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Clindamycin
CAS No. : 18323-44-9
MCE 国际站：Clindamycin
产品活性：Clindamycin 是一种具有口服活性的广谱抑菌林可酰胺类抗生素 (antibiotic)。Clindamycin 有效抑制细菌蛋白质合成，其具有以亚抑制浓度 (sub-MICs) 在金黄色葡萄球菌中毒力因子表达的能力。Clindamycin 的抗性是由 50S 核糖体亚基 (23S rRNA) 中抗生素结合位点的酶促甲基化产生。Clindamycin 降低杀白细胞毒素 (PVL)，毒性休克-葡萄球菌毒素 (TSST-1) 或 α-溶血素 (Hla) 的产生。Clindamycin 也可用于疟疾的研究。
研究领域：Anti-infection
作用靶点：Bacterial | Antibiotic | Parasite
In Vitro: Clindamycin (25 μg/mL, 1-18 h) inhibits ceftazidime (HY-B0593)-induced endotoxin release pretreatment in E. coli O55:B5.
Clindamycin (50-100 μg/mL, 0-12 min) enhances antibody- and complement-dependent phagocytosis in Staphylococcus aureus.
Clindamycin (0-500 μg/mL, 24-72 h) inhibits the cell proliferation in osteoblast cell culture model, stimulates the cell metabolism of osteoblast at the contratibution of 10 μg/mL.
In Vivo: Clindamycin (50-300 mg/kg; i.v., p.o.) dosage doesn’t affect pharmacokinetic parameters in rats.
Clindamycin (160-600 mg/kg; i.v.) improves survival in a dose-dependent manner in endotoxic shock mouse model.
Clindamycin (17-50 mg/kg, i.v.) has good penetration into rat muscle tissue that can be applied to inhibit the main bacteria causing odontogenic infections.
Pharmacokinetic Analysis in Rat Model
| Route | Dose (mg/kg) | t1/2 (h) | Cmax (mg/mL) | Tmax (h)a | AUC0-inf (h.mg/L) | ∱T |
| i.v. | 51(Plasma) | 2.51 (2.37–2.83) | 35.21 (25.04–42.65) | 0.08 ± 0.00 | 44.78 (28.82–65.65) | / |
| i.v. | 51(Tissue) | 2.82 (2.57–3.05) | 14.20 (10.63–14.89) | 0.25 ± 0.00 | 16.54 (13.83–18.35) | 1.10 |
| i.v. | 17(Tissue) | 3.25 (3.13–3.44) | 4.82 (3.35–6.66 | 0.25 ± 0.00 | / | / |
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