EDITOR’S CHOICE – Novel Findings of Anti-cancer Property of Propofol – Anti-Cancer Agents in Medicinal Chemistry

Journal: Anti-Cancer Agents in Medicinal Chemistry

Author(s): Jiaqiang Wang, Chien-shan Cheng, Yan Lu, Xiaowei Ding, Minmin Zhu, Changhong Miao*, Jiawei Chen*

Graphical Abstract:


Background: Propofol, a widely used intravenous anesthetic agent, is traditionally applied for sedation and general anesthesia.

Explanation: Recent attention has been drawn to explore the effect and mechanisms of propofol against cancer progression in vitro and in vivo. Specifically, the proliferation-inhibiting and apoptosis-inducing properties of propofol in cancer have been studied. However, the underlying mechanisms remain unclear.

Conclusion: This review focused on the findings within the past ten years and aimed to provide a general overview of propofol’s malignance-modulating properties and the potential molecular mechanisms.

Read more here: http://www.eurekaselect.com/155527/article


EDITOR’S CHOICE – Asymmetric Michael Addition Mediated by Chiral Ionic Liquids – Mini-Reviews in Organic Chemistry

Journal: Mini-Reviews in Organic Chemistry

Author(s): Yumiko Suzuki

Graphical Abstract:


Chiral ionic liquids with a focus on their applications in asymmetric Michael additions and related reactions were reviewed. The examples were classified on the basis of the mode of asymmetric induction (e.g., external induction/non-covalent interaction or internal induction/covalent bond formation), the roles in reactions (as a solvent or catalyst), and their structural features (e.g., imidazolium-based chiral cations, other chiral oniums; proline derivatives). Most of the reactions with high chiral induction are Michael addition of ketones or aldehydes to chalcones or nitrostyrenes where proline-derived chiral ionic liquids catalyze the reaction through enamine/ iminium formation. Many reports demonstrate the recyclability of ionic liquid-tagged pyrrolidines.

Read more here: http://www.eurekaselect.com/158214/article


EDITOR’S CHOICE – Mechanical and Viscoelastic Properties of In-situ Amine Functionalized Multiple Layer Graphene /epoxy Nanocomposites – Current Nanoscience

Journal: Current Nanoscience

Author(s): Pradeep Kumar Singh*, Kamal Sharma*

Graphical Abstract:



Introduction: Graphene is flat monolayer of carbon atoms (one atom thick), covalently bonded to three other atoms in tightly packed two-dimensional (2D) hexagonal single layer stable crystalline honeycomb lattice structure. In this paper, In-situ amine functionalized exfoliated graphene with multiple layers (3-6) with low defect contents and average aspect ratio upto 10 microns (average X and Y dimensions) and thickness upto 2-3 nm (average Z-direction) which have been produced with the combined effort of chemical vapor deposition (CVD) and chemical graphite exfoliation method.

Methods: This paper also focuses on the effect of the reinforcement of amine functionalized multiple graphene layers (AF-MGL) on the mechanical and visco-elastic properties of epoxy composites. AFMGL/ epoxy composites (AF-MGL/EpC) were prepared with graphene fractions ranging from 0.5 to 2.0 wt%. The four different samples were prepared using an amount of graphene as 0.0, 0.5, 1.5, and 2.0. A series of tensile three point bend tests were performed on the different AFMGL/epoxy composites. Optical and scanning electron microscopy (SEM) was used to examine the micro structural features and fractured surfaces of AF-MGL/EpC.

Results: Increased graphene content results in improved tensile strength and the modulus of an epoxy matrix when compared with the pure epoxy matrix. The 1.5 wt% AF-MGL/EpC showed an increase in tensile strength and modulus by 50.2 and 52.8% respectively. However, a shrink was noticed beyond 1.5 wt.% samples of AF-MGL/EpC composite. Moreover, an improvement of 28.8% in the storage modulus was also recorded when compared with epoxy composites.

Conclusion: The effect of the amine functional group on the mechanical and viscoelastic properties was also explored using molecular dynamics (MD) simulations and predicted results were then compared with experimental results.

Read more here: http://www.eurekaselect.com/158477/article


EDITOR’S CHOICE – Macrophage Polarization as a Therapeutic Target in Myocardial Infarction – Current Drug Targets

Journal: Current Drug Targets

Author(s): Yuanyuan Cheng, Jianhui Rong*

Graphical Abstract:



Background: Myocardial infarction is characterized by the interruption of blood flow through the heart, directly causing mortality and disability worldwide. Cardiac macrophages exhibit distinct phenotypes (e.g., M1 or M2) and functions (e.g., proinflammatory or anti-inflammatory) in response to the alterations of myocardial microenvironment, and subsequently exacerbate or resolve inflammation in the infarcted hearts. Regulation of macrophage polarization was implicated in myocardial infarction for the quality and outcome of cardiac healing.

Objective: The purpose of this review was to summarise the current understanding on the regulation of macrophage polarization in myocardial infarction and highlight the therapeutic potential of pharmacological regulators in the treatment of myocardial injury via modulating macrophage polarization.

Results: Timely control of M2/M1 ratio by endogenous mediators and pharmacological regulators should help the resolution of inflammation, promote wound healing and prevent cardiac fibrosis after myocardial infarction.

Conclusion: Macrophage polarization deserves better investigations as the therapeutic target for the development of novel drugs against myocardial injury.

Read more here: http://www.eurekaselect.com/156685/article


EDITOR’S CHOICE – Y-shaped Folic Acid-Conjugated PEG-PCL Copolymeric Micelles for Delivery of Curcumin – Anti-Cancer Agents in Medicinal Chemistry

Journal: Anti-Cancer Agents in Medicinal Chemistry

Author(s): Runliang Feng, Wenxia Zhu, Wei Chu, Fangfang Teng, Ning Meng, Peizong Deng, Zhimei Song


Background: Curcumin is a natural hydrophobic product showing anticancer activity. Many studies show its potential use in the field of cancer treatment due to its safety and efficiency. However, its application is limited due to its low water-solubility and poor selective delivery to cancer.

Objective: A Y-shaped folic acid-modified poly (ethylene glycol)-b-poly (ε-caprolactone)2 copolymer was prepared to improve curcumin solubility and realize its selective delivery to cancer.

Method and Results: The copolymer was synthesized through selective acylation reaction of folic acid with α- monoamino poly(ethylene glycol)-b-poly(ε-caprolactone)2. Curcumin was encapsulated into the copolymeric micelles with 93.71% of encapsulation efficiency and 11.94 % of loading capacity. The results from confocal microscopy and cellular uptake tests showed that folic acid-modified copolymeric micelles could improve cellular uptake of curcumin in Hela and HepG2 cells compared with folic acid-unmodified micelles. In vitro cytotoxicity assay showed that folic acid-modified micelles improved anticancer activity against Hela and HepG2 cells in comparison to folic acidunmodified micelles. Meanwhile, both drug-loaded micelles demonstrated higher activity against Hela cell lines than HepG2.
Conclusion: The research results suggested that the folic acid-modified Y-shaped copolymeric micelles should be used to enhance hydrophobic anticancer drugs’ solubility and their specific delivery to folic acid receptors-overexpressed cancer.


EDITOR’S CHOICE – Advances in Anti-Doping Analytical Approaches – Current Pharmaceutical Analysis

Journal: Current Pharmaceutical Analysis

Author(s): Xianchi Li, Peiying Zhang*

Graphical Abstract:



Background: Performance enhancement substances and methods other than exercise training and physical conditioning have become a major problem in athletic competitions. Over the last few years, there has been an increase in the number of these doping approaches used by some athletes, including pharmaceuticals, slightly modified endogenous compounds and also blood transfusions. In order to control and prevent these doping practices by athletes, World Anti-Doping Agency has stipulated several guidelines and approved various methods on the basis of reproducibility, sensitivity and adaptability. The number, design and type of doping substances are increasing on daily basis necessitating the rapid development of analytical methods to detect these substances and to prevent doping.

Objective: In this review, we address the various methodological developments in the last few years to track down the novel doping substances as well as doping methods.

Results: There have been significant advances in the area of mass spectroscopy and the associated detection devices to measure small quantities of test substance or their metabolites in body tissues and fluids. Some of the doping substances have short biological half-life but leave imprints of their action in the form of altered gene expression, protein expression or metabolism, which can be detected by OMICs technologies.

Conclusion: The rapid advance in biological instrumentation and our understanding of the molecular basis of the actions of doping substances have paved the way to enforce ‘true play’ in athletic competitions. But this is an incessant and a continuous process as long as the doping practices continue.

Read more here: http://www.eurekaselect.com/151469/article



EDITOR’S CHOICE – Cytotoxicity of Silver Nanoparticles Against Bacteria and Tumor Cells – Current Protein & Peptide Science

Journal: Current Protein & Peptide Science

Author(s): Tianyuan Shi, Xuesong Sun*, Qing-Yu He


With the rapid increase of multiple drug-resistant bacteria, silver nanoparticles (AgNPs) with broad-spectrum antibacterial activities have been widely applied in the treatment of bacterial infection. Meanwhile, AgNPs also have anticancer activities against different cell lines. The toxic effects of AgNPs depend on concentration, size, shape, coated materials and surrounding environments. In order to better understand the antibacterial and antitumor effects of AgNPs, various investigations have been carried out to uncover the molecular mechanism of action. This review summarizes the recent studies on the action mechanisms of AgNPs related to their antibacterial activities including collapsing cell walls, inducing reactive oxygen species, inhibiting aerobic respiration and damaging DNA and their antitumor effects including impairing mitochondria, blocking cell cycle, and activating apoptosis. In these investigations, the systematic approaches have not been extensively applied. Increasingly matured omics techniques including genomics, transcriptomic, translatomics and proteomics should be more widely explored to provide the comprehensive views of the cytotoxic effects of AgNPs to bacteria and tumor cells and thus globally illustrate the molecular mechanisms of the cytotoxicity, promoting the better medical application of AgNPs in the future.

Read more here: http://www.eurekaselect.com/147155/article


EDITOR’S CHOICE – Gamma-Decanolactone Improves Biochemical Parameters Associated with Pilocarpine-Induced Seizures in Male Mice – Current Molecular Pharmacology

Journal: Current Molecular Pharmacology

Author(s):  Pricila Pfluger, Gabriela Gregory Regner, Vanessa Rodrigues Coelho, Lucas Lima da Silva,Leopoldo Nascimento, Cassiana Macagnan Viau, Regis Adriel Zanette, Cleonice Hoffmann, Jaqueline Nascimento Picada, Jenifer Saffi, Patricia Pereira*

Graphical Abstract:



Background and Objective: Gamma-decanolactone (GD) is a monoterpene effective against seizures induced by pentylenetetrazole. The mechanism of action of GD is likely to be via glutamate antagonism. GD also inhibits intracellular reactive oxygen species (ROS) generation and the lipopolysaccharide-induced expression of inducible nitric oxide synthase (iNOS) and tumor necrosis factor-alpha (TNF-α) in vitro. Considering the neuropharmacological profile of GD studied so far, we investigated the effect of intraperitoneal administration of GD 100 and 300 mg/kg on pilocarpine (PIL)-induced status epilepticus (SE) in mice.

Methods: GD was administered 30 min before PIL. Behavioral (latency to first seizure and the percentage of clonic forelimb seizures), biochemical, and oxidative stress parameters were evaluated. DNA damage in the cerebral cortex of mice was assessed using the comet assay and mutagenic activity of GD was evaluated using Salmonella/microsome assay in TA100, TA98, TA97a, TA102, and TA1535 strains, with and without metabolic activation (S9 mix).

Results: The behavioral results showed that only the latency to the first clonic seizure increased in the groups treated with GD 300 mg/kg, but not when the animals received GD 100 mg/kg. Both GD doses were able to increase superoxide dismutase and catalase activities, inducing a decrease in ROS and nitrite production and in DNA damage in the cerebral cortex. GD was not able to induce base pair substitution and frameshift mutations in the absence or in the presence of metabolic activation.

Conclusion: These findings demonstrate that GD does not improve behavioral parameters in the PIL model, but it was able to protect seizure-related oxidative stress and DNA damage in mice, without inducing gene mutations.

Read more here: http://www.eurekaselect.com/156031/article

EDITOR’S CHOICE – Role of Zebrafish fhl1A in Satellite Cell and Skeletal Muscle Development – Current Molecular Medicine

Journal: Current Molecular Medicine

Author(s):  F. Chen, W. Yuan, X. Mo, J. Zhuang, Y. Wang, J. Chen, Z. Jiang, X. Zhu, Q. Zeng, Y. Wan, F. Li, Y. Shi, L. Cao, X. Fan, S. Luo, X. Ye, Y. Chen, G. Dai, J. Gao, X. Wang, H. Xie*, P. Zhu*, Y. Li*, X. Wu


Background: Four-and-a-half LIM domains protein 1 (FHL1) mutations are associated with human myopathies. However, the function of this protein in skeletal development remains unclear.

Methods: Whole-mount in situ hybridization and embryo immunostaining were performed.

Results: Zebrafish Fhl1A is the homologue of human FHL1. We showed that fhl1A knockdown causes defective skeletal muscle development, while injection with fhl1A mRNA largely recovered the muscle development in these fhl1A morphants. We also demonstrated that fhl1A knockdown decreases the number of satellite cells. This decrease in satellite cells and the emergence of skeletal muscle abnormalities were associated with alterations in the gene expression of myoD, pax7, mef2ca and skMLCK. We also demonstrated that fhl1A expression and retinoic acid (RA) signalling caused similar skeletal muscle development phenotypes. Moreover, when treated with exogenous RA, endogenous fhl1A expression in skeletal muscles was robust. When treated with DEAB, an RA signalling inhibitor which inhibits the activity of retinaldehyde dehydrogenase, fhl1A was downregulated.

Conclusion: fhl1A functions as an activator in regulating the number of satellite cells and in skeletal muscle development. The role of fhl1A in skeletal myogenesis is regulated by RA signaling.

Read more here: http://www.eurekaselect.com/160312/article

EDITOR’S CHOICE – Up-regulation of DMN Connectivity in Mild Cognitive Impairment Via Network-based Cognitive Training – Current Alzheimer Research

Journal: Current Alzheimer Research

Author(s): Matteo De Marco, Francesca Meneghello, Cristina Pilosio, Jessica Rigon, Annalena Venneri*


Background: Previous work designed a network-based protocol of cognitive training. This programme exploits a mechanism of induced task-oriented co-activation of multiple regions that are part of the default mode network (DMN), to induce functional rewiring and increased functional connectivity within this network.

Objective: In this study, the programme was administered to patients with a diagnosis of mild cognitive impairment to test its effects in a clinical sample.

Method: Twenty-three patients with mild cognitive impairment (mean age: 73.74 years, standard deviation 5.13, female/male ratio 13/10) allocated to the experimental condition, underwent one month of computerised training, while fourteen patients (mean age: 73.14 years, standard deviation 6.16, female/ male ratio 7/7) assigned to the control condition underwent a regime of intense social engagement. Patients were in the prodromal stage of Alzheimer’s disease (AD) as confirmed by clinical follow ups for at least two years. The DMN was computed at baseline and retest, together with other, control patterns of connectivity, grey matter maps and neuropsychological profiles.

Results: A condition-by-timepoint interaction indicating increased connectivity triggered by the programme was found in left parietal DMN regions. No decreases as well as no changes in the other networks or morphology were found. Although between-condition cognitive changes did not reach statistical significance, they correlated positively with changes in DMN connectivity in the left parietal region, supporting the hypothesis that parietal changes were beneficial.

Conclusion: This programme of cognitive training up-regulates a pattern of connectivity which is pathologically down-regulated in AD. We argue that, when cognitive interventions are conceptualised as tools to induce co-activation repeatedly, they can lead to clinically relevant improvements in brain functioning, and can be of aid in support of pharmacological and other interventions in the earliest stages of AD.

Read more here: http://www.eurekaselect.com/158224/article