Article by Disease | Electrochemical Determination of Non-Steroidal Anti-Inflammatory Drugs

Anti Inflammatory -> RHEUMATOID ARTHRITIS

 

Electrochemical methods have been used for the determination of nonsteroidal antiinflammatory drugs (NSAID) just as used in the determination of various drugs. Among voltammetric methods; differential pulse voltammetric method, square wave voltammetric method and linear sweep voltammetric method are the most commonly used ones. NSAIDs are widely used in the treatment of inflammatory conditions such as musculoskeletal disorders (rheumatoid arthritis, osteoarthritis, acute gouty arthritis) and dental pain, menstrual pain, postoperative pain and migraine. In this review, some selected recent electrochemical studies were selected related to the nonsteroidal antiinflammatory drug analyzes. The aim of this review is to evaluate and discuss the advantages, details and usages of electroanalytical methods in the determination of nonsteroidal anti-inflammatory drug. Read out more at: http://www.eurekaselect.com/node/165494/article?tracking-code=4

 

Non-Steroidal-Anti-Inflammatory-Drugs

Article by Disease | Therapeutic Utilities of Pediatric Cardiac Catheterization

 

Bentham Cardiovascular Disorders Collection | Cardiovascular Disorders | Aortic Coarctation 

Therapeutic cardiac catheterization constantly evolves and widens its spectrum of usage in the pediatric population. The advent of sophisticated devices and well-designed equipment has made the management of many congenital cardiac lesions more efficient and safer, while providing more comfort to the patient.

 

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Read out more at: http://www.eurekaselect.com/node/139921/article

Article by Disease | Statins in Aortic Disease

Bentham Cardiovascular Disorders Collection | Cardiovascular Disorders | Aortic Coarctation 

 

Abstract:

Background: Numerous studies indicate that statins have multiple beneficial actions (known as ‘pleiotropic actions’) on cardiovascular system through the improvement of endothelial dysfunction, inflammation, oxidative stress, excessive arterial thrombosis, and stabilization of the atherosclerotic plaque. Aortic disease primarily consists of aortic valve stenosis, aortic valve regurgitation, aneurysm disease, and genetic disorders such as Marfan syndrome, bicuspid aortic valve and aortic coarctation. Many studies have revealed the cardioprotective actions of statins in aortic disease.

Objective: Our aim was to present current data concerning the value of treatment with statins in aortic diseases.

Methods: A thorough search of PubMed and the Cochrane Database was conducted to identify the studies and novel articles related to the use of statins in aortic disease.

Results: Numerous studies in animals and humans indicate a beneficial effect of treatment with statins in the previous conditions apart from a few conflicting data.

Conclusion: There is a need of further investigation in this field, especially for the estimation of the optimal type and dose of statins required in each clinical condition of aortic disease.

 

Read out more at: http://www.eurekaselect.com/node/157165/article

Article by Disease | Notch Signaling in Normal and Disease States: Possible Therapies Related to Glycosylation

 

Bentham Cardiovascular Disorders Collection | Alagille Syndrome

 

 

 

Abstract:

The Notch signaling pathway is involved in a wide variety of highly conserved developmental processes in mammals. Importantly, mutations of the Notch protein and components of its signaling pathway have been implicated in an array of human diseases (T-cell leukemia and other cancers, Multiple Sclerosis, CADASIL, Alagille Syndrome, Spondylocostal Dysostosis). In mammals, Notch becomes activated upon binding of its extracellular domain to ligands (Delta and Jagged/Serrate) that are present on the surface of apposed cells. The extracellular domain of Notch contains up to 36 tandem Epidermal Growth Factor-like (EGF) repeats. Many of these EGF repeats are modified at evolutionarily-conserved consensus sites by an unusual form of O-glycosylation called O-fucose. Work from several groups indicates that O-fucosylation plays an important role in ligand mediated Notch signaling. Recent evidence also suggests that the enzyme responsible for addition of O-fucose to Notch, protein O-fucosyltransferase-1 (POFUT1), may serve a quality control function in the endoplasmic reticulum. Additionally, some of the O-fucose moieties are further elongated by the action of members of the Fringe family of β-1,3-N-acetylglucosaminyltransferases. The alteration in O-fucose saccharide structure caused by Fringe modulates the response of Notch to its ligands. Thus, glycosylation serves an important role in regulating Notch activity. This review focuses on the role of glycosylation in the normal functioning of the Notch pathway. As well, potential roles for glycosylation in Notch-related human diseases, and possible roles for therapeutic targeting of POFUT1 and Fringe in Notch-related human diseases, are discussed.

 

Read out more at: http://www.eurekaselect.com/node/59354/article

Article by Disease | Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

Bentham Oncology Collection| Oncology | Cervical Cancer

 

 

 

Abstract:

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, – synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity.

Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine).

Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods.

Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 μM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration.

Conclusion: the somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

 

Read out more at: http://www.eurekaselect.com/node/161359/article

Article by Disease | New Medical Strategies for Midgut Carcinoids

Bentham Oncology Collection | Oncology | CARCINOID TUMOURS

Abstract:

Patients with well-differentiated neuroendocrine tumours of the gastrointestinal tract often present with metastases and hormonal symptoms. These patients can be palliated by interventional tumour reduction and medical treatment with somatostatin analogues; no effective chemotherapy is available. Radionuclide therapy via somatostatin receptors is one new therapeutic alternative. The recognition that neuroendocrine tumours express specific receptors for growth factors and chemokines, which are of importance for tumour growth, vascularization, and spread, may open the way for new therapeutic approaches. The signalling pathways in carcinoid tumours are incompletely explored. This review summarizes potential new treatment strategies from clinical and experimental studies, e.g. inhibition of angiogenesis, targeting of growth factors or their receptors by tyrosine kinase inhibitors, interference with specific cellular pathways (mTOR, PI3K, RAS/RAF, Notch), and also inhibition of the proteasome and histone deacetylation. Combining targeted therapy with chemotherapy, or using drugs to sensitize for radionuclide therapy, may enhance the treatment outcome.

 

Read out more at: http://www.eurekaselect.com/node/71224/article

Article by Disease | Design, Synthesis, and Biological Evaluation of New Azole Derivatives as Potent Aromatase Inhibitors with Potential Effects against Breast Cancer

Bentham Oncology Collection | Oncology | Breast Cancer

 

Graphical Abstract:

Abstract:

Purpose: Some aromatase inhibitors are FDA-approved agents as first-line therapy in the treatment of endocrine-responsive breast cancer. In this study, we aimed to develop new azole derivatives with higher specificity and potency.

Methods: New aromatase inhibitors were designed by Molecular Operating Environment (MOE) software and synthesized in a one-step SN2 reaction. These compounds were characterized by melting point, 1H- and 13CNMR, elemental analysis and mass spectra. The in vitro and in vivo aromatase inhibition of these compounds was evaluated using the Estrone ELISA assay, and by measuring the inhibition of androstenedione-induced uterine hypertrophy. The selectivity of aromatase inhibition was investigated by the inhibition of ACTH stimulation on the plasma concentrations of aldosterone and cortisol.

Results: Docking simulations showed that four new azole derivatives could efficiently interact with enzyme active sites. The in vitro aromatase-inhibition assay showed that the compounds 1,3,5-tris(imidazol-1- ylmethyl)benzene (3b) and 1,3-Bis(imidazole-1- ylmethyl) benzene (3d) effectively inhibited aromatase, with IC50 values of 0.2 nM and 6.8 nM, respectively; these values were similar to known aromatase inhibitor letrozole (IC50 0.3 nM). The in vivo aromatase-inhibitory potency of compound 3b was similar to letrozole, although compound 3b acted more selectively.

Conclusion: This report introduced a new compound that can be considered as a new lead for further investigation to explore more-potent and more-selective aromatase inhibitors.

 

 

Read out more at: http://www.eurekaselect.com/node/159088/article

Article by Disease |Design, Synthesis and Anti-breast Cancer Activity of Some Novel Substituted Isoxazoles as Anti-breast Cancer Agent

Bentham Oncology Collection | Oncology | Breast Cancer

Graphical Abstract:

 

 

Abstract:

Methods: A novel series of isoxazole (S21-S30) derivatives were designed, synthesized and screened for their anticancer activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. The synthesized derivative has the ability to inhibit the growth of the human breast cancer cell line at low concentrations. In vivo anticancer activity was performed on virgin female sprague dawley rats.

Results: The result shows that compound S23 has more selectivity and marked estrogen modulator activity than the standard tamoxifen.

 

Article by Disease | New Medical Strategies for Midgut Carcinoids

Bentham Oncology Collection | Oncology Carcinoid Tumours

 

Abstract:

Patients with well-differentiated neuroendocrine tumours of the gastrointestinal tract often present with metastases and hormonal symptoms. These patients can be palliated by interventional tumour reduction and medical treatment with somatostatin analogues; no effective chemotherapy is available. Radionuclide therapy via somatostatin receptors is one new therapeutic alternative. The recognition that neuroendocrine tumours express specific receptors for growth factors and chemokines, which are of importance for tumour growth, vascularization, and spread, may open the way for new therapeutic approaches. The signalling pathways in carcinoid tumours are incompletely explored. This review summarizes potential new treatment strategies from clinical and experimental studies, e.g. inhibition of angiogenesis, targeting of growth factors or their receptors by tyrosine kinase inhibitors, interference with specific cellular pathways (mTOR, PI3K, RAS/RAF, Notch), and also inhibition of the proteasome and histone deacetylation. Combining targeted therapy with chemotherapy, or using drugs to sensitize for radionuclide therapy, may enhance the treatment outcome.

 

Read out more at: http://www.eurekaselect.com/node/71224/article

 

Article by Disease | Design and Characterization of Mucoadhesive Gelatin-Ethylcellulose Microparticles for the Delivery of Curcumin to the Bladder

Bentham Oncology Collection | Oncology | Bladder Cancer 

 

Graphical Abstract:

 

Abstract:

Background: Bladder cancer is the second type of malignant carcinoma of the urinary tract. The treatment is time-consuming and requires maintenance doses of the drug for long period of time with important side effects. Curcumin has shown evident clinical advances in the treatment of cancer. The technology of microencapsulation and the use of mucoadhesive materials can contribute to modify the delivery and improve the bioavailability of curcumin.

Objective: The aim of this study was to design and characterize mucoadhesive microparticles containing curcumin using multivariate analysis and the spray-drying technique.

Methods: A factorial design 32+1 was employed to investigate the influence of gelatin, ethylcellulose, and curcumin on size, polydispersity index, drug content and entrapment efficiency. Microparticles were also evaluated by ATR-FTIR, X-ray diffraction, antioxidant activity, in-vitro release profile, exvivo mucoadhesion performance, and in-vitro cytotoxicity.

Results: Microparticles showed non-uniform surface, mean diameter from 2.73 µm to 4.62 µm and polydispersity index from 0.72 to 1.09, according to the different combinations of the independent factors. These independent variables also had a significant effect on the drug content. The highest values of drug trapping efficiency were obtained with the highest concentration of curcumin and polymers. Formulations displayed slow drug release and important antioxidant activity. The good mucoadhesive performance of microparticles was assessed by the falling film technique. Moreover, the formulations did not display in vitro toxicity against Artemia salina and Fibroblasts LM(TK).

Conclusion: The design results were useful for developing of curcumin dosage form with good physicochemical characteristics and mucoadhesive properties for the bladder administration.

 

Find out more at: http://www.eurekaselect.com/node/161813/article

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