1. Anti-infection Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Bacterial Reactive Oxygen Species
  3. Antibacterial agent 237

Antibacterial agent 237 (compound Ru-8) 是金黄色葡萄球菌的抑菌剂,MIC 为 0.78-1.56 μg/mL。Antibacterial agent 237 通过破坏细菌细胞膜,改变其通透性,诱导细菌产生 活性氧,导致细菌死亡且不引起耐药性。Antibacterial agent 237 对兔红细胞和 Raw 264.7 细胞有较低溶血毒性,在小鼠皮肤创面感染模型和大蜡杆菌幼虫感染模型中,对金黄色葡萄球菌有显著抗菌作用。

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Antibacterial agent 237 Chemical Structure

Antibacterial agent 237 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antibacterial agent 237 (compound Ru-8) is a bacteriostatic agent for Staphylococcus aureus, with MIC of 0.78-1.56 μg/mL. Antibacterial agent 237 destroys bacterial cell membranes, changes their permeability, and induces bacteria to produce Reactive Oxygen Species, leading to bacterial death without causing drug resistance. Antibacterial agent 237 has low hemolytic toxicity to rabbit red blood cells and Raw 264.7 cells, and has significant antibacterial effects against Staphylococcus aureus in mouse skin wound infection models and Bacillus major larvae infection models[1].

体外研究
(In Vitro)

Antibacterial agent 237 对 S. aureus Newman,S. aureus ATCC 29213,Methicillin-resistant S. aureus ATCC 33591,E. coli 25922,PAO1 有抗菌作用,MIC 为 0.78 μg/mL,1.56 μg/mL,1.56 μg/mL,100 μg/mL,50 μg/mL[1]
Antibacterial agent 237 在高盐浓度下仍然保持抑制 S. aureus Newman 的活性,MIC 为 0.78 μg/mL,且在哺乳动物体液 (血清,血浆,血液) 中保持稳定性[1]
Antibacterial agent 237 (0-4.68 μg/mL,0-120 min) 能够高效快速杀伤 S. aureus Newman,且具有浓度依赖性,有效避免产生耐药性[1]
Antibacterial agent 237 (0-49.92 μg/mL,24 h) 可去除 S. aureus Newman 的生物膜,且呈剂量依赖效应[1]
Antibacterial agent 237 (0.39 μg/mL,5-6 h) 不易诱导 S. aureus Newman 耐药[1]
Antibacterial agent 237 (0.78-4.68 μg/mL,0-6 h) 破坏 S. aureus Newman 细胞膜,产生 ROS,使细菌内容物渗漏,导致细菌死亡[1]
Antibacterial agent 237 (0-100 μg/mL,24 h) 对 S. aureus Newman 有杀伤作用且不损伤正常细胞[1]

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

Cell Viability Assay[1]

Cell Line: S. aureus Newman
Concentration: 0, 1.56, 3.12, 4.68 μg/mL; 0, 0.78, 1.56, 3.12, 6.24, 12.48, 24.96, 49.92 μg/mL; 0.39 μg/mL; 0.78, 1.56, 3.12, 4.68 μg/mL; 0-100 μg/mL
Incubation Time: 0, 30, 60, 90, 120 min; 24 h; 5-6 h; 0-6 h
Result: Killed S. aureus Newman within 2 hours at a concentration of 6 × MIC.
Did not significantly remove the biofilm at 1 × MIC (0.78 μg/mL), whereas when the concentration increased to 16 × MIC (12.48 μg/mL), the biofilm removal effect decreased by 60%.
Did not change the sensitivity of S. aureus Newman and showed no obvious resistance to other antibiotics.
Disrupted the cell membrane, causing ROS to accumulate.

Cell Cytotoxicity Assay[1]

Cell Line: RAW 264.7
Concentration: 0, 6.25, 12.5, 25, 50, 100 μg/mL
Incubation Time: 24 h
Result: Had a killing effect on bacteria without damaging normal cells and had good biocompatibility.

Immunofluorescence[1]

Cell Line: S. aureus Newman
Concentration: 4.68 μg/mL
Incubation Time: 2 h
Result: Showed strong red fluorescence, indicating that it had the ability to destroy bacterial cell membranes and had a concentration-dependent depolarization.
体内研究
(In Vivo)

Antibacterial agent 237 (0-256 mg/kg,注射在尾巴的第二对腹足处) 在大蜡杆菌幼虫模型中显示出良好的药物安全性,且对大蜡杆菌幼虫体内感染有良好的治疗效果[1]
Antibacterial agent 237 (50,100 μg/mL,涂抹无菌乳膏) 对 S. aureus Newman 感染的小鼠模型有良好的治疗效果[1]

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

Animal Model: Large wax borer larvae; G. mellonella larvae model[1]
Dosage: 0, 32, 64, 128, 256 mg/kg; 128, 256 mg/kg
Administration: Inject at the second pair of abdominal feet in the tail
Result: Showed concentration was 32 mg/kg, the survival rate of the larvae of Bacillus waxii was 100%, and even when it was increased to 256 mg/kg, the survival rate of the larvae of Bacillus waxii was still 75%.
Showed concentration was 128 mg/kg, the survival rate of the larvae of Bacillus waxii was 75%, and when the dose was increased to 256 mg/kg, the survival rate of the larvae of Bacillus waxii increased by 10%.
Animal Model: A mouse back wound infection model[1]
Dosage: 50 and 100 μg/mL
Administration: Apply
Result: Healed wounds and reduced bacterial content in wounds.
分子量

1261.87

Formula

C65H69Cl3N10RuS2

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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Antibacterial agent 237
目录号:
HY-162818
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