Hexanic lipidosterolic extract of Serenoa repens inhibits the expression of two key inflammatory mediators, MCP‐1/CCL2 and VCAM‐1, in vitro

What's known on the subject? and What does the study add? Pervasive inflammatory infiltrates, mainly composed of chronically activated T cells and monocytes/macrophages, have been observed in benign prostatic hyperplasia (BPH). Permixon®, a hexanic lipidosterolic extract of Serenoa repens (hexanic LSESr) used to treat urinary dysfunction in BPH patients, has anti‐inflammatory activities. This paper provides new insights into the anti‐inflammatory properties of Permixon®. We report that hexanic LSESr inhibits early steps of leukocyte infiltration in vitro by downregulating MCP‐1/CCL2 and VCAM‐1 expression. OBJECTIVE • To investigate the mechanisms by which hexanic lipidosterolic extract of Serenoa repens (hexanic LSESr) may prevent leukocyte infiltration in benign prostatic hyperplasia by studying its impact on monocyte chemoattractant protein 1/chemokine (C‐C motif) ligand 2 (MCP‐1/CCL2) and vascular cell adhesion molecule 1 (VCAM‐1) expression in vitro. MATERIALS AND METHODS • After pretreatment with hexanic LSESr, human prostate (epithelial and myofibroblastic) cells and vascular endothelial cells were stimulated with proinflammatory cytokines. • MCP‐1/CCL2 and VCAM‐1 mRNA expression was quantified by real‐time PCR. • ELISA kits were used to determine MCP‐1/CCL2 levels in culture supernatants and VCAM‐1 expression in living cells. RESULTS • Hexanic LSESr reduced MCP‐1/CCL2 mRNA levels in both epithelial (BPH‐1) and myofibroblastic (WPMY‐1) prostate cell lines. • Hexanic LSESr downregulated MCP1/CCL2 secretion by WPMY‐1 cells in a concentration‐dependent manner, more efficiently than Serenoa repens extracts obtained by supercritical carbon dioxide extraction. • Hexanic LSESr inhibited tumour‐necrosis‐factor‐α‐induced MCP‐1/CCL2 secretion by the human vascular endothelial cell line EAhy.926, as well as surface VCAM‐1 protein expression, in a concentration‐dependent manner. CONCLUSIONS • Hexanic LSESr impedes key steps of monocyte and T cell attraction and adherence by inhibiting MCP‐1/CCL2 and VCAM‐1 expression by human prostate and vascular cells in an inflammatory environment. • These findings provide new insights into the anti‐inflammatory effects of the hexanic lipidosterolic extract of Serenoa repens, Permixon®, in benign prostatic hyperplasia.