺杆菌以及耐甲氧西林金黄色葡萄球菌的生长。Amicoumacin A 可用于肺癌、乳腺癌、细菌感染、炎症水肿及胃溃疡的研究。

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Amicoumacin A

Amicoumacin A Chemical Structure

CAS No. : 78654-44-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Amicoumacin A is an orally active antibiotic. Amicoumacin A targets bacterial ribosomes and inhibits bacterial translation by stabilizing the interaction between mRNA and ribosomes. Amicoumacin A induces cancer cell death by targeting eukaryotic ribosomes. Amicoumacin A exhibits anti-inflammatory and anti-ulcer activities, inhibits carrageenan-induced paw edema, and prevents stress-induced gastric ulcers. Amicoumacin A inhibits the growth of Gram-positive bacteria, Salmonella spp., Shigella spp., Helicobacter pylori, and methicillin-resistant Staphylococcus aureus. Amicoumacin A can be used in the research of lung cancer, breast cancer, bacterial infections, inflammatory edema and gastric ulcers[1][2][3][4][5].

体外研究
(In Vitro)

Amicoumacin A (0-5 μM; 25-120 min) 可抑制 HEK293T 细胞、Krebs-2 无细胞体系和 S. cerevisiae 无细胞提取物中扫描依赖型和 IRES 依赖型的 mRNA 翻译[1]
Amicoumacin A (100 μM; 5 min pre-incubation + 10 min mRNA incubation) 在兔网织红细胞裂解液中可通过使 80S 核糖体沿 mRNA 停滞来抑制哺乳动物翻译延伸过程[1]
Amicoumacin A (50 nM-100 μM; 72 h) 对人类癌细胞系 (A549、MCF-7) 的细胞毒性是对非癌细胞系 (HEK293T、VA13) 的 2-4 倍,其 IC50 值范围为 0.2 μM 至 1.2 μM[1]
Amicoumacin A (30 μM; 10 min) 可降低 E. coli 核糖体中三肽的生成水平,削弱大部分核糖体完成多轮延伸循环的能力[3]
Amicoumacin A (30 min at 37 °C) 可强效抑制 E. coli S30 细胞提取物中的蛋白质合成,其 IC50 为 0.45 μM,抑制由纯化翻译组分构成的 PURE 系统中的蛋白质合成,其 IC50 为 0.20 μM[4]
Amicoumacin A (0-1000 μM; 30 sec at 37 °C) 可在体外以浓度依赖的方式抑制核糖体移位,在 1000 μM 时观察到近乎完全的抑制作用[4]
Amicoumacin A (2 μM; 30 min at 37 °C) 可抑制 E. coli S30 细胞提取物中萤火虫荧光素酶的合成[4]
Amicoumacin A 对革兰氏阳性菌具有抑制活性[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: A549 cells, MCF-7 cells, HEK293T cells, VA13 cells
Concentration: 50 nM to 100 μM
Incubation Time: 72 h
Result: Achieved an IC50 of 0.2 μM for A549 lung cancer cells.
Achieved an IC50 of 0.3 μM for MCF-7 breast cancer cells.
Achieved an IC50 of 0.55 μM for HEK293T non-cancerous embryonic kidney cells.
Achieved an IC50 of 1.2 μM for VA13 non-cancerous lung fibroblast cells.
体内研究
(In Vivo)

Amicoumacin-A (10-50 mg/kg; p.o.; single dose) 呈剂量依赖性抑制雄性 Wistar 大鼠角叉菜胶诱导的足肿胀[5]
Amicoumacin-A (10-25 mg/kg; p.o.; single dose) 可剂量依赖性地预防雄性 Sprague-Dawley 大鼠的应激性胃溃疡[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (male)[5]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.,single dose
Result: Reduced paw edema swelling to 66.7% (7.6% inhibition) at 10 mg/kg.
Reduced paw edema swelling to 61.0% (15.5% inhibition) at 25 mg/kg.
Reduced paw edema swelling to 49.4% (31.6% inhibition) at 50 mg/kg.
Animal Model: Sprague-Dawley rats (male)[5]
Dosage: 10 mg/kg; 25 mg/kg
Administration: p.o., single dose
Result: Reduced the mean ulcer index to 2.80 (34.1% preventive ratio) at 10 mg/kg.
Reduced the mean ulcer index to 1.20 (71.8% preventive ratio) at 25 mg/kg.
分子量

423.46

Formula

C20H29N3O7

CAS 号
结构分类
初始来源

Bacillus pumilus

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Amicoumacin A
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