Herbal medicines for the treatment of cardiovascular diseases: Benefits and risks - A narrative review.

Herbal medicines (HMs) have been traditionally used for the prophylaxis/treatment of cardiovascular diseases (CVDs). Their use is steadily increasing and many patients with CVDs often combine HMs with prescribed cardiovascular medications. Interestingly, up to 70% of patients do not notify cardiologists/physicians the use of HMs and up to 90% of cardiologists/physicians may not routinely inquire them about the use of HMs.

Non-Covalent Albumin Ligands in FDA-Approved Therapeutic Peptides and Proteins.

An increasing number of drugs that consist of a therapeutic peptide or protein linked to an albumin-binding structure are being approved. In this perspective, the pharmacokinetic data of currently marketed drugs of this type will be presented. Acylation with fatty acids or fatty α,ω-dicarboxylic acids has been used successfully to prepare long-acting analogs of insulin, GLP-1, and other peptides but not of larger proteins.

Flavonoids: Antiplatelet Effect as Inhibitors of COX-1.

Flavonoids are compounds with a benzopyranic structure that exhibits multiple pharmacological activities. They are known for their venotonic activity, but their mechanism of action remains unclear. It is thought that, as this mechanism is mediated by prostaglandins, these compounds may interfere with the arachidonic acid (AA) cascade.

A New Approach to the Management of COVID-19. Antagonists of IL-6: Siltuximab.

Since the beginning of the pandemic, numerous national and international clinical trials have been conducted with a large number of drugs. Many of them are intended for the treatment of other pathologies; however, despite the great effort made, no specific drug is available for the treatment of the symptoms of respiratory disease caused by SARS-CoV-2 infection. The aim of this article is to provide data to justify the use of drugs to tackle the effects produced by IL-6 as the main inflammatory mediator in patients with COVID-19 with severe respiratory complications, considering all clinical evidence linking the poor prognosis of these patients with increased IL-6 levels in the context of cytokine release syndrome.

Binding and antiplatelet activity of quercetin, rutin, diosmetin, and diosmin flavonoids.

Platelets exert an essential role in vascular inflammation and thrombosis. Flavonoids are natural compounds employed for the clinical management of vascular disorders preventing capillary permeability, working as phlebotonics and improving the blood rheology, although their mechanism of action remains partially unknown. The effects of quercetin, rutin, diosmetin and diosmin were investigated in platelet activation utilizing blood from healthy and non-treated volunteers.

Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1.

Atherosclerotic cardiovascular disease is the leading cause of death in developed countries. Therefore, there is an increasing interest in developing new potent and safe antiplatelet agents. Coumarins are a family of polyphenolic compounds with several pharmacological activities, including platelet aggregation inhibition.

Selective nickel-catalyzed fluoroalkylations of olefins.

Mild and selective nickel-catalyzed trifluoromethylation and perfluoroalkylation reactions of alkenes were developed to provide fluorinated olefins, including natural products, pharmaceuticals, and variety of synthetic building blocks in good to excellent yields (38 examples). Control experiments, kinetic measurements and in situ EPR studies reveal the importance of radical species and the formation of 1,2-adducts as intermediates.

Monte Carlo Computation of Dose-Volume Histograms in Structures at Risk of an Eye Irradiated with Heterogeneous Ruthenium-106 Plaques.

Background/aims: The aim of this work is to compare Monte Carlo simulated absorbed dose distributions obtained from Ru eye plaques, whose heterogeneous emitter distribution is known, with the common homogeneous approximation. The effect of these heterogeneities on segmented structures at risk is analyzed using an anthropomorphic phantom.

Methods: The generic CCA and CCB, with a homogeneous emitter map, and the specific CCA1364 and CCB1256 Ru eye plaques are modeled with the Monte Carlo code PENELOPE.

Profile of Cardiovascular Disease Patients Who are Diagnosed with COPD in a Smoking-Cessation Unit.

Introduction: Cardiovascular diseases (CVDs) and chronic obstructive pulmonary disease (COPD) have similar prevalence rates and risk factors, and both frequently occur in the same patient. The primary objective of the study was to evaluate the rate of COPD patients among subjects with some form of CVD referring to a smoking cessation unit. The secondary objective was to analyze the demographic and clinical profile of these subjects and to identify independent factors potentially associated with COPD.

Potential Therapeutic Anti-Inflammatory and Immunomodulatory Effects of Dihydroflavones, Flavones, and Flavonols.

Systemic inflammation, circulating immune cell activation, and endothelial cell damage play a critical role in vascular pathogenesis. Flavonoids have shown anti-inflammatory effects. In this study, we investigated the effects of different flavonoids on the production of pro-inflammatory interleukin (IL) 1β, 6, and 8, and tumor necrosis factor α (TNF-α), in peripheral blood cells.

Monte Carlo Simulation of the Treatment of Uveal Melanoma Using Measured Heterogeneous Ru Plaques.

Background/aims: Ruthenium plaques are used for the treatment of ocular tumors. The aim of this work is the comparison between simulated absorbed dose distributions tallied in an anthropomorphic phantom, obtained from ideal homogeneous plaques, and real eye plaques in which the actual heterogeneous distribution of Ru was measured. The placement of the plaques with respect to the tumor location was taken into consideration to optimize the effectiveness of the treatment.

Monte Carlo Estimation of Absorbed Dose Distributions Obtained from Heterogeneous Ru Eye Plaques.

Background: The distribution of the emitter substance in Ru eye plaques is usually assumed to be homogeneous for treatment planning purposes. However, this distribution is never homogeneous, and it widely differs from plaque to plaque due to manufacturing factors.

Methods: By Monte Carlo simulation of radiation transport, we study the absorbed dose distribution obtained from the specific CCA1364 and CCB1256 Ru plaques, whose actual emitter distributions were measured.

Antiplatelet activity of flavonoid and coumarin drugs.

Polyphenols are used as phlebotonic drugs, but their mechanism of action remains unknown. Since platelet activity and platelet-endothelial cell interactions are involved in the pathogenesis of cardiovascular disease, this work examines whether different flavonoid and coumarin drugs are able to inhibit platelet aggregation. This specific case of coumarins, the antiplatelet effect is not linked with a possible interaction over blood coagulation since this effect only dicoumarols have it.

Palladium-Catalyzed Trifluoromethylation of (Hetero)Arenes with CF3 Br.

The CF3 group is an omnipresent motif found in many pharmaceuticals, agrochemicals, catalysts, materials, and industrial chemicals. Despite well-established trifluoromethylation methodologies, the straightforward and selective introduction of such groups into (hetero)arenes using available and less expensive sources is still a major challenge. In this regard, the selective synthesis of various trifluoromethyl-substituted (hetero)arenes by palladium-catalyzed C-H functionalization is herein reported.

One-Step Conversion of Methyl Ketones to Acyl Chlorides.

Treatment of aromatic and heteroaromatic methyl ketones with sulfur monochloride and catalytic amounts of pyridine in refluxing chlorobenzene leads to the formation of acyl chlorides. Both electron-rich and electron-poor aryl methyl ketones can be used as starting materials. The resulting C1-byproduct depends on the precise reaction conditions chosen.

Monte Carlo Simulation of the Treatment of Eye Tumors with (106)Ru Plaques: A Study on Maximum Tumor Height and Eccentric Placement.

Background/aims: Ruthenium plaques are used for the treatment of ocular tumors. There is, however, a controversy regarding the maximum treatable tumor height. Some advocate eccentric plaque placement, without a posterior safety margin, to avoid collateral damage to the fovea and optic disc, but this has raised concerns about marginal tumor recurrence.

Optimal management of breakthrough cancer pain (BCP).

Breakthrough cancer pain (BCP) is common in patients with cancer, causing a negative impairment in quality of life. Recent diagnostic criteria allow for differentiation of background chronic pain and BCP, for which proportion of unpredictable episodes is very high. Five characteristics define BCP: rapid onset, high intensity, maximum intensity (minutes), mean duration 30 min, and unpredictable onset.

Breakthrough cancer pain - still a challenge.

Breakthrough cancer pain is defined as transient pain exacerbation in patients with stable and controlled basal pain. Although variable, the prevalence of breakthrough cancer pain is high (33%-95%). According to the American Pain Foundation, breakthrough pain is observed in 50%-90% of all hospitalized cancer patients, in 89% of all patients admitted to homes for the elderly and terminal-patient care centers, and in 35% of all ambulatory care cancer patients.

Accurate estimation of dose distributions inside an eye irradiated with 106Ru plaques.

Background: Irradiation of intraocular tumors requires dedicated techniques, such as brachytherapy with (106)Ru plaques. The currently available treatment planning system relies on the assumption that the eye is a homogeneous water sphere and on simplified radiation transport physics. However, accurate dose distributions and their assessment demand better models for both the eye and the physics.

Electron irradiation of conjunctival lymphoma--Monte Carlo simulation of the minute dose distribution and technique optimization.

Purpose: External beam radiotherapy is the only conservative curative approach for Stage I non-Hodgkin lymphomas of the conjunctiva. The target volume is geometrically complex because it includes the eyeball and lid conjunctiva. Furthermore, the target volume is adjacent to radiosensitive structures, including the lens, lacrimal glands, cornea, retina, and papilla.

[Pharmacology].

Two of the main characteristics of western societies in the last fifty years have been the medicalization of the human life and the environmental degradation. The first one has forced human being to consider medicines use related to what would be rational, reasonable and well-reasoned. The second one brought us to a new ecologist conscience.

Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors.

Herein is described the synthesis of a novel class of peptidyl FVIIa inhibitors having a C-terminal benzyl ketone group. This class is designed to be potentially suitable as stabilization agents of liquid formulations of rFVIIa, which is a serine protease used for the treatment of hemophilia A and B inhibitor patients. A library of compounds was synthesized with different tripeptide sequences, N-terminals and d-amino acids in the P3 position.

[Promotion of basic research in the European Union: the European research council (ERC) and the initiative for science in Europe (ISE )].

Europe has today a function of intellectual guidance and watch tower that will be unable to accomplish if remains far of the forefront in scientific research and application of knowledge The "delocalization of talents" towards the west is much worst than that of production towards the east. From January 1st 2007, the ERC, with an annual budget of 1.5 billion Euros, represents an important step to improve the situation.