Cardiovascular & Hematological Agents in Medicinal Chemistry
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1871-5257

Author(s):  
Ozgur Karcioglu ◽  
Sehmus Zengin ◽  
Bilgen Ozkaya ◽  
Eylem Ersan ◽  
Sarper Yilmaz ◽  
...  

Background and Objective: Direct (new) Oral Anticoagulants (DOACs) have emerged as a contemporary and promising option in the treatment of thromboses and VTE, while protecting the coagulation cascade against untoward bleeding events. They are used in the management and prophylaxis of Venous Thromboembolism (VTE) and other thrombotic diseases. The most prominent complication of these agents is bleeding. These agents have similar or lower rates of major intracranial hemorrhages, while they had a higher risk of major gastrointestinal bleeding when compared to warfarin. This manuscript is aimed to revise and update the literature findings to outline the side effects of DOACs in various clinical scenarios. Methods: A narrative review of currently published studies was performed. Online database searches were performed for clinical trials published before July 2021, on the efficacy and adverse effects attributed to the anticoagulant treatment, especially DOACs. A literature search via electronic databases was carried out, beginning with the usage of the agents in the Western Languages papers. The search terms initially included direct (new) oral anticoagulants, dabigatran, rivaroxaban, apixaban, edoxaban, idarucizumab, andexanet, prothrombin complex concentrates, and fresh frozen plasma. Papers were examined for methodological soundness before being included. Results: Severe bleeding episodes require aggressive interventions for successful management. Therefore, bleeding should be evaluated in special regard to the location and rate of hemorrhage, and total volume of blood loss. Patient's age, weight and organ dysfunctions (e.g., kidney/liver failure or chronic respiratory diseases) directly affect the clinical course of overdose. Conclusion: Management recommendations for hemorrhage associated with DOAC use vary, depending on the class of the culprit agent (direct thrombin inhibitor vs. FXa inhibitor), the clinical status of the patient (mild/ moderate vs. severe/life-threatening), and capabilities of the institution. Specific reversal agents (i.e., idarucizumab and andexanet alfa) can be used if available, while prothrombin complex concentrates, fresh frozen plasma and/ or tranexamic acid can also be employed as nonspecific replacement agents in the management of DOAC-related bleeding diathesis.


Author(s):  
Ozgur Karcioglu ◽  
Sarper Yilmaz ◽  
Göksu Afacan ◽  
Eylem Ersan ◽  
Derya Abuşka ◽  
...  

: Direct (New-generation) Oral Anticoagulants (DOACs) have emerged as effective agents which are used in place of vitamin-K antagonists in treatment and prophylaxis of Venous Thromboembolism (VTE), atrial fibrillation and other thrombotic diseases. Among them, the FIIa-direct thrombin inhibitor dabigatran and FXa inhibitors (rivaroxaban, apixaban, edoxaban) are the most broadly used. Anticoagulant dosing may differ under special considerations. The patients’ physiological reserves, organ functional status and failures should be taken into account in clinical decision-making processes. The advantages and drawbacks of each specific agent should be weighed with special regard to metabolism, pharmacokinetics and pharmacodynamics, along with the efficiency of the agents in different indications. This article aims to review the most recent literature to highlight the usage and efficacy of the agents in different clinical conditions.


Author(s):  
Francisca De Oliveira E Silva ◽  
Julio Cesar Mendes Soares ◽  
Aniele Valdez ◽  
Marcos Vinícios da Silva Ferreira ◽  
Marcelo da Silva Cecim

: Essential oils are complex mixtures of volatile compounds, primarily composed of terpenes and abundant aromatic plants. For example, Cymbopogon citratus (lemongrass) is an aromatic plant that produces a monoterpene-rich essential oil, and studies show that this essential oil has excellent antioxidant activity. Erythrocytes incubated under high sugar levels are constantly exposed to reactive oxygen species, which results in the oxidation of their membranes. Objective: The aim of this article is to investigate the antioxidant activity of lemongrass essential oil and its protective effect on erythrocytes exposed to high levels of glucose. Materials and Methods: The essential oil was obtained by steam dragging distillation; blood cell suspensions were incubated with glucose 5, 20, 50, and 100 mmol/L. The amount of TBARS produced was measured at 532 nm. In addition, the percentage of antioxidant activity was assessed by DPPH free radical assay. Results: Lemongrass essential oil showed an increase in the antioxidant activity up to 240 mg/ml, while ascorbic acid used as positive control showed a dose-dependent increase in antioxidant activity starting at 1 mmol/L up to 18 mmol/L. However, such a lemongrass dose prevented peroxidation in erythrocytes incubated under a high glucose media, whereas ascorbic acid showed a protective effect only at a concentration of 1 mmol/L. Conclusion: Lemongrass essential oil has high antioxidant activity compared to standard antioxidant as ascorbic acid, and also acts as a protective agent against erythrocyte lipoperoxidation due to hyperglycemia in vitro.


Author(s):  
Antonio Siniscalchi ◽  
Sean Murphy ◽  
Cleona Gray ◽  
Giovambattista De Sarro ◽  
Luca Gallelli

Aims: To study the role of cytokines and vascular inflammatory biomarkers in unstable carotid plaque. Background: Clinical studies showed that not only the degree of stenosis but also the type of carotid plaque can be responsible for ipsilateral ischemic stroke. Objective: The objective of this study is to suggest a role for vulnerable carotid atherosclerotic disease in the occurrence of ischemic stroke. Methods: PubMed, Embase, Cochrane library, and reference lists have been used to evaluate articles published until February 15, 2021. Results: Several factors may be involved in unstable plaque. Clinical studies support the involvement of brain inflammatory biomarkers as well as cytokines in the unstable carotid plaque. Conclusions: Biomarkers could help to stratify patients with a vulnerable carotid plaque and to personalize the drug treatment. In this review, we briefly discuss the characteristics of vulnerable plaque and the role of biomarkers in the vulnerable carotid plaque.


Author(s):  
Amine Azzane ◽  
Ayou Amssayef ◽  
Mohame Eddouks

Aims: The aim of the study was to evaluate the antihyperglycemic effect of Chenopodium quinoa. Background: Chenopodium quinoa is a pseudocereal plant with several medicinal properties. Objective: The goal of this investigation was to determine the antihyperglycemic activity of Chenopodium quinoa in both normal and streptozotocin(STZ)-induced diabetic rats. Methods: In this study, the effect of the aqueous extract of Chenopodium quinoa seeds (AECQS) (60 mg/kg) on blood glucose levels was evaluated in both normal and diabetic rats after a single (6 hours) and repeated oral administration (7 days of treatment). The effect of this herb on glucose tolerance and lipid profile was also studied. Additionally, histopathological examination of liver was carried out using the Hematoxylin-Eosin method. Furthermore, the in vitro antioxidant activity as well as a preliminary phytochemical screening and quantification of some secondary metabolites (phenolic compounds, flavonoids and tannins) were performed according to standard methods. Results: AECQS produced a significant lowering effect on plasma glucose levels in STZ-induced diabetic rats. In addition, this extract exhibited a remarkable amelioration on hepatic histopathology in diabetic rats. In addition, the extract exerted a remarkable antioxidant activity which could be due to the presence of some compounds found in this herb. Conclusion: In conclusion, this study demonstrates that the aqueous extract of Chenopodium quinoa seeds has a favorable effect in controlling diabetes mellitus.


Author(s):  
Ayobami Dare ◽  
Ahmed A Elrashedy ◽  
Mahendra L. Channa ◽  
Anand Nadar

Background: Diabetic cardiotoxicity is commonly associated with oxidative injury, inflammation, and endothelial dysfunction. L-ergothioneine (L-egt), a diet-derived amino acid, has been reported to decrease mortality and risk of cardiovascular injury, provides cytoprotection to tissues exposed to oxidative damage, and prevents diabetes-induced perturbation. Objective: This study investigated the cardioprotective effects of L-egt on diabetes-induced cardiovascular injuries and its probable mechanism of action. Methods: Twenty-four male Sprague-Dawley rats were divided into non-diabetic (n=6) and diabetic groups (n=18). Six weeks after the induction of diabetes, the diabetic rats were divided into three groups (n=6) and administered distilled water, L-egt (35mg/kg), and losartan (20mg/kg) by oral gavage for six weeks. Blood glucose and mean arterial pressure (MAP) were recorded pre-and post-treatment, while biochemical, ELISA, and Rt-PCR analyses were conducted to determine inflammatory, injury-related and antioxidant biomarkers in cardiac tissue after euthanasia. Also, an in-silico study, including docking and molecular dynamic simulations of L-egt toward the Keap1-Nrf2 protein complex, was done to provide a basis for the molecular antioxidant mechanism of L-egt. Results: Administration of L-egt to diabetic animals reduced serum triglyceride, water intake, MAP, biomarkers of cardiac injury (CK-MB, LDH), lipid peroxidation, and inflammation. Also, L-egt increased body weight, antioxidant enzymes, upregulated Nrf2, HO-1, NQO1 expression, and decreased Keap1 expression. The in-silico study showed that L-egt inhibits Keap1-Nrf2 complex by binding to the active site of Nrf2 protein, thereby preventing its degradation. Conclusion: L-egt protects against diabetes-induced cardiovascular injury via the upregulation of Keap1-Nrf2 pathway and its downstream cytoprotective antioxidants.


Author(s):  
Mauro Gitto ◽  
Dimitrios A. Vrachatis ◽  
Gianluigi Condorelli ◽  
Konstantinos Papathanasiou ◽  
Bernhard Reimers ◽  
...  

: Sodium-glucose cotransporter 2 (SGLT2) inhibitors are a class of anti-diabetic agents that block the reabsorption of glucose in the proximal convoluted tubule of the nephron, thereby contributing to glycosuria and lowering blood glucose levels. SGLT2 inhibitors have been associated with improved cardiovascular outcomes in patients with diabetes, including a reduced risk of cardiovascular death and hospitalizations for heart failure. Recently, DAPA-HF and EMPEROR REDUCED trials showed the beneficial cardiovascular effect of SGLT2 inhibitors in patients with heart failure with consistently reduced ejection fraction (HFrEF) regardless of the presence of diabetes. Moreover, some exploratory studies suggested that these drugs improve Left Ventricular (LV) systolic function and oppose LV adverse remodeling in patients with HFrEF. However, the exact mechanisms that mediated for this benefit are not fully understood. Beyond glycemic control, enhanced natriuresis, increased erythropoiesis, improved endothelial function, changes in myocardial metabolism, anti-inflammatory and anti-oxidative properties may all play an active role in SGLT2 inhibitors’ cardiovascular benefits. A deep understanding of the pathophysiological interplay is key to define which HF phenotype could benefit more from SGLT2 inhibitors. Current clinical evidence on the comparison of different HF etiologies is limited to posthoc subgroup analysis of DAPA-HF and EMPEROR-REDUCED, which showed similar outcomes in patients with or without ischemic HF. On the other hand, in earlier studies of patients suffering from diabetes, rates of classic ischemic endpoints, such as myocardial infarction, stroke or coronary revascularization, did not differ between patients treated with SGLT2 inhibitors or placebo. The aim of this review is to discuss whether SGLT2 inhibitors may improve prognosis in patients with ischemic HF, not only in terms of reducing re-hospitalizations and improving left ventricular function but also by limiting coronary artery disease progression and ischemic burden.


Author(s):  
Zemene Demelash Kifle ◽  
Agumas Alemu Alehegn ◽  
Baye Yrga Adugna ◽  
Abebe Basazn Mekuria ◽  
Engidaw Fentahun Enyew

Background: Diabetes mellitus is one of the major and common metabolic, and chronic disorders in the world. Several medicinal plants have been used globally for the management of diabetes mellitus. The current study aimed to study the anti-hyperglycemic and anti-hyperlipidemic effects of Bersama abyssinica. Methods: Antidiabetic effect of 80% methanolic crude extract of Bersama abyssinica was studied in repeated dose-treated STZ-induced diabetic mice model. The activities of Bersama abyssinica on serum lipid level and body weight were investigated on STZ-induced diabetic mice. Data were analyzed using one-way ANOVA and significant when the p-value was less than 0.05. Results: All doses of the crude 80% methanolic extract of Bersama abyssinica (100 mg/kg, 200 mg/kg, and 400 mg/kg) exhibited a noticeable BGL reduction when compared with baseline blood glucose level and diabetic control on the 7th and 14th days of administration. Moreover, the higher dose of the extract (at 400 mg/kg) significantly (p < 0.001, 54.3%) decreased the BGL in STZ-induced diabetic mice. The maximum decrement in fasting BGL was achieved at the 14th days: 34.92%, 41.10%, 54.30%, and 59.66%, respectively for BAC 100 mg/kg, BAC 200 mg/kg, BAC 400 mg/kg, and GLC 5 mg/kg treated groups. Bersama abyssinica also displayed a significant (p < 0.05) improvement of serum lipid levels and body weight. Conclusion: Bersama abyssinica crude extract exhibited a significant antidiabetic effect and prevented body weight loss in streptozotocin-induced diabetic mice. The finding also confirmed the valuable biochemical activity of Bersama abyssinica by improving serum lipid levels.


Author(s):  
Eleni Tsotridou ◽  
Eleni Vasileiou ◽  
Elpis Mantadakis ◽  
Athanasios Tragiannidis

Despite the marked improvement in overall survival rates of paediatric patients with haematological malignancies that has been achieved during the last decades, there is still a pressing need for novel therapeutic approaches for the subset of patients with relapsed or refractory disease. Immune checkpoint inhibitors aim to induce potent anti-tumour immune responses by targeted blockade of inhibitory receptors and have shown great promise in preclinical models and studies in the adult population. However, paediatric malignancies present unique features and so far, experience with these agents remains limited. In the current review we present an overview of efficacy and safety data from case reports, case series and clinical trials employing the use of immune checkpoint inhibitors in children, adolescents and young adults with haematological malignancies. We also discuss new possibilities involving novel targets and combination treatments and provide a summary of the currently registered clinical trials.


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