Special Issue "Drug Candidates for the Prevention and Treatment of Cardiovascular Diseases"

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

Deadline for manuscript submissions: 30 April 2022.

Special Issue Editor

Dr. Nikolaos Kadoglou
E-Mail Website
Guest Editor
Medical School, University of Cyprus, Nicosia, Cyprus
Interests: cardiovascular disease prevention; atherosclerotic plaque vulnerability; heart failure

Special Issue Information

Dear Colleagues,

Cardiovascular diseases (CVDs) comprise the first leading cause of morbidity and mortality in the western world. Despite the great advances in pharmaceutical therapy, there is still an increasing need to develop and apply more effective medications for primary and secondary prevention of CVDs. The aim of the present Special Issue is to attract more than 10 high-quality papers that focus on drugs with potentiality to contribute to CVD prevention and treatment. Those drug candidates may be substances that target several aspects of pathophysiological mechanisms of CVDs or may comprise therapeutic regimes of other, non-cardiovascular diseases, with potential expansion of their indications to CVDs. Among all, lipid lowering remains the cornerstone of prevention and treatment of CVDs. Novel, especially gene-oriented, lipid-lowering agents seem quite promising. Medicinal chemistry has introduced technological and conceptual innovations with wide potential application in CVDs. In this context, gene delivery methods may provide an alternative in otherwise untreated CVDs, such as pulmonary hypertension. In parallel, emerging medications in non-CVDs but with established cardiovascular benefits, such as sodium-glucose co-transporter 2 inhibitors with ever expanding use in patients with heart failure or the anti-inflammatory agents and immunomodulators used in auto-immune diseases, have opened a new era in pharmaceutical treatment of patients with CVDs. In addition to this, drugs targeting the main pathophysiological mechanisms of CVDs, such as the inhibition of myocardial fibrosis or cardiovascular inflammatory infiltration, are quite promising as well. Finally, herbal medicine remains a very promising source of drug candidate and requires further investigation. Taken together, there is an increasing burden of drugs that could serve effectively in primary and secondary CVD prevention. A thorough discussion about them should start in order to improve the quality of life of all patients.

Dr. Nikolaos Kadoglou
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • lipid lowering
  • anti-diabetic drugs
  • hypercholesterolemia
  • hypertriglyceridemia
  • PCSK9
  • SGLT-2
  • immunomodulators
  • gene therapy
  • anti-inflammatory drugs
  • regenerative medicine
  • herbal medicine

Published Papers (3 papers)

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Research

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Article
A Novel Statin Compound from Monacolin J Produced Using CYP102A1-Catalyzed Regioselective C-Hydroxylation
Pharmaceuticals 2021, 14(10), 981; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14100981 - 26 Sep 2021
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Abstract
Statins inhibit the 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMG-CoA reductase), which is the rate-limiting enzyme in cholesterol biosynthesis. Statin therapy reduces morbidity and mortality in those who are at high risk of cardiovascular disease. Monacolin J is a statin compound, which is an intermediate in [...] Read more.
Statins inhibit the 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMG-CoA reductase), which is the rate-limiting enzyme in cholesterol biosynthesis. Statin therapy reduces morbidity and mortality in those who are at high risk of cardiovascular disease. Monacolin J is a statin compound, which is an intermediate in the lovastatin biosynthesis pathway, in the fungus Aspergillus terreus. It is also found in red yeast rice, which is made by culturing rice with the yeast Monascus purpureus. Monacolin J has a hydroxyl substituent at position C’-8 of monacolin L. Here, a new statin derivative from monacolin J was made through the catalysis of CYP102A1 from Bacillus megaterium. A set of CYP102A1 mutants of monacolin J hydroxylation with high catalytic activity was screened. The major hydroxylated product was C-6′a-hydroxymethyl monacolin J, whose structure was confirmed using LC–MS and NMR analysis. The C-6′a-hydroxymethyl monacolin J has never been reported before. It showed a greater ability to inhibit HMG-CoA reductase than the monacolin J substrate itself. Human liver microsomes and human CYP3A4 also showed the ability to catalyze monacolin J in producing the same product of the CYP102A1-catalyzed reaction. This result motivates a new strategy for the development of a lead for the enzymatic and chemical processes to develop statin drug candidates. Full article
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Review

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Review
Empagliflozin—A New Chance for Patients with Chronic Heart Failure
Pharmaceuticals 2022, 15(1), 47; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15010047 - 30 Dec 2021
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Abstract
The heart failure (HF) epidemic is one of the challenges that has been faced by the healthcare system worldwide for almost 25 years. With an ageing world population and a fast-paced lifestyle that promotes the development of cardiovascular disease, the number of people [...] Read more.
The heart failure (HF) epidemic is one of the challenges that has been faced by the healthcare system worldwide for almost 25 years. With an ageing world population and a fast-paced lifestyle that promotes the development of cardiovascular disease, the number of people suffering from heart failure will continue to rise. To improve the treatment regimen and consequently the prognosis and quality of life of heart failure patients, new therapeutic solutions have been introduced, such as an inclusion of Sodium-glucose co-transporter 2 (SGLT-2) inhibitors in a new treatment regimen as announced by the European Society of Cardiology in August 2021. This article focuses on the SGLT2 inhibitor empagliflozin and its use in patients with heart failure. Empagliflozin is a drug originally intended for the treatment of diabetes due to its glycosuric properties, yet its beneficial effects extend beyond lowering glycemia. The pleiotropic effects of the drug include nephroprotection, improving endothelial function, lowering blood pressure and reducing body weight. In this review we discuss the cardioprotective mechanism of the drug in the context of the benefits of empagliflozin use in patients with chronic cardiac insufficiency. Numerous findings confirm that despite its potential limitations, the use of empagliflozin in HF treatment is advantageous and effective. Full article
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Review
Treatment of Cardiovascular Disease in Rheumatoid Arthritis: A Complex Challenge with Increased Atherosclerotic Risk
Pharmaceuticals 2022, 15(1), 11; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15010011 - 22 Dec 2021
Viewed by 368
Abstract
Rheumatoid arthritis (RA) carries significant risk for atherosclerotic cardiovascular disease (ASCVD). Traditional ASCVD risk factors fail to account for this accelerated atherosclerosis. Shared inflammatory pathways are fundamental in the pathogenesis of both diseases. Considering the impact of RA in increasing cardiovascular morbidity and [...] Read more.
Rheumatoid arthritis (RA) carries significant risk for atherosclerotic cardiovascular disease (ASCVD). Traditional ASCVD risk factors fail to account for this accelerated atherosclerosis. Shared inflammatory pathways are fundamental in the pathogenesis of both diseases. Considering the impact of RA in increasing cardiovascular morbidity and mortality, the characterization of therapies encompassing both RA and ASCVD management merit high priority. Despite little progress, several drugs discussed here promote remission and or lower rheumatoid disease activity while simultaneously conferring some level of atheroprotection. Methotrexate, a widely used disease-modifying drug used in RA, is associated with significant reduction in cardiovascular adverse events. MTX promotes cholesterol efflux from macrophages, upregulates free radical scavenging and improves endothelial function. Likewise, the sulfonamide drug sulfasalazine positively impacts the lipid profile by increasing HDL-C, and its use in RA has been correlated with reduced risk of myocardial infraction. In the biologic class, inhibitors of TNF-α and IL-6 contribute to improvements in endothelial function and promote anti-atherogenic properties of HDL-C, respectively. The immunosuppressant hydroxychloroquine positively affects insulin sensitization and the lipid profile. While no individual therapy has elicited optimal atheroprotection, further investigation of combination therapies are ongoing. Full article
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