Ciprofloxacin (Bay-09867) 是一种口服有效的拓扑异构酶 IV 抑制剂。Ciprofloxacin 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 具有抗增殖活性并诱导细胞凋亡 (apoptosis)。Ciprofloxacin 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) is a potent, orally activetopoisomeraseIVinhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and inducesapoptosis. Ciprofloxacin is a fluoroquinoloneantibiotic, exhibiting potentantibacterialactivity[1][2][3][4]. |
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体外研究
(In Vitro) | Ciprofloxacin (Bay-09867) (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) shows potent activity againstY. pestisandB. anthraciswith MIC90of 0.03 μg/mL and 0.12 μg/mL, respectively[2].
Cell Cycle Analysis[1] | Cell Line: | Tendon cells | | Concentration: | 5, 10, 20 and 50 μg/mL | | Incubation Time: | 24 hours | | Result: | Decreased the cellularity of tendon cells. |
Apoptosis 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) (30 mg/kg; i.p.; for 24 hours; BALB/c mice) has protection againstY. pestisin murine model of pneumonic plague[3].
Ciprofloxacin (Bay-09867) (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) (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, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: 0.1 M HCL : 16.67 mg/mL(50.31 mM;ultrasonic and warming and adjust pH to 2 with HCl and heat to 60℃) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 3.0180 mL | 15.0902 mL | 30.1805 mL | | 5 mM | 0.6036 mL | 3.0180 mL | 6.0361 mL | | 10 mM | 0.3018 mL | 1.5090 mL | 3.0180 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 (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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