Abstract
BackgroundAlthough statins (STs) are drugs of first choice in hypercholesterolemic patients, especially in those at high cardiovascular risk, some of them are intolerant to STs or refuse treatment with these drugs. In view of this, we have evaluated the lipid-lowering effect of a nutraceutical pill containing berberine (BBR) and of ezetimibe, as alternative treatments, in monotherapy or in combination, in 228 subjects with primary hypercholesterolemia (HCH), with history of STs intolerance or refusing STs treatment. In addition, since PCSK9 was found up-regulated by STs dampening their effect through an LDL receptors (LDLRs) degradation, and BBR suppressed PCSK9 expression in cellular studies, we supplemented the stable lipid-lowering therapy of 30 genotype-confirmed Familial Hypercholesterolemia heterozygotes (HeFH) with BBR, searching for a further plasma cholesterol reduction. Plasma lipid pattern was evaluated at baseline and during treatments.ResultsIn HCH subjects the nutraceutical pill resulted more effective than EZE in lowering LDL cholesterol (−31.7% vs −25.4%, P < 0.001) and better tolerated. On treatment, LDL-C level below 3.36 mmol/L (≤130 mg/dl) was observed in 28.9% of subjects treated with the nutraceutical pill and 11.8% of those treated with EZE (P <0.007). In the group treated with EZE the subjects carrying the G allele of the g.1679 C > G silent polymorphism of NPC1L1 gene showed a higher response to EZE than homozygous for the common allele (GG + CG: LDL-C −29.4±5.0%, CC −23.6±6.5%, P <0.001). Combined treatment with these drugs was as effective as STs in moderate doses (LDL cholesterol −37%, triglycerides −23%). In HeFH patients the addition of BBR resulted in LDL cholesterol reductions inversely related to those induced by the stable therapy (r = −0.617, P <0.0001), with mean 10.5% further decrease.ConclusionsThe alternative treatments tested in our HCH subjects were rather effective and safe. The findings in HeFH patients suggest that BBR might act in vivo increasing expression and stability of LDLRs and/or suppressing PCSK9 expression.
Highlights
Statins (STs) are drugs of first choice in hypercholesterolemic patients, especially in those at high cardiovascular risk, some of them are intolerant to STs or refuse treatment with these drugs
Subjects Comparison between the lipid-lowering effect of a nutraceutical-combined pill containing berberine (BBR/P/Red yeast rice (RR)) and of ezetimibe (EZE) in monotherapy Among outpatients attending our Lipid Clinic we considered eligible for this study subjects with primary polygenic HCH, diagnosed on the basis of personal and family studies, who had a negative history of cardiovascular disease and were previously found to be intolerant to STs or were refusing treatment with these drugs
The comparison of the two treatments in terms of percent lipid variations showed that BBR/P/RR was more effective than EZE in reducing total cholesterol (TC), LDL cholesterol (LDL-C) and non-High-density lipoprotein cholesterol (HDL-C) levels, and showed a tendency to lower TG more than EZE
Summary
Statins (STs) are drugs of first choice in hypercholesterolemic patients, especially in those at high cardiovascular risk, some of them are intolerant to STs or refuse treatment with these drugs. We have evaluated the lipid-lowering effect of a nutraceutical pill containing berberine (BBR) and of ezetimibe, as alternative treatments, in monotherapy or in combination, in 228 subjects with primary hypercholesterolemia (HCH), with history of STs intolerance or refusing STs treatment. The HMG-CoA reductase inhibitors (Statins, STs) are the drugs of first choice to lower plasma cholesterol, especially in patients at high or very high risk for cardiovascular disease (CVD), in view of their documented and dose-related efficacy in reducing CVD morbidity and mortality in both primary and secondary prevention [2,3,4,5]. Alternative hypocholesterolemic treatments to be considered for the above mentioned cases include plant sterols and stanols, the cholesterol absorption inhibitor ezetimibe, bile acid sequestrants (especially the well tolerated colesevelam) and some nutraceutical products containing various associations of red yeast rice, policosanols, phytosterols and berberine [2,6,7,8].
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