Dyslipidemia in patients with hypercholesterolemia has been recently linked to increased human cathelicidin LL-37 (LL-37) serum concentration. We tested a hypothesis that upregulated expression of LL-37 gene in peripheral blood leucocytes is involved in dyslipidemia in patients with hypercholesteremia. Patients with hypercholesterolemia were used in the study. Expression of LL-37 and human glyceraldehyde-3-phosphate dehydrogenase in peripheral blood leucocytes were quantified by real-time RT-PCR. Serum LL-37 concentration was estimated by enzyme-linked immunosorbent assay. Serum lipid levels were assessed by absorptiometry in all cases. Patients with hypercholesterolemia as compared to control ones were characterized by (a) an up-regulation of LL-37 gene expression in peripheral blood leucocytes with parallel increase of serum LL-37 concentration and (b) an increase of serum total and low-density lipoprotein cholesterol concentrations. Patients with hypercholesterolemia after a treatment with atorvastatin calcium 20 mg daily as compared to that patients before the treatment: an down-regulation of LL-37 gene expression in peripheral blood leucocytes with parallel decrease of serum LL-37 concentration. We also found significant correlation between serum LL-37 and high-density lipoprotein cholesterol levels (r = 0.7290, P < 0.0001). The results suggest that hypercholesterolemia is associated with an increased LL-37 gene expression in peripheral blood leucocytes. The correlation between serum LL-37 and high-density lipoprotein cholesterol levels suggests that LL-37 may play a key role in regulation of cholesterol levels in hypercholesterolemia.