Characterization of Caerulomycin A as a dual-targeting anticancer agent.

ABSTRACT: Caerulomycin A (CaeA), isolated from actinomycetes, has a featured 2,2'-bipyridine core structure. Based on the results of in silico drug-protein docking analysis, CaeA shows potential ligands for interacting with both tubulin and DNA topoisomerase I (Topo-1). The result was confirmed by cell-free tubulin polymerization assay and Topo-1 activity assay. In vitro assays also demonstrated that CaeA increases the polymerization of tubulin and increases cell size. In addition, CaeA inhibits cell viability and growth of various cancer cells, yet exhibits low cytotoxicity. CaeA also affects paclitaxel-resistant cancer cells and synergizes the effect with paclitaxel in reducing cancer cell colony formation rate. In vivo experiments confirm the effect of CaeA on reducing tumor size and weight in nu

SUBMITTER: Tong L 

PROVIDER: S-EPMC9077901 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature