Cardiovascular & hematological agents in medicinal chemistry最新文献

Background: Beta-blockers are essential agents in the management of cardiovascular diseases, such as heart failure, acute myocardial infarction (MI), and cardiac arrhythmias. However, there are diurnal variations in the cardioprotective effects of the subgroups as a result of their different pharmacokinetic, pharmacodynamic, and pharmacogenetic profiles.

Objectives: We aimed to compare metoprolol and bisoprolol in terms of electrocardiogram (ECG) outcomes.

Methods: A retrospective cross-sectional study was conducted at Prince Sultan Cardiac Center. The trial included 404 patients who met the inclusion criteria (204 in the metoprolol arm and 200 in the bisoprolol arm). Using case record forms that had already been created, information, such as patient demographics, medical histories, and treatment histories, was taken from their medical files. The most recent ECG records were also gathered. The ethical approval for this study was obtained from Qassim ethical committee (approval number: 45-44-902).

Results: There was no significant difference found between the patients in both arms in terms of baseline characteristics, age, or sex.

Conclusion: In this retrospective cross-sectional study, we have compared the effects of metoprolol and bisoprolol beta blockers on ECG changes. The findings have indicated no difference between metoprolol and bisoprolol groups in terms of all ECG readings, particularly PR/ms, QTC-ms, and ventricular rate. Further studies are required to confirm these findings.

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.

The endoplasmic reticulum (ER) is a sub-cellular organelle that is responsible for the correct folding of proteins, lipid biosynthesis, calcium storage, and various post-translational modifications. In the disturbance of ER functioning, unfolded or misfolded proteins accumulate inside the ER lumen and initiate downstream signaling called unfolded protein response (UPR). The UPR signaling pathway is involved in lipolysis, triacylglycerol synthesis, lipogenesis, the mevalonate pathway, and low-density lipoprotein receptor recycling. ER stress also affects lipid metabolism by changing the levels of enzymes that are involved in the synthesis or modifications of lipids and causing lipotoxicity. Lipid metabolism and cardiac diseases are in close association as the deregulation of lipid metabolism leads to the development of various cardiovascular diseases (CVDs). Several studies have suggested that lipotoxicity is one of the important factors for cardiovascular disorders. In this review, we will discuss how ER stress affects lipid metabolism and their interplay in the development of cardiovascular disorders. Further, the current therapeutics available to target ER stress and lipid metabolism in various CVDs will be summarized.

Aims: The study aimed to investigate the antihypertensive activity of Scorzonera undulata ssp. deliciosa.

Background: Scorzonera undulata ssp deliciosa, locally known as "Guiz", is used in traditional medicine in Morocco as a diuretic and mainly against snake bites.

Objectives: This study investigated the possible antihypertensive effect of the aqueous extract of Scorzonera undulata (AESU).

Materials and methods: In the present study, the antihypertensive activity of AESU was tested in normotensive and hypertensive rats Results: The results indicated that AESU decreased the systolic, diastolic, and mean arterial blood pressure in hypertensive rats. The data revealed that AESU exerted its antihypertensive effect through vasodilatory properties. Interestingly, the study demonstrated that the vasorelaxation ability of AESU might be mediated through receptor-operated calcium channels (ROCCs). However, AESU dhad effect on inhibiting ACE-2.

Conclusion: The present study indicates the antihypertensive and vasorelaxant activities of AESU in hypertensive rats.

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.

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.

Diabetes is a series of metabolic disorders that can be categorized into three types depending on different aspects associated with age at onset, intensity of insulin resistance, and beta- cell dysfunction: Type 1 and 2 Diabetes, and Gestational Diabetes Mellitus. Type 2 Diabetes Mellitus (T2DM) has recently been found to account for more than 85% of diabetic cases. The current review intends to raise awareness among clinicians/researchers that combining vitamin D3 with metformin may pave the way for better T2DM treatment and management. An extensive literature survey was performed to analyze vitamin D's role in regulating insulin secretion, their action on the target cells and thus maintaining the normal glucose level. On the other side, the anti-hyperglycemic effect of metformin as well as its detailed mechanism of action was also studied. Interestingly both compounds are known to exhibit the antioxidant effect too. Literature supporting the correlation between diabetic phenotypes and deficiency of vitamin D was also explored further. To thoroughly understand the common/overlapping pathways responsible for the antidiabetic as well as antioxidant nature of metformin and vitamin D3, we compared their antihyperglycemic and antioxidant activities. With this background, we are proposing the hypothesis that it would be of great interest if these two compounds could work in synergy to better manage the condition of T2DM and associated disorders.

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.

Introduction: Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive disorder, in which genetic and environmental factors are involved in disease onset. Although, by definition, the disease is considered idiopathic in nature, evidence-based studies have indicated familial cases of pulmonary fibrosis, in which genetic factors contribute to IPF pathogenesis.

Methods: Both common as well as rare genetic variants are associated with sporadic as well as familial forms of IPF. Although clinical inferences of the genetic association have still not been explored properly, observation-based studies have found a genotypic influence on disease development and outcome.

Results: Based on genetic studies, individuals with a risk of IPF can be easily identified and can be classified more precisely. Identification of genetic variants also helps to develop more effective therapeutic approaches.

Conclusion: Further comprehensive research is needed to get a blueprint of IPF pathogenesis. The rapidly evolving field of genetic engineering and molecular biology, along with the bioinformatics approach, will possibly explore a new horizon very soon to achieve this goal.

Background: Plants have been used for ages in traditional medicine, and it is exciting to perceive how recent research has recognized the bioactive compounds liable for their beneficial effects. Green synthesis of metal nanoparticles is a hastily emergent research area in nanotechnology. This study describes the synthesis of silver nanoparticles (AgNPs) using Coriandrum sativum and Murraya koenigii leaf extract and its thrombolytic activity.

Objective: The aim of the study was to determine the clot lysis activity of Coriandrum sativum and Murraya koenigii synthesized silver nanoparticles.

Methods: Leaves of Coriandrum sativum and Murraya koenigii were collected. Methanolic extraction of the plant sample was done through a Soxhlet extractor. The methanolic extract obtained from both the leaves was subjected to GC-MS analysis. The synthesized NPs from leaf extracts were monitored for analysis, where the typical X-ray diffraction pattern and its diffraction peaks were identified. 3D image of the NPs was analysed by Atomic Force Microscopy. The surface charge of nanoparticles was identified by Zeta potential. The Clot lysis activity of Coriandrum sativum and Murraya koenigii synthesized silver nanoparticles were analysed by the modified Holmstorm method.

Results: The thrombolytic property of the methanolic extract of plants Coriandrum sativum showed clot lysis activity at 2.5 mg/mL with 45.99% activity, and Murraya koenigii extract with 66.56% activity. The nanoparticles (Nps) from Coriandrum sativum showed clot lysis activity at 2.5 mg/mL with 58.29% activity, and NPs from Murraya koenigii with 54.04% activity. Coriandrum sativum in GC-MS exhibited 3 peaks, whereas Murraya koenigii extract showed five peaks with notable bioactive compounds.

Conclusion: These NPs were further used for biomedical applications after being fixed by an organic encapsulation agent. The present research reveals the usefulness of Coriandrum sativum and Murraya koenigii for the environmentally friendly manufacture of silver nanoparticles.