Ciprofloxacin (hydrochloride)
(Synonyms: 盐酸环丙沙星; Bay-09867 monohydrochloride) 目录号 : GC15241
Ciprofloxacin (hydrochloride)是一种有效的、具有口服活性的氟喹诺酮类抗生素，具有抗微生物和免疫调节活性。
Cas No.:93107-08-5
Sample solution is provided at 25 µL, 10mM.
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Ciprofloxacin (hydrochloride) is an effective and orally active fluoroquinolone antibiotic with antimicrobial and immunomodulatory activities [1]. Ciprofloxacin is an inhibitor of DNA gyrase and topoisomerase IV, enzymes that are responsible for negative supercoiling of chromosomes and separation of DNA strands, thereby hindering the initiation of bacterial replication [2]. Ciprofloxacin is active against a variety of Gram-positive and Gram-negative bacteria, including Staphylococcus aureus, Listeria monocytogenes, Pseudomonas aeruginosa, Legionella, Neisseria gonorrhoeae, and Helicobacter pylori. Ciprofloxacin can be used for the treatment of various bacterial infections [3].
In vitro, Ciprofloxacin (5-50μg/mL; 0-24h) can inhibit cell proliferation and cause cell cycle arrest at the G2/M phase [4]. Ciprofloxacin (100, 200 and 500μg/ml; 18, 24, 48 and 72h) inhibits DNA synthesis in colon cancer cells (CC-531, HT-29, SW-403) in a time- and dose-dependent manner, activates caspases 3, 8 and 9, upregulates the expression of pro-apoptotic Bax, reduces cell proliferation and induces cell apoptosis [5].
In vivo, Ciprofloxacin (30mg/kg/d; single dose; i.p) significantly reduces bacterial load in the lungs and spleens of the Pneumonic Plague mouse model and increases the survival rate of mice [6]. Ciprofloxacin (100mg/kg/day for 4 weeks; gavage) treatment reduces the expression and activity of lysyl oxidase (LOX) in aortic aneurysm and aortic dissection (AAD) mouse model, increases the levels and activities of matrix metalloproteinases (MMP), and increases the fragmentation of elastic fibers and cell damage, and increases the incidence of aortic dissection and rupture [7].
References:
[1] Fukumoto R, Cary LH, Gorbunov NV, et al. Ciprofloxacin modulates cytokine/chemokine profile in serum, improves bone marrow repopulation, and limits apoptosis and autophagy in ileum after whole body ionizing irradiation combined with skin-wound trauma. PLoS One. 2013;8(3):e58389.
[2] Drlica K, Zhao X. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997;61(3):377-392.
[3] Nilius, A.M., Shen, L.L., Hensey-Rudloff, D., et al. Antimicrob. Agents Chemother. 47(10), 3260-3269(2003).
[4] Tsai WC, Hsu CC, Tang FT, Wong AM, Chen YC, Pang JH. Ciprofloxacin-mediated cell proliferation inhibition and G2/M cell cycle arrest in rat tendon cells. Arthritis Rheum. 2008;58(6):1657-1663.
[5] Herold C, Ocker M, Ganslmayer M, et al. Ciprofloxacin induces apoptosis and inhibits proliferation of human colorectal carcinoma cells[J]. British journal of cancer, 2002, 86(3): 443-448.
[6] Hamblin KA, Armstrong SJ, Barnes KB, Davies C, Laws T, Blanchard JD, Harding SV, Atkins HS. Inhaled Liposomal Ciprofloxacin Protects against a Lethal Infection in a Murine Model of Pneumonic Plague. Front Microbiol. 2017 Feb 6;8:91.
[7] LeMaire SA, Zhang L, Luo W, et al. Effect of Ciprofloxacin on Susceptibility to Aortic Dissection and Rupture in Mice. JAMA Surg. 2018;153(9):e181804.
Ciprofloxacin (hydrochloride)是一种有效的、具有口服活性的氟喹诺酮类抗生素，具有抗微生物和免疫调节活性 [1]。Ciprofloxacin是DNA回旋酶和拓扑异构酶IV的抑制剂，这些酶负责染色体的负超卷曲和DNA链的分离，从而阻碍细菌复制的启动[2]。Ciprofloxacin对多种革兰氏阳性菌和革兰氏阴性菌都有活性，包括金黄色葡萄球菌、单核细胞增生李斯特菌、铜绿假单胞菌、军团菌、淋病奈瑟菌和幽门螺杆菌。Ciprofloxacin可用于治疗等多种细菌感染 [3]。
在体外，Ciprofloxacin（5-50μg/mL; 0-24h）可抑制细胞增殖，并在 G2/M 期阻滞导致细胞周期 [4]。Ciprofloxacin（100, 200 and 500μg/ml; 18, 24, 48 or 72h）在时间和剂量依赖性上抑制了结肠癌细胞（CC-531, HT-29, SW-403）的DNA合成，激活caspases 3, 8和9，上调促凋亡Bax的表达，减少结肠癌细胞的增殖并诱导细胞凋亡 [5]。
在体内，Ciprofloxacin（30mg/kg/d; single dose; i.p）显著降低了肺鼠疫模型小鼠中肺和脾脏的细菌负荷并提高小鼠存活率 [6]。Ciprofloxacin（100mg/kg/day for 4 weeks; gavage）治疗降低了主动脉瘤和主动脉夹层（AAD）模型小鼠的赖氨酰氧化酶（LOX）的表达和活性，提高了基质金属蛋白酶（MMP）的水平和活性以及增加了弹性纤维的断裂以及细胞损伤，并增加主动脉夹层和破裂的发生率 [7]。
| Cell experiment [1]: | |
Cell lines | CC-531 cells, HT-29 cells, and SW-403 cells |
Preparation Method | CC-531 cells, HT-29 cells, and SW-403 cells were starved for 24h in medium containing 0.125% FCS, trypsinized, seeded at a density of 0.5 × 106 per well in six-well plates (9cm2) or at a density of 5 × 103 per well in 96-well plates (1cm2) and incubated with 100, 200 or 500μg/ml Ciprofloxacin. Ciprofloxacin was dissolved in water and further diluted in culture medium. Collection of cells supernatants were saved after 18, 24, 48 or 72h of incubation and centrifuged together with the trypsinized cells (1000rpm. for 10min). Perform flow cytometry analysis and protein blotting analysis, etc. for the detection of cell apoptosis. |
Reaction Conditions | 100, 200 and 500μg/ml; 18, 24, 48 or 72h |
Applications | Ciprofloxacin inhibited the DNA synthesis of colon cancer cells in a time- and dose-dependent manner, activated caspases 3, 8 and 9, upregulated the expression of pro-apoptotic Bax, reduced the proliferation of colon cancer cells and induced cell apoptosi. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | To evaluate the effect of Ciprofloxacin on moderate sporadic atherosclerotic disease (AAD) in a mouse model, the mice were randomly divided into 4 treatment groups. Male and female wild-type (C57BL/6J) mice aged 4 weeks were given a high-fat diet for 8 weeks and then received subcutaneous injections of angiotensin II for the last 4 weeks. The control group without stimulation was fed normal diet and received saline injections. Both groups received Ciprofloxacin or solvent through daily gavage during the infusion period. At the end of the study, the mice were sacrificed, and the aorta was processed for AAD assessment and tissue analysis. |
Dosage form | 100mg/kg/day for 4 weeks; gavage |
Applications | Ciprofloxacin treatment enhanced the disintegration of elastic fibers and cell damage, as well as increasing the incidence of aortic dissection and rupture. |
References: | |
| Cas No. | 93107-08-5 | SDF | |
| 别名 | 盐酸环丙沙星; Bay-09867 monohydrochloride | ||
| 化学名 | 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid, monohydrochloride | ||
| Canonical SMILES | FC1=CC2=C(C=C1N3CCNCC3)N(C4CC4)C=C(C(O)=O)C2=O.Cl | ||
| 分子式 | C17H18FN3O3 • HCl | 分子量 | 367.8 |
| 溶解度 | Water : 74 mg/mL (201.19 mM);DMSO : 7 mg/mL (19.03 mM) | 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 | 2.7189 mL | 13.5943 mL | 27.1887 mL |
| 5 mM | 543.8 μL | 2.7189 mL | 5.4377 mL |
| 10 mM | 271.9 μL | 1.3594 mL | 2.7189 mL |
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| 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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- Purity: >98.00%
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