bluuebunny/crossref_metadata_2025 huggingface dataset:
Historia natural de la reparación endoscópica preaponeurótica (REPA)
Authors: Pou Santonja Guillermo
Published: October 2018

La diástasis de los músculos rectos del abdomen es uno de los temas de mayor interés en la actualidad a nivel de consultas sobre patología de pared abdominal. Pero sigue siendo controvertido respecto a su consideración de «problema patológico» o «estético » por parte de los profesionales implicados en su tratamiento. Años atrás, todos hemos tenido pacientes en nuestras consultas que acudían por esta patología y los enviábamos a cirugía plástica para su valoración.
Treatment of Patellar Fractures and Injuries to the Extensor Mechanism of the Knee
Authors: Bui Christopher N. , Learned James R. , Scolaro John A.
Published: October 2018

* Patellar fractures occur as a result of a direct blow to the knee and/or as a result of tension when the forces generated between the quadriceps tendon and patellar tendon overcome the strength of the bone.

* Patellar fractures that include a functional disruption to the extensor mechanism should be treated with stable open reduction and internal fixation.

* If necessary, partial (or, rarely, complete) excision of the patella can be performed to provide a stable extensor mechanism repair.

* Acute quadriceps and patellar tendon ruptures, if complete, require primary repair.

* Delayed intervention for any complete extensor mechanism disruption may result in the need for reconstruction, augmentation, or advanced techniques to facilitate early motion.
Особенности роста десятиногих ракообразных в рециркуляционных установках на примере австралийского рака Cherax quadricarinatus (Decapoda: Parastacidae)
Authors: Борисов Р. Р. , Никонова И. Н.
Published: October 2018

Объёмы производства декапод методами аквакультуры в последние годы постоянно увеличиваются. При этом особую актуальность приобретают исследования, направленные на интенсификацию технологических процессов. Одним из них является использование рециркуляционных установок. В работе на примере австралийского рака Cherax quadricarinatus проведён анализ основных факторов, тормозящих интенсификацию культивирования десятиногих ракообразных в рециркуляционных установках. Главными среди этих факторов являются каннибализм и подавление крупными особями роста мелких. В экспериментах исследовалось влияние на рост и выживаемость: группового и индивидуального содержания; размерного состава групп; объёма ёмкостей для культивирования. Все использованные особи получены от одной самки C. quadricarinatus. Продолжительность экспериментов составила шесть месяцев. Выявлена прямая корреляция каннибализма с плотностью посадки особей. В ёмкостях небольшого размера в группах раков отмечено формирование одной-двух доминирующих особей, подавляющих рост остальных раков в группе. При индивидуальном содержании скорость роста у мелких особей была выше, чем у крупных. Эксперименты с разноразмерными группами молоди раков показали, что проведение сортировки по размеру позволяет получить более быстро и равномерно растущие группы особей, но не помогает решить проблему каннибализма. На основании собранных данных рекомендовано в первые три месяца культивирования дважды проводить сортировку особей по размеру и снижать плотности посадки. Полностью исключить каннибализм возможно только при индивидуальном содержании раков.
Diversity and functions of loricae in ciliates (Ciliophora)
Authors: Dovgal I. V. , Gavrilova N. A.
Published: October 2018

The article focused on morphological peculiarities, chemical composition and function of the loricae in ciliates. Pseudochitinous (tectinous), hyaline and mucopolysaccharide loricae differ by chemical composition. There are also composite (pseudochitinous + mucopolysaccharide) and agglutinated loricae. The morphological features and associated protective properties of loricae and semi-loricae of sessile ciliates are also discussed. The increase in floatability of cells has been reported in literature as the main function of mucopolysaccharide and hyaline loricae in planktonic ciliates. It is the authors’ opinion that the main function of the lorica is to prevent the contact of extrusomes or other capturing organelles of unicellular predators or parasites from the cellular membrane of ciliates. It is also assumed that another important function of the semi-loricae and loricae in sessile ciliates is to protect joints between their stalk and zooid from hydrodynamic loads.
Особенности питания керчака-яока Myoxocephalus jaok (Cuvier, 1829) (Cottidae) и его место в трофической системе прикамчатских вод
Authors: Токранов А. М.
Published: October 2018

По материалам 1978–2008 гг. (975 желудков обработано количественно-весовым методом, около 2 тыс. желудков вскрыто и проанализировано в полевых условиях) рассмотрены особенности питания керчака-яока Myoxocephalus jaok в прикамчатских водах Охотского, Берингова морей и Тихого океана и предпринята попытка выяснить место этого вида рогатковых в трофической системе данного района. Показано, что керчак-яок характеризуется широким спектром питания (свыше 100 кормовых объектов), однако наибольшее значение в его рационе имеют рыбы (в среднем 64,1 % массы пищи) и десятиногие раки (32,2 %). Основу первых составляют камбалы Pleuronectidae (24,3 % массы пищи), минтай Theragra chalcogramma (14,4 %), тихоокеанская песчанка Ammodytes hexapterus (9,5 %) и рогатковые Cottidae (5,6 %); вторых ― крабы семейства Majidae (22,4 %) (главным образом краб-стригун Chionoecetes opilio (14,2 %) и краб-паук Hyas coarctatus (8,1 %)), а также крабы семейства Atelecyclidae (4,7 %) (преимущественно пятиугольный волосатый краб Telmessus cheiragonus (4,5 %)) и креветки семейства Crangonidae (3,1 %). Рассмотрены сезонные, локальные, межгодовые и возрастные изменения состава пищи керчака-яока. Установлено, что этот вид является факультативным хищником-засадчиком; ему свойственна высокая пластичность питания, дающая возможность использовать значительный набор пищевых компонентов. В трофической системе прикамчатских вод выделены звенья, формирующие биомассу керчака-яока.
Dynamic Stochastic General Equilibrium model for the Islamic economy
Authors: Dahani Khawla , Aboulaich Rajae
Published: October 2018

This article is concerned with the debate around the economic knowledge evolution and the role of ethics in economy. It reports on the 2008 crisis, the research literature reveals two main problems: the efficiency of the economic modeling and the failure of the ethical system.The authors explore the use of the new Dynamic Stochastic General Equilibrium “DSGE” model in the case of Islamic economy, it can enable to develop a new approach, taking into account the criticism of the models used before the crisis, and giving more importance to the ethical principles.The question is to know if the principles of Islamic economy feed into a sustainable economic system.The characteristic of this model lies in the consideration of Islamic principles, namely the abolition of interest rates and their replacement by the rate of return of the capital. In this perspective, it is supposed that the intervention of the monetary authorities is done by an unconventional approach. The model also distinguishes itself by the integration of Zakat. The model is applied in the case of Morocco.The results of simulations show that the introduction of these Islamic principles has no negative effects on the macroeconomic and financial conditions of Morocco and that the stability of the economic system is maintained.
Biopolymer Substrates in Buccal Drug Delivery: Current Status and Future Trend
Authors: Sun Bo , Wang Weijun , He Zhibin , Zhang Min , Kong Fangong , Sain Mohini
Published: October 2018

Background:

This paper provides a critical review of biopolymer-based substrates, especially the cellulose derivatives, for their application in buccal drug delivery. Drug delivery to the buccal mucous has the benefits of immobile muscle, abundant vascularization and rapid recovery, but not all the drugs can be administered through the buccal mucosa (e.g., macromolecular drugs), due to the low bioavailability caused by their large molecular size. This shortfall inspired the rapid development of drug-compounding technologies and the corresponding usage of biopolymer substrates.

Methods:

Cellulose derivatives have been extensively developed for drug manufacturing to facilitate its delivery. We engaged in structured research of cellulose-based drug compounding technologies. We summarized the characteristic cellulose derivatives which have been used as the biocompatible substrates in buccal delivery systems. The discussion of potential use of the rapidly-developed nanocellulose (NC) is also notable in this paper.

Results:

Seventy-eight papers were referenced in this perspective paper with the majority (sixty-five) published later than 2010. Forty-seven papers defined the buccal drug delivery systems and their substrates. Fifteen papers outlined the properties and applications of cellulose derivatives. Nanocellulose was introduced as a leading edge of nanomaterial with sixteen papers highlighted its adaptability in drug compounding for buccal delivery.

Conclusion:

The findings of this perspective paper proposed the potential use of cellulose derivatives, the typical kind of biopolymers, in the buccal drug delivery system for promoting the bioavailability of macromolecular drugs. Nanocellulose (NC) in particular was proposed as an innovative bio-binder/carrier for the controlled-release of drugs in buccal system.
Effect of Diterpenes on Hepatic System
Authors: Paz Márcia F.C.J. , Islam Muhammad T. , Tabrez Shams , Firoz Chelapram K. , Jabir Nasimudeen R. , Kamal Mohammad A. , Melo-Cavalcante Ana A.C. , Almeida Fernanda R.C.
Published: October 2018

Complication in the hepatic system is a major concern for human being. To control and keep the hepatic
system healthy, a number of measures, including drug treatments are considered. Diterpenes are essential
oils having promising antioxidant and cytotoxic properties along with their genotoxic and mutagenic effects.
These agents are good targets for health promotion, especially in the light of their potential organo-protectivity.
We searched in the databases, PUBMED and SCIENCE DIRECT from June 2011 to June 2016 for publishing
evidence on diterpenes and their effects on hepatic system. After sorting the data, activity-wise findings are discussed
in this current article. The results suggest that diterpenes have hepatoprotectivity property via antioxidant
and anti-inflammatory, antimicrobial, anticancer/antitumor, hypolipidemic, anti-apoptosis, autophagic, antimetastasize,
anti-proliferating, anti-fibrosis as well as receptor and serum biomarkers mediated pathways. On the
other hand, hepatoxic effects of diterpenes are also accounted with cytotoxicity, apoptotic cell death and downregulation
of cytochrome P450 systems. A number of important diterpenes have been reported in the literatures
that act on the hepatic system. Some of them exert toxic effects on the liver, especially in rodent model. Hence,
more extensive researches are recommended that will highlight their mechanism of action on the liver.
Protective Mechanisms of Butyrate on Inflammatory Bowel Disease
Authors: Silva João P.B. , Navegantes-Lima Kely C. , Oliveira Ana L.B. , Rodrigues Dávila V.S. , Gaspar Sílvia L.F. , Monteiro Valter V.S. , Moura Davi P. , Monteiro Marta C.
Published: October 2018

Inflammatory bowel disease (IBD) is a multifactorial chronic disease, commonly associated with alteration
in the composition and function of gut microbiota. This process can lead to a decreased production of short
chain fatty acids (SCFAs) by the gut microbiota, mainly butyrate, which is an important immunomodulatory
molecule in the intestine. Butyrogenic bacteria normally produces butyrate through carbohydrate fermentation or
amino acids degradation pathways. This molecule plays an important protective role in intestinal homeostasis
acting in both adaptive immunity and innate immunity. This review summarizes the current knowledge about the
role of butyrate on the development of IBD and the protective mechanisms of this metabolite on the intestinal
mucosa and the whole body, as reported by in vitro and in vivo studies. Thus, butyrate can regulate the activation
of regulatory T cells, increasing the acetylation of histones and decreasing the activation of NF-κB. In addition, it
can also stimulate the mucus production from epithelial cells and the rearrangement of tight junction proteins.
Complementary Functional Strategy for Modulation of Human Gut Microbiota
Authors: Vamanu Emanuel
Published: October 2018

Two pathologies commonly associated with gut microbiota dysbiosis are type 2 diabetes and cardiovascular
diseases. Since diet and medication are two important causes of microbiome fingerprint modifications,
new complementary and alternative methods can include wild edible mushrooms, which serve as functional products,
given their properties in modulating the microbial pattern at the colon level. A disturbance in microbial
balance translates into the occurrence of degenerative dysfunctions that are also associated with other pathologies,
such as obesity, colon cancer. The metagenomic study has enabled the identification of some competitive microbiological
and biochemical biomarkers which allow the development of innovative strategies in controling microbial
disbalance from human gut. Thus, the aim of this review was to present the significant findings related to
human microbiome modulation via the prebiotic effects of wild edible mushrooms as a complementary strategy to
modern treatment. Certain mushroom species have been approached and their effects on the microbiota fingerprint
of two major target groups are highlighted.
A Survey for Predicting Enzyme Family Classes Using Machine Learning Methods
Authors: Tan Jiu-Xin , Lv Hao , Wang Fang , Dao Fu-Ying , Chen Wei , Ding Hui
Published: October 2018

Enzymes are proteins that act as biological catalysts to speed up cellular biochemical processes. According to their main Enzyme Commission (EC) numbers, enzymes are divided into six categories: EC-1: oxidoreductase; EC-2: transferase; EC-3: hydrolase; EC-4: lyase; EC-5: isomerase and EC-6: synthetase. Different enzymes have different biological functions and acting objects. Therefore, knowing which family an enzyme belongs to can help infer its catalytic mechanism and provide information about the relevant biological function. With the large amount of protein sequences influxing into databanks in the post-genomics age, the annotation of the family for an enzyme is very important. Since the experimental methods are cost ineffective, bioinformatics tool will be a great help for accurately classifying the family of the enzymes. In this review, we summarized the application of machine learning methods in the prediction of enzyme family from different aspects. We hope that this review will provide insights and inspirations for the researches on enzyme family classification.
Natural Products for Vulvovaginal Candidiasis Treatment: Evidence from Clinical Trials
Authors: González-Burgos E. , Gómez-Serranillos M.P.
Published: October 2018

Background:

Candida albicans is an opportunistic yeast that causes more than 90% of all
vulvovaginal infections. Because of being inherently resistant to antifungals drugs such as azole derivatives,
the search for anti-Candida albicans agents with new pharmacological targets is considered as the
main therapeutic strategy to prevent and treat these types of infections. In this context, products of natural
origin are a promising source of compounds with antifungal activity.

Objective:

The current review analyzes clinical evidence on the effectiveness of natural products in the
vulvovaginal Candida albicans infections.

Method:

A literature review in the electronic databases PubMed, Google Scholar, Cochrane Library
Plus, Web of Science, Latin American and Caribbean Literature on Health Sciences (Lilacs) and Scientific
Electronic Library Online (SciELO) using the search terms “Natural Products”, “Phytotherapy”,
“Vulvovaginal Candidiasis” and “Clinical Trials” together with the Boolean term ‘AND’ was performed.
English, Spanish and French articles without restriction of date of publication were considered.

Results:

A total of 13 clinical trials (most of them randomized clinical trials which used azoles as control
group) evaluated the anti-Candida activity of a total of 11 different natural products (i.e. Zataria
multiflora essential oils, Ageratina pichinchensis and Solanum nigrescens extracts and saponins from
Solanum chrysotrichum, among others) against vulvovaginitis have been included in the current review.

Conclusion:

Because of the few clinical trials it is difficult to establish a consistent conclusion about the
effectiveness of natural products in the prevention and treatment of vulvovaginitis caused by Candida
albicans. Future studies should be aimed at evaluating new natural products as well as conducting more
clinical research with promising natural substances already investigated in clinical trials.
Paracoccidioides spp. and Histoplasma capsulatum: Current and New Perspectives for Diagnosis and Treatment
Authors: Taborda C.P. , Buccheri R. , Benard G. , Duarte-Neto A.N. , Nosanchuk J.D. , Travassos L.R.
Published: October 2018

The thermally-dimorphic systemic fungal group includes several important human pathogens:
Blastomyces dermatitides, Coccidioides immitis and C. posadasii, Histoplasma capsulatum, Paracoccidioides
brasiliensis, P. lutzii, and Talaromyces (Penicillium) marneffei. They usually are geographically
restricted and have natural habitats in soil or in plants, and when fungal propagules invade mammalian
host by inhalation, they initiate an inflammatory reaction that can result in self-resolution of the
infection or cause an acute or chronic disease. In the setting of the AIDS pandemic and the developments
in modern medicine, such as immunosuppressive therapy in cancer surgery patients and in transplantation
and autoimmune diseases, the incidence of endemic mycoses has progressively increased. Another important
factor of the increased incidence of systemic mycoses in certain regions is the progressive devastation
of tropical and subtropical forests. In this review, we focus on two of the most important systemic
mycoses: paracoccidioidomycosis and histoplasmosis, and their major characteristics in epidemiology,
clinical aspects and laboratorial diagnosis.
Molecular Conformational Analysis, Spectroscopic Characterization, Intramolecular Hydrogen Bonding and Natural Bond Analysis of (E,Z)-2-(4- Amino-5-oxo-3-(thiophene-2-ylmethyl)-4,5-dihydro-1,2,4-triazole-1-yl)-N'- (thiophene-2-ylmethylene) Acetohydrazide
Authors: Atalay Abdurrahman , Çelik Fatih , Ünver Yasemin , Sancak Kemal , Kaygusuz Kamil
Published: October 2018

The optimized structural parameters and electronic properties including frontier molecular
orbital (FMO) analysis, molecular electrostatic potential and NBO charge analysis of (E,Z)-2-(4-
amino-5-oxo-3-(thiophene-2-ylmethyl)-4,5-dihydro-1,2,4-triazole-1-yl)-N'-(thiophene-2-ylmethylene)
acetohydrazide were investigated by using density functional theory (DFT) at B3LYP/6-311++G(d,p)
level. The global reactivity parameters were evaluated in accordance with the energy values of HOMO
and LUMO of each determined conformer. The molecule was experimentally characterized by means
of FT-IR and NMR spectroscopic methods and also theoretically by B3LYP/6-311++G(d,p) and
B3LYP/cc-pVTZ method (FT-IR and NMR, respectively). The theoretical results of spectroscopic
analysis show good agreement with experimental outcomes. The natural bond orbital (NBO) analyses
for studied conformers were performed at B3LYP/6-311++G(d,p) level to find hyperconjugative interactions
as well as intramolecular hydrogen bond interaction. Besides, theoretical results indicate that
the optimized structure of conformer E and Z possesses N‒H···N and N‒H···S weak hydrogen bonding,
respectively.
Facile One-Pot Friedlander Synthesis of Functionalized Quinolines using Graphene Oxide Carbocatalyst
Authors: Singhal Anchal , Kumari Pratibha , Nisa Kharu
Published: October 2018

Background:

Quinolines represent an important class of bioactive molecules which are present in
various synthetic drugs, biologically active natural compounds and pharmaceuticals. Quinolines find their potential
applications in various chemical and biomedical fields. Thereby, the demand for more efficient and simple
methodologies for the synthesis of quinolines is growing rapidly.

Objective: The green one-pot Friedlander Synthesis of Functionalized Quinolines has been demonstrated by
using graphene oxide as a carbocatalyst.

Method: The graphene oxide catalyzed condensation reaction of 2–aminoaryl carbonyl compounds with different
cyclic/ acyclic/ aromatic carbonyl compounds in methanol at 70°C affords different quinoline derivatives.

Results: The reaction has been examined in different protic and aprotic solvents and the best yield of quinoline
is observed in methanol at 70°C.

Conclusion:

The present method of quinoline synthesis offers various advantages over other reported methods
such as short reaction time, high yield of product, recycling of catalyst and simple separation procedure. The
graphene oxide carbocatalyst can be easily recovered from the reaction mixture by centrifugation and then can
be reused several times without any significant loss in its activity.
DNA Cleavage Properties, Antimicrobial and Cytotoxic Activity and 4D-QSAR Analysis of Some Pyrazole Derivatives
Authors: Kopru Semiha , Küp Fatma Ozturk , Sabanci Nazmiye , Çadir Mehmet , Bulut Duygu Cemre , Duman Fatih , İlhan Ilhan Ozer , Saripinar Emin
Published: October 2018

Background:

An extensive study of 19 pyrazole derivatives were carried out based on the evaluation of DNA cleavage properties, antimicrobial and cytotoxic activities and 4D-QSAR analysis including pharmacophore modelling and bioactivity prediction by the Electron Conformational-Genetic Algorithm (EC-GA) method.

Methods:

The pyrazole derivatives were tested for their antimicrobial activity against certain human pathogenic organisms using the agar diffusion procedure. Binding of compounds with DNA was studied by gel electrophoresis using plasmid pBR322 DNA. The compounds were investigated for their properties as cytotoxic agents by brine shrimp lethality bioassay. To identify the pharmacophoric elements and find out the most important molecular properties which govern cytotoxic activity, multiple conformations of the compounds were used.

Results:

The urea derivatives of pyrazole had higher antibacterial activities against Gram-negative bacteria than against Gram-positive bacteria. Many of the compounds were found to cleave plasmid pBR322 DNA from the supercoiled form to the nicked circular. The cytotoxicity values of the compounds ranged from 13.87 to 84.1 µg/mL. The generated QSAR model was evaluated through the use of the Leave-One-Out Cross Validation (LOO-CV) method. A statistically significant and considerably predictive QSAR model was obtained with 4- descriptors resulting in R2 training =0.8223, R2 test =0.9346, q2=0.6201, q2 ext1=0.8672, q2 ext2= 0.8662 and q2 ext3=0.9511.

Discussion:

The generated model demonstrates that geometrical parameters are more correlated with cytotoxic activity. The resulting EC-GA model would provide benefits to design novel bioactive pyrazole derivatives which are more potent and have less side effects.

Conclusion:

It is believed that the generated QSAR model gives insight into developing new more potent pyrazole derivative drugs.
New Procaspase Activating Compound (PAC-1) Like Molecules as Potent Antitumoral Agents Against Lung Cancer
Authors: Yurttaş Leyla , Öztürk Ömer , Cantürk Zerrin
Published: October 2018

Background:

In this study, novel ortho-hydroxy N-acyl hydrazone moiety including
compounds (3a-l) were designed, based on procaspase activating compound (PAC-1) which is a
small molecule known with antitumor activity. The antitumor activity was evaluated on A549 (human
lung cancer cell line) and CCD 19Lu (human lung normal cell line).

Methods:

Twelve N'-arylidene-2-[4-(methylsulfonyl)piperazin-1-yl]acetohydrazide derivatives
(3a-l) were synthesized starting from ethyl 1-piperazinylacetate. All compounds were tested using
MTT method and Xcelligence-Real time cell analysis system (RTCA DP) to determine their antitumor
activity.

Results:

Some physicochemical properties of four active compounds were also predicted using
MolSoft, PreADMET and PROTOX software. Four of them, 3h, 3j, 3k and 3l bearing 3-hydroxy,
4-dimethylamino, 2,6-dichloro and 3,4-dichloro substituents in order exhibited selective cytotoxicity.

Conclusion:

Eligible values were obtained in the specified ranges as to be an oral/intravenous drug
considering the physicochemical calculations.
The Impact of Depressive Symptoms on the Quality of Life of Patients with Type 2 Diabetes in Jazan Region, KSA
Authors: Albasheer Osama B.
Published: October 2018

Background:

The purpose of this study is to determine the impact of depressive symptoms
on the quality of life of type 2 diabetic patients (T2DM).

Methods:

A cross-sectional study of 332 T2DM patients aged ≥18 years living in Jazan region of Saudi
Arabia was conducted. Validated questionnaire was used for demographic and disease characteristics.
Depressive symptoms of the participants were assessed using the Patient Health Questionnaire (PHQ-9).
The Quality of Life Enjoyment and Satisfaction Questionnaire-Short Form (Q-LES-Q-SF) was utilized
to assess the degree of life enjoyment and satisfaction.

Results:

Depressive symptoms were observed in 34.7% (112) of the total participants. The overall sense
of wellbeing (mean 3.23, P. value 0.000), physical (mean 3.37, P. value 0.003), psychosocial (mean
2.99 P. value 0.000) and social domains (mean 3.53, P. value 0.000) of quality of life were significantly
reduced in T2DM patients with depressive symptoms.

Conclusion:

The impact of depressive symptoms on quality of life of T2DM patients was more significant
than the impact of diabetes alone. Symptoms of depression reduce the individual coping and hence
reduce functioning. This study emphasizes the vital importance of an integrated holistic approach that
addresses both the practical and emotional issues in diabetes care.
Myxedema Heart Disease: A Rare Disease Entity: Case Report and Brief Review of the Literature
Authors: Chaudhry Muhammad Ali , Grazette Luanda , Fong Michael W.
Published: October 2018

Background:

Myxedema heart disease is an extremely rare disease entity and should be
suspected in patients with unexplained heart failure refractory to conventional treatment.
Myxedema coma with co- existent heart disease is not well known and very few cases have been
reported.

Conclusion:

Here, we present an interesting case of myxedema coma with severe valvular cardiomyopathy
followed by a concise review of the literature with special emphasis on epidemiology,
pathophysiology, diagnosis and therapeutic modalities.
In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans
Authors: de Azambuja Gabriel O. , Svetaz Laura , Gonçalves Itamar L. , Corbelini Patricia F. , von Poser Gilsane L. , Kawano Daniel F. , Zacchino Susana , Eifler-Lima Vera L.
Published: October 2018

Background:

Since the Monastrol discovery in 1999 as the first inhibitor of Eg5, functionalized
dihydropyrimidinones/thiones (DHPMs) have emerged as prototypes for drug design in different
targets. The present work aimed to evaluate the antifungal activity of a chemical library of DHPMs.

Methods:

The compounds were obtained employing Biginelli reaction. Their antifungal activities were
assessed against C. neoformans and C. albicans.

Results:

The compounds 1-i and 1-k inhibited moderately the fungal growth of C. neoformans, with
compound 2-k presenting MIC80 values of 62.5-125 µg·mL-1. Considering activity against C. albicans,
the compounds 1-i and 1-n present an MIC50 value of 125-250 µg·mL-1.

Conclusion:

The changes performed in DHPM scaffold appear to be valuable for generating compounds
with potential antifungal effect.
Improved Solubility of Itraconazole Binary Dispersions using Neem Gum: Development and Characterization of Topical Gel
Authors: Nagpal Manju , Raj Nisha , Thakur Gurjeet Singh , Aggarwal Geeta
Published: October 2018

Background:

Itraconazole is a triazole derivative and possesses structural similarities to the
azole group (imidazoles and triazoles). It is a broad spectrum fungistatic. It belongs to BCS class II
category i.e. it has poor solubility and high permeability.

Objective:

Dissolution enhancement of poorly soluble itraconazole using purified neem gum as a natural
carrier via binary dispersions and other methods was studied. Topical gel formulations of binary dispersions
were developed and evaluated for in vitro and in vivo antifungal activity.

Methods:

Five batches of solid dispersions (SD1-SD5) in various ratios of drug: neem gum were prepared
by the solvent evaporation technique. Other mixtures were also prepared by kneading, cogrinding,
physical mixing methods and evaluated further. Topical gel formulations were further developed
and evaluated for antifungal activity (both in vitro and in vivo).

Results:

Equilibrium solubility studies of various mixtures indicated SD3 (1:3) as the optimum batch
out of all solid dispersion batches. Equilibrium solubility studies of mixtures (KM, CGM, PM, SM)
indicated significant solubility enhancement of kneading mixture in comparison to other mixtures. FTIR
studies indicated no interaction of the drug to the polymer. DSC, SEM and XRD studies indicated a
transition from crystalline to the amorphous state of the drug. SD3 batch showed remarkably improved
dissolution characteristics (100% drug release in 1.5 h) in comparison to the pure drug (38% in 2h).
Further, the topical gel of SD3 was evaluated for in vitro diffusion, in vitro and in vivo antifungal activity.
Sustained drug release (53% in 24 h) was observed in SD3 based gel formulation which is significantly
higher than that in comparison to pure drug based gel (30% in 24 h). The increased area of zone
of inhibition of SD3 based gel indicated better antifungal activity of the SD3 gel formulation. Further
histopathology examination of skin specimens indicated enhanced efficacy of SD3 based gel in comparison
to pure drug based gel.

Conclusion:

Solid dispersion based topical gel formulation exhibits better antifungal activity in comparison
to pure drug based gel.
Characterization, Bioactive Compounds and Antioxidant Potential of Açaí (Euterpe oleracea) Genotypes
Authors: do C.M.R. Torma Priscila , de L. Monteiro Patric , Carvalho Ana V. , Flôres Simone H. , Augusti Paula R. , de O. Rios Alessandro
Published: October 2018

Background:

Açaí (Euterpe oleracea), a “superfruit” consumed worldwide, is a Brazilian
Amazon native fruit, with high nutritive value due to its high content of lipids, proteins, and fibers, besides
bioactive compounds, such as anthocyanins, carotenoids and phenolic compounds in its composition
associated with biological action beneficial to health. The increased consumption of this fruit has
stimulated breeding programs in the search of plants and fruits with higher productivity and bioactive
compounds, generating information for the development of new cultivars with improved attributes. This
work aimed to study six different genotypes of açaí, developed by the breeding program, evaluating
their physicochemical characteristics and proximate composition, bioactive compounds and antioxidant
activity.

Methods:

The genotypes were analyzed for titratable acidity, pH, total soluble solids and proximate
composition, such as moisture, protein, lipids, total fiber, carbohydrates and ashes contents. A spectrophotometric
method using Folin-Ciocalteau reagent performed the phenolic compounds analysis and
HPLC evaluated carotenoids and anthocyanins extracted exhaustively. The ABTS assay evaluated the
antioxidant activity.

Results:

The L06P13 and L09P09 genotype presented higher content of total fiber, carbohydrates, and
ashes when compared to the commercial sample used as a standard. Furthermore, L22P13 genotype
showed the highest content of total anthocyanins (6745.81 mg/100g), total carotenoids (118 μg/g) and
antioxidant activity (674.83 μM Trolox/g) when compared to commercial sample.

Conclusion:

The results revealed promising açaí genotypes and support the importance of advances in
the area of functional foods and breeding programs.
Hypoglycemia among Insulin-treated Patients with Diabetes: Egypt Cohort of IO HAT Study
Authors: El Hefnawy Mohamed Hesham Mohamed Fahmy , Abdelaaty Talaat Abd el Fattah , Bassyouni Atef Abdelmoniem , Saleem Hesham Magdeldin , Khalid Mohsen Mostafa Mussa , Toaima Dalia Nabil , Maree Mohamed Ahmed Gaber
Published: October 2018

Objectives:

The study aims to assess the real-world incidence of hypoglycemia in patients with Type 1 Diabetes Mellitus (T1DM) or Type 2 Diabetes Mellitus (T2DM) in Egypt cohort of the International Operations Hypoglycemia Assessment Tool (IO HAT) study.

Methods:

This is a non-interventional study to estimate hypoglycemia in eligible patients with T1DM or T2DM, aged ≥18 years and treated with insulin for >12 months, who have completed self-assessment questionnaires to record demography, treatment information, and hypoglycemia during the 6-month/4-week retrospective and 4-week prospective periods. Data on hypoglycemia for this sub-analysis were collected from DM patients of Egyptian cohort who were recruited in IO HAT study across 36 sites in Egypt between 22 Nov 2014 and 15 Apr 2015.

Results:

Percentage of patients who reported at least one hypoglycemic event in the prospective period was any: T1DM: 96.3% (95% confidence interval [CI]: 89.6%, 99.2%) and T2DM: 93.1% (95% CI: 89.8%, 95.6%) and severe: T1DM: 67.5% (95% CI: 56.1%, 77.6%) and T2DM: 64.2% (95% CI: 58.7%, 69.4%). An estimated rate of any and severe hypoglycemia in the prospective period was 63.3 (95% CI: 57.2, 69.9) events per patient year (PPY) and 28.9 (95% CI: 24.8, 33.4) events PPY, respectively, for patients with T1DM and 32.0 (95% CI: 29.8, 34.3) events PPY and 15.5 (95% CI: 14.0, 17.1) events PPY, respectively, for patients with T2DM. Hypoglycemic rate was independent of glycated hemoglobin levels.

Conclusion:

The self-reported hypoglycemia data from Egypt confirms that hypoglycemia is under-reported. The high impact of hypoglycemia on the Egyptian DM patients and healthcare system warrants patient education to prevent hypoglycemia.
Novel Diazenyl Containing Phenyl Styryl Ketone Derivatives As Antimicrobial Agents
Authors: Sivasankerreddy L. , Nagamani B. , Rajkumar T. , Babu M.S. , Subbaiah N.Y. , Harika M.S. , Nageswarao R.
Published: October 2018

Background:

Antibiotics play an important role in the treatment of infections to the humans
and at the same time, irrational, frequent prescription of higher antibiotics, change in gene
composition of microorganisms are all the reasons behind the development and introduction of new
antibiotics against different microorganisms.

Objective:

In this project, an attempt has been made to synthesize some derivatives of diazenyl
containing phenyl styryl ketones and also their in vitro screening was conducted against Mycobacterium
tuberculosis, Escherichia coli, Klebsiella pneumonia, Bacillus subtilis, Staphylococcus aureus,
Aspergillus niger and Candida albicans.

Methods:

Ten molecules were synthesized which are diazenyl containing chalcones. 4-
aminoacetophenone was diazotised and piperidine was coupled with the formed diazonium chloride.
Further, the acetoxy group underwent Claisen-Schmidt condensation with differently substituted
aldehydes to form the final compounds- the chalcones. The proposed chemical structures
were confirmed by different spectroscopic techniques like FTIR, 1H NMR and Mass spectroscopy.
TLC was used to know that the reactants were exhausted and the formation of the product occurred.
Sharp melting point of the compounds concludes the purity.

Results:

The MIC of the compounds 3CP, 3DP, 3EP and 3GP is 20 times the MIC of the standard
fluconazole drug against Aspergillus niger. The compound 3GP is as equipotent as the standard
drug Pyrazinamide with MIC of 3.12 µg/ml against Mycobacterium tuberculosis.

Conclusion:

The results are quite promising which on further studies may lead to drug molecules
against different microorganisms. Especially, 3EP can be considered as a broad spectrum agent due
to its potent activity against different microorganisms like Staphylococcus aureus, Escherichia
coli, Klebsiella pneumonia and Candida albicans.
ATC/DDD Directed Classification of Neural Ayurvedic Medicines
Authors: Arora Malika , Kaur Manpreet , Bansal Parveen , Arora Manish
Published: October 2018

Introduction:

People have been using herbs for health care since Vedic times. Due to resurgence of ayurveda, utilization and consumption of herbal medicines is tremendously increasing leading to a significant percentage of the pharmaceutical market. The huge commercial benefits of herbal products are capturing the interest of pharmaceutical companies worldwide. Hence the safety and quality of medicinal plant materials and finished herbal medicinal products have become a major concern for health authorities, pharmaceutical industries as well as to the public. Presently, plenty of clinical trials are being conducted on herbal medicines; however, absence of harmonized classification has led to various confusions. The most important concern is the disputed identity of ayurvedic formulations sold under different brand names in different regions of the country and world. Recently, allopathic medicines have been classified by WHO on the basis of ATC/DDD (Anatomical- Therapeutic-Chemical/Daily Defined Dose) pattern of classification. The absence of such type of classification for ayurvedic products creates a situation of non recognition of these products in the international market. Hence there is a need to develop a classification system that is on the lines of ATC/DDD so that particular herb may qualify a product to be recognised under one name all over the world.

Materials and Methods:

Keeping in view the above scenario, a classification system is being proposed for ayurvedic products. The ayurvedic formulations and their site of action have been searched from various Ayurvedic texts. Internet sources such as Pubmed, Google Scholar, JSTOR etc.

Results:

The major reason for adopting similar classification for herbal medicines is that ayurvedic texts given by various scholars are published in Sanskrit or in the local/regional languages which make it difficult for the researchers to access, understand and interpret the knowledge shared.

Conclusion:

It is utmost important to generate such classification for herbal medicines as it will generate a classification data which can further be exploited for safety, efficacy as well as quality control purposes. Moreover, innovative classification will be helpful to provide standardized as well as a uniform way to classify the various herbal drugs and to generate new avenues for further ayurvedic research with more degree of precision. The classification will enable a product to be known under one banner/name at international level. Since the market is flooded with formulations related with neural disorders, hence herbal products used in neural disorders have been taken in the first phase.
INFLUENCE OF CONGRESS IN SUPPORTING ON ENVIRONMENTAL ISSUE IN RONALD REAGAN ADMINISTRATION
Authors: Fatkurrohman Fatkurrohman
Published: October 2018

This research aims to analyze the influence of the United States Congress in influencing the policies of the Ronald Reagan administration in ratifying the Montreal Protocol. This research uses one of the models proposed by Graham T. Allison, a bureaucratic political model. This model is used to analyze the political process associated with the bargaining position and compromise between the actors involved in the governments of Ronald Reagan, Congress and DuPont (the company). To understand how these actors play their role in the domestic political process, researchers use qualitative research by collecting data in the form of books, journals and other documents. Explorative methods are used to explore related argumentative basics related to the political process that occurs between the three actors. The result of this study shows that Congress in the era of the Ronald Reagan administration, especially in the House of Representatives is more dominated than the Democratic Party than the Republicans, while in the Senate during 1981-1989, the Democratic Party was only dominant in 1987-1989. The important three things in this research that all actors obtained their interests. Firstly, it is DuPont Company. It received benefits from CFC (Chlorofluorocarbon) changing such as HFC (Hydrofluorocarbon), HC (Hydrocarbon), and PFC (Perfluorocarbon). Secondly, it is Congress Agency. It which was dominated by the members of Democratic Party that stressing on environmental issues could reach their political program such as environmental protection. Thirdly, it is the Executive Agency. It gained benefits in saving of budget $503 million up to $2,8 billion for treating many diseases such as cortical cataract cancer, decrease of body immunity, and environmental problems.
PEMBERDAYAAN MASYARAKAT BERBASIS LINGKUNGAN HIDUP DI DESA MARGALAKSANA KABUPATEN BANDUNG BARAT
Authors: Subekti Priyo , Setianti Yanti , Hafiar Hanny
Published: October 2018

The empowerment approach becomes the main base of West Bandung Regency Government in the development of society to welcome the development of industrial estate. Empowerment has the meaning of generating resources, opportunities, knowledge, and skills to increase capacity in determining the future. Researchers are interested in conducting initial mapping in advance about environmental conditions, socio-economic conditions, government policies, responses, and community needs related to the development of industrial parks. The community empowerment conducted by the working group working together with the agriculture department, Disperindag, and BPWC and getting full support from the village of Margalaksana itself. There are many activities conducted by the working group by utilizing the natural potential that exist in Margalaksana Village. Some potentials of the Community Empowerment Program in Margalaksana Village: 1) The potency of fish using floating net pond in Cirata reservoir; 2) The potency of batik; 3) The potency of water hyacinth waste; and 4) The potency of tourism. Human capital plays a major role in as a modifying factor of community resources in achieving the success of the empowerment process. Good human capital is characterized by the level of education that able to provide motivation so as to develop independence in the community.
EDITORIAL
Authors: Maarif Samsul
Published: October 2018

Edisi ini membahas delapan (8) topik yang berbeda, tetapi memiliki benang merah pada hubungan politik, lingkungan, dan ekonomi. Tiga artikel permata secara khusus menunjukkan hubungan langsung antara politik (dan kebijakan) dan lingkungan. Artikel pertama (Genta Mahardhika Rozalinna dan Lutfi Amiruddin) membahas tentang politisasi lingkungan oleh Perhutani di Jawa Timur, artikel kedua (Fatkurrohman) membahas tentang peran Kongres Amerika dalam mendukung kebijakan lingkungan pemerintah Ronald Reagon. Artikel ketiga (Endiarjati Dewandaru Sadono dan kawan-kawan) menunjukkan upaya Pemerintah Daerah Istimewa Yogyakarta dalam mengemban amanat RPJMN 2015-2019 tentang pemenuhan kebutuhan warga atas air. Penulis secara khusus meneliti empat desa untuk mengevaluasi kesiapannya sebagaimana dicanangkan Pemda. Hasilnya ditunjukkan bahwa keempatnya tampak belum siap dan menyarankan agar program desa tersebut diintegrasikan dengan program BUMDes.
Importance of assessing and adjusting for cross-study heterogeneity in network meta-analysis: a case study of psoriasis
Authors: Cameron Chris , Hutton Brian , Druchok Cheryl , McElligott Sean , Nair Sandhya , Schubert Agata , Situ Aaron , Varu Abhishek , Villacorta Reggie
Published: October 2018

Aim:
The importance of adjusting for cross-study heterogeneity when conducting network meta-analyses (NMAs) was demonstrated using a case study of biologic therapies for moderate-to-severe plaque psoriasis.
Methods:
Bayesian NMAs were conducted for Psoriasis Area and Severity Index 90 response. Several covariates were considered to account for cross-trial differences: baseline risk (i.e., placebo response), prior biologic use, body weight, psoriasis duration, age, race and baseline Psoriasis Area and Severity Index score. Model fit was evaluated.
Results:
The baseline risk-adjusted NMA, which adjusts for multiple observed and unobserved effect modifiers, was associated with the best model fit. Lack of adjustment for cross-trial differences led to different clinical interpretations of findings.
Conclusion:
Failure to adjust for cross-trial differences in NMA can have important implications for clinical interpretations when studying the comparative efficacy of healthcare interventions.
A PILOT ANALYSIS: CAN THE BULGARIAN SPLIT-SQUAT POTENTIATE SPRINT ACCELERATION IN STRENGTH-TRAINED MEN?
Authors: Lockie Robert George , Orjalo Ashley , Moreno Matthew
Published: October 2018

This study determined whether a five repetition-maximum Bulgarian split-squat (5RM BSS) could potentiate a 0-5, 0-10, and 0-20 m (meter) sprint performance. Seven men were assessed in the 5RM BSS (a linear position transducer measured peak power [PP] and force [PF] for each leg), and completed two post activation potentiation (PAP) sessions. One session involved a control condition (CC) of 4 minutes (min) rest; the other the 5RM BSS. Participants were assessed in baseline sprints, and sprints of 15 seconds, 2, 4, 8, 12, and 16 min post-PAP intervention. A repeated measures ANOVA (p < 0.05) calculated significant changes in sprint times. The best potentiated time for each interval was also compared to the baseline. Spearman’s correlations (r; p < 0.05) calculated relationships between absolute and relative strength, PP and PF, with percent potentiation in sprint times. The BSS did not potentiate speed at any time, although there was great individual variation. The best 0-5 m time was significantly different from the baseline (p = 0.022), with no differences between PAP conditions. Significant correlations were found between strength and sprint potentiation at 16 min for the 0-5 m interval, and at 8 min and the best times for the 0-20 m interval (r = -0.786 to -0.893). There were correlations between PP and PF for each leg with sprint potentiation from 2-12 min across all intervals (r = -0.786 to -0.964). Stronger individuals who generate greater PP and PF in a 5RM BSS will be more likely to potentiate 20-m sprint performance.