scholarly journals Resveratrol in Cancer Patients: From Bench to Bedside

2020 ◽  
Vol 21 (8) ◽  
pp. 2945 ◽  
Author(s):  
Massimiliano Berretta ◽  
Alessia Bignucolo ◽  
Raffaele Di Francia ◽  
Francesco Comello ◽  
Gaetano Facchini ◽  
...  
Keyword(s):  
Cancer Patients ◽  
Red Wines ◽  
Red Rice ◽  
Biological Targets ◽  
Physico Chemical ◽  
Pharmacokinetic Properties ◽  
Clinical Models ◽  
Vegetables And Fruits ◽  
Potential Use ◽  
Reactive Molecule

Resveratrol (3,5,4′-trihydroxystilbene) is a natural phytoalexin that accumulates in several vegetables and fruits like nuts, grapes, apples, red fruits, black olives, capers, red rice as well as red wines. Being both an extremely reactive molecule and capable to interact with cytoplasmic and nuclear proteins in human cells, resveratrol has been studied over the years as complementary and alternative medicine (CAM) for the therapy of cancer, metabolic and cardiovascular diseases like myocardial ischemia, myocarditis, cardiac hypertrophy and heart failure. This review will describe the main biological targets, cardiovascular outcomes, physico-chemical and pharmacokinetic properties of resveratrol in preclinical and clinical models implementing its potential use in cancer patients.

Treatment and secondary prevention of venous thromboembolism in cancer patients

2012 ◽  
Vol 03 (03) ◽  
pp. 121-125
Author(s):  
I. Pabinger ◽  
C. Ay
Keyword(s):  
Clinical Trials ◽  
Venous Thromboembolism ◽  
Cancer Patients ◽  
Oral Anticoagulants ◽  
Factor Xa ◽  
New Oral Anticoagulants ◽  
Phase Iii ◽  
Patients With Cancer ◽  
Potential Use

SummaryCancer is a major and independent risk factor of venous thromboembolism (VTE). In clinical practice, a high number of VTE events occurs in patients with cancer, and treatment of cancerassociated VTE differs in several aspects from treatment of VTE in the general population. However, treatment in cancer patients remains a major challenge, as the risk of recurrence of VTE as well as the risk of major bleeding during anticoagulation is substantially higher in patients with cancer than in those without cancer. In several clinical trials, different anticoagulants and regimens have been investigated for treatment of acute VTE and secondary prophylaxis in cancer patients to prevent recurrence. Based on the results of these trials, anticoagulant therapy with low-molecular-weight heparins (LMWH) has become the treatment of choice in cancer patients with acute VTE in the initial period and for extended and long-term anticoagulation for 3-6 months. New oral anticoagulants directly inhibiting thrombin or factor Xa, have been developed in the past decade and studied in large phase III clinical trials. Results from currently completed trials are promising and indicate their potential use for treatment of VTE. However, the role of the new oral thrombin and factor Xa inhibitors for VTE treatment in cancer patients still has to be clarified in further studies specifically focusing on cancer-associated VTE. This brief review will summarize the current strategies of initial and long-term VTE treatment in patients with cancer and discuss the potential use of the new oral anticoagulants.

Homologation: A Versatile Molecular Modification Strategy to Drug Discovery

2019 ◽  
Vol 19 (19) ◽  
pp. 1734-1750 ◽  
Author(s):  
Lídia M. Lima ◽  
Marina A. Alves ◽  
Daniel N. do Amaral
Keyword(s):  
Protein Structure ◽  
Homologous Series ◽  
Molecular Conformation ◽  
Chemical Properties ◽  
Lead Optimization ◽  
Pharmacokinetic Property ◽  
Molecular Modification ◽  
Physico Chemical ◽  
Pharmacokinetic Properties ◽  
Lead Identification

Homologation is a concept introduced by Gerhard in 1853 to describe a homologous series in organic chemistry. Since then, the concept has been adapted and used in medicinal chemistry as one of the most important strategies for molecular modification. The homologation types, their influence on physico-chemical properties and molecular conformation are presented and discussed. Its application in lead-identification and lead optimization steps, as well as its impact on pharmacodynamics/pharmacokinetic properties and on protein structure is highlighted from selected examples. <p> • Homologation: definition and types <p> • Homologous series in nature <p> • Comparative physico-chemical and conformational properties <p> • Application in lead-identification and lead-optimization <p> • Impact on pharmacodynamic property <p> • Impact on pharmacokinetic property <p> • Impact on protein structure <p> • Concluding remarks <p> • Acknowledgment <p> • References

scholarly journals MRI-Based Radiomics Analysis for the Pretreatment Prediction of Pathologic Complete Tumor Response to Neoadjuvant Systemic Therapy in Breast Cancer Patients: A Multicenter Study

Cancers ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 2447
Author(s):  
Renée W. Y. Granzier ◽  
Abdalla Ibrahim ◽  
Sergey P. Primakov ◽  
Sanaz Samiei ◽  
Thiemo J. A. van Nijnatten ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Patients ◽  
Systemic Therapy ◽  
Tumor Response ◽  
Added Value ◽  
Breast Cancer Patients ◽  
Neoadjuvant Systemic Therapy ◽  
Clinical Models ◽  
Combined Models ◽  
Complete Tumor

This retrospective study investigated the value of pretreatment contrast-enhanced Magnetic Resonance Imaging (MRI)-based radiomics for the prediction of pathologic complete tumor response to neoadjuvant systemic therapy in breast cancer patients. A total of 292 breast cancer patients, with 320 tumors, who were treated with neo-adjuvant systemic therapy and underwent a pretreatment MRI exam were enrolled. As the data were collected in two different hospitals with five different MRI scanners and varying acquisition protocols, three different strategies to split training and validation datasets were used. Radiomics, clinical, and combined models were developed using random forest classifiers in each strategy. The analysis of radiomics features had no added value in predicting pathologic complete tumor response to neoadjuvant systemic therapy in breast cancer patients compared with the clinical models, nor did the combined models perform significantly better than the clinical models. Further, the radiomics features selected for the models and their performance differed with and within the different strategies. Due to previous and current work, we tentatively attribute the lack of improvement in clinical models following the addition of radiomics to the effects of variations in acquisition and reconstruction parameters. The lack of reproducibility data (i.e., test-retest or similar) meant that this effect could not be analyzed. These results indicate the need for reproducibility studies to preselect reproducible features in order to properly assess the potential of radiomics.

Potential clinical applications of circulating cell-free DNA in ovarian cancer patients

2018 ◽  
Vol 20 ◽  
Author(s):  
Ana Barbosa ◽  
Ana Peixoto ◽  
Pedro Pinto ◽  
Manuela Pinheiro ◽  
Manuel R. Teixeira
Keyword(s):  
Ovarian Cancer ◽  
Cancer Patients ◽  
Liquid Biopsy ◽  
Clinical Applications ◽  
Epigenetic Alterations ◽  
Cell Free Dna ◽  
Non Invasive ◽  
Free Dna ◽  
Potential Use ◽  
Circulating Cell Free Dna

AbstractCirculating cell-free DNA (cfDNA) consists of small fragments of DNA that circulate freely in the bloodstream. In cancer patients, a fraction of cfDNA is derived from tumour cells, therefore containing the same genetic and epigenetic alterations, and is termed circulating cell-free tumour DNA. The potential use of cfDNA, the so-called ‘liquid biopsy’, as a non-invasive cancer biomarker has recently received a lot of attention. The present review will focus on studies concerning the potential clinical applications of cfDNA in ovarian cancer patients.

Treatment and secondary prevention of venous thrombo -embolism in cancer patients

2012 ◽  
Vol 32 (02) ◽  
pp. 139-144 ◽  
Author(s):  
I. Pabinger ◽  
C. Ay
Keyword(s):  
Clinical Trials ◽  
Cancer Patients ◽  
Oral Anticoagulants ◽  
Initial Period ◽  
Factor Xa ◽  
Secondary Prophylaxis ◽  
Phase Iii ◽  
Patients With Cancer ◽  
Potential Use

SummaryCancer is a major and independent risk factor of venous thromboembolism (VTE). In clinical practice, a high number of VTE events occurs in patients with cancer, and treatment of cancer-associated VTE differs in several aspects from treatment of VTE in the general population. However, treatment in cancer patients remains a major challenge, as the risk of recurrence of VTE as well as the risk of major bleeding during anticoagulation is substantially higher in patients with cancer than in those without cancer. In several clinical trials, different anticoagulants and regimens have been investigated for treatment of acute VTE and secondary prophylaxis in cancer patients to prevent recurrence. Based on the results of these trials, anticoagulant therapy with low-molecular-weight heparins (LMWH) has become the treatment of choice in cancer patients with acute VTE in the initial period and for extended and long-term anticoagulation for 3–6 months. New oral anti-coagulants directly inhibiting thrombin or factor Xa, have been developed in the past decade and studied in large phase III clinical trials. Results from currently completed trials are promising and indicate their potential use for treatment of VTE also in cancer patients. However, the role of the new oral thrombin and factor Xa inhibitors for VTE treatment in cancer patients still has to be clarified in further studies specifically focusing on cancer-associated VTE. This brief review will summarize the current strategies of initial and long-term VTE treatment in patients with cancer and discuss the potential use of the new oral anticoagulants.

scholarly journals Pharmacokinetic Profiling and Simultaneous Determination of Thiopurine Immunosuppressants and Folic Acid by Chromatographic Methods

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3469 ◽  
Author(s):  
Brusač ◽  
Jeličić ◽  
Amidžić Klarić ◽  
Nigović ◽  
Turk ◽  
...  
Keyword(s):  
Folic Acid ◽  
Fixed Dose ◽  
Reliable Determination ◽  
Pharmaceutical Ingredients ◽  
Physico Chemical ◽  
Pharmacokinetic Properties ◽  
On Line ◽  
Inflammatory Bowel ◽  
Tablet Formulations

With the increase in the number of medicines patients have to take, there has been a rapid rise of fixed-dose combinations (FDCs) in the last two decades. Prior to FDC development, pharmacokinetic properties of active pharmaceutical ingredients (APIs) have to be evaluated, as well as methods for their determination developed. So as to increase patient compliance in inflammatory bowel disease, three novel FDCs of thiopurine immunosuppressants and folic acid are proposed; physico-chemical and pharmacokinetic properties such as hydrophobicity, lipophilicity and plasma protein binding of all APIs are evaluated. Moreover, experimental results of different properties are compared to those computed by various on-line prediction platforms so as to evaluate the viability of the in silico approach. A simultaneous method for their determination is developed, optimized, validated and applied to commercial tablet formulations. The method has shown to be fast, selective, accurate and precise, showing potential for reliable determination of API content in proposed FDCs during its development.

scholarly journals Stepwise linear discriminant analysis to differentiate Spanish red wines by their Protected Designation of Origin or category using physico-chemical parameters

OENO One ◽  
2020 ◽  
Vol 54 (1) ◽  
pp. 86-99
Author(s):  
Rubén Del Barrio Galán ◽  
Marta Bueno Herrera ◽  
Pedro López de la Cuesta ◽  
Silvia Pérez-Magariño
Keyword(s):  
Discriminant Analysis ◽  
Linear Discriminant Analysis ◽  
Average Molecular Weight ◽  
Red Wines ◽  
Grape Variety ◽  
Chemical Parameters ◽  
Good Discrimination ◽  
Linear Discriminant ◽  
Protected Designation Of Origin ◽  
Physico Chemical

Aim: The aim of this work was to determine the physico-chemical variables that differentiating red wines from the “Castilla y León” Spanish region by their Protected Designation of Origin (PDO) and wine category ("young", “oak”, “crianza”, or “reserve”).Methods and results: A total of 135 commercial red wines from four Spanish PDOs in the region of Castilla and León were analysed. Forty physico-chemical parameters, related to classical enological parameters, phenolic and polysacharidic composition, and content of higher alcohols were evaluated. Differences in physico-chemical composition were found in red wines from different PDOs and different categories. Stepwise linear discriminant analysis (SLDA) was applied to find a linear combination of the physico-chemical variables that separate and classify the red wines according to the PDO or category. One SLDA model selected 15 physico-chemical variables that allowed for good discrimination and classification of the wines from different PDOs. The SLDA model selected seven variables for wine category differentiation, but only allowed for good discrimination between young wines and aged wines (“crianza” and “reserve”).Conclusions: The variables that contributed most to the separation of Tempranillo red wines were total polyphenols, total tannins, and absorbance values at 230 nm and 280 nm. The polysaccharides with an average molecular weight of 10 kDa, flavanols, stilbenes and 2-methyl-1-butanol were those most associated with the differentiation of the wines elaborated with the Mencía grape variety. The percentage of polymeric anthocyanins and absorbance at 230 nm could be proposed as good indicators for aged wines, and total tannins for young wines.Significance and impact of the study: This study provides improved knowledge of the physico-chemical variables that could be used as markers of the origin of wines and/or the grape variety (Tempranillo and Mencía) and that allow differentiating young wines from those aged for a long time.

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