Cardiovascular and Hematological Agents in Medicinal Chemistry最新文献

Immune thrombocytopenia is an immune condition where antibodies are produced against platelets. Eltrombopag is a thrombopoietin receptor agonist that stimulates and promotes platelet production approved for treating thrombocytopenia in patients with chronic immune thrombocytopenia, where other treatments such as corticosteroids, splenectomy or immunoglobulins are inadequate. The aim of this meta-analysis was to evaluate the efficacy and safety of the eltrombopag in adults and children with immune thrombocytopenia. We included 7 studies with a total of 765 patients (606 adults and 159 children). We evaluated the number of patients that achieved a post-treatment platelet count equal or above 50x10⁹/L (primary result-target) without the need of rescue treatment for at least 4 weeks. Our data showed that patients who received eltrombopag were almost 4 times more probable in achieving the primary target when compared to patients who received placebo (RR 3.84, 95% CI 2.39 to 6.14; I² = 46%). The number of patients needed rescue treatment and the number of bleeding incidents were reduced in the group that received eltrombopag when compared to those who received placebo (RR 0.40, 95% CI 0.25 to 0.62; I² = 40%) (RR 0.74, 95% CI 0.62 to 0.89; I² = 68%). The total number of side effects did not statistically differ between the two groups (RR 0.99, 95% CI 0.90 to 1.08; I² = 14%). Our findings were similar to previously published studies and confirm that eltrombopag is safe and efficient in immune thrombocytopenia. However, more clinical trials are needed in order to enhance our findings.

Background: Heart disease (cardiovascular disease: CVD) is considered the leading cause of worldwide death. These diseases are recognized as group of disorders which are related to heart and blood vessels. Generally, heart diseases are considered life style associated diseases but many other factors are also found associated with cardiovascular diseases.

Objective: The aim of this review is to provide the till date information regarding local and circulatory disorders, role of different vitamins and herbs on heart diseases.

Methods: This review article contains a detailed survey of literature about cardiovascular diseases, which was available in different online databases such as; PubMed, Web of Science, Science Direct, Elsevier, and Google Scholar, etc. In this review, the authors have focused on the description of cardiovascular disorders, their pathophysiological properties and importance of micronutrients, vitamins and herbs in the management of cardiovascular diseases.

Results: Cardiovascular diseases are considered responsible for approximately 17.9 million deaths annually at the global level. Surprisingly, low- and middle-income countries count for 75% of CVD deaths. These diseases represent disorders related to circulatory systems specially heart and coronary arteries. Many lifestyle associated factors such as; high cholesterol consumption, smoking, alcohol consumption, tobacco use, metabolic disorders, stress, and other factors such as; family history, age, gender and genetic factors, etc. have been found involved in occurrence of CVDs. That's why management of diet, management of tobacco and alcohol consumption, management of stress, increased physical activities are considered population-wide strategies for control cardiovascular diseases. On the basis of pathophysiology, heart diseases are of many types and out of them, Acute Myocardial Infarction (AMI) and Sudden Cardiac Death (SCD) are considered serious and catastrophic cardiac disorders. Intake of vitamins, micronutrients, lycopene, omega 3 fatty acid and many herbs like Crataegus oxyacantha (Hawthron), Allium sativum (garlic), Salvia miltiorrhiza (Danshen), Ganoderma lucidum (lingzhi), Ginkgo biloba have been identified good for cardiovascular diseases management and treatment.

Conclusion: Cardiovascular diseases are considered one of the fatal clinical conditions, as many of them are asymptomatic. The regulation of diet, increased physical activities, and healthy lifestyle are recommended to control the development of cardiovascular problems. Including this, scientific studies have supported the role of many vitamins, nutrients and herbs as beneficial in cardiovascular diseases, but many of them could not demonstrate their role at clinical level but it is suggested that their role as nutrients can not be ignored and their consumption may reduce the cardiovascular risks

Background: Drug-drug interactions are undesirable, as they reduce drug bioavailability. Drug-reagent interactions in biochemical tests may directly affect the accuracy of test results.

Objective: The aim of the present study was to investigate the impact of drug-reagent interactions of drugs used in cardiology on different cardiac markers (troponin I, Nt-proBNP, CK-MB mass, CK, AST, and LDH) and the D-dimer test.

Methods: Eleven drugs (enoxaparin, tirofiban hydrochloride monohydrate, diltiazem, glyceryl trinitrate, metoprolol, epinephrine, heparin sodium, atropine sodium, furosemide, norepinephrine tartrate, and amiodarone HCl) were tested in an interference study. The interference protocol was applied to the control material of troponin I, CK-MB mass, Nt-proBNP, CK, AST, LDH tests with 11 different drugs and performed with analyzers. Cardiac Markers Plus Control (Bio-Rad, Irvine, CA, USA; Lot: 23662) materials were used to assess the impact of drug-reagent interactions on the accuracy of tests of cardiac markers based on immunoassay methods. The bias rate, defined as the extent of deviation from the target value (bias %), in the interference study was calculated in each test.

Results: For all 11 drugs, positive interference in the range of 43.58% to 130.06% occurred in the CK-MB mass test, whereas positive interference in the range of 11.98% to 107.44% occurred in the troponin I test. All the drugs, except enoxaparin sodium, led to negative interference in the range of - 84.21 to -29.6% in the Nt-proBNP test. In the D-dimer test, amiodarone HCl and diltiazem caused interference (122.87% and 28.08%, respectively). The percentage of interference caused by the other drugs ranged from -1.27% to 11.44%. Minimal deviations in the target values (between -3.31% and 3.86%) were observed in the CK, AST, and LDH tests measured using spectrophotometric methods.

Conclusion: Parenteral drugs used in cardiology can significantly interfere with troponin I, CK-MB mass, Nt-proBNP, and D-dimer tests in the analytical phase because of drug-reagent interactions. Minimal deviations in the CK, AST, and LDH tests were observed using spectrophotometric methods. Thus, changes in test results may be due to drug interference rather than the treatment itself. Clinicians should consider the possibility of drug interference in cases of doubtful cardiac test results that do not comply with the diagnosis.

In recent years, excessive use of antibiotics has been raising its head to a serious problem all around the world, as pathogens become drug-resistant and create challenges to the medical field. This failure of the most potent antibiotics that kill pathogens increases the thirst for researchers to look for another way of killing pathogens. It has led to the findings of antimicrobial peptide, which are the most potent peptides to destroy pathogens. This review gives special emphasis to the usage of marine bacteria and other microorganisms for antimicrobial peptide (AMP), which are eco-friendly as well as a developing class of natural and synthetic peptides with a wide spectrum of targets to pathogenic microbes. Consequently, a significant attention has been paid mainly to (i) the structure and types of antimicrobial peptides and (ii) mode of action and mechanism of antimicrobial peptide resistance to pathogens. In addition to this, the designing of AMPs has been analyzed thoroughly for reducing toxicity and developing better potent AMP. It has been done by the modified unnatural amino acids by amidation to target the control of biofilm and persister cells.

Aim: To study the pretreatment effect of ethanolic extract of Azolla microphylla (EAM) on rat liver induced with Isoproterenol (ISO) and to identify the phytochemicals present in EAM using HPTLC and GC-MS techniques.

Materials and methods: 42 male Wistar rats were divided into 7 groups. Rats were pre-treated with EAM (250 and 500 mg/kg bw) orally for 28 days and induced with ISO (85 mg/kg; intra-peritoneal) on the 29th and 30th days. Blood and liver samples were collected from all the rats on the 30th day for biochemical and histopathological observations. HPTLC and GC-MS analyses of EAM were done using the standard protocols.

Results: The ISO-induced group of rats displayed a significant decrease in the hepatic tissue level and activities of total protein and Aspartate Transaminase (AST), Alanine Transaminase (ALT), Alkaline Phosphatase (ALP) enzymes, respectively. Moreover, a significant decline in enzymatic and non-enzymatic antioxidants levels was spotted in the same group. However, EAM pretreatment for 28 days significantly protected the rat liver from the aforementioned alterations. Nevertheless, histopathological analysis revealed central vein dilation, necrosis, and infiltration of inflammatory cells in the ISO-induced group, wherein, EAM pretreatment significantly protected the hepatocytes from the above-mentioned changes indicating its antioxidant and cytoprotective potential. HPTLC analysis displayed the presence of flavonoids. The GC-MS analysis confirmed the presence of quercetin in EAM.

Conclusion: The overall results suggest that EAM pretreatment possesses an ameliorative effect against the ISO-induced oxidative damage in the rat hepatocytes.

Roadsides are habitats with very specific environmental conditions, often substantially differing from their natural surroundings. Roadside trees provide a home for many floral and faunal species and have many environmental benefits including removing air pollutants, supporting wildlife, etc. Many medicinal plants including roadside trees have been discovered and traditionally they are being used for treating many kinds of diseases. Phytochemicals are chemical compounds that are usually secreted by the plants for performing functions like defense against insects, fungi, diseases, and animals that feed on them. These phytochemicals with potential biological activities have been identified from various plant species, yet many of the medicinal potency of the plants remain unexplored. Modern knowledge of the potential value of medicinal plants has made it possible for researchers and medical practitioners to use plant-derived products in modern medicine with diminished adverse effects. Roadside plants in Tamilnadu also possess many such pharmacologically active compounds with therapeutical actions.

Aims: The aim of the study was to study the antidiabetic effect of Traganum nudatum in an animal model of diabetes.

Background: Traganum nudatum (T. nudatum) is a medicinal plant widely used in folk medicine by the Moroccan population to treat various diseases including diabetes.

Objective: The objective of the study was to evaluate the antihyperglycemic and hypoglycemic of the aqueous Traganum nudatum extract in normal and streptozotocin-induced diabetic rats.

Methods: Normal and streptozotocin-induced diabetic rats were treated orally by the extract of Traganum nudatum (T. nudatum) at a dose of 50 mg/kg. The blood glucose levels were determined for 6 hours and 15 days during this treatment. The oral glucose tolerance and phytochemical tests and the analysis of histopathological changes of the liver were performed. The antioxidant activity of aqueous T. nudatum extract was also assessed using the method of trapping of free radical 2,2- diphenyl-1 picrylhydrazyl (DPPH).

Results: T. nudatum Aerial Part Aqueous Extract (TNAPAE) reduced the blood glucose levels in both normal and diabetic rats. The results demonstrated that TNAPAE treatment exhibited a significant hypoglycemic effect without altering the body weight. In addition, a noticeable influence on glucose tolerance was also observed after TNAPAE treatment. Moreover, TNAPAE was able to exhibit a beneficial effect on the histological structure of the liver. Finally, a potential antioxidant effect has been shown in vitro.

Conclusion: In conclusion, this study demonstrates the antihyperglycemic and hypoglycemic effects of T. nudatum in rats supporting its traditional use for the management of diabetes.

In this era of potent medications and interventional cardiovascular (CV) procedures, the importance of beginning with and including Therapeutic Lifestyle Changes (TLC) is frequently forgotten. A major goal of this review article is to show and emphasize that modification of CV risk with nonmedication approaches makes an essential contribution to CV risk reduction. Available information on TLC and modifiable CV risk factors was reviewed and assessed. Modifiable major CV risk factors include diabetes mellitus, hypertension, hyperlipidemia, tobacco abuse, obesity, stress, and a sedentary lifestyle. Age as a major CV risk factor is, of course, not susceptible to modification. A contribution to the control of CV risk factors can occur without the start of medications and there is proof of benefit for beginning with a non-pharmacological approach. TLC can benefit all of the major modifiable CV risk factors and there is good evidence for the additional benefit of supervised and group TLC. TLC includes physical activity, diet, and smoking cessation. Evidence for the benefits of TLC in reducing CV disease events is well established. However, medications must be added in those patients with higher CV risk to obtain maximum cholesterol reduction (lower is better for the low-density lipoprotein cholesterol) and good blood pressure control. The benefit of TLC is frequently forgotten in this era of potent medications and invasive procedures. The benefits of diet and physical activity are emphasized with supporting data. Many motivated patients can prolong their lives significantly by dedication to TLC. Therapeutic Lifestyle Change (TLC) especially encompasses increased physical activity, a healthy diet, and smoking cessation. There is extensive proof for the benefit of TLC in contributing to cardiovascular (CV) disease prevention. CV diseases have strong metabolic and inflammatory components, both of which can be improved by TLC.

Natural products have a unique place in the healthcare industry. The genus Commiphora emerged as a potential medicinal source with huge benefits as evidenced through its use in various traditional and modern systems of medicine. Therefore, we aimed to prepare a concise review on the pharmacological activities and the indigenous uses of various plant species belonging to the genus Commiphora along with the structural information of various active botanical ingredients present in these plants based on the published literatures and scientific reports. To collect the published literatures on Commiphora in various journals; to study and classify the available information on the pharmacological uses and chemical constituents; and to present the gathered information as a precise review to serve as a potential reference for future research. Pharmacological and phytochemical data on Commiphora plant species were collected from various journals, books, reference materials, websites including scientific databases, etc. for compilation. This review article describes the various pharmacological properties of plants of Commiphora species viz., anti-arthritic and anti-inflammatory, anti-atherogenic, antibacterial, anti-coagulant, antidicrocoeliasis, anti-epileptic, anti-fascioliasis, anti-fungal, anti-heterophyidiasis, anti-hypercholesterolemic, anti-hyperlipidemic, anti-hypothyroidism, anti-obesity, anti-osteoarthritic, antiosteoclastogenesis, anti-oxidant, anti-parasitic, anti-pyretic, anti-schistosomiasis, anti-septic, antithrombotic, anti-ulcer, cardioprotective, COX enzyme inhibitory, cytotoxic /anti-carcinogenic/anticancer, DNA cleavage, hypotensive, inhibits lipid peroxidation, inhibits NO and NO synthase production, insecticidal, local anesthetic, molluscicidal, smooth muscle relaxant, and tick repellent activities along with toxicity studies. Furthermore, the review also included various secondary metabolites isolated from various species of Commiphora genus along with their chemical structures serving as a ready resource for researchers. We conclude that the plant species belonging to the genus Commiphora possesses abundant pharmacological properties with a huge treasure of diverse secondary metabolites within themselves. This review indicates the necessity of further in-depth research, pre-clinical, and clinical studies with Commiphora genus, which may help to detect the unidentified potential of the Commiphora plant species.

The major physiopathological mechanism underlying Acute Coronary Syndromes (ACS) is atherosclerotic plaque rupture with resultant coronary thrombosis, posing a big burden in health care systems. Dual anti-platelet therapy (DAPT) can improve CV outcome with a prolonged regimen, albeit at the cost of increased bleeding rates. We performed a narrative literature review on the topic, in which we explored databases through April 15th, 2020, with no restrictions on language. Keywords related to antiplatelet therapy, P2Y12 inhibitor, aspirin and DAPT were utilized. Randomized clinical trials, large prospective studies, systematic reviews and meta-analysis were included. We hand-searched the reference lists of included articles and relevant reviews. The review revealed that when choosing antiplatelet agents, the decision should be driven by pharmacodynamic properties as well as demonstrated efficacy and safety. Additionally, it was noted that in patients undergoing percutaneous coronary intervention, prasugrel and ticagrelor are preferred. In patients with a high risk of bleeds or receiving thrombolysis, or when cost or specific patient issues exist, clopidogrel is considered though it is a second-line therapy. Due to an elevated risk of bleeds, triple therapy should be avoided, as evidence shows effectiveness and safety with regimens without ASA. Furthermore, multiple studies have also shown that regimens shorter than 12 months of DAPT could be adequate for many patients, and newer guidelines are likely to reflect it. There are specific recommendations for switching among antiplatelets, mostly based on registries and pharmacodynamic studies.