Bafilomycin C1

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[2]. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC)[2].

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Fungal

Signaling Pathways >> Anti-infection >> Bacterial

Bafilomycin C1 (0.33-10 μM; 6 days) inhibits the growth and proliferation of SMMC7721 and HepG2 cells in a timeand dose-dependent manner[2]. 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[2]. Bafilomycin C1 (3.3-10 μM; 24 hours) causes morphological alterations and increases the population of apoptotic cells by Hoechst 33258 (HY-15558) staining compared to vehicle[2]. Cell Viability Assay[2] 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[2] 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[2] Cell Line: SMMC7721 and HepG2 cells Concentration: 3.3 μM; 10 μM Incubation Time: 24 hours Result: Induced apoptosis in SMMC7721 and HepG2 cells.

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[1]. Animal Model: BALB/c nude mice (weighing 18-20 g) subcutaneous injected by SMMC7721 cell suspension (5×106 cells/100 μL)[2] Dosage: 0.2 mg/kg Administration: Subcutaneous injection; 20 days Result: Suppressed tumor growth of SMMC7721 tumor xenografts.

[1]. E J Bowman, et al. Bafilomycins: A Class of Inhibitors of Membrane ATPases From Microorganisms, Animal Cells, and Plant Cells. Proc Natl Acad Sci U S A. 1988 Nov;85(21):7972-6.

[2]. Xiaoxiao Gao,et al.Bafilomycin C1 Induces G0/G1 Cell-Cycle Arrest and Mitochondrial-Mediated Apoptosis in Human Hepatocellular Cancer SMMC7721 Cells. J Antibiot (Tokyo). 2018 Sep;71(9):808-817.