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Special Issue "Pharmacotherapy of Dyslipidemias"

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A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 November 2023 | Viewed by 2686

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Special Issue Editors

Dr. Daniel Dias Rufino Arcanjo

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Guest Editor

LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil
Interests: bioactive peptides; cardiovascular; diabetes; dyslipidemia; endothelium; hypertension; medicinal plants; natural products; pharmacology; preclinical toxicology; vasorelaxant
Special Issues, Collections and Topics in MDPI journals

Dr. Maria do Carmo de Carvalho e Martins

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Guest Editor

Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil
Interests: arterial hypertension; diabetes; effects of physical training; general and exercise physiology; health conditions of population groups; nutrition and public health; obesity; pharmacology of natural products

Special Issue Information

Dear Colleagues,

Dyslipidemia is a clinical condition characterized by changes in plasma lipoprotein concentrations in relation to reference values considered as normal. The increase in the concentration of blood circulating lipids induces an inflammatory process which leads to endothelial damage and then the formation of atherosclerosis plaques, an important cardiovascular risk factor responsible for complications such as acute myocardial infarction and stroke. Most of these complications are a result of atherosclerotic plaque rupture or erosion, thrombin generation, platelet activation, and cloth formation. Many hypotheses about its pathogenesis and progression suggest the involvement of oxidative stress, considering that LDL oxidation is a fundamental factor in initiating the atherogenic process. In this sense, the presence of lipid peroxidation products can trigger oxidative changes in LDL particles. Such lesions can be prevented or reduced by the action of antioxidant phytochemicals present in fruits and vegetables, which have been shown to be a promising alternative to the adverse effects associated with the use of classic lipid-lowering drugs, such as myalgia and the elevation of hepatic transaminases induced using statins. In this sense, this Special Issue focuses on non-clinical and clinical studies which report advances in the pharmacological therapy of dyslipidemias, from classical treatments to novel promising compounds synthetically obtained or from natural sources. Both original and review articles are welcomed.

Dr. Daniel Arcanjo
Dr. Maria do Carmo de Carvalho e Martins
Guest Editors

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Keywords

atherosclerosis
dyslipidemia
endothelial dysfunction
fatty acids
high-fat diet
hyperlipidemia
hypertriglyceridemia
polyunsaturated fatty acids
PUFA
statins

Published Papers (3 papers)

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Research

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Open AccessArticle

Lycopene from Red Guava (Psidium guajava L.): From Hepatoprotective Effect to Its Use as Promising Self-Emulsifying Drug Delivery System for Anti-Inflammatory and Antioxidant Applications

Pharmaceuticals 2023, 16(6), 905; https://doi.org/10.3390/ph16060905 - 20 Jun 2023

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Abstract

Lycopene is a carotenoid with potential use in the treatment of chronic illnesses. Here, different formulations of lycopene were studied: lycopene-rich extract from red guava (LEG), purified lycopene from red guava (LPG) and a self-emulsifying drug delivery system loaded with LPG (nanoLPG). The effects of administering orally various doses of LEG to hypercholesterolemic hamsters were evaluated regarding the liver function of the animals. The cytotoxicity of LPG in Vero cells was analyzed by a crystal violet assay and by fluorescence microscopy. In addition, nanoLPG was employed in stability tests. LPG and nanoLPG were tested for their cytotoxic effect on human keratinocytes and antioxidant capacity on cells in an endothelial dysfunction model in an isolated rat aorta. Finally, the effect of different nanoLPG concentrations on the expression of immune-related genes (IL-10, TNF-α, COX-2 and IFN-γ) from peripheral blood mononuclear cells (PBMC) using real-time PCR was also analyzed. Results suggest that LEG, despite not being able to improve blood markers indicative of liver function in hypercholesterolemic hamsters, reduced hepatic degenerative changes. Additionally, LPG did not show cytotoxicity in Vero cells. In relation to nanoLPG, the effects produced by heat stress evaluated by Dynamics Light Scattering (DLS) and visually were loss of color, texture change and phase separation after 15 days without interfering with the droplet size, so the formulation proved to be efficient in stabilizing the encapsulated lycopene. Although LPG and nanoLPG showed moderate toxicity to keratinocytes, which may be related to cell lineage characteristics, both revealed potent antioxidant activity. LPG and nanoLPG showed vasoprotective effects in aortic preparations. The gene expression assay indicates that, although no significant differences were observed in the expression of IL-10 and TNF-α, the PBMCs treated with nanoLPG showed a reduction in transcriptional levels of IFN-γ and an increased expression of COX-2. Thus, the work adds evidence to the safety of the use of lycopene by humans and shows that tested formulations, mainly nanoLPG due to its stability, stand out as promising and biosafe products for the treatment of diseases that have oxidative stress and inflammation in their etiopathology. Full article

(This article belongs to the Special Issue Pharmacotherapy of Dyslipidemias)

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Open AccessReview

Current Management and Future Perspectives in the Treatment of Lp(a) with a Focus on the Prevention of Cardiovascular Diseases

Susan M. Halli Demeter

Chadi Ayoub

and

Reza Arsanjani

Pharmaceuticals 2023, 16(7), 919; https://doi.org/10.3390/ph16070919 - 23 Jun 2023

Cited by 1 | Viewed by 871

Abstract

Lipoprotein(a) [Lp(a)] is a lipid molecule with atherogenic, inflammatory, thrombotic, and antifibrinolytic effects, whose concentrations are predominantly genetically determined. The association between Lp(a) and cardiovascular diseases (CVDs) has been well-established in numerous studies, and the ability to measure Lp(a) levels is widely available in the community. As such, there has been increasing interest in Lp(a) as a therapeutic target for the prevention of CVD. The impact of the currently available lipid-modifying agents on Lp(a) is modest and heterogeneous, except for the monoclonal antibody proprotein convertase subtilisin/kexin type 9 inhibitors (PCSK9i), which demonstrated a significant reduction in Lp(a) levels. However, the absolute reduction in Lp(a) to significantly decrease CVD outcomes has not been definitely established, and the magnitude of the effect of PCSK9i seems insufficient to directly reduce the Lp(a)-related CVD risk. Therefore, emerging therapies are being developed that specifically aim to lower Lp(a) levels and the risk of CVD, including RNA interference (RNAi) agents, which have the capacity for temporary and reversible downregulation of gene expression. This review article aims to summarize the effects of Lp(a) on CVD and to evaluate the available evidence on established and emerging therapies targeting Lp(a) levels, focusing on the potential reduction of CVD risk attributable to Lp(a) concentrations. Full article

(This article belongs to the Special Issue Pharmacotherapy of Dyslipidemias)

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Open AccessCase Report

Rapid Resolution of Life-Threatening Hypertriglyceridemia after Evinacumab Administration in a Pediatric HSCT Recipient: A Case Report

and

Pharmaceuticals 2023, 16(8), 1069; https://doi.org/10.3390/ph16081069 - 27 Jul 2023

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Abstract

Evinacumab, a human monoclonal antibody against angiopoietin-like protein 3 (ANGPTL3), has recently been approved by the U.S. Food and Drug Administration as an add-on therapy for homozygous familial hypercholesterolemia (HoFH) in patients of 12 years and older. Its role as a triglyceride-lowering drug is also emerging in the literature. However, it has not been approved for this indication yet, neither in the adult nor in the pediatric population. We describe the case of a 10-year-old boy who underwent an allogeneic hematopoietic stem cell transplant for acute lymphoblastic leukemia complicated by chronic graft-versus-host disease (GVHD) and presented life-threatening refractory hypertriglyceridemia due to the concomitant use of ruxolitinib and sirolimus. After the failure of the insulin treatment and due to the technical impossibility of performing lipid apheresis, the child underwent evinacumab treatment, obtaining a dramatic rapid reduction in triglyceride and cholesterol levels. This is the first report of a pediatric patient younger than 12 years in Europe receiving evinacumab to treat severe hypertriglyceridemia. The therapy with angiopoietin-like proteins inhibitors has been effective, safe, and well-tolerated in our patient, suggesting that evinacumab may be used in the pediatric population when other therapeutic strategies are ineffective or contraindicated. Full article

(This article belongs to the Special Issue Pharmacotherapy of Dyslipidemias)

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