Cardiovascular & hematological agents in medicinal chemistry最新文献

{"title":"Combined Administration of Metformin and Vitamin D: A Futuristic Approach for Management of Hyperglycemia.","authors":"Sakshi Tyagi, Shalini Mani","doi":"10.2174/0118715257261643231018102928","DOIUrl":"10.2174/0118715257261643231018102928","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"258-275"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71490019","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antihypertensive and ACE-2 Inhibitory Effects of <i>Daphne gnidium</i> in Rats.","authors":"Ismail Bouadid, Adil Qabouche, Mohamed Eddouks","doi":"10.2174/0118715257251651231212045407","DOIUrl":"10.2174/0118715257251651231212045407","url":null,"abstract":"<p><strong>Aims: </strong>The antihypertensive activity of <i>Daphne gnidium</i> was tested.</p><p><strong>Background: </strong><i>Daphne gnidium</i> (Thymelaeaceae) is used against hypertension.</p><p><strong>Objective: </strong>The antihypertensive effect of <i>Daphne gnidium</i> was evaluated in this study.</p><p><strong>Methods: </strong>The effect of <i>Daphne gnidium</i> 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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>The aqueous extract of <i>Daphne gnidium</i> exhibits antihypertensive activity and induces vasodilatation via the inhibition of Ca²⁺ entry.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"432-440"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139567713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Genetic Underpinnings of Pulmonary Fibrosis: An Overview.","authors":"Sushweta Mahalanobish, Sumit Ghosh, Parames C Sil","doi":"10.2174/0118715257261006231207113809","DOIUrl":"10.2174/0118715257261006231207113809","url":null,"abstract":"<p><strong>Introduction: </strong>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.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"367-374"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139571601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Green Synthesis of Silver Nanoparticles using <i>Coriandrum sativum</i> and <i>Murraya koenigii</i> Leaf Extract and its Thrombolytic Activity.","authors":"Priyanca Pram, Nikita Mishra, Mohanasrinivasan Vaithilingam, Merlyn Keziah Samuel, Maneesha Mohanan, Neeti Kothari, Subathra Devi Chandrasekaran","doi":"10.2174/0118715257279159240118050207","DOIUrl":"https://doi.org/10.2174/0118715257279159240118050207","url":null,"abstract":"<p><strong>Background: </strong>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 <i>Coriandrum sativum</i> and <i>Murraya koenigii</i> leaf extract and its thrombolytic activity.</p><p><strong>Objective: </strong>The aim of the study was to determine the clot lysis activity of <i>Coriandrum sativum</i> and <i>Murraya koenigii</i> synthesized silver nanoparticles.</p><p><strong>Methods: </strong>Leaves of <i>Coriandrum sativum</i> and <i>Murraya koenigii</i> 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 <i>Coriandrum sativum</i> and <i>Murraya koenigi</i>i synthesized silver nanoparticles were analysed by the modified Holmstorm method.</p><p><strong>Results: </strong>The thrombolytic property of the methanolic extract of plants <i>Coriandrum sativum</i> showed clot lysis activity at 2.5 mg/mL with 45.99% activity, and <i>Murraya koenigii</i> extract with 66.56% activity. The nanoparticles (Nps) from <i>Coriandrum sativum</i> showed clot lysis activity at 2.5 mg/mL with 58.29% activity, and NPs from <i>Murraya koenigii</i> with 54.04% activity. <i>Coriandrum sativum</i> in GC-MS exhibited 3 peaks, whereas <i>Murraya koenigii</i> extract showed five peaks with notable bioactive compounds.</p><p><strong>Conclusion: </strong>These NPs were further used for biomedical applications after being fixed by an organic encapsulation agent. The present research reveals the usefulness of <i>Coriandrum sativum</i> and <i>Murraya koenigii</i> for the environmentally friendly manufacture of silver nanoparticles.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":"22 2","pages":"230-239"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141556141","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"MicroRNAs Targeting Critical Molecular Pathways in Diabetic Cardiomyopathy Emerging Valuable for Therapy.","authors":"Priyanka Mathur, Sharad Saxena, Bhawna Saxena, Vibha Rani","doi":"10.2174/0118715257265947231129074526","DOIUrl":"10.2174/0118715257265947231129074526","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"298-307"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139543758","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of Quercetin's Bioenhancing Effect on Oral Pharmacokinetics of Rosuvastatin in Wistar Rats Using RP-HPLC Method.","authors":"Rachana S Bhimanwar, Lata P Kothapalli, Akshay Khawshi","doi":"10.2174/0118715257258735231016112348","DOIUrl":"https://doi.org/10.2174/0118715257258735231016112348","url":null,"abstract":"<p><strong>Background: </strong>The absolute oral bioavailability of rosuvastatin (RST), a secondgeneration statin, is low i.e. 20% and only 10% is recovered as metabolite N-desmethy l rosuvistatin. Since it is a hydrophilic statin, RST relies on the organic anion transporting polypeptide- 1B1 (OATP-1B1), as the key mechanism for active transport into hepatocytes. Quercetin (QUE) being a bio enhancer and inhibitor of OATP1B1 can augment the bioavailability and pharmacokinetics of RST.</p><p><strong>Objectives: </strong>The present study includes the development of a simple and validated bioanalytical Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) method for the estimation of RST and to study the effect of co-administration of QUE as a bio enhancer on its bioavailability.</p><p><strong>Methods: </strong>An analytical column of Kromasil 100, C18 (250 mm × 4.6 mm, 5 μm), was used for chromatographic separationand acetonitrile (ACN): acetic acid buffer pH 3.0 adjusted with glacial acetic acid (55:45 Vol. %) as mobile phase with flow rate 1.0 ml/min monitored at 242 nm. The ACN: methanol (50:50 Vol. %) was employed as the final solvent for extraction. The developed method has been successfully applied in a study on the pharmacokinetics of the drug RST in rats after co-administration of QUE, which was carried out using non-compartmental analysis in order to estimate the blood concentration of the drug.</p><p><strong>Results: </strong>The pharmacokinetics of RST was found to be altered significantly (highest concentration of RST in the blood (<i>C</i>_max) = 67.3 ng/ml to 122.2 ng/ml) (p < 0.001), area under curve (AUC)_0-t (p < 0.0001) and AUC_0-inf (p = 0.0005) when co-administered with QUE at 120 min (<i>t</i>_max).</p><p><strong>Conclusion: </strong>The results are in accordance with the fact that QUE increases plasma levels in rats through herb-drug interactions.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":"22 4","pages":"456-465"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142483078","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Herbal Medicine- A Friend or a Foe of Cardiovascular Disease.","authors":"Harmanjit Kaur, Samneet Singh, Sai G Kanagala, Vasu Gupta, Meet A Patel, Rohit Jain","doi":"10.2174/0118715257251638230921045029","DOIUrl":"10.2174/0118715257251638230921045029","url":null,"abstract":"<p><strong>Background: </strong>Herbal remedies are used by 80% of the Asian population in primary health care as per WHO. According to current research, the herbal medicine market was valued at nearly USD 166 billion in 2021 and is expected to reach approximately USD 348 billion by 2028. Increased incidence of chronic conditions such as diabetes, asthma, coronary artery disease, osteoarthritis, has fueled the growing interest in traditional herbal and plant-derived treatments among researchers. In addition, rural communities in developing nations have renewed interest in herbal treatments due to lower cost and easy availability.</p><p><strong>Objectives: </strong>Aim of the paper is to highlight the role of five of more commonly used herbal medicines that are Ginkgo biloba, Garlic, Flaxseed, Ginseng, <i>Salvia miltiorrhiza</i> in cardiovascular disorders.</p><p><strong>Methods: </strong>A PubMed search was done using the keywords Herbal Medicine, Ginkgo biloba, Garlic, Flaxseed, Ginseng, <i>Salvia miltiorrhiza</i>. Articles which were available for free access were utilized. No formula inclusion or exclusion criteria was followed. A total of 42 papers were included for the study.</p><p><strong>Conclusion: </strong>Although there have been encouraging outcomes with the use of these herbal medications, many of these products are poorly monitored and are yet to be studied in detail regarding their adverse effects. Moreover, these medicinal products are known to interact with various drugs. To compete with the expanding pharmaceutical industry, more medicinally helpful herbal items must be used and scientifically validated.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"101-105"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41223566","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Association between waist circumference and magnesium and uric acid in indigenous Argentinean children living at high altitude.","authors":"Valeria Hirschler, M Esteban, C González, C Molinari, L Castano","doi":"","DOIUrl":"","url":null,"abstract":"<p><strong>Background: </strong>Studies in adults show that central obesity increases the likelihood of Type 2 diabetes (T2DM).</p><p><strong>Objective: </strong>To determine the association between waist circumference (WC) and non-traditional risk factors such as magnesium (Mg), phosphorus, and uric acid in indigenous children living at high altitudes.</p><p><strong>Methods: </strong>A total of 354 (166 M) indigenous school children, aged 9.6 + 2.3 years, were enrolled in a cross-sectional study in November 2011. Central obesity was defined as WC &gt; 90th percentile according to age and sex. Low Mg and phosphorus levels were defined as serum Mg &lt;1.8 mg/dL and phosphorus &lt;2.4 mg/dL . Hyperuricemia was defined as serum uric acid &gt; 7 mg/dL.</p><p><strong>Results: </strong>The prevalence of central obesity was 6.8% (24/354). None of the children had hyperuricemia or low P levels. HypoMg was identified in 21.7% (57/263). There was a significant association between WC (z-score) and Mg (r-015), uric acid (r0.28), phosphorus (r-0.30), HOMA-IR (r0.49), Triglycerides (r0.24), and HDL-C (r0.24). However, calcium, sodium, and potassium were not significantly associated with WC. As z-WC quartiles increased Mg and phosphorus levels significantly decreased, whereas uric acid levels increased. Multiple linear regression analysis showed that z-WC was associated significantly and directly with uric acid (B0.31), triglycerides (B0.004), and HOMA-IR (B0.35); and inversely with Mg (B-0.83) and phosphorus (B-0.25), adjusted for confounding variables (R2 0.34).</p><p><strong>Conclusion: </strong>Our results indicate that central obesity was significantly and inversely associated with Mg and phosphorus and directly with uric acid in indigenous school children. Supplementation with Mg and/or phosphorus could prevent future cardiovascular disease. Prospective and randomized studies should be performed to confirm these findings.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"None"},"PeriodicalIF":0.0,"publicationDate":"2016-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139975014","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological evidence of α-adrenergic receptors in the hypotensive effect of Chamaemulum nobile L.","authors":"M Hebi, M Ajebli, N A Zeggwagh, M Eddouks","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>This study aims to evaluate the underlying mechanism of action involved in the hypotensive effect of Chamaemulum nobile L. (Cn) aqueous extract and in anesthetized Wistar rats. Lyophilized aqueous extract was administered in the jugular vein, arterial blood pressure and heart rate were measured in the carotide artery over 120 min of injection throughout an invasive direct blood pressure measuring procedure. Intravenous bolus injection of aqueous Cn extract at the doses of 50, 100 and 200 mg/kg produced a dose dependent reduction in arterial blood pressure and heart rate (p<0.001). Specific receptor antagonists (Phentolamine, Terazosin and Atropine) and pharmacological agents (N(omega)-Nitro-L-Arginine Methyl Ester and Captopril) were used for determining the underlying mechanism involved in the hypotensive effect of Cn. Only Phentolamine treatment (2 mg/kg) reduced significantly the hypotensive effect of aqueous Cn extract at a dose of 200 mg/kg. Intravenous perfusion of aqueous Cn extract caused a significant reduction of arterial blood pressure (p<0.01) and reduced the hypertensive effect of intravenous injection of norepinephrine at a dose of 1 &#181;g/kg. We conclude that aqueous Cn extract exhibits a hypotensive effect which may be probably due to an alpha adrenergic receptor blockade mechanism.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"None"},"PeriodicalIF":0.0,"publicationDate":"2016-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139975016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"New Insights on the Impact of Statin Therapy in the Susceptibility to Hypovitaminosis D Through Serum Lipidome Profiling.","authors":"Ana Rita Santos Estrela, Frederico Cerveira, Bárbara Regadas Correia, Ana Reis, Margarida Fardilha, Pedro Domingues, Rita Ferreira, M Rosário M Domingues","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Hypovitaminosis D is a worldwide clinical problem, affecting populations in numerous ways. Several factors seem to affect vitamin D metabolism, including the suggestion that therapy with the lipid lowering HMG-CoA inhibitors might modulate vitamin D levels. However, the relationship between statins intake and serum levels of vitamin D is still controversial. The present work aimed to add new insights on the association between statins therapy, and more specifically the generation of statins, and the lipid profile in a population of 106 subjects treated with these HMG-CoA inhibitors. Data showed that despite a higher prevalence of hipovitaminosis D in subjects treated with statins, there is no association between statin generation, total and LDL cholesterol and vitamin D levels. Moreover, second generation statins, the most common treatment of hypercholesterolemia in the studied population, promoted the remodelling of serum fatty acids that was characterized by the increase of arachidonic acid (AA) relative levels without affecting eicosapentaenoic acid (EPA) levels. Among statin treated subjects, vitamin D levels did not affect serum fatty acid profile. The statin-related increased ratio AA/EPA suggests a pro- inflammatory status, whose long-term impact should be better clarified in the future.</p>","PeriodicalId":93924,"journal":{"name":"Cardiovascular & hematological agents in medicinal chemistry","volume":" ","pages":"None"},"PeriodicalIF":0.0,"publicationDate":"2016-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139975015","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}