Berberine, the main
isoquinoline alkaloid obtained from traditional plants, e.g., Berberis, Coptis, Coscinium
spps., etc., is known to exhibit anticancer activity in vitro and in vivo. In this study, the anticancer potential of
berberine combined with
PEGylated liposomal doxorubicin (
polyethylene glycol (PEG)-lip-DOX) was investigated. At first, the effect of
berberine on endothelial cells was examined in vitro by use of human umbilical vein endothelial cells (HUVECs):
Berberine inhibited HUVEC growth with an IC50 at 24 h of about 144 µg/mL and that at 72 h of about 29 µg/mL. In contrast, less than 50 µg/mL
berberine inhibited the
vascular endothelial growth factor (
VEGF) expression to some extent after a 24-h incubation, suggesting that
berberine suppressed angiogenic action under the condition of little cytotoxicity. Next, the in vivo anticancer activity of the combination of
berberine (intraperitoneally (i.p.)) and PEG-lip-DOX (intravenously (i.v.)) was examined in Meth A
sarcoma-transplanted BALB/c mice. The results showed that either
berberine or PEG-lip-DOX exhibited antiproliferative activity against Meth A cells. Moreover, treatment with the combination of
berberine and PEG-lip-DOX suppressed the
tumor growth more strongly than that with
berberine or PEG-lip-DOX alone. Based on these findings, the combination
cancer chemotherapy with
berberine and
PEGylated liposomal doxorubicin may be beneficial for the treatment of
cancer.