EDITOR’S CHOICE – Neoflavonoids as Prospective Compounds Against Parasitic Neglected Tropical Infections and Human Immunodeficiency Virus – Current Bioactive Compounds

Journal: Current Bioactive Compounds 

Author(s): Gláucio B. Saldanha, George L.S. Oliveira, José C.C.L. da Silva, Maria C.P. Oliveira, Ana P.S.C.L. da Silva*, Juceni P. de Lima David

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Abstract:

Background: Neoflavonoids comprise a group of compounds that have a C6-C3-C6 carbon skeleton and that naturally occur in higher plants from families Clusiaceae, Leguminosae, Rubiaceae, Passifloraceae, Asteraceae and Rutaceae.

Objective: Neoflavonoids have drawn great interest lately due to their pharmacological and biochemical properties found in vitro and in vivo studies, which is attributed to the pattern of substitutions found in their basic chemical structure.

Methods: This review was prepared by analyzing articles selected from Science Direct, Scopus, Pub Med, Web of Science and SciFinder.
Results: Among other pharmacological activities, in vitro and in vivo studies have highlighted these compounds as promising bioactive molecules in the treatment of some parasitic neglected tropical infections (NTIs) such as malaria, leishmaniasis and American trypanosomiasis (Chagas Disease). Neoflavonoids have also showed activity against HIV-1 (human immunodeficiency virus type 1), and have been used to develop new molecules for the treatment of HIV/AIDS.
Conclusion: Therefore, a more intensive research of neoflavonoids can provide inputs to discover and develop alternative therapies from new bioactive molecules. Thus, this review summarizes the results of studies involving neoflavonoids and their derivatives with therapeutic implications in the treatment of NTIs and HIV.

EDITOR’S CHOICE – Differences in Relative Levels of 88 microRNAs in Various Regions of the Normal Adult Human Brain – MicroRNA

Journal: MicroRNA

Author(s): Elena V. Filatova, Anelya Alieva, Maria I. Shadrina, Petr A. Slominsky.

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Abstract:

Aim of Study: Since the discovery of microRNAs (miRNAs) in the 1990s, our knowledge about their biology has grown considerably. The increasing number of studies addressing the role of miRNAs in development and in various diseases emphasizes the need for a comprehensive catalogue of accurate sequence, expression and conservation information regarding the large number of miRNAs proposed recently in all organs and tissues. The objective of this study was to provide data on the levels of miRNA expression in 15 tissues of the normal human brain.

Materials and Methods: We conducted an analysis of the relative levels of 88 of the most abundantly expressed and best characterized miRNA derived postmortem from well-characterized samples of various regions of the brains from five normal individuals.

Results: The cluster analysis revealed some differences in the relative levels of these miRNAs among the brain regions studied. Such diversity can be explained by different functioning of these brain regions.
Conclusion: We hope that the data from the current study are a resource that will be useful to our colleagues in this exciting field, as more hypotheses will be generated and tested with regard to small noncoding RNA in the human brain in healthy and disease states.

 

EDITOR’S CHOICE – Integration of DNA Methylation Data and Gene Expression Data for Prostate Adenocarcinoma: A Proof of Concept – Current Bioinformatics

Journal: Current Bioinformatics

Author(s): Arpit Singh, Razia Rahman, Yasha Hasija

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Abstract:

Background: Epigenetics is gaining rapid recognition as it accounts for heritable changes that do not involve changes in the coding sequence, but influences change in gene expressions. DNA methylation is the most extensively studied epigenetic mechanism and has been observed to play a significant role in gene regulation and silencing process.

Objective: In our present work, we focused on understanding the relationship between DNA methylation and gene expression. As a proof of concept, Prostate Adenocarcinoma (PRAD), the second leading cause of death in men, was extensively studied to unravel the epigenetic abnormalities associated with disease pathogenesis which may contribute to better diagnosis and prevention of prostate cancer.

Method: DNA methylation data (level 1) and Gene expression data (level 3) was taken from The Cancer Genome Atlas (TCGA). A total of 36 samples comprising of 18 normal samples and 18 tumor samples were collected from a batch of 184 and matched with tumor samples and normal samples, respectively. The differentially methylated regions were identified and statistical analysis was carried out for the gene expression data amongst the normal and tumor samples. Further, functional enrichment analysis and pathway analysis were carried out for the filtered genes.

Results: Our analysis indicated 453 differentially methylated regions with p-value < 0.05, FDR (false discovery rate) value < 0.05 and beta value (methylation) > 0.2. The integration of gene expression data with methylation data resulted in 180 significant correlations from which 112 genes were filtered under stringent conditions. Out of these 112 genes, 74 genes were filtered through visual inspection of results and their functional enrichment analysis resulted in total 27 clusters with a maximum enrichment score of ~1.86.

Conclusion: The genes “GSTP1” and “FGFR2” were present in our prioritized filtered significant correlations, and it was discovered that these genes were known to play a primary role in prostate cancer pathway and progression. Therefore, this approach may help to prioritize other novel genes and suggest their involvement in the prostate cancer pathway

 

Read more here: http://www.eurekaselect.com/151165

Editor’s Choice – PEGylated Liposomes of Meloxicam: Optimization by Quality by Design, in vitro Characterization and Cytotoxicity Evaluation – Pharmaceutical Nanotechnology

Journal: Pharmaceutical Nanotechnology

Author(s): Jessy Shaji*, Ipshita Menon

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Abstract:

Background: Chemoprevention is a strategy which uses drugs which are traditionally not used as anti-cancer drugs; however, they prevent the carcinogenesis. Meloxicam (MLX) is traditionally used as a non-steroidal anti-inflammatory drug (NSAID), but it has been proven to have activity against colorectal cancer. Subsequently MLX seems to be a likely candidate to be utilized in the chemopreventive therapy of colorectal cancer. However, MLX poses shortcomings with respect to its dose required to elicit cytotoxicity. To improve the formulation, we used Quality by design (QbD) for optimization. QbD is a method that employs quality-improving scientific methods that build quality into the formulation by isolating the factors which affect the critical quality attributes of the formulation. The aim of the present study was to utilize the principles of QbD to formulate MLX into a formulation so as to exploit its potential to the fullest.

Methods: Conventional (CLM) and PEGylated liposomes (MPL) of MLX was prepared using hydrogenated soya phosphatidylcholine (HSPC), distearyl phosphatidyl glycerol (DSPG), cholesterol and 1, 2-distearoyl- phosphatidylethanolamine-methyl-polyethyleneglycol conjugate-2000 sodium salt (MPEG 2000 DSPE). The liposomes were prepared using thin film hydration method. The optimization of the formulation was done by employing the QbD approach. The formulation was optimized on the basis of the factors which were affecting the critical quality attributes (CQAs) such as particle size and entrapment efficiency. The final optimized formulation was characterized by assessing the particle size, percent entrapment efficiency, zeta potential, long-term stability, morphology, in vitro release and in vitro cytotoxic activity.

Result: PEGylated liposomes having high percent entrapment efficiency (87.25 %±0.72%) could be obtained. The entrapment of drug in the liposomes was confirmed using Differential Scanning Calorimetry (DSC), Fourier Transform Infrared spectroscopy (FT-IR) and Powder X-Ray diffraction (PXRD) studies. The mean particle size of the liposomes was 113 nm±67nm and they were found to exhibit sustained release profile (56.59 %±0. 43% drug in 24h). The Small Angle Neutron Scattering (SANS) analysis revealed that the liposomes were uniform sized LUVs (nm) and were spherical in shape. The shape of the liposomes was further confirmed by transmission electron microscopy (TEM). Long term stability study indicated that the formulation was stable for three months. Sulphorhodamine B (SRB) cytotoxicity assay was carried out in HT-29 cell to prove that the PEGylated liposomal formulations had higher cytotoxicity than the conventional liposomes after 48 hours of incubation.
Conclusion: The study affirmed that MLX loaded PEGylated liposomes had superior in vitro cytotoxicity as compared to the free drug as well as conventional liposomes. QbD resulted in the fabrication of a stable liposomal formulation with all the desirable characteristics. Hence, MLX loaded PEGylated liposomes can be considered to be a promising system for the delivery of MLX.

Read more here: http://www.eurekaselect.com/152024

Editor’s Choice – Localized Scleroderma: A Clinical Review – Current Rheumatology Reviews

Journal: Current Rheumatology Reviews

Author(s): Mark Tratenberg, Farrah Gutwein, Varuni Rao, Kirk Sperber, Amy Wasserrman, Julia Ash

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Abstract:

Localized scleroderma (LS) is characterized by excessive collagen deposition leading to thickening of the dermis, subcutaneous tissue or both. The outcome for most patients with localized scleroderma is directly related to the type and stage of the affected tissue. The major challenge for untreated patients is not increased mortality risk, rather deformity and growth defects from skin, muscle and bone abnormalities. Treatment is individualized to type and stage of the lesion and may include pharmacologic and non-pharmacologic therapies. Among the pharmacologic modalities, methotrexate with systemic glucocorticoids is currently the mainstay of treatment. More controlled trials are needed to determine the length of treatment and the maintenance dose of this combination therapy.

 

Read more here: http://www.eurekaselect.com/145424

Editor’s Choice – Advances and Perspectives in Cancer Nanotherapy – Current Nanomedicine

Journal: Current Nanomedicine

Author(s): Costas Demetzos, Natassa Pippa, Stergios Pispas.

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Abstract:

Background: Cancer nanotherapy integrate efficacious molecules that otherwise could not be used because of their high toxicity and exploit multiple mechanisms of actions (e.g. multifunctional gels, functional polymers, hybrid nanoparticles). The aim of this review is to contemplate the designed and developed nanoparticulate systems that exhibit a benefit in cancer nanotherapy strongly related with the properties of the nanoplatforms formulation.

Method: Systemic search and review of papers regarding cancer nanotherapy took place via MedLine and abstract presentations of international conferences.

Results: The recent advances in the development of self-assembled structures of lipids- (i.e. liposomes, niosomes, etc.) and of polymers- (micelles, polymersomes, dendrimers, polymeric nanoparticles, hydrogels, etc.) as well as clinical perspectives will be discussed on the basis of pharmaceutical nanotechnology considerations, and on their in vitro and in vivo evaluation. Chimeric/Mixed nanoplatforms that are composed at least of two different in nature biomaterials (i.e. phospholipids and polymers) can be considered as new technological outcomes in cancer nanotherapy that could be able to deliver anticancer drugs to specific tissues.

Conclusion: They can improve the pharmacokinetics/pharmacodynamics behavior of antitumor molecules, affect their total bioavailability and provide innovative delivery behavior due to their nanotechnological profile.

Read more here: http://www.eurekaselect.com/151515

 

 

Editor’s Choice – The Impact of Cancer and its Treatment on the Growth and Development of the Pediatric Patient – Current Pediatric Reviews

Journal: Current Pediatric Reviews

Author(s): Sarah Brand, Joanne Wolfe, Chase Samsel.

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Abstract:

Background: Cancer treatment can have profound effects on the growth and development of pediatric patients. Different models of psychosocial development and behavioral treatment approaches aid children receiving medical treatment. Providing education, anticipatory guidance, and individualized support to child and their families is a psychosocial standard.

Objective: Clarify the different models of psychosocial development and applicable psychosocial interventions to better prepare and tailor cancer treatment to pediatric patients.

Methods: Authors reviewed existing evidenced-based literature in oncology, psychology, developmental, and psychiatric while drawing on case examples and expert knowledge to illustrate the impact of cancer treatment on pediatric patients, analyze developmentally individualized needs, and describe facilitative interventions.
Result: Pediatric patients of all ages cope and adjust better to all phases of treatment when their care is delivered in a developmentally-informed and psychosocially thoughtful way.
Conclusion: Providers can comprehensively prepare their patients and families for treatment better by utilizing a psychosocially- and developmentally-informed framework while meeting individualized unique needs of patients. An integrated multidisciplinary psychosocial support team is facilitative in anticipating and meeting the needs of pediatric cancer patients and has recently become a psychosocial standard of care.

Editor’s Choice – Differences in Relative Levels of 88 microRNAs in Various Regions of the Normal Adult Human Brain – MicroRNA

Journal: MicroRNA

Author(s): Elena V. Filatova, Anelya Alieva, Maria I. Shadrina, Petr A. Slominsky.

Graphical Abstract:

 

Abstract:

Aim of Study: Since the discovery of microRNAs (miRNAs) in the 1990s, our knowledge about their biology has grown considerably. The increasing number of studies addressing the role of miRNAs in development and in various diseases emphasizes the need for a comprehensive catalogue of accurate sequence, expression and conservation information regarding the large number of miRNAs proposed recently in all organs and tissues. The objective of this study was to provide data on the levels of miRNA expression in 15 tissues of the normal human brain.

Materials and Methods: We conducted an analysis of the relative levels of 88 of the most abundantly expressed and best characterized miRNA derived postmortem from well-characterized samples of various regions of the brains from five normal individuals.

Results: The cluster analysis revealed some differences in the relative levels of these miRNAs among the brain regions studied. Such diversity can be explained by different functioning of these brain regions.
Conclusion: We hope that the data from the current study are a resource that will be useful to our colleagues in this exciting field, as more hypotheses will be generated and tested with regard to small noncoding RNA in the human brain in healthy and disease states.

 

Editor’s Choice – Model Validity in Nanoimmunosafety: Advantages and Disadvantages of In vivo vs In vitro Models, and Human vs Animal Models – Current Bionanotechnology

Journal: Current Bionanotechnology

Author(s): Diana Boraschi, Paola Italiani.

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Abstract:

The thorough understanding of the interaction between nanomaterials and the immune system is the starting point both for nanomaterial exploitation in nanomedicine and for the implementation of an effective regulatory framework concerning nanosafety for human health and the environment. In this context, the use of valid models, in vitro and in vivo, is central for assessing both the positive and the detrimental effects of nanomaterials, thereby predicting their possible risks for human and environmental health. Thus, predicting models are sought that allow us on one side defining hazard posed by nanomaterials, and therefore implementing safety regulation and safe-by-design nanotechnologies, and on the other side exploiting nanomaterials for more effective therapeutic and preventive medical strategies. Here, we consider the advantages and limitation of the current in vitro and in vivo human and animal models, and the appropriateness of their use for assessing the effects of nanomaterials on immunity.

Read more here: http://www.eurekaselect.com/142770

Editor’s Choice – A Review on Advances in Organoborane-Chemistry – Current Organic Synthesis

Journal: Current Organic Synthesis

Author(s): Paranjeet Kaur, Gopal L. Khatik, Surendra Kumar Nayak.

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Abstract:

Background: In the past decades, the hydroboration reaction was serendipitously discovered which occurred by the facile addition of diborane to alkenes and alkynes. Hydroboration reactions produce organoboranes. The organoboranes have marked a new era in the field of organic chemistry because they are versatile chemical intermediates that are readily available to chemists.

Objective: The review focuses on recent advancements in organoborane reagents in asymmetric synthesis. We searched the scientific database using relevant keywords such an asymmetric hydroboration, organoboranes etc. The quality research papers were included in the review which discusses the asymmetric synthesis via organoborane compounds.

Conclusion: The development of organoborane compounds increased remarkably in few years after hydroboration reaction discovered. Later on, new selective hydroboration agents were developed (for example thexylborane, disiamylborane, dipinylborane, 9-borabicyclenonane, and diisopinocamphylborane which have proven valuable in syntheses of organic compounds with new carbon-carbon bonds. H.C Brown and his co-workers established various procedures to synthesize asymmetric compounds with high enantiomeric excess (ee). There are many different types of strategies in the asymmetric syntheses, but asymmetric syntheses via chiral organoborane reagents have proven to be truly general and have been used to achieve reactions resulting in excellent ee. This review focuses on the advancement.