Cardiovascular & hematological agents in medicinal chemistry最新文献

Background and objective: Hypercholesterolemia is one of the main risk factors for vascular thrombosis in individuals. Therefore, the use of statins is very effective in reducing cholesterol and can reduce the risk of thrombosis in these patients. Rosuvastatin, a member of the statin family which, inhibits cholesterol synthesis. Very few studies have been done in relation to how rosuvastatin can affect thrombosis. So, this research has been tried whether rosuvastatin can have an effect on coagulation factors and homocysteine as risk factors for thrombosis in hypercholesterolemia?

Methods: In this experimental study, 60 patients (30 men and 30 women with a mean age of 40- 70 years) diagnosed with hypercholesterolemia (cholesterol >250 mg/dl) participated in this research. 30 patients were prescribed rosuvastatin (20 mg/day), and 30 patients were simultaneously taken placebo for three months. All parameters, including FVIII, FV, Fibrinogen, D-Dimer, plasma homocysteine level and lipid profile, were measured before and after treatment. All the results were statistically compared between the two groups.

Results: In patients who took rosuvastatin, the drug was able to significantly reduce the concentrations of total cholesterol, triglycerides, high-density lipoprotein (HDL) and low-density lipoprotein (LDL) (P <0.001). Also, rosuvastatin was able to reduce the concentrations of homocysteine significantly, D-Dimer (P <0.001), coagulation factor VIII and factor V (P <0.05). In patients with hypercholesterolemia who took the placebo, did not affect the mentioned variables (P >0.05).

Conclusion: According to the results, it seems that rosuvastatin may be able to reduce the risk of thrombosis in patients by affecting coagulation factors and homocysteine levels.

It is possible that gut bacteria may have a beneficial effect on cardiovascular health in humans. It may play a major role in the progression of a variety of cardiovascular diseases, including Heart Failure (HF), Atherosclerosis, Coronary Arterial Disease (CAD), Ischemic Heart Disease (IHD), and Others. Dysbiosis of the gut microbiota, along with its direct and indirect impact on gut health, may induce cardiovascular disorders. Although advanced studies have demonstrated the relationship of various metabolites to cardiovascular diseases (CVD) in animals, translating their functional capacity to humans remains a significant area of research. This paper simplifies the demonstration of some compounds, pathways, and components like Trimethylamine N-oxide (TMAO), short-chain fatty acids (SCFAs), and butyrate production. It demonstrates how a change in eating habits causes TMAO and how the impact of different drugs on gut microbiota species and high consumption of Westernized food causes several heartrelated problems, such as atherosclerosis and inflammation that can even become the cause of heart failure. Modulation of the gut microbiome, on the other hand, is a novel therapeutic measure because it can be easily altered through diet and other lifestyle changes. It could then be used to lower the risk of several CVDs.

Background: Studies have shown the combination treatment effectiveness of using rosuvastatin and ezetimibe in patients with chronic coronary artery disease. Our study aim to evaluate the effectiveness of dyslipidemia treatment with the combination of rosuvastatin and ezetimibe 10mg in patients with chronic coronary artery disease compared with 20 mg rosuvastatin.

Objectives: To evaluate the effectiveness of dyslipidemia treatment with the target of LDL-c < 1.4 mmol/L between combination therapy with rosuvastatin 10 mg and ezetimibe 10 mg in patients with chronic coronary artery disease compared with monotherapy increasing the dose of rosuvastatin 20 mg in Vietnam.

Methods: A randomized controlled clinical trial, single-blind, parallel-group with a 1:1 randomized ratio in 103 outpatients with chronic coronary syndromes treated with rosuvastatin 10mg daily. Group A received the combination therapy with rosuvastatin 10 mg plus ezetimibe 10 mg daily, and group B received rosuvastatin 20 mg daily. The primary outcome was to assess the efficacy of low-density lipoprotein - cholesterol (LDL-c) control between rosuvastatin 10 mg plus ezetimibe 10 mg versus rosuvastatin 20 mg after 4 weeks and 8 weeks.

Results: After 8 weeks of intervention, the proportion of archived treatment target patients with LDL-c < 1.4 mmol/L in groups A and B was 69.2% and 44.2%, respectively (Risk ratio (RR) = 1.57, p < 0.01), 50% LDL reduction was 27.9% and 55.8%, respectively (RR = 2.00, p < 0.01), and archived both targets were 51.9% and 25.6% (RR = 2.03, p < 0.01).

Conclusion: Group A's LDL-c reduction effect and target achievement proportion (Rosuvastatin 10mg + Ezetimibe 10 mg) were significantly higher than Group B's (Rosuvastatin 20 mg). Both medication therapies were safe in patients, and the increased dose of monotherapy showed more side effects than the combination therapy.

Aims: The antihypertensive activity of Daphne gnidium was tested.

Background: Daphne gnidium (Thymelaeaceae) is used against hypertension.

Objective: The antihypertensive effect of Daphne gnidium was evaluated in this study.

Methods: The effect of Daphne gnidium aqueous extract (DGAE, 100 and 180 mg/kg) on blood pressure was evaluated in rats. In addition, the vasorelaxant effect of this extract was also tested.

Results: DGAE lowered blood pressure in hypertensive rats and exhibited vasorelaxant activity. In addition, cumulative concentrations of DGAE induced vasodilatation through receptoractivated calcium channels (ROCCs) without affecting ACE-2.

Conclusion: The aqueous extract of Daphne gnidium exhibits antihypertensive activity and induces vasodilatation via the inhibition of Ca2+ entry.

MicroRNAs have emerged as an important regulator of post-transcriptional gene expression studied extensively in many cancers, fetal development, and cardiovascular diseases. Their endogenous nature and easy manipulation have made them potential diagnostic and therapeutic molecules. Diseases with complex pathophysiology such as Diabetic Cardiomyopathy display symptoms at a late stage when the risk of heart failure has become very high. Therefore, the utilization of microRNAs as a tool to study pathophysiology and device-sustainable treatments for DCM could be considered. The present review focuses on the mechanistic insights of diabetic cardiomyopathy and the potential role of microRNAs.

Background: Numerous complications, such as postoperative arrhythmia and stroke, have been observed following coronary artery bypass graft (CABG) surgery.

Aims: This study sought to examine the impact of aging on the incidence of post-coronary artery shunt complications.

Objectives: Aging is a physiological process experienced by every living cell, beginning early in development. Age plays a crucial role in determining postoperative complications, including those related to CABG.

Materials and methods: A retrospective analysis was conducted on 290 patients who underwent CABG at the Mordovian Republic Hospital between 2017 and 2021. The sample was divided into two age-based groups: the first group comprised 126 patients (mean age range: 55.21-60.00), and the second group included 163 patients (mean age range: 66.11-80.00). Statistical analyses employed in this study encompassed descriptive statistics, Chi-square test, T-test, one-way ANOVA test, ROC analysis, and Pearson correlation using Statistica 12 software.

Results: Elderly patients in the second group demonstrated a higher incidence of post-CABG arrhythmia (p<0.012528). Moreover, the second group experienced markedly longer ICU and total hospitalization days following CABG, with p-values of less than 0.000000 and 0.000072, respectively. Notably, elderly individuals in the second group faced an increased risk of developing psychosis after CABG surgery (p<0.007379). Furthermore, psychosis was found to be significantly associated with longer ICU hospitalization (p<0.000140). Postoperative stroke occurred more frequently among the elderly (second group) with a p-value of less than 0.037736. Consequently, postoperative stroke was associated with extended ICU hospitalization (p<0.000747). The usage of internal thoracic arteries (ITAs) was lower among the elderly (second group), with a p-value of less than 0.016145. Regarding correlations, a direct association was observed between age and ICU days, total hospitalization days, and the number of complications, with correlation coefficients (r) of 0.189046, 0.141415, and 0.138565, respectively.

Conclusion: Elderly individuals in the second group who undergo CABG face a greater risk of developing psychosis, arrhythmia, prolonged total and ICU hospitalization, and stroke. The presence of arrhythmia, which is commonly observed in patients aged 63 years and older, significantly affects total hospitalization days. The number of complications is influenced by age, cardiopulmonary bypass (CPB) time, aortic cross-clamp time, ICU hospitalization, and total hospitalization duration.

Entropy is a natural process that affects all living cells, including senescence, an irreversible physiological process that impairs cell homeostasis. Age is a significant factor in disease development, and the pathogenesis of endothelial cell aging is multifactorial. Autophagy dysfunction accelerates endothelial cell aging and cell death, while autophagy preserves endothelial cell youthfulness through intracellular homeostasis and gene expression regulation. Sirt, mTORC1, and AMPK are youthfulness genes that induce autophagy by inhibiting mTOR and upregulating FIP200/Atg13/ULK1. Aged endothelial cells have decreased levels of Lamin B1, γH2AX, Ki67, BrdU, PCNA, and SA β-Gal. Maintaining healthy young endothelial cells can prevent most cardiovascular diseases. Autophagy targeting is a potential future therapeutic strategy to modify endothelial cell age and potentially slow or reverse the aging process. This article provides state-of-the-art research on the role of autophagy in endothelial cell aging. Hypothesizing that autophagy dysregulation is associated with early endothelial cell dysfunction and further clinical sequelae, including atherosclerosis formation, leading to various cardiovascular diseases.

Oral cancer is a significant global health concern, with a high mortality rate mainly due to late-stage diagnosis. Early detection plays a critical role in improving patient outcomes, highlighting the need for non-invasive and accessible screening methods. Salivary biomarkers have emerged as a promising avenue for oral cancer detection, leveraging advancements in human DNA and RNA analysis. Several DNA-based biomarkers, such as genetic mutations, chromosomal aberrations, and epigenetic alterations, have shown promise in detecting oral cancer at various stages. Likewise, RNA-based biomarkers, including microRNAs, long non-coding RNAs, and messenger RNAs, have demonstrated potential for diagnosing oral cancer and predicting treatment outcomes. The integration of high-throughput sequencing technologies, such as next-generation sequencing and transcriptomic profiling, has enabled the identification of novel biomarkers and provided deeper insights into the molecular mechanisms underlying oral cancer development and progression. Despite the promising results, challenges remain in standardizing sample collection, establishing robust biomarker panels, and validating their clinical utility. Nevertheless, salivary biomarkers hold great promise as a non-invasive, cost-effective, and accessible approach for oral cancer detection, ultimately leading to improved patient outcomes through early diagnosis and intervention. The analysis of genetic material obtained from saliva offers several advantages, including ease of collection, non-invasiveness, and the potential for repeated sampling. Furthermore, saliva reflects the physiological and pathological status of the oral cavity, making it an ideal source for biomarker discovery and validation. This article presents a comprehensive review of the current research on salivary biomarkers for oral cancer detection, focusing on insights gained from human DNA and RNA analysis.

The genus Anabasis has long been used in phytomedicine. The studied parts of Anabasis species are used as antirheumatic, diuretic, antidotes against poison, anti-erosion, anti-ulcer, and antidiabetic agents, as well as against headache and skin diseases. The objective of the present review was to summarize the phytochemical and pharmacological aspects related to the genus Anabasis. The results of this literature analysis show that among all the species of the Anabasis (A) family, A. aphylla, A. Iranica, A. aretioides, and A. articulata showed antibacterial activity; A. aretioides and A. articulata have antioxidant activity, A. aretioides and A. articulata have antidiabetic activity, A. articulata has cytotoxic activity and A. setifera, A. aretioides, and A. articulata exhibit anti-inflammatory activity. The Anabasis genus contains saponins, and alkaloids, such as anabasine, anabasamine, lupinine, jaxartinine, and triterpenic sapogenins. The study of 15 Anabasis plants has identified 70 compounds with an array of pharmacological activities especially antibacterial, antioxidant, antidiabetic, cytotoxic, and anti-inflammatory activities. However, there is a need for further studies on Anabasis plants before they can be fully used clinically as a potential drug.

Background: Hospital-acquired venous thromboembolism (HA-VTE) is defined as cases of venous thromboembolism (VTE) that occur in a hospital and within ninety days of a hospital admission. Deep vein thromboses (DVTs) most commonly occur within the deep veins of the pelvis and legs. If the thrombus dislodges and travels to the lungs, it can result in a pulmonary embolus (PE). VTE is associated with significant morbidity and mortality, accounting for almost 10% of all hospital deaths. If risk factors are correctly identified and VTE prophylaxis is prescribed, VTE can be a preventable condition. In 2010, NHS England launched The National Venous Thromboembolism Prevention Programme. This included NICE guidance, and a VTE risk assessment tool, which must be completed for at least 95% of patients on admission. The National Thrombosis Survey, published by Thrombosis UK, studied how this program was implemented locally, and audited HA-VTE prevention strategies nationally.

Objectives: Using the Thrombosis Survey and NICE guidance as an aide, this study collects data about hospital-acquired DVT (HA-DVT) at the Queen Elizabeth Hospital in Gateshead (QEH) and aims to: 1. Identify cases of HA-DVT and understand the clinical circumstances surrounding these cases 2. Assess the quality of VTE preventative measures at QEH 3. Outline potential improvement in reducing the incidence of HA-VTE at this hospital Methods: This retrospective cohort study used electronic records to identify all cases of DVT between April 2019 and April 2022 at QEH. Cases of HA-DVT were defined as: a positive ultrasound doppler report and either the case occurring in the 90 days following an inpatient stay, or beyond two days into an admission. For these cases of HA-DVT, we recorded the: reason for admission; admitting specialty; presence of an underlying active cancer and deaths occurring within 90 days of diagnosis. We assessed the quality of VTE preventative measures, by recording the: completion of VTE risk assessments; prescription of weight-adjusted pharmacological VTE prophylaxis and provision of VTE prophylaxis on discharge. For HA-DVT cases occurring within 90 days of an inpatient stay, the preventative measures were assessed on the original admission. Electronic records were used to record the completion rate of the National VTE risk assessment tool for all inpatients during this time frame.

Results: The VTE risk assessment tool was completed for 98.5% of all admissions. One hundred and thirty-five cases of HA-DVT were identified between April 2019 and April 2022. Sixteen patients with HA-DVT did not have VTE prophylaxis prescribed on admission. Eleven of these patients had a clearly documented reason why anticoagulation was avoided. In HA-DVT cases where pharmacological VTE prophylaxis was prescribed, 23% were prescribed an inappropriate dose for their weight. If anticoagulation was required on discharge, this was p