scholarly journals The role of monacolin in the treatment of dyslipidaemia

2021 ◽  
Vol 17 (3) ◽  
pp. 221-226
Author(s):  
Krzysztof Ozierański ◽  
Marcin Grabowski

Dyslipidaemia is one of the major modifiable risk factors for cardiovascular diseases. According to the current epidemiological data, excessively high serum cholesterol levels are found in 64% of women and 70% of men aged ≥20 years in Poland. Statins are the treatment of choice in patients with high-to-very high cardiovascular risk and high low-density lipoprotein (LDL) cholesterol levels. At the other end of the spectrum, there is a group of patients with low-to-moderate cardiovascular risk and low or moderate LDL cholesterol levels, who should be put on well-planned and appropriately adjusted therapy involving lifestyle modification and, if needed, pharmacotherapy. In such cases, the current guidelines of the European Society of Cardiology make it possible to use monacolin, a nutraceutical which is a natural statin (chemically identical to lovastatin). Monacolin is found in red yeast rice and its action is based on the known mechanism of inhibition of HMG-CoA reductase, a key enzyme in endogenous cholesterol synthesis. Data on the efficacy and safety of monacolin come from many clinical trials showing a significant decrease in triglycerides, total and LDL cholesterol, resulting in a reduced number of cardiovascular events in the absence of significant adverse effects. Monacolin is likely to become an effective pharmaceutical to combat dyslipidaemia in the growing group of (relatively young) patients with low-to-moderate baseline cardiovascular risk and lowto- moderate LDL cholesterol levels, without concomitant indications for statins. This paper summarises the current knowledge on the efficacy, safety and potential indications for the use of monacolin in the treatment of dyslipidaemia.

Nutrients ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 2538
Author(s):  
Ismael San Mauro Martín ◽  
Elena Garicano Vilar ◽  
Sara Sanz Rojo ◽  
Luis Collado Yurrita ◽  
Eva Pérez Arruche ◽  
...  

Cardiovascular disease is linked to high serum low density lipoprotein (LDL)-cholesterol levels. Cardiovascular risk may be indirectly influenced by genetic load. Serum LDL-cholesterol levels may be reduced by the consumption of food enriched with plant sterols (PS). The aim was to test a plant sterol treatment on cholesterol levels according to different genetic polymorphisms. A pilot interventional trial was performed in 26 children (n = 16 girls, n = 10 boys). Seven hundred milliliters/day of commercial skimmed milk with added plant sterols delivering 2.2 g plant sterols were ingested for three weeks. Blood draws were performed at the baseline and end of the study. Significant modifications of non-high density lipoprotein (HDL)-cholesterol (p = 0.010; p = 0.013) and LDL-cholesterol (p = 0.004; p = 0.013) levels appeared in the genes LIPC C-514T and PPAR-α L162V carriers. No statistically significant differences were observed for other genes. LIPC C-514T and PPAR-alpha L162V carriers could benefit from a plant sterol supplement to ameliorate hypercholesterolemia.


2020 ◽  
Vol 20 (4) ◽  
pp. 182-193
Author(s):  
SuJin Song ◽  
Yun Jung Lee ◽  
YoonJu Song

Background: Low-density lipoprotein (LDL) cholesterol is a strong predictor of cardiovascular disease, resulting in the promotion of low-fat diets that emphasize the need to lower LDL cholesterol levels. We investigated the relationship between dietary carbohydrate intake and cardiovascular risk factors according to LDL cholesterol levels in Korean adults who typically consumed high-carbohydrate, low-fat diets.Methods: A total of 25,925 Korean adults were selected from the 2007-2015 Korea National Health and Nutrition Examination Surveys. Dietary carbohydrate intake was grouped into quintiles and cardiovascular risk factors included obesity, metabolic syndrome, type 2 diabetes, and dyslipidemia. Multiple logistic regression models were used to examine association between carbohydrate intake and cardiovascular risk factors by sex and LDL cholesterol levels.Results: Subjects with LDL cholesterol ≥130 mg/dL had significantly less energy and fat intake than those with LDL cholesterol <130 mg/dL both in men and women. In men, a higher carbohydrate intake was related to increased prevalence of atherogenic dyslipidemia and low high-density lipoprotein (HDL) cholesterol regardless of LDL cholesterol levels. Meanwhile, dietary carbohydrate intake was positively associated with low HDL cholesterol but inversely associated with hypercholesterolemia only in women with LDL cholesterol <130 mg/dL.Conclusions: High carbohydrate intake in Korean adults is associated with low HDL cholesterol or atherogenic dyslipidemia regardless of LDL cholesterol levels. Carbohydrate intake should be carefully recommended according to the lipid profiles of individuals for the prevention and management of cardiovascular disease.


2020 ◽  
Vol 17 (6) ◽  
pp. 147916412097525
Author(s):  
Gisle Langslet ◽  
Bernard Zinman ◽  
Christoph Wanner ◽  
Stefan Hantel ◽  
Rosa-Maria Espadero ◽  
...  

Objective: It is well established that higher low-density lipoprotein (LDL)-cholesterol levels are associated with increased cardiovascular risk. We analyzed whether effects of empagliflozin on cardiovascular outcomes varied by different LDL-cholesterol levels at baseline in EMPA-REG OUTCOME. Methods: Participants with type 2 diabetes and high cardiovascular risk received empagliflozin (10/25 mg) or placebo in addition to standard of care. We investigated the time to first 3P-MACE, cardiovascular death, hospitalization for heart failure (HHF) and all-cause mortality for empagliflozin versus placebo between baseline LDL-cholesterol categories <1.8, 1.8–<2.2, 2.2– <2.6, 2.6–3.0, and > 3.0 mmol/L, by a Cox regression including the interaction of baseline LDL-cholesterol category and treatment. Results: Of the 7020 participants randomized and treated, 81.0% received lipid lowering therapy (77.0% statins). Mean ± SD LDL-cholesterol was 2.2 ± 0.9 mmol/L, and 38%/18%, had LDL-cholesterol <1.8/>3.0 mmol/L. Age, BMI, and HbA1c levels were balanced between the LDL-cholesterol subgroups, but those in the lowest versus highest group, had more coronary artery disease (83.0% vs 59.9%) and statin treatment (88.2% vs 50.9%). Empagliflozin consistently reduced all outcomes across LDL-cholesterol categories (all interaction p-values > 0.05). Conclusion: The beneficial cardiovascular effects of empagliflozin was consistent across higher and lower LDL-cholesterol levels at baseline.


1998 ◽  
pp. 141-145 ◽  
Author(s):  
G Michalopoulou ◽  
M Alevizaki ◽  
G Piperingos ◽  
D Mitsibounas ◽  
E Mantzos ◽  
...  

OBJECTIVE: The association between established hypothyroidism and high cholesterol levels is well known. The aim of the present study was to investigate the effect of thyroxine (T4) administration on cholesterol levels in hypercholesterolemic subjects with TSH levels within the normal range ('high-normal' TSH compared with 'low-normal' TSH). DESIGN AND METHODS: We determined TSH levels in 110 consecutive patients referred for hypercholesterolemia (serum cholesterol >7.5 mmol/l). Those with 'high-normal' TSH (2.0-4.0 microU/ml) as well as those with 'low-normal' TSH (0.40-1.99 microU/ml) were randomly assigned to receive either 25 or 50 microg T4 daily for two months. Thus, groups A and B (low-normal TSH) received 25 and 50 microg T4 respectively and groups C and D (high-normal TSH) received 25 and 50 microg T4 respectively. Serum T4, tri-iodothyronine (T3), TSH, free thyroxine index, resin T3 uptake and thyroid autoantibodies (ThAab) as well as total cholesterol, high and low density lipoprotein cholesterol (HDL, LDL), and triglycerides were determined before and at the end of the two-month treatment period. RESULTS: TSH levels were reduced in all groups. The most striking effect was observed in group D (TSH levels before: 2.77+/-0.55, after: 1.41+/-0.85 microU/ml, P < 0.01). Subjects in groups C and D had a higher probability of having positive ThAabs. A significant reduction in total cholesterol (P < 0.01) and LDL (P < 0.01) was observed after treatment only in group D. In those subjects in group D who were ThAab negative, there was no significant effect of thyroxine on cholesterol levels. CONCLUSIONS: Subjects with high-normal TSH levels combined with ThAabs may, in fact, have subclinical hypothyroidism presenting with elevated cholesterol levels. It is possible that these patients might benefit from thyroxine administration.


10.1038/4027 ◽  
1998 ◽  
Vol 4 (12) ◽  
pp. 1434-1437 ◽  
Author(s):  
Matti K. Karvonen ◽  
Ullamari Pesonen ◽  
Markku Koulu ◽  
Leo Niskanen ◽  
Markku Laakso ◽  
...  

Circulation ◽  
2012 ◽  
Vol 125 (suppl_10) ◽  
Author(s):  
Joseph L Evans ◽  
Harold Bays ◽  
Kevin C Maki ◽  
Mal Evans ◽  
Veronique Maquet ◽  
...  

Oxidized low-density lipoprotein (OxLDL) is believed to play a role in the progression of atherosclerotic coronary heart disease (CHD) and the development of diabetes complications. This randomized, double-blind, placebo-controlled study of a novel insoluble fiber derived from the mycelium Aspergillus niger , chitin-glucan (CG) (ARTINIA™), evaluated 135 patients with fasting LDL-cholesterol 130-189.9 mg/dl and fasting glucose <=125 mg/dl. Participants were randomly assigned to receive CG (4.5 g/day; n=34), CG (1.5 g/day; n=33), CG (1.5 g/day) plus olive extract (n=33), or matching placebo (n=35) for 6 weeks. The primary outcome measure was the between-group difference in OxLDL. Secondary outcome measurements included effects upon lipid, glucose, insulin, and F2-isoprostane levels. After 6 weeks, CG 4.5 g/day (CG-4.5) significantly reduced mean OxLDL 3.8 U/L compared to baseline (58.0 U/L vs 61.8 U/L, respectively; P =0.006), and reduced OxLDL 4.97 U/L compared to placebo (P=<0.05). Other treatment groups generally had no significant effect upon OxLDL. CG treatment groups reduced LDL-cholesterol levels 3.2–;6.5% compared to placebo (P<0.05). In this study population without diabetes mellitus or elevated glucose levels, CG did not significantly affect high density lipoprotein cholesterol, triglycerides, glucose, insulin, F2-isoprostanes, or the homeostasis model assessment of insulin resistance. Treatments were well tolerated and with adverse experiences comparable to placebo. These results suggest that chitin-glucan, a novel insoluble fiber, may significantly reduce OxLDL and LDL-cholesterol levels, which may have therapeutic implications for patients at risk for CHD or other diabetes complications.


1998 ◽  
Vol 42 (12) ◽  
pp. 3146-3152 ◽  
Author(s):  
Kishor M. Wasan ◽  
Allison L. Kennedy ◽  
Shawn M. Cassidy ◽  
Manisha Ramaswamy ◽  
Lorilynne Holtorf ◽  
...  

ABSTRACT The purpose of this study was to determine if a relationship exists among total serum and lipoprotein cholesterol concentration, the severity of amphotericin B (AmpB)-induced renal toxicity, and the serum pharmacokinetics of AmpB in hypercholesterolemic rabbits administered AmpB and AmpB lipid complex (ABLC). After 10 days of cholesterol-enriched diet (0.50% [wt/vol]) or regular rabbit diet (control), each rabbit was administered a single intravenous bolus of AmpB or ABLC (1.0 mg/kg of body weight). Blood samples were obtained before administration and serially thereafter for the assessment of serum pharmacokinetics, kidney toxicity, and serum lipoprotein distribution. Rabbits were humanely sacrificed after all blood samples were obtained, and tissues were harvested for drug analysis. Before drug treatment, cholesterol-fed rabbits demonstrated marked increases in total serum cholesterol and low-density lipoprotein (LDL) cholesterol levels compared with levels in rabbits on a regular diet. No significant differences in triglyceride levels were observed. A significant increase in serum creatinine levels was observed in cholesterol-fed and regular diet-fed rabbits administered AmpB. However, the magnitude of this increase was 2.5-fold greater in cholesterol-fed rabbits than in regular diet-fed rabbits. No significant differences in triglyceride levels were observed. A significant increase in serum creatinine levels was observed in cholesterol-fed and regular diet-fed rabbits administered ABLC. Whereas AmpB pharmacokinetics were significantly altered in cholesterol-fed rabbits administered free AmpB, similar AmpB pharmacokinetics were observed in both rabbit groups administered ABLC. Renal AmpB levels were significantly increased in cholesterol-fed rabbits administered AmpB compared with those in all other groups. Hepatic and lung AmpB levels were elevated in cholesterol-fed rabbits administered free AmpB compared to controls. In addition, hepatic, lung, and spleen AmpB levels were significantly decreased in cholesterol-fed rabbits administered ABLC compared to controls. An increased percentage of AmpB was recovered in LDL–very-low-density lipoprotein fraction when free AmpB was administered to cholesterol-fed rabbits compared with those in all other groups. These findings suggest that increases in cholesterol, specifically, LDL cholesterol levels, modify the disposition and renal toxicity of free AmpB. However, the pharmacokinetics and renal toxicity of ABLC were independent of elevations in total and LDL cholesterol levels.


2012 ◽  
Vol 32 (suppl_1) ◽  
Author(s):  
Arya Mani ◽  
Gwang-Woong Go ◽  
Zhi-jia Ye ◽  
Rajvir Singh

Genetic variations in LRP6 gene are associated with high serum LDL cholesterol levels and atherosclerosis. We examined the role of LRP6 in LDL receptor (LDLR) mediated LDL uptake. LDL uptake was increased when LRP6 was overexpressed and reduced when it was knocked down in LDLR deficient CHO cells. Interestingly, LRP6 knockdown in wildtype CHO cells resulted in a much greater decline in LDL uptake compared to ldlA7 cells. This finding suggested interaction between LRP6 and other proteins involved in LDL uptake. Strikingly, LDL receptor internalization was severely diminished when LRP6 was knocked down and was restored after LRP6 was reintroduced. Further investigations showed that LRP6 forms a complex with the LDL endocytic machinery including LDLR, clathrin and ARH and undergoes endocytosis after stimulation with LDL. LDLR internalization was defective in skin fibroblasts of the LRP6 R611C mutation carriers. LDLR and LRP6 internalizations as well as LDL uptake were significantly impaired in wildtype CHO cells expressing LRP6 R611C mutation(figa,b). These studies introduce LRP6 as a critical modulator of receptor-mediated LDL endocytosis and identify a mechanism by which variation in LRP6 may contribute to high serum LDL levels and atherosclerosis.


Author(s):  
Heinz Drexel

Lipid metabolism has gained cardiological interest only after statins were demonstrated to reduce cardiovascular disease in secondary and primary prevention. Therefore, this chapter first introduces the physiological and atherogenic properties of lipoproteins, before focusing on interventions. Both the efficacy and safety of statins have been proven in numerous randomized clinical trials. Because there is a considerable residual risk in statin-treated patients, additional approaches have been investigated. The focus is now on further reductions in low-density lipoprotein (LDL) cholesterol levels. First, high-intensity statin regimens were shown to reduce residual risk. Subsequently, ezetimibe was demonstrated, for the first time, to have a beneficial effect as a non-statin lipid intervention. More recently, inhibitors of the enzyme PCSK9 have demonstrated a very high efficacy in reducing LDL cholesterol levels. Although the causality of LDL for atherosclerotic cardiovascular disease has been proven in epidemiological studies, including Mendelian randomization studies, as well as interventional trials, adherence to statins and other therapies is far from optimal. In contrast, interventions to increase high-density lipoprotein (HDL) cholesterol levels could not proven to have further benefits when combined with statins.


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