Background: Hepatocellular carcinoma (HCC) is related to chronic liver inflammation. M2 polarization of
tumor-associated macrophages (TAMs) in the tumor microenvironment promotes liver cancer stem-like cell (LCSLC)
self-renewal capability and carcinogenicity. Therefore, reversing M2 polarization of TAMs could be an effective
approach to cure HCC.
Objective: To evaluate whether 8-bromo-7-methoxychrysin (BrMC) has an effect on M2 polarization of TAMs.
Method: LCSLC and conditional medium were obtained by sphere forming assay. Identification of LCSLC were
analyzed by sphere forming, wound-healing and invasion assay. TAM and effects of BrMC on it were validated by
immunofluorescence staining, ELISA and griess assay. Expressions of cancer stem cell and macrophage marker were
analyzed by western blotting.
Results: Our results showed that BrMC significantly suppressed the expression of the M2 macrophage marker CD163.
Furthermore, BrMC influenced the secretion profile of cytokines of TAMs. Mechanistically, BrMC reversed M2
polarization of TAMs due to inhibition of NF-κB activation.
Conclusion: BrMC may be a potentially novel flavonoid agent that can be applied for disrupting the interaction of
LCSLCs and TAMs.