Cardiovascular and Hematological Agents in Medicinal Chemistry最新文献

Aims: The aim of the study was to assess the effect of Cleome arabica on lipid metabolism.

Background: Cleome arabica (L.) is a medicinal plant used traditionally by the population of North Africa for managing diabetes mellitus.

Objective: This study was designed to evaluate the antidyslipidemic and antiatherogenic capacities of Cleome arabica (L.) in normal and streptozotocin(STZ)-induced diabetic rats.

Methods: The hypolipidemic, antihyperglycemic and antiatherogenic effects of oral administration of the aqueous extract of Cleome arabica (CAAE) (100 mg/kg) were evaluated in normal and diabetic rats. In addition, the quantification of polyphenols, flavonoids and tannins as well as the antioxidant activity were performed.

Results: The results showed that the extract (CAAE) revealed an antidyslipidemic action by attenuating plasma levels of Total Cholesterol (TC), Triglycerides (TGs), Low-Density Lipoprotein cholesterol (LDL-c), Very low-density lipoprotein cholesterol (VLDL-c) and glucose. Additionally, CAAE exhibited a potent antiatherogenic activity by reducing Atherogenic Coefficient (AC), Castelli's Risk index-I (cri-I), and Castelli's Risk Index-II (CRI-II). Furthermore, the findings indicated that CAAE is abundant with polyphenols, flavonoids and tannins, and exhibited an important antioxidant capacity.

Conclusion: The study demonstrates that aqueous Cleome arabica extract was able to ameliorate lipid abnormalities associated with diabetes mellitus. This pharmacological activity might be due to the antioxidant capacities of phytochemical compounds.

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 blocking of inhibitory receptors and have shown promising results in preclinical models and studies on the adult population. However, paediatric malignancies present unique features, and so far, experience with these agents is 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.

Background: This study aimed to investigate the potential bioactivity and the ameliorative role of Galaxaura oblongata (G. oblongata) against LPS-induced toxicity using hematological parameters.

Objective: The objective of this study is to examine its protective effect using the immunohistochemistry of the liver and lungs as biomarkers in male BALB/C albino mice.

Materials and methods: The current study was carried out using different in-vitro and in-vivo assays, such as phytochemicals, antioxidants and anti-inflammatory for in-vitro where the hematological and immunohistochemistry for lung and liver were investigated in vivo.

Results: No previous studies were performed to investigate the in vivo and in vitro effects of the G. oblongata extracts as antioxidant and anti-inflammatory due to their rareness compared to other red algae. LPS treated mice revealed a significant decrease in the total number of WBCs, RBCs, platelets, and HGB%, MPV, MCV and MCHC compared to the control group. In contrast, the HCT and MCHC were increased in the induction group, which was treated with LPS compared to the control group. Furthermore, the immunohistochemistry results of the present study revealed the protective effect of G. oblongata compared to the induction group. G. oblongata can be used as protective marine natural products against the toxicity induced by LPS.

Conclusion: It exhibited a significant ameliorative role against the alterations in the hematological parameters and immunohistochemistry of the liver and lungs, and reduced as well as coordinated the acute inflammations caused by TNF.

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.

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 antihyperglycemic and antihyperlipidemic effects of Bersama abyssinica.

Methods: Antidiabetic effect of 80% methanolic crude extract of Bersama abyssinica was studied in a 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 were 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, 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.

Objective: Salvia miltiorrhiza (SM) is a traditional Chinese medicine used clinically to treat cardiovascular diseases, including atherosclerosis and myocardial infarction. Its therapeutic effect has been confirmed by many clinical and pharmacological studies. However, the optimal formulation of active ingredients in SM for treating cardiovascular diseases remains unclear. In this study, we determined the ratio of the optimal compatibility of SM ingredients DSS, Sal-A, Sal-B, and PAL (SABP)with a uniform and orthogonal optimized experimental design. In addition, we determined the anti-oxidation effect of SABP using Adventitial Fibroblasts (AFs).

Methods: By using a combination of uniform and orthogonal designs, we determined the optimal formulation of aqueous extract from SM. MTT assay was used to determine the inhibitory effects of these 4 components of SM on the AFs, which were isolated and cultured from the aorta. The reactive oxygen species (ROS) production in AFs was compared before and after SABP treatment.

Results: The optimal formulation of these 4 aqueous extracts from SM were 150 : 7 : 300 : 500, and their concentrations were S(1.5×10-4 mol/L), A(7×10-6 mol/L), B(3×10-4 mol/L), and P(5×10-4 mol/L). There were some synergies between these 4 components. Moreover, SABP decreased ROS production in AFs.

Conclusion: These findings suggest that SABP inhibits the proliferation and oxidation stress in AFs. The present study provides new evidence that the efficacy and function generated from the optimal formulation of active ingredients in SM are better than lyophilized powder of SM.

Rheumatic valve disease is present in 0.4 % of the word population, mainly in lowincome countries. Rheumatic mitral stenosis affects more women and between 40 to 75 % of patients may have atrial fibrillation (AF), more frequently in upper-middle income countries. This rhythm disturbance is due to increased atrial pressure, chronic inflammation, fibrosis, and left atrial enlargement. There is also an increase in the prevalence of AF with age in patients with mitral stenosis. The risk of stroke is 4 % per year. Success rates for cardioversion, Cox-Maze procedure, and catheter ablation are low. Therefore, anticoagulation with vitamin K antagonist is mandatory for Evaluated Heart valves, Rheumatic or Artificial (EHRA) classification type 1. However, this anticoagulation is used by less than 80 % of those eligible and less than 30 % have the international normalized ratio in the therapeutic range. The safety and efficacy of using rivaroxaban, a direct factor Xa inhibitor anticoagulant, were demonstrated in the RIVER trial with a sample of 1005 patients with AF and bioprosthetic mitral valve. The indication for valve replacement, that is, if severe mitral stenosis or severe mitral regurgitation, was not specified. A randomized, open-label study (DAVID-MS) is underway to compare the effectiveness and safety of dabigatran and warfarin therapy for stroke prevention in patients with AF and moderate or severe mitral stenosis. Thus, the applicability of the use of direct anticoagulants in patients with AF and mitral stenosis and also in those undergoing mitral bioprostheses surgery will be the subject of further studies. The findings may explain if specific atrial changes of mitral stenosis even after the valve replacement will influence thromboembolic events with direct anticoagulants.

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.

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 the liver was carried out using the Hematoxylin-Eosin method. Furthermore, the in vitro antioxidant activity as well as, 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.