bluuebunny/crossref_metadata_2025 huggingface dataset:
Student-led seminars as an active learning strategy to enhance English as a foreign language procrastinating students’ achievement
Authors: Al-Amri Majid
Published: August 2018

Research has demonstrated that high percentages of undergraduate college students self-report they engage in academic procrastination which has significant adverse effects on academic progress with relative consistency. The present study was designed to help English as a foreign language (EFL) procrastinators study on a regular basis, and also to extend the learning of the high achievers. To do so, seventy English as a Foreign Language students in the study were classified by level of procrastination based on scores on the Procrastination Scale (Tuckman, 1991). Half of the students experienced the student-led seminars condition; the other half experienced the assignments condition. Although the student-led seminars condition produced significantly higher scores overall on a final achievement examination than the outline condition did, a significant interaction between condition and student procrastination level reflected an almost 14% advantage for the student-led seminars condition among high procrastinators. There was almost no difference between student-led seminars and assignments conditions for medium and low procrastinators. In addition, the qualitative data revealed high levels of satisfaction among students in the experimental group regarding the seminars and the instructor, as well as the perceived amount of new information learned.

ﻟﻘد أﺛﺑﺗ ت اﻟ د ر ا ﺳ ﺎ ت اﻟ ﺳ ﺎﺑﻘﺔ ا ر ﺗﻔﺎ ع ﻧ ﺳ ﺑ ﺔ اﻟﺗ ﺳ وﯾ ف ا ﻷ ﻛﺎ دﯾ ﻣ ﻲ ﻟ د ى ط ﻼ ب اﻟ ﺟ ﺎ ﻣﻌﺎ ت و ﺗﺄﺛﯾ ر ه اﻟ ﺳ ﻠﺑ ﻲ ﻋ ﻠ ﻰ ﺗﺣﺻ ﯾﻠ ﮭم ا ﻷﻛﺎدﯾ ﻣ ﻲ. ﻟذ ﻟ ك ﺗم ﺗﺻﻣﯾم ھذه اﻟدرا ﺳﺔ ﻟﻐر ض ﻣﺳﺎ ﻋدة اﻟﻣﺳوﻓﯾ ن أﻛﺎ د ﯾ ﻣ ﯾ ﺎً ﻣ ن ط ﻼ ب ا ﻟ ﻠ ﻐ ﺔ ا ﻹ ﻧ ﺟ ﻠ ﯾ ز ﯾ ﺔ ﻛ ﻠ ﻐ ﺔ أ ﺟ ﻧ ﺑ ﯾ ﺔ وﻛ ذﻟ ك ﻟﺗﻌزﯾ ز ﻣ ﺳﺗ و ى اﻟ طﻼب ذو ي اﻟ ﺗ ﺣﺻ ﯾل ا ﻷﻛﺎدﯾﻣﻲ اﻟﻣرﺗﻔﻊ. وا ﺷﺗﻣﻠ ت ﻋ ﯾ ﻧ ﺔ ا ﻟ ﺑ ﺣ ث ﻋ ﻠ ﻰ ﺳ ﺑ ﻌ ﯾ ن ط ﺎ ﻟ ﺑ ﺎً ﻣ ن ط ﻼ ب ا ﻟ ﻠ ﻐ ﺔ ا ﻹ ﻧ ﺟ ﻠ ﯾ ز ﯾ ﺔ ﻛ ﻠ ﻐ ﺔ أ ﺟ ﻧ ﺑ ﯾ ﺔ ﻓ ﻲ ا ﻟ ﻣ ر ﺣ ﻠ ﺔ ا ﻟ ﺟ ﺎ ﻣ ﻌ ﯾ ﺔ . وﺗ م ﺗﻘ ﺳﯾم اﻟ طﻼب ﺑﻧ ﺎ ء ﻋ ﻠ ﻰ ﻣﻘ ﯾﺎ س اﻟﺗ ﺳوﯾ ف ) Tuckman, 1991 ( اﻟ ﻰ ﺛﻼث ﻣ ﺳﺗ وﯾﺎ ت: ﻋﺎﻟ ﻲ، ﻣﺗ وﺳط، وﻣﻧ ﺧﻔ ض ، وﺗم ا ﺳﺗ ﺧدام اﻟﺣ ﻠﻘﺎ ت اﻟد ر ا ﺳ ﯾ ﺔ اﻟ ﺗ ﻲ ﯾﻘ و دھ ﺎ اﻟط ﺎﻟ ب ﻣﻊ إ ﺣ د ى اﻟ ﺷ ﻌ ب اﻟ د ر ا ﺳ ﯾ ﺔ ) 30 طﺎ ﻟ ب(، وﺗم أ ﺳﺗ ﺧدام اﻟ وا ﺟﺑﺎ ت اﻟد را ﺳﯾﺔ ﻣﻊ طﻼب اﻟ ﺷﻌﺑﺔ اﻷﺧر ى. أظﮭر ت اﻟد را ﺳﺔ ﻓﺎﻋ ﻠﯾ ﺔ اﻟ ﺣ ﻠﻘﺎت اﻟ د ر ا ﺳ ﯾ ﺔ اﻟﺗ ﻲ ﯾﻘ ودھﺎ اﻟ ط ﺎﻟ ب ﻋ ﻠ ﻰ ا ﻷ دا ء ا ﻷ ﻛﺎ دﯾ ﻣ ﻲ ﻟ د ى اﻟ ط ﻼب ﻓ ﻲ اﻟﻣﺟﻣوﻋﺔ اﻟ ﺗ ﺟ ر ﯾﺑﯾ ﺔ و ﺧ ﺻ و ﺻ ﺎً ﻟ د ى ا ﻟ ط ﻼ ب ذ و ا ﻟ ﻣ ﺳ ﺗ و ى ا ﻟ ﻌ ﺎ ﻟ ﻲ ﻣ ن ا ﻟ ﺗ ﺳ و ﯾ ف ا ﻷ ﻛ ﺎ د ﯾ ﻣ ﻲ ) 14 %( . ﻛذﻟ ك أ ظﮭر ت اﻟدرا ﺳﺔ ر ﺿﺎ اﻟ طﻼب ﻋن اﻟ ﺣﻠﻘﺎ ت اﻟد ر ا ﺳ ﯾ ﺔ و أ ﺳ ﺗﺎ ذ اﻟﻣﻘ ر ر و ﻛذﻟ ك ﻛﻣﯾ ﺔ اﻟﻣﻌر ﻓﺔ اﻟﺟ دﯾدة اﻟ ﺗ ﻲ ﺗم ا ﻛﺗ ﺳ ﺎﺑ ﮭﺎ.
Novel Coordination Compounds Based on 2-Methylimidazole and 2,2’-dimethylglutarate Containing Ligands: Synthesis and Characterization
Authors: KÖSE YAMAN Pelin , ERER Hakan
Published: August 2018

Two novel copper
and cadmium complexes with 2-methylimidazole (2-meim) and 2,2¢-dimethylglutarate (dmg2-) as ligands, [Cu2(m-dmg)2(2-meim)4]∙5H2O (1) and {[Cd(m-dmg)(2-meim)2]∙H2O}n (2), have
been systematically synthesized and characterized. The result in organic-inorganic crystalline solid. Their solid-state
structures have been solved with elemental analysis, IR spectroscopy, and the single-crystal
X-ray diffraction. The Cu(II) ions distorted
square planar geometry (CuO2N2) while Cd(II) ions
showed a distorted octahedral geometry (CdO4N2). Complex 1
is dimeric structure, in which Cu(II) ions were bridged by dmg ligand. These dimeric units
are extended to the 3D supramolecular structure with hydrogen bonding, C–H∙∙∙p, C–O∙∙∙p and p∙∙∙p interactions. The
complex 2 is
1D polymeric structure, where Cd(II) ions are connected by bis(bidentate) dmg
ligands to form 1D zig-zag polymeric chains which are further extended in 3D supramolecular structure through hydrogen bonding, C–H∙∙∙p and C–O∙∙∙p interactions. The thermal properties of the complexes
were investigated.
Synthesis of Some Mono-, Bis- NH-substituted-1,4-Benzoquinones
Authors: KACMAZ Aysecik
Published: August 2018

The preparation of new mono-
and bis- NH-substituted-1,4-benzoquinones, namely 2,5-bis(5,6-dimethylbenzo[d]thiazol-2-ylamino)cyclohexa-2,5-diene-1,4-dione
(3), 2,5-bis(3-(2-methylpiperidin-1-yl)propylamino)-3-chlorocyclohexa-2,5-diene-1,4-dione
(6), 2-(4-tert-butylbenzylamino)-3,5,6-trichlorocyclohexa-2,5-diene-1,4-dione
(9), 2-(4-fluorophenylamino)-6-tert-butylcyclohexa-2,5-diene-1,4-dione
(12) is
reported. The synthesis of new quinone derivatives (3, 6, 9, 12)
have been carried out from the reactions between quinones (p-benzoquinone (1), 2,6-dichloro-1,4-benzoquinone
(4), tetrachloro-1,4-benzoquinone (7), 2-tert-butyl-1,4-benzoquinone (10)) and different amines (2-Amino-5,6-dimethylbenzothiazole
(2), N-(3-aminopropyl)-2-pipecoline (5), 4-tert-butylbenzylamine (8), 4-fluoroaniline (11)). The new compounds were characterized by elemental analysis,
mass spectrometry, IR, 1H-NMR, 13C-NMR spectroscopy.
Agresividad de aislados de Bipolaris sorokiniana y Alternaria alternata en variedades de trigo en México
Authors: Mata-Santoyo Cassandra Itzel , Leyva-Mir Santos Gerardo , Camacho-Tapia Moisés , Tovar-Pedraza Juan Manuel , Huerta-Espino Julio , Villaseñor-Mir Héctor Eduardo , García-León Elizabeth
Published: August 2018

A partir de muestras de trigo de la variedad CIRNO C2008 con síntomas de tizón foliar y provenientes del Sur de Sonora, México, se obtuvieron cuatro aislados de Bipolaris sorokiniana y cuatro de Alternaria alternata. Las especies fúngicas se identificaron mediante caracterización morfológica y análisis de secuencias ITS del DNA ribosomal. En invernadero, se inocularon los ocho aislados en 13 variedades de trigo harinero (Triticum aestivum) y 6 de trigo cristalino (Triticum durum). La agresividad de los aislados se evaluó con una escala de severidad de 1 a 9, donde 1 fue lesiones mínimas y 9 necrosis y clorosis generalizada que indicó susceptibilidad. Las variedades Vicam S70, Kronstad F2004 y Río Bravo C2016 fueron moderadamente resistentes a B. sorokiniana; en contraste, Bárcenas S2002, Morocco, Borlaug 100 F2014, Bacanora T88, Luminaria F2012, la línea avanzada C, Villa Juárez F2009, Maya S2007, Urbina S2007, PBW343, Nana F2007, Local red, Noio y la línea avanzada JC fueron altamente susceptibles. Adicionalmente, se observó que A. alternata es un patógeno secundario que invade las lesiones provocadas por B. sorokiniana.
A Model Proposal for Solving Problems Encountered in Performance Tasks
Authors: Şahin Melek Gülşah , Boztunç Öztürk Nagihan
Published: August 2018

This study aims to establish a model proposal for solving problems in the
use of performance tasks at the high school level. The study which adopted qualitative
research method was planned in two stages. First, the problems faced by high school
teachers (n = 40) using performance tasks
were determined, and for the second stage the opinions of academicians (n = 8) related to the solution of the determined
problems were consulted. Three stakeholders were identified in solving the problems
identified during the first step of the study; those being the university, the Ministry
of National Education (MoNE), and the teachers. Although the perceptions
of the teachers’ use of performance tasks in general were positive, it was seen
that there problems were experienced in their application. Emphasis was placed on
the importance of communication between the university, the MoNE and the teachers
in order to overcome these problems. For the effective function of performance tasks,
points such as diversity in classroom practices, attention to the characteristics
of students and environmental conditions, and the use of rubrics were emphasised.
Recent Developments on Future Antidepressant-related Serotonin Receptors
Authors: Amidfar Meysam , Kim Yong-Ku
Published: August 2018

Conventional serotonin-enhancing antidepressants including selective serotonin reuptake inhibitors
(SSRIs) and serotonin and norepinephrine reuptake inhibitors (SNRIs) have shown effectiveness in the treatment
of major depression, but their significant limitations such as slowness of action have led to intensive research
efforts to develop new antidepressants. Increased synaptic neurotransmission of serotonin (5-hdroxytryptamine;
5-HT) through orchestration of stimulation and blockade of various subtypes of 5-HT receptors is involved in the
mechanisms of action of SSRIs. Agonists at the 5-HT1A, 5-HT1B, 5-HT2C, 5-HT4, and 5-HT6 receptors and
antagonists at the 5-HT1A, 5-HT2A, 5-HT2C, 5-HT3, 5- HT6, and 5-HT7 receptors have shown antidepressant
properties in clinical and preclinical studies. However, paradoxical antidepressant-like effects of both agonists
and antagonists at particular 5-HT receptors suggest the need to consider the neurochemical mechanisms of each
5-HT receptor subtype. Therefore, better knowledge of the involvement of individual 5-HT receptors in the
mechanisms of action of currently used antidepressants as well as antidepressant effects of selective ligands of 5-
HT receptor subtypes will provide opportunities for the development of future antidepressants with more rapid
onset of action, fewer side effects, and better efficacy than SSRIs.
Circadian Rhythm and Melatonin in the Treatment of Depression
Authors: Satyanarayanan Senthil Kumaran , Su Huanxing , Lin Yi-Wen , Su Kuan-Pin
Published: August 2018

Background:

Circadian rhythm disruption underlies the pathophysiology of psychiatric disorders,
especially depression. Both pharmacological and non-pharmacological strategies affecting endogenous circadian
rhythms have been developed with specificity to alter the circadian dysfunction. The current management strategy
with antidepressants is far from being satisfactory in addressing this issue. In recent years, attempts at discovering
new antidepressants focused on a melatonergic system which is known to be altered in depression have led to a
potential option for treatment of depression.

Methods:

We reviewed all recently published relevant articles on melatonin and its analogues to look for their
implication in the treatment of circadian rhythm disruption and depression.

Results:

Melatonin, a pleiotropic regulator molecule and its analogues (ramelteon, agomelatine, TIK-301, Neu-
P11 and tasimelteon) have been observed to resynchronize the circadian rhythm and some were said to alleviate
depressive symptoms in depressed subjects.

Conclusion:

This review focuses on substantial advances in the melatonin-based chronobiologic intervention and
its responses in the treatment of depression.
Recent Advances in Nutrition for the Treatment of Depressive Disorder
Authors: Wang Xu , Zhao Fei , Wang Xufeng , Niu Yabing , Niu Lijuan , Wang Chunling
Published: August 2018

Depression is one of the leading causes of disability in the world. Current pharmaceutical treatment for
depression remains unsatisfactory due to its limited therapeutic efficacy and undesirable side effects. There is
increasing interest in looking for alternative strategies from diet for the treatment of depressive disorder. The
nutrition factors have the potential to regulate several neurochemical pathways implicated in depression. This
review gives an overview of the recent advances in depression treatment using nutrition factors including vitamins,
polyunsaturated fatty acid, elements and natural products. The review covers most recent publications from
2016 to mid-2018. The results of basic experimental and clinical studies were summarized. The risk of deficiency
and effect of intervention using nutrition factors for the depression were also discussed. Although the results are
controversial in some cases due to the experimental design, the relationship has been observed between deficiency
of certain nutrition factors and incidence of depression in the majority of studies. The dietary nutrition
supplements may play significant or synergic role in treating or improving depressive disorders.
Blastocystis sp., Parasite Associated with Gastrointestinal Disorders: An Overview of its Pathogenesis, Immune Modulation and Therapeutic Strategies
Authors: Kumarasamy Vinoth , Anbazhagan Deepa , Subramaniyan Vetriselvan , Vellasamy Shalini
Published: August 2018

Blastocystis sp. is a unicellular parasitic microorganism commonly found in the gastrointestinal tracts
of humans and animals. It causes symptomatic or asymptomatic infection and its route of transmission is via
fecal-oral. High prevalence of Blastocystis infection in developing countries is usually due to poor hygiene practices,
exposure to animals infected with the parasite and intake of contaminated water or food. Blastocystis infected
individuals often suffer from diarrhea, abdominal pain, nausea, and stomach bloating. Even though
pathogenicity of Blastocystis is unclear, it is commonly associated with irritable bowel syndrome. In this review,
we have analysed the evidence that shows the association between this microorganism and gastrointestinal disorders.
There have been a number of studies which showed that the pathogenicity of Blastocystis is related to its
different STs. The pathogenicity is speculated to be due to cysteine proteases formation which stimulates mucosal
cells to release interleukin-8 which has been associated with extreme dehydration and gut inflammation. In vitro
studies on human colonic epithelial cells revealed that incubation of Blastocystis modulated the host immune
response by stimulating the formation of pro-inflammatory cytokines and granulocyte macrophage colonystimulating
factor. Metronidazole is found to be the first-line drug of choice. Another treatment option is the
combination therapy with trimethoprim/sulfamethoxazole.
Targeted Liposomes for siRNA Delivery to Cancer
Authors: Eloy Josimar O. , Petrilli Raquel , Raspantini Giovanni Loureiro , Lee Robert J.
Published: August 2018

Background:

RNA interference is a promising therapeutic tool for the treatment of a variety of diseases,
with great potential for cancer therapy. Small interfering RNA (siRNA), however, presents several drawbacks
that hamper its therapeutic application. Lipid nanoparticles, including liposomes, are delivery systems with
great potential for siRNA delivery, protecting it from degradation, enhancing its cell uptake with the ability of
controlled release. However, non-specific delivery and side effects could potentially limit the in vivo application.
Therefore, targeting lipid nanoparticles to overexpressed receptors of cancer cells represents a strategy for better
therapeutic outcome, with improved efficacy and reduced toxicity. For this purpose, lipid nanoparticles could be
functionalized with several moieties that can be recognized by cancer cells more than by normal cells. These
ligands include folate, transferrin, peptides, oligosaccharides, monoclonal antibodies and aptamers.

Methods:

In this paper, we reviewed functionalization strategies and addressed the major in vitro and in vivo
findings in the field of cancer treatment with siRNA.

Results:

Many papers showed enhanced siRNA delivery by targeted liposomes, resulting in enhanced drug uptake
and better cytotoxicity, with consequent better tumor growth control in xenograft studies.

Conclusion:

siRNA delivery mediated by functionalized liposomes is promising, but clinical trials need to be
conducted.
Nucleic Acid Delivery System by the Combination of Lipid bubbles and Ultrasound
Authors: Endo-Takahashi Yoko , Maruyama Kazuo , Negishi Yoichi
Published: August 2018

Background:

RNA interference (RNAi)-based therapy has gained attention because of its potent genesilencing
effect and high specificity. However, the efficient delivery of nucleic acids to the target site is a major
challenge to the clinical implementation. Recently, ultrasound-mediated gene delivery systems have been developed
and attracted interest due to its safety and site-specificity. By the combination with contrast agents, called
microbubbles, not only the delivery effects but also the imaging effects are significantly enhanced. We developed
lipid bubbles (LBs) entrapping an ultrasound contrast gas to enhance the efficacy of ultrasound-mediated delivery
and imaging. In this review, we summarize ultrasound-mediated nucleic acid delivery systems and discuss the
possibility of combining LBs and ultrasound for RNAi-based therapies.

Methods:

We prepared polyethylene glycol-modified liposomes and entrapped an echo-contrast gas within the
liposomes. Small interfering RNA (siRNA) were transfected into cells and muscles using LBs and ultrasound.
Moreover, we also developed nucleic acid-loaded LBs using cholesterol-conjugated siRNA or positively-charged
lipid for an efficient systemic delivery of siRNA and microRNA. The usability of LBs for RNA delivery system
was evaluated by the silencing effects of target genes and the therapeutic effects on ischemia hind limb.

Results:

A combination of LBs and therapeutic ultrasound was able to enhance the gene silencing effects by
siRNA. Nucleic acid-loaded LBs were able to efficiently deliver siRNA or microRNA by systemic administration.
A combination of LBs and diagnostic ultrasound also enhanced the imaging efficiency. Using a hindlimb
ischemia mouse model, microRNA-loaded LBs could lead to increased angiogenic factors and improved blood
flow.

Conclusion:

Ultrasound technology is widely used in clinical settings not only for diagnosis but also for therapy.
Ultrasonic devices are being actively developed. Computer-controlled ultrasound systems can provide precise
exposure to the target site. The combination of precise ultrasound exposure and LBs might be useful for target
site-specific nucleic acids delivery, and holds potential to be developed into a beneficial therapeutic and diagnostic
system for various diseases.
Nanostructured Hyaluronic Acid-based Materials for the Delivery of siRNA
Authors: Shah Keval , Chawla Sunita , Gadeval Anuradha , Reddy Goutham , Maheshwari Rahul , Kalia Kiran , Tekade Rakesh Kumar
Published: August 2018

Background:

The search for the effective treatment strategies to combat a disease that is characterized
by abnormal cell growth and known as cancer is still required to reach its destiny. To address the problem, recently
several gene therapies based on novel RNA interference (RNAi) have been proposed such as siRNA, micro
RNA, shRNA, etc. out of which, siRNAs (silencing RNA) promises to show significant progress in pharmacotherapy,
including considerable expansion of the druggable target space and the possibility of treating cancer.

Methods:

This review aims to uncover the hyaluronic acid (HA) and HA-hybridized nanoplatforms for siRNA
delivery systems with a particular focus on the discussion of available reports while addressing the future potential
of HA-based treatment strategies.

Results:

HA modified siRNA delivery, as promised, provided better targeting potential in many types of cancers.
In addition, it was able to modify the release of siRNA as well. Toxicity of HA is well mentioned however, the
loophole is yet to be filled by exploring various remedies for overcoming toxicity.

Conclusion:

To overcome the problems associated with these emerging genetic tools, investigators have employed
glycosaminoglycan HA-based biopolymers. This biopolymer offers a variety of properties such as biodegradability,
biocompatibility, aqueous solubility, viscoelasticity, and non-immunogenicity.
Gene Silencing using siRNA for Preventing Liver Ischaemia-Reperfusion Injury
Authors: Marinho H. Susana , Marcelino Paulo , Soares Helena , Corvo Maria Luísa
Published: August 2018

Background:

Ischaemia-reperfusion injury (IRI), a major complication occurring during organ transplantation,
involves an initial ischemia insult, due to loss of blood supply, followed by an inflammation-mediated
reperfusion injury. A variety of molecular targets and pathways involved in liver IRI have been identified. Gene
silencing through RNA interference (RNAi) by means of small interference RNA (siRNA) targeting mediators of
IRI is a promising therapeutic approach.

Objective:

This study aims at reviewing the use of siRNAs as therapeutic agents to prevent IRI during liver transplantation.

Method:

We review the crucial choice of siRNA targets and the advantages and problems of the use of siRNAs.

Results:

We propose possible targets for siRNA therapy during liver IRI. Moreover, we discuss how drug delivery
systems, namely liposomes, may improve siRNA therapy by increasing siRNA stability in vivo and avoiding
siRNA off-target effects.

Conclusion:

siRNA therapeutic potential to preclude liver IRI can be improved by a better knowledge of what
molecules to target and by using more efficient delivery strategies.
Advances in Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 1: Overview of the Chemical and Biological Research
Authors: Jankowska Agnieszka , Świerczek Artur , Wyska Elżbieta , Gawalska Alicja , Bucki Adam , Pawłowski Maciej , Chłoń-Rzepa Grażyna
Published: August 2018

Phosphodiesterase 10A (PDE10A) is a double substrate enzyme that hydrolyzes second messenger
molecules such as cyclic-3’,5’-adenosine monophosphate (cAMP) and cyclic-3’,5’-guanosine
monophosphate (cGMP). Through this process, PDE10A controls intracellular signaling pathways in the
mammalian brain and peripheral tissues. Pharmacological, biochemical, and anatomical data suggest that
disorders in the second messenger system mediated by PDE10A may contribute to impairments in the
central nervous system (CNS) function, including cognitive deficits as well as disturbances of behavior,
emotion processing, and movement. This review provides a detailed description of PDE10A and the recent
advances in the design of selective PDE10A inhibitors. The results of preclinical studies regarding
the potential utility of PDE10A inhibitors for the treatment of CNS-related disorders, such as schizophrenia
as well as Huntington’s and Parkinson’s diseases are also summarized.
Application of Machine Learning Approaches for the Design and Study of Anticancer Drugs
Authors: Hu Yan , Lu Yi , Wang Shuo , Zhang Mengying , Qu Xiaosheng , Niu Bing
Published: August 2018

Background: Globally the number of cancer patients and deaths are continuing to increase yearly, and cancer has, therefore, become one of the world's highest causes of morbidity and mortality. In recent years, the study of anticancer drugs has become one of the most popular medical topics.  Objective: In this review, in order to study the application of machine learning in predicting anticancer drugs activity, some machine learning approaches such as Linear Discriminant Analysis (LDA), Principal components analysis (PCA), Support Vector Machine (SVM), Random forest (RF), k-Nearest Neighbor (kNN), and Naïve Bayes (NB) were selected, and the examples of their applications in anticancer drugs design are listed.  Results: Machine learning contributes a lot to anticancer drugs design and helps researchers by saving time and is cost effective. However, it can only be an assisting tool for drug design.  Conclusion: This paper introduces the application of machine learning approaches in anticancer drug design. Many examples of success in identification and prediction in the area of anticancer drugs activity prediction are discussed, and the anticancer drugs research is still in active progress. Moreover, the merits of some web servers related to anticancer drugs are mentioned.
Exploring Proteomic Drug Targets, Therapeutic Strategies and Protein - Protein Interactions in Cancer: Mechanistic View
Authors: Dar Khalid Bashir , Bhat Aashiq Hussain , Amin Shajrul , Anjum Syed , Reshi Bilal Ahmad , Zargar Mohammad Afzal , Masood Akbar , Ganie Showkat Ahmad
Published: August 2018

Protein-Protein Interactions (PPIs) drive major signalling cascades and play critical role in cell proliferation, apoptosis, angiogenesis and trafficking. Deregulated PPIs are implicated in multiple malignancies and represent the critical targets for treating cancer. Herein, we discuss the key protein-protein interacting domains implicated in cancer notably PDZ, SH2, SH3, LIM, PTB, SAM and PH. These domains are present in numerous enzymes/kinases, growth factors, transcription factors, adaptor proteins, receptors and scaffolding proteins and thus represent essential sites for targeting cancer. This review explores the candidature of various proteins involved in cellular trafficking (small GTPases, molecular motors, matrix-degrading enzymes, integrin), transcription (p53, cMyc), signalling (membrane receptor proteins), angiogenesis (VEGFs) and apoptosis (BCL-2family), which could possibly serve as targets for developing effective anti-cancer regimen. Interactions between Ras/Raf; X-linked inhibitor of apoptosis protein (XIAP)/second mitochondria-derived activator of caspases (Smac/DIABLO); Frizzled (FRZ)/Dishevelled (DVL) protein; beta-catenin/T Cell Factor (TCF) have also been studied as prospective anticancer targets. Efficacy of diverse molecules/ drugs targeting such PPIs although evaluated in various animal models/cell lines, there is an essential need for human-based clinical trials. Therapeutic strategies like the use of biologicals, high throughput screening (HTS) and fragment-based technology could play an imperative role in designing cancer therapeutics. Moreover, bioinformatic/computational strategies based on genome sequence, protein sequence/structure and domain data could serve as competent tools for predicting PPIs. Exploring hot spots in proteomic networks represents another approach for developing targetspecific therapeutics. Overall, this review lays emphasis on a productive amalgamation of proteomics, genomics, biochemistry, and molecular dynamics for successful treatment of cancer.
Perturbation Theory Machine Learning Models: Theory, Regulatory Issues, and Applications to Organic Synthesis, Medicinal Chemistry, Protein Research, and Technology
Authors: Arrasate Sonia , Duardo-Sanchez Aliuska
Published: August 2018

Machine Learning (ML) models are very useful to predict physicochemical properties of
small organic molecules, proteins, proteomes, and complex systems. These methods may be useful to
reduce the cost of research in terms of materials resources, time, and laboratory animal sacrifice. Recently
different authors have reported Perturbation Theory (PT) methods combined with ML to obtain
PTML (PT + ML) models. They have applied PTML models to the study of different biological systems
and in technology as well. Here, we present one state-of- the-art review about the different applications
of PTML models in Organic Synthesis, Medicinal Chemistry, Protein Research, and Technology.
In this work, we also embrace an overview of regulatory issues for acceptance and validation of
both: the Cheminformatics models, and the characterization of new Biomaterials. This is a main question
in order to make scientific result self for humans and environment.
Microencapsulation of Carvacrol Using Pectin/Aloe-gel as a Novel Wound Dressing Films
Authors: Gomez-Rodriguez Gabriel Humberto , Lopez-Mata Marco Antonio , Valbuena-Gregorio Edith , Melchor Ramon Gertrudis Valdez , Campos-Garcia Julio Cesar , Silva-Beltran Norma Patricia , Quihui-Cota Luis , Ruiz-Cruz Saul , Juarez Josue
Published: August 2018

Recently, Pectin (PEC) and Aloe-Gel (AG) have received great attention for their use in the
encapsulation of hydrophobic bioactive compounds such as Carvacrol (CAR). The aim of this study is to
assess the physical, chemical and biological properties of a novel PEC/AG film and evaluate its capability
to entrap CAR into microencapsulates. For this purpose, the casting method was used to prepare the
PEC/AG membranes (70:30 % w/w). The CAR-loaded PEC/AG film was prepared adding different
proportions of CAR (0.25%, 0.50% and 1.00% v/v) to the mixture of PEC/AG, previously emulsified
with tween 80 (1.0%). The optical properties, Water Vapor Permeability (WVP), ATR-FTIR spectroscopy,
microstructure, antibacterial activity and size of microcapsules were evaluated. The PEC/AG
membranes loaded with CAR showed yellowish appearance and they were transparent to the UV electromagnetic
radiation (190, 200 and 280 nm). The film prepared with the lowest amount of CAR
(PC/AG-CAR-0.25%) showed the highest values of WVP (66.2%) and, according to SEM micrograph,
the largest microcapsules (≈1005± 39 µm3). The FTIR analysis showed the characteristic absorption
peaks located at 1015 cm-1 to 1030 cm-1 and a small shoulder to 990 cm-1 of benzene ring 1:2:4 substituted
that suggested the presence of CAR-loaded in the PC/AG film. On the other hand, E. coli O157:H7
showed the highest sensitivity to the PEC/AG-CAR-1.00% film, while S. aureus was not sensitive.
Dermal Collagen Stabilization by Polyphenols and Spray Drying as an Encapsulation Strategy
Authors: Anazco Carolina , Rojas Armando , Gonzalez Ileana , Castro Maite A. , Robert Paz , Oyarzun-Ampuero Felipe
Published: August 2018

Collagen, the most abundant component in mammalian tissues, has a crucial impact at skin
level. Both promotion and maintenance of cross-linked collagen at the skin are critical to sustain the
functionality and appearance of that tissue. Lysyl oxidases, also known as LOX enzymes, are the major
collagen cross-linking enzymes that play a pivotal role in homeostasis. This minireview summarizes
evidence that describes an amino oxidase-like activity, which could be attributed to polyphenols, or
where polyphenols could be required. We also discuss some available collagen formulations and the scientific
evidence that describes the impact on dermal extracellular matrix. In addition, information about
encapsulation strategies to carry polyphenols, and some examples are also provided.
Rational Surface Engineering of Colloidal Drug Delivery Systems for Biological Applications
Authors: Escareno Noe , Topete Antonio , Taboada Pablo , Daneri-Navarro Adrian
Published: August 2018

The use of colloidal particles as drug delivery carriers holds a great promise in terms of improvement
of traditional treatment and diagnosis of human diseases. Nano- and microsized particles of a
different composition including organic and inorganic materials can be fabricated with a great control
over size, shape and surface properties. Nevertheless, only some few formulations have surpassed the
benchtop and reached the bedside. The principal obstacle of colloidal drug delivery systems is their poor
accumulation in target tissues, organs and cells, mainly by efficient sequestration and elimination by the
mononuclear phagocytic system. Recent evidence suggests that, besides size, the surface character of
colloidal systems is the most determinant design parameter that may ultimately guarantee successful
biological performance. To approach these issues, materials designers and engineers can make use of
multiple strategies and tools to finely modulate the particles’ surface towards highly efficient and biocompatible
materials. In this article, we provide an overview of the most relevant colloidal drug delivery
systems, a summary of the available literature regarding the effects of surface charge, hydrophobicity
and softness on biological response, and finally, we review the key points of surface modification strategies
with organic, inorganic and biological materials.
Targeted Drug Delivery Via Human Epidermal Growth Factor Receptor for Sustained Release of Allyl Isothiocyanate
Authors: Encinas-Basurto David , Juarez Josue , Valdez Miguel A. , Burboa Maria G. , Barbosa Silvia , Taboada Pablo
Published: August 2018

In this study, allyl-isothiocyanate (AITC)-loaded Polylactic-Co-Glycolic Acid (PLGA)
Nanoparticles (NPs) were prepared for targeting epithelial squamous carcinoma cells using a specific
antibody targeting the Epidermal Growth Factor (EGF) receptor overexpressed on the cell membranes.
AITC-loaded PLGA NPs showed more effective anticancer properties compared with free AITC, and
their cytotoxicity was even more pronounced when the anti-EGFR antibody was covalently attached to
the NPs surface. This targeting ability was additionally tested by co-culturing cervical HeLa cells, with
very few EGFR on the membranes, and epithelial squamous carcinoma A431 cells, which largely overexpressed
EFGR, being observed the specific localization of the antibody-functionalized AITC-loaded
PLGA NPs solely in the latter types of cells, whereas non-functionalized NPs were distributed randomly
in both cell types in much lesser extents. Thus, our findings support the development of drug delivery
strategies that enhances the delivery of anti-cancer natural compounds to tumor tissue, in this case, by
targeting specific tumor cell receptors with cell-specific ligands followed by tumor sensitization.
Mechanical Properties of Composite Hydrogels for Tissue Engineering
Authors: Rial Ramon , Soltero J.F. Armando , Verdes Pedro V. , Liu Zhen , Ruso Juan M.
Published: August 2018

Tissue engineering provides solutions that require medicine to restore damaged tissues or
even complete organs. This discipline combines biologically active scaffolds, cells and molecules; being
the addition of nanoparticles into the scaffolds, one of the techniques that is attracting more interest
these days. In this work, Hydroxyapatite Nanorods (HA) were added to the network of Gelatin hydrogel
(GE), and the particular properties resulting from their interaction were studied. Specifically, viscoelastic
properties were characterized as a function of gel and nanoparticle concentration, varying ratios and
temperatures. Oscillatory Time Sweeps (OTS) provided the necessary information about how the timeresolved
material property/structure alteration. A wide variety of Continuous Flow Tests and Frequency
Sweeps were used to describe the mechanical properties of the material, proving that the presence of
nanoparticles led to a reinforcement of the gel network, mechanical stiffness and strength. The thixotropic
nature of the gels was also evaluated and the most common theoretical models were described
and commented. The attributes inferred from the data, showed a material that can allow the natural
growth of bone tissue whilst withstanding properly the mechanical efforts; resulting in a material with
an outstanding suitability to be used in regenerative medicine.
Effect of Geographical Location and Type of Extract on Total Phenol/Flavon Contents and Antioxidant Activity of Different Fruits Extracts of Withania somnifera
Authors: Adhikari Lokesh , Kotiyal Rupali , Pandey Mukesh , Bharkatiya Meenakshi , Sematy Ajay , Semalty Mona
Published: August 2018

Background:

Withania somnifera (family solanaceae) is a well-investigated medicinal plant which is also called Indian ginseng due to its wide spectrum of medicinal properties. The contents and activity of the plant may vary depending on the habitat and part of the plant and the solvent used for extraction. The present study deals with the comparative chemical analysis and in vitro antioxidant activity of methanolic fruits extracts and its subfractions (in ethyl acetate, butanol and water) of W. somnifera collected from two different geographical locations.

Methods:

In the present study, Withania somnifera fruits were collected from two different geographical locations (Uttarakhand and Rajasthan). The different fruit extracts were prepared and studied for total phenolic contents and total flavone contents. The in vitro antioxidant activity was assessed by DPPH free radical scavenging assay and peroxide scavenging assay.

Results:

Methanol extract of W. somnifera Uttarakhand and ethyl acetate subfraction of W. somnifera Rajasthan showed the highest amount of Total Phenolic Contents (TPC). In W. somnifera Uttarakhand, ethyl acetate extract showed the highest amount of Total flavonoids while in W. somnifera Rajasthan, methanol extract was found to be the richest in flavonoids. Methanolic extract of W. somnifera Uttarakhand showed the highest free radical scavenging activity while in W. somnifera Rajasthan, the highest antioxidant activity was shown by the methanolic extract followed by butanolic extract, water extract and then ethyl acetate. In the peroxide scavenging assay of antioxidant activity, water extract of W. somnifera Uttarakhand showed the highest activity, while in W. somnifera Rajasthan, ethyl acetate extract showed highest scavenging activity.

Conclusion:

It was concluded that the geographical location exerts a vital effect on the presence of active constituents and also on the antioxidant potential of W. somnifera.
Chemistry and Pharmacological Activities of Biginelli Product- A Brief Overview
Authors: George Namy , Manakkadan Asha Asokan , Ariyath Ajish , Maniyamma Surya , Vijayakumar Vishnu , Pai Rajasree G. , Zachariah Subin Mary
Published: August 2018

Dihydropyrimidinones are extremely advantageous small sized molecules owning adaptable
pharmaceutical properties. With a molecular formula C4H6N2O, they hold a wide range of biological
activities. It is a heterocyclic moiety having two N-atoms at positions 1 and 3. They are derivatives
of pyrimidine containing an additional ketone group. They have inspired development of a
wide range of synthetic methods for preparation and chemical transformations. Taking into consideration
their structural similarity and involvement with DNA and RNA, they have become very imperative
in the world of synthetic organic chemistry. Aryl substituted moieties and their derivatives
are significant class of substances in medicinal and organic chemistry. Many alkaloids from natural
marine sources comprising dihydropyrimidinones core have been isolated which possess fascinating
biological properties. Intensive explorations have been carried out on these compounds because
they possess close similitude to clinically used nifedipine, nicardipine etc. which are also Biginelli
product analogues. Due to the interesting pharmacological properties associated with the privileged
DHPM structures, the Biginelli reaction and related procedures have received increasing attention in
recent years.
Identification and Ranking of Clinical Compounds with Activity Against Log-phase Growing Uropathogenic Escherichia coli
Authors: Niu Hongxia , Yee Rebecca , Cui Peng , Zhang Shuo , Tian Lili , Shi Wanliang , Sullivan David , Zhu Bingdong , Zhang Wenhong , Zhang Ying
Published: August 2018

Background:

Uropathogenic Escherichia coli (UPEC) is a major cause of Urinary
Tract Infections (UTIs). Due to increasing antibiotic-resistance among UPEC bacteria, new
treatment options for UTIs are urgently needed.

Objective:

To identify new agents targeting growing bacteria that may be used for the treatment of
antibiotic-resistant UTIs.

Methods:

We screened a clinical compound library consisting of 1,524 compounds using a high
throughput 96-well plate assay and ranked the activities of the selected agents according to their
MICs against the UPEC strain UTI89.

Results:

We identified 33 antibiotics which were active against log-phase clinical UPEC strain
UTI89. Among the selected antibiotics, there were 12 fluoroquinolone antibiotics (tosufloxacin,
levofloxacin, sparfloxacin, clinafloxacin, pazufloxacin, gatifloxacin, enrofloxacin, lomefloxacin,
norfloxacin, fleroxacin, flumequine, ciprofloxacin), 15 beta-lactam or cephalosporin antibiotics
(cefmenoxime, cefotaxime, ceftizoxime, cefotiam, cefdinir, cefoperazone, cefpiramide,
cefamandole, cefixime, ceftibuten, cefmetazole, cephalosporin C, aztreonam, piperacillintazobactam,
mezlocillin), 3 tetracycline antibiotics (meclocycline, doxycycline, tetracycline), 2
membrane-acting agents (colistin and clofoctol), and 1 protein synthesis inhibitor (amikacin).
Among them, the top 7 hits were colistin, tosufloxacin, levofloxacin, sparfloxacin, clinafloxacin,
cefmenoxime and pazufloxacin, where clinafloxacin and pazufloxacin were the newly identified
agents active against UPEC strain UTI89. We validated the key results obtained with UTI89 on
two other UTI strains CFT073 and KTE181 and found that they all had comparable MICs for
fluoroquinolones while CFT073 and KTE181 were more susceptible to cephalosporin antibiotics
and tetracycline antibiotics but were less susceptible to colistin than UTI89.

Conclusion:

Our findings provide possible effective drug candidates for the more effective
treatment of antibiotic-resistant UTIs.
The Effect of Neuropathic Pain Symptoms on Remission in Patients with Early Rheumatoid Arthritis
Authors: Salaffi Fausto , Di Carlo Marco , Carotti Marina , Sarzi-Puttini Piercarlo
Published: August 2018

Background:

The presence of neuropatic pain (NeP) is common in subjects with established Rheumatoid Arthritis (RA), and it can influence the disease remission. These aspects have not been investigated in patients with Early Rheumatoid Arthritis (ERA).

Objective:

To investigate the effect of NeP on the achievement of remission in patients with ERA.

Method:

The study involved consecutive ERA patients with moderate or high disease activity. The painDETECT Questionnaire (PDQ), the 36-item Short Form Health Survey (SF-36), and the Euro- QoL-5 Dimensions (EQ-5D) were administered to all the patients, and their co-morbidity data were used to calculate their modified Rheumatic Disease Comorbidity Index (mRDCI). After six months’ follow-up, the presence or otherwise of NeP in each individual patient was calculated, and whether or not the Boolean remission criteria were satisfied.

Results:

The study was completed by 115 patients (76% females) whose PDQ scores indicated that 13% had probable NeP. At the end of the follow-up period, 25 patients (21.7%) met the Boolean remission criteria. Logistic regression analysis showed that baseline PDQ scores (p=0.0023) and the mRDCI (p=0.0054) were the strongest predictors of not being in Boolean remission. Only one of the 15 patients with concomitant NeP achieved Boolean remission.

Conclusion:

The presence of NeP may affect the achievement of remission in ERA patients. The PDQ can be a useful tool to measure central pain sensitisation in such patients.
An Unusual Presentation of a Rare Scleroderma Mimic: What is Behind the Scenes?
Authors: Ibrahim Rehab Ali , Abdalla Nour El-Hoda Hussien , Shabaan Engy Amr Husssein , Mostafa Noha Bassiouny Hassan
Published: August 2018

Background:

Scleroderma or systemic sclerosis (SSc) is a rare systemic autoimmune
disease. Many conditions mimic the presentation of SSc, especially skin thickening and fibrosis.
One of these conditions is scleredema, a rare collagen and mucin deposition disorder which was
found to be associated with diabetes mellitus, streptococcal infection or monoclonal gammopathy.

Case Presentation:

A 55 years old female presented with insidious onset and progressive course of
diffuse skin thickening of face, neck, arms, forearms, thighs, chest, back, and excluding both hands
and feet of 6 years’ duration associated with arthralgia, dysphagia and dyspnea on exertion of 1-
year duration. There was no history of Raynaud’s phenomenon. Erythrocyte sedimentation rate was
100 mm/1st h, autoantibodies for SSc were negative, nail fold capillaroscopy normal, pulmonary
function tests showed restrictive pattern and high-resolution computed tomography showed interstitial
lung fibrosis. Patient was not fulfilling the American collage of rheumatology/European League
Against Rheumatism classification criteria for SSc. Skin biopsy was done and revealed histological
appearance of scleredema. Investigations were done for disease association with scleredema. The
patient was not diabetic, antistreptolysin O titer was normal, serum protein electrophoresis, immunofixation
and bone marrow biopsy were done, and the patient was diagnosed as scleredema associated
with immunoglobulin A kappa multiple myeloma. Treatment by combination of bortezomib,
cyclophosphamide, and dexamethasone was started with marked clinical and hematological
improvement.

Conclusion:

Many conditions mimic SSc including scleredema, which may be the initial presentation
of multiple myeloma. Rheumatologists and dermatologists should be able to recognize these
conditions to provide the suitable management and follow-up for these patients.
The Role of Vascular Endothelial Growth Factor in Systemic Sclerosis
Authors: Flower Victoria A. , Barratt Shaney L. , Ward Stephen , Pauling John D.
Published: August 2018

The pathological hallmarks of Systemic Sclerosis (SSc) constitute an inter-related triad of autoimmunity, vasculopathy and tissue remodeling. Many signaling mediators have been implicated in SSc pathology; most focusing on individual components of this pathogenic triad and current treatment paradigms tend to approach management of such as distinct entities. The present review shall examine the role of Vascular Endothelial Growth Factor (VEGF) in SSc pathogenesis. We shall outline potential mechanisms whereby differential Vascular Endothelial Growth Factor-A (VEGF-A) isoform expression (through conventional and alternative VEGF-A splicing,) may influence the relevant burden of vasculopathy and fibrosis offering novel insight into clinical heterogeneity and disease progression in SSc. Emerging therapeutic approaches targeting VEGF signaling pathways might play an important role in the management of SSc, and differential VEGF-A splice isoform expression may provide a tool for personalized medicine approaches to disease management.
Androgen Therapy in Male Patients Suffering from Type 2 Diabetes: A Review of Benefits and Risks
Authors: Hassanabad Mortaza F. , Fatehi Mohammad
Published: August 2018

Background:

The current estimated numbers of patients with Type 2 Diabetes (T2D) is believed to be close to 10% of the whole populations of many geographical regions, causing serious concerns over the resulting elevated morbidity and mortality as well as the impact on health care systems around the world. In addition to negatively affecting the quality of life, diabetes is associated with cardiovascular and cerebrovascular complications, indicating that appropriate drug therapy should not only deal with metabolic dysfunction but also protect the vascular system, kidney function and skeletal muscle mass from the effects of the epigenetic changes induced by hyperglycaemia.

Objective:

To provide an insight into the management of hypogonadism associated with T2D, this review focuses on clinical observations related to androgen therapy in qualified diabetic patients, and discusses the lines of evidence for its benefits and risks. The potential interactions of testosterone with medicines used by patients with T2D will also be discussed.

Conclusion:

From recent clinical findings, it became evident that a considerable percentage of patients suffering from T2D manifested low serum testosterone and experienced diminished sexual activity, as well as reduced skeletal muscle mass and lower bone density. Although there are some controversies, Testosterone Replacement Therapy (TRT) for this particular population of patients appears to be beneficial overall only if it is implemented carefully and monitored regularly.