Bacitracin
(Synonyms: 杆菌肽) 目录号 : GC10925
Bacitracin是由地衣芽孢杆菌Bacillus subtilis var Tracy产生的一种多肽类抗生素。
Cas No.:1405-87-4
Sample solution is provided at 25 µL, 10mM.
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Bacitracin is a polypeptide antibiotic produced by organisms of the licheniformis group of Bacillus subtilis var Tracy[1]. Bacitracin inhibits cell wall biosynthesis and permeability through binding to the undecaprenyl pyrophosphate[2]. Bacitracin is typically used in the study of antibacterial mechanisms[3][4].
In vitro, treatment of human melanoma MeWo cells with Bacitracin (1mM; 48h) competitively inhibits dipeptidyl peptidase IV (DPP-IV) and aminopeptidase N (APN), reduces cell viability, and induces DNA fragmentation (sub-G₁ peak elevated to 24.3%) and cell apoptosis[5].
In vivo, Bacitracin (0-100mg/kg; i.m.; once daily for 12 days) markedly suppressed tumor growth, increased the percentages of apoptotic cells, decreased microvessel density and increased central necrotic area in MH134 hepatocellular carcinoma xenografts in C3H mice[6]. Bacitracin (20mg per mouse; p.o.; once daily for 7 days) lowers serum FITC-dextran levels, upregulates ileal ZO-1, JAM-A, occludin and colonic ZO-1, claudin-3, and claudin-4 mRNA expression, and reduces intestinal permeability in C57BL/10 mice[7].
References:
[1] Piepenbreier H, Sim A, Kobras CM, et al. From Modules to Networks: a Systems-Level Analysis of the Bacitracin Stress Response in Bacillus subtilis. mSystems. 2020;5(1):e00687-19.
[2] Economou NJ, Cocklin S, Loll PJ. High-resolution crystal structure reveals molecular details of target recognition by bacitracin. Proc Natl Acad Sci U S A. 2013;110(35):14207-14212.
[3] Buijs NP, Vlaming HC, Kotsogianni I, et al. A classic antibiotic reimagined: Rationally designed bacitracin variants exhibit potent activity against vancomycin-resistant pathogens. Proc Natl Acad Sci U S A. 2024;121(29):e2315310121.
[4] Si W, Wang L, Usongo V, Zhao X. Colistin Induces S. aureus Susceptibility to Bacitracin. Front Microbiol. 2018;9:2805.
[5] Méndez LR, Arrebola Y, Valdés-Tresanco ME, et al. Bestatin and bacitracin inhibit porcine kidney cortex dipeptidyl peptidase IV activity and reduce human melanoma MeWo cell viability. Int J Biol Macromol. 2020;164:2944-2952.
[6] Yu SJ, Yoon JH, Yang JI, et al. Enhancement of hexokinase II inhibitor-induced apoptosis in hepatocellular carcinoma cells via augmenting ER stress and anti-angiogenesis by protein disulfide isomerase inhibition. J Bioenerg Biomembr. 2012;44(1):101-115.
[7] Nevado R, Forcén R, Layunta E, Murillo MD, Grasa L. Neomycin and bacitracin reduce the intestinal permeability in mice and increase the expression of some tight-junction proteins. Rev Esp Enferm Dig. 2015;107(11):672-676.
Bacitracin是由地衣芽孢杆菌Bacillus subtilis var Tracy产生的一种多肽类抗生素[1]。Bacitracin通过与十一异戊烯焦磷酸结合，抑制细胞壁的生物合成与通透性[2]。Bacitracin通常用于抗菌机制的研究[3][4]。
体外实验中，Bacitracin（1mM；48h）可竞争性抑制人黑色素瘤MeWo细胞中的二肽基肽酶IV（DPP-IV）及氨肽酶N（APN），降低细胞活力，诱导DNA碎片化（sub-G₁峰升高至24.3%），并触发细胞凋亡[5]。
体内实验中，Bacitracin（0–100mg/kg；肌肉注射；每日一次，连续12天）显著抑制C3H小鼠MH134肝癌异种移植瘤的生长，提高凋亡细胞比例，降低微血管密度，并扩大肿瘤中心坏死区域[6]。此外，Bacitracin（每只小鼠20mg；灌胃；每日一次，连续7天）可降低C57BL/10小鼠血清FITC-dextran水平，上调回肠ZO-1、JAM-A、occludin及结肠ZO-1、claudin-3和claudin-4的mRNA表达，并减少肠道通透性[7]。
| Cell experiment [1]: | |
Cell lines | MeWo (HTB-65) tumor cells |
Preparation Method | DPP-IV and APN activities present in the membrane of the MeWo (HTB-65) tumor cells were measured spectrophotometrically using L-Gly-Pro-pNA and L-Leu-pNA as substrates, respectively. 5×104 cells per well were seeded, in a volume of 100μL of complete growth medium, in flat end 96 well plates and incubated with Bacitracin (1mM) in culture conditions for 48h. After this, the medium was removed, and 90μL of DMEM-F12 was added. To initiate the enzymatic reaction 10μL of L-Gly-Pro-pNA (0.7mM) or L-Leu-pNA (3mM) were added to each well. The reaction was done at 37°C for 30min. The formation of pNA was followed by absorbance at 405nm, inside a 96 well plate kinetic spectrophotometer. |
Reaction Conditions | 1mM; 48h |
Applications | Bacitracin inhibits DPP-IV and APN activities in the human melanoma MeWo cells. |
| Animal experiment [2]: | |
Animal models | C3H/He mice |
Preparation Method | 2.5×106 viable MH134 cells suspended in 0.1mL of RPMI-1640 were injected subcutaneously to produce a bleb in the left flanks of the C3H/He mice. When the tumor volumes reached 0.5-1.0cm3 , Bacitracin was given i.m. for 12 consecutive days. Thirteen days after injecting Bacitracin (0, 10mg/kg, 50mg/kg, or 100mg/kg), the mice were sacrificed by exsanguination through cardiac puncture under general anesthesia (isoflurane inhalation). Tumor masses and liver tissues were then harvested, fixed in 10% formaldehyde, and cryopreserved for further analyses. |
Dosage form | 0-100mg/kg; i.m.; once daily for 12 days |
Applications | Bacitracin markedly suppressed tumor growth and increased central necrotic area in MH134 hepatocellular carcinoma xenografts in C3H mice. |
References: | |
| Cas No. | 1405-87-4 | SDF | |
| 别名 | 杆菌肽 | ||
| Canonical SMILES | CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCCCCC(C(=O)NC(C(=O)N1)CCCN)NC(=O)C(C(C)C)NC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)C2CSC(=N2)C(C(C)CC)N)CC(=O)N)CC(=O)O)CC3=CN=CN3)CC4=CC=CC=C4 | ||
| 分子式 | C66H103N17O16S | 分子量 | 1422.69 |
| 溶解度 | ≥ 228.9mg/mL in Water | 储存条件 | 4°C, protect from light |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7029 mL | 3.5145 mL | 7.0289 mL |
| 5 mM | 0.1406 mL | 0.7029 mL | 1.4058 mL |
| 10 mM | 0.0703 mL | 0.3514 mL | 0.7029 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
- View current batch:
- Biological Activity: 77.0 U/mg
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet