Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).
体外研究
Bafilomycin C1 (0.33-10 μM; 6 days) inhibits the growth and proliferation of SMMC7721 and HepG2 cells in a timeand dose-dependent manner. Bafilomycin C1 (0.33-3.3 μM; 24 hours) decreases cyclin D3, cyclin E1, CDK2, CDK4, and CDK6 expression in both mRNA and protein expression in SMMC7721 cells. Bafilomycin C1 (3.3-10 μM; 24 hours) causes morphological alterations and increases the population of apoptotic cells by Hoechst 33258 staining compared to vehicle.
Cell Viability Assay
Cell Line:
SMMC7721 cell and HepG2 cell
Concentration:
0.33 μM, 1.1 μM, and 3.3 μM for SMMC7721 1.1 μM, 3.3 μM, and 10.0 μM for HepG2
Incubation Time:
6 days
Result:
Retarded the cell growth.
Western Blot Analysis
Cell Line:
SMMC7721 cells
Concentration:
3.3 μM
Incubation Time:
24 hours
Result:
Decreaed cyclin D3/E1,CDK2/4/6 protein expression and increased p21.
Apoptosis Analysis
Cell Line:
SMMC7721 and HepG2 cells
Concentration:
3.3 μM; 10 μM
Incubation Time:
24 hours
Result:
Induced apoptosis in SMMC7721 and HepG2 cells.
体内研究
Bafilomycin C1 (subcutaneous injection; 0.2 mg/kg; 20 days) retards the tumor growth without apparent adverse reactions or side effects in nude mice model.