Ciprofloxacin (Bay-09867) hydrochloride monohydrate 是一种口服有效的拓扑异构酶 IV 抑制剂。Ciprofloxacin hydrochloride monohydrate 诱导线粒体 DNA 和核 DNA 损伤并导致线粒体功能障碍和活性氧产生。Ciprofloxacin hydrochloride monohydrate 具有抗增殖活性并诱导细胞凋亡 (apoptosis)。Ciprofloxacin hydrochloride monohydrate 是一种氟喹诺酮类抗生素，具有强大的抗菌活性。
| 生物活性 | Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally activetopoisomeraseIVinhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and inducesapoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinoloneantibiotic, exhibiting potentantibacterialactivity[1][2][3][4]. |
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体外研究
(In Vitro) | Ciprofloxacin (Bay-09867) hydrochloride monohydrate (5-50 μg/mL; 0-24 h; tendon cells) inhibits cell proliferation and causes cell cycle arrest at the G2/M phase[1].
Ciprofloxacin (Bay-09867) hydrochloride monohydrate shows potent activity againstY. pestisandB. anthraciswith MIC90of 0.03 μg/mL and 0.12 μg/mL, respectively[2].
Cell Viability Assay[1] | Cell Line: | Tendon cells | | Concentration: | 5, 10, 20 and 50 μg/mL | | Incubation Time: | 24 hours | | Result: | Decreased the cellularity of tendon cells. |
Cell Cycle Analysis[1] | Cell Line: | Tendon cells | | Concentration: | 50 μg/mL | | Incubation Time: | 24 hours | | Result: | Arrested cell cycle at the G2/M phase and inhibited cell division in tendon cells. |
Western Blot Analysis[1] | Cell Line: | Tendon cells | | Concentration: | 50 μg/mL | | Incubation Time: | 0, 6, 12, 17 and 24 hours | | Result: | Down-regulated the expression of CDK-1 and cyclin B protein and mRNA. Up-regulated the expression of PLK-1 protein. |
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体内研究
(In Vivo) | Ciprofloxacin (Bay-09867) hydrochloride monohydrate (30 mg/kg; i.p.; for 24 hours; BALB/c mice) has protection againstY. pestisin murine model of pneumonic plague[3].
Ciprofloxacin (Bay-09867) hydrochloride monohydrate (100 mg/kg; i.g.; daily, for 4 weeks; C57BL/6J mice) accelerates aortic root enlargement and increases the incidence of aortic dissection and rupture by decreases LOX level and increases MMP levels and activity in the aortic wall[4].
Ciprofloxacin (Bay-09867) hydrochloride monohydrate (100 mg/kg; i.g.; daily, for 4 weeks; C57BL/6J mice) induces DNA damage and release of DNA to the cytosol, mitochondrial dysfunction, and activation of cytosolic DNA sensor signaling. Ciprofloxacin lactate increases apoptosis and necroptosis in the aortic wall[4].
| Animal Model: | BALB/c mice[3] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection; for 24 hours | | Result: | Reduced the lung bacterial load in murine model of pneumonic plague. |
| Animal Model: | C57BL/6J mice[4] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; daily, for 4 weeks | | Result: | Had aortic destruction that was accompanied by decreased LOX expression and increased MMP expression and activity. |
| Animal Model: | C57BL/6J mice[4] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; daily, for 4 weeks | | Result: | Caused mitochondrial DNA and nuclear DNA damage, leading to mitochondrial dysfunction and ROS production. Increased apoptosis and necroptosis in the aortic wall. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(12.96 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.5919 mL | 12.9594 mL | 25.9188 mL | | 5 mM | 0.5184 mL | 2.5919 mL | 5.1838 mL | | 10 mM | 0.2592 mL | 1.2959 mL | 2.5919 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 (sealed storage, away from moisture)。-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: ≥ 0.5 mg/mL (1.30 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 5.0 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: ≥ 0.5 mg/mL (1.30 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 5.0 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: ≥ 0.5 mg/mL (1.30 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.30 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 5.0 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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