bluuebunny/crossref_metadata_2025_split huggingface dataset:
Two novel lupane triterpenoids from Paullinia pinnata L. with fibroblast stimulatory activity
Authors: Annan Kofi , Houghton Peter J 
Published: September 2015

Abstract

Objectives
Novel lupane triterpenoids from Paullinia pinnata L., a Ghanaian plant traditionally used for wound healing, were examined for in-vitro fibroblast stimulatory activity using the 142BR cell line.

Methods
Bioactivity-guided isolation of the crude extract of P. pinnata L. was carried out in order to determine the nature of the compounds responsible for the stimulation of fibroblast proliferation.

Key findings
Two novel compounds were isolated and characterised, namely, 6β-(3′-methoxy-4′-hydroxybenzoyl)-lup-20(29)-ene-one (1) and 6β-(3′-methoxy-4′-hydroxybenzoyl)-lup-20(29)-ene-ol (2), together with three known compounds, friedelin (3), β-sitosterol (4) and β-sitosterol-3-d-glucoside (5). The methanol extract of the roots of P. pinnata caused a significant in-vitro increase (94%) in 142BR cell line proliferation at 20 µg/ml compared with the control.

Conclusions
Compounds 1 and 2, which were isolated from the active chloroform fraction, have not previously been reported and showed a dose-dependent increase in proliferation of 142BR cells up to 3 µm; compounds 3, 4 and 5 had no effect on the 142BR cell line at the concentrations tested.
Transdermal iontophoretic delivery of a novel series of dopamine agonists in vitro: physicochemical considerations
Authors: Ackaert Oliver W , De Graan Jeroen , Capancioni Romano , Dijkstra Durk , Danhof Meindert , Bouwstra Joke A 
Published: September 2015

Abstract

Objectives
The transdermal iontophoretic delivery of a novel series of 2- aminotetralins and chromanamine-based dopamine agonists was investigated in vitro.

Methods
Systematic structural modifications allowed us to investigate their effect on solubility in the donor phase and iontophoretic delivery across human skin. Transport profiles were analysed with nonlinear mixed effect modelling, utilizing an extension to an existing compartmental model. Furthermore, relationships between physicochemical properties and transport parameters were addressed.

Key findings
A solubility increase was observed: 5,6-di-OH-DPAT &lt; 5-OH-MPAT &lt; 5-OH-EPAT &lt; 8-OH-DPAC. The structure significantly affected the iontophoretic delivery across human stratum corneum and dermatomed human skin with the highest flux for 5-OH-EPAT and 5-OH-MPAT. The extended model with two skin release constants (KR1, KR2) described more adequately iontophoretic transport profiles than the existing model with one release constant. The extended model suggested two parallel transport pathways during current application. Across human stratum corneum, the electrophoretic mobility, measured with capillary electrophoresis, showed a linear relationship with the electromigrative flux and the zero-order iontophoretic mass input into the skin (I0).

Conclusions
Combining transport parameters (I0, KR1 and KR2), predicted from physicochemical properties, with compartmental modelling provided a powerful tool to simulate iontophoretic transport profiles for screening potential candidates and designing experiments.
Surface tension and wettability in transdermal delivery: a study on the in-vitro permeation of haloperidol with cyclodextrin across human epidermis
Authors: Azarbayjani Anahita Fathi , Lin Haishu , Yap Chun Wei , Chan Yew Weng , Chan Sui Yung 
Published: September 2015

Abstract

Objectives
The aim of this work was to study the effect of surface tension and contact angle on the permeation of haloperidol across human skin using cyclodextrin derivatives.

Methods
Surface tension and contact angle of randomly methylated β-cyclodextrin (RM β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) solutions were measured. Haloperidol solubility and molecular modelling were carried out using the two cyclodextrin derivatives. In-vitro skin permeation was carried out using human skin models.

Key findings
The highest increase in drug solubility was observed when the drug was in solution with pH 5 when compared to non-ionised solution, resulting in a 128-fold increase in the intrinsic solubility of the drug. Surface tension measurements indicate a surface-active effect for RM β-CD and HP β-CD. Contact angle measurements showed that vehicles with higher skin wettability increased the contact of the drug with the skin surface and therefore resulted in higher drug permeation across human epidermis.

Conclusions
It is concluded that transdermal flux of a drug through the skin may be optimised by controlling surface tension, drug solubility and skin wettability.
Chitosan-coated antifungal formulations for nebulisation
Authors: Albasarah Yacoub Y , Somavarapu Satyanarayana , Stapleton Paul , Taylor Kevin M G 
Published: September 2015

Abstract

Objectives
The aim of this study was to produce and characterise amphotericin B (AmB) containing chitosan-coated liposomes, and to determine their delivery from an air-jet nebuliser.

Methods
Soya phosphatidylcholine : AmB (100 : 1) multilamellar vesicles were generated by dispersing ethanol-based proliposomes with 0.9% sodium chloride or different concentrations of chitosan chloride. These liposomes were compared with vesicles produced by the film hydration method and micelles. AmB loading, particle size, zeta potential and antifungal activity were determined for formulations, which were delivered into a two-stage impinger using a jet nebuliser.

Key findings
AmB incorporation was highest for liposomes produced from proliposomes and was greatest (approximately 80% loading) in chitosan-coated formulations. Following nebulisation, approximately 60% of the AmB was deposited in the lower stage of the two-stage impinger for liposomal formulations, for which the mean liposome size was reduced. Although AmB loading in deoxycholate micellar formulations was high (99%), a smaller dose of AmB was delivered to the lower stage of the two-stage impinger compared to chitosan-coated liposomes generated from proliposomes. Chitosan-coated and uncoated liposomes loaded with AmB had antifungal activities against Candida albicans and C. tropicalis similar to AmB deoxycholate micelles, with a minimum inhibitory concentration of 0.5 µg/ml.

Conclusions
This study has demonstrated that chitosan-coated liposomes, prepared by an ethanol-based proliposome method, are a promising carrier system for the delivery of AmB using an air-jet nebuliser, having a high drug-loading that is likely to be effectively delivered to the peripheral airways for the treatment of pulmonary fungal infections.
Investigation of solute permeation across hydrogels composed of poly(methyl vinyl ether-co-maleic acid) and poly(ethylene glycol)
Authors: Raj Singh Thakur Raghu , Woolfson A David , Donnelly Ryan F 
Published: September 2015

Abstract

Objectives
Swelling kinetics and solute permeation (theophylline, vitamin B12 and fluorescein sodium) of hydrogels composed of poly(methyl vinyl ether-co-maleic acid) (PMVE/MA) and poly(ethylene glycol) (PEG) are presented.

Methods
The effects of PMVE/MA and PEG 10 000 content on swelling behaviour (percentage swelling, the type of diffusion and swelling rate constant) were investigated in 0.1 m phosphate buffer. Network parameters, such as average molecular weight between crosslinks (Mc) and crosslink density, were evaluated.

Key findings
The percentage swelling and Mc of hydrogels increased with decrease in PMVE/MA content, where the water diffusion mechanism into the hydrogels was Class-II type. In contrast, increase in PMVE/MA content caused an increase in the crosslink density. Permeation of theophylline, vitamin B12 and fluorescein sodium, with increasing hydrodynamic radii, was studied through the equilibrium swollen hydrogels composed of PMVE/MA and PEG. In general, the permeability and diffusion coefficients of all three solutes decreased with increase in the PMVE/MA content. In addition, permeability and diffusion coefficient values increased with decreases in the hydrodynamic radii of the solute molecules.

Conclusions
The hydrogels have shown a change in swelling behaviour, crosslink density, Mc and solute permeation with change in PMVE/MA content, thus suggesting a potential application in controlled drug-delivery systems.
Enhancement of the intranasal delivery of insulin via a novel mucoadhesive Carbopol gel
Authors: El-Dakrouri Walaa Ahmed , Ibrahim Howida Kamal , Ghorab Mohamed Khaled , Ghorab Mahmoud Mohamed 
Published: September 2015

Abstract

Objectives
The objectives of this study were to develop an intranasal insulin gel using Carbopol homogenization rather than neutralization and to examine the effectiveness of the gel compared with a subcutaneous injection.

Methods
Four factors, namely the molecular weight of polyethylene glycol (PEG), the concentration of Carbopol, the temperature of preparation and the type of absorption enhancer, were evaluated for their effect on viscosity and in-vitro insulin release. Bioavailability of insulin from selected formulations was compared with an intranasal solution and subcutaneous injection in rabbits.

Key findings
Increasing the molecular weight of PEG and Carbopol concentration increased the gel viscosity and changed the release mechanism from diffusion to case II transport. Applying heat during preparation resulted in a lower viscosity gel and increased the in-vitro insulin release. Among the two enhancers studied, sodium deoxycholate resulted in a higher viscosity gel than Tween 80. In vivo, the intranasal gel showed a stronger and longer hypoglycaemic effect with 1.7- and 3.1-fold higher maximum decrease in blood glucose level and area above the curve, respectively, compared with the subcutaneous injection.

Conclusions
The homogenized Carbopol intranasal gel could be an efficient noninvasive way for insulin delivery but selection of gel components and method of preparation are critical for achieving the most desired effect.
The orally combined neuroprotective effects of sodium ferulate and borneol against transient global ischaemia in C57 BL/6J mice
Authors: Chen Xiao-hong , Lin Zhu-zhen , Liu An-min , Ye Jian-tao , Luo Yan , Luo Yu-yan , Mao Xue-xuan , Liu Pei-qing , Pi Rong-biao 
Published: September 2015

Abstract

Objectives
This study aimed to investigate the possible modification of the neuroprotective effect of sodium ferulate, when orally co-administered with borneol, in transient global cerebral ischaemia-induced functional, histological and cellular alterations in mice.

Methods
The bilateral common carotid artery occlusion was conducted in C57 BL/6J mice for 25 min. The mice were then subjected to a water maze test over an extended recovery period, followed by an assessment of neuronal loss in the CA1 region of the hippocampus (haematoxylin and eosin staining). The blood–brain barrier permeability (Evans blue tracing), brain oedema and oxidative stress were assayed and histological sections were also immunostained for gliofibrillar acid protein (GFAP) expression.

Key findings
The ischaemia reperfused mice were associated with long-lasting spatial learning deficits in the absence of other behavioural impairments and with neurodegeneration in the hippocampal CA1 region. However, the histological injuries were significantly attenuated by oral co-administration of sodium ferulate and borneol. Furthermore, combined treatment with sodium ferulate and borneol resulted in a significant reduction in brain oedema, GFAP-positive cells, malonaldialdehyde levels and blood–brain barrier permeability, but an increase in superoxide dismutase activity.

Conclusions
Borneol may have benefits for the neuroprotective effect of sodium ferulate against injury induced in the brain by ischaemia/reperfusion.
Systemic chemotherapy-induced microsatellite instability in the mononuclear cell fraction of women with breast cancer can be reproduced in vitro and abrogated by amifostine
Authors: Pinto Jorge L F , Fonseca Fernando L A , Marsicano Sarah R , Delgado Pamela O , Sant'Anna Aleksandra V L , Coelho Patrícia G , Maeda Patríca , Del Giglio Auro 
Published: September 2015

Abstract

Objectives
Microsatellite instability (MSI) induction by alkylating agent-based chemotherapy (ACHT) may underlie both tumor resistance to chemotherapy and secondary leukaemias in cancer patients. We investigated if ACHT could induce MSI in tumor-derived plasma-circulating DNA (pfDNA) and in normal peripheral blood mononuclear (PBMN) cells. We also evaluated if amifostine could interfere with this process in an in-vitro model.

Methods
MSI was determined in pfDNA, PBMN cells and urine cell-free DNA (ufDNA) of 33 breast cancer patients before and after ACHT. MCF-7 cells and PBMN from normal donors were exposed in vitro to melphalan, with or without amifostine.

Results
We observed at least one MSI event in PBMN cells, pfDNA or ufDNA of 87, 80 and 80% of patients, respectively. In vitro, melphalan induced MSI in both MCF-7 and normal PBMN cells. In PBMN cells, ACHT-induced MSI occurred together with a significant decrease in the expression of the DNA mismatch repair gene hMSH2. Amifostine decreased hMSH2 expression and also prevented MSI induction only in normal PBMN cells.

Conclusions
ACHT induced MSI in PBMN cells and in tumour-derived pfDNA. Because of its protective effect against ACHT induction of MSI in normal PBMN cells in vitro, amifostine may be a potential agent for preventing secondary leukaemias in patients exposed to ACHT.
Protection by apple peel polyphenols against indometacin-induced oxidative stress, mitochondrial damage and cytotoxicity in Caco-2 cells
Authors: Carrasco-Pozo Catalina , Gotteland Martin , Speisky Hernán 
Published: September 2015

Abstract

Objectives
Exposure of Caco-2 cells to indometacin can be a useful model to assess some of the cytotoxic events that appear to underlie the gastrointestinal lesions associated with the use of this anti-inflammatory agent. Using such a cellular model, we addressed here the cytoprotective potential of a recently standardized apple peel polyphenol extract, APPE.

Methods
We firstly characterized APPE in terms of its free radical scavenging and antioxidant properties, and subsequently investigated its potential to protect Caco-2 cells against the deleterious effects of indometacin on cellular oxidative status (redox state, malondialdehyde, glutathione (GSH) and oxidized glutathione (GSSG) levels), mitochondrial function (ATP and mitochondrial membrane potential) and cell viability (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction and lactate dehydrogenase (LDH) leakage). For comparative purposes, the free radical scavenging properties and reducing capacity of quercetin, epicatechin and rutin were also estimated.

Key findings
In the absence of APPE, indometacin induced mitochondrial perturbations (reducing ATP and the mitochondrial membrane potential), enhanced the oxidative status (decreasing the GSH/GSSG ratio and increasing dichlorofluorescein oxidation and malondialdehyde) and lowered the cell viability (decreasing MTT reduction and increasing LDH leakage). APPE, whether pre-added or co-incubated with indometacin, concentration-dependently prevented these mitochondrial, oxidative and cell viability alterations. Prompted by the recently recognized ability of indometacin to enhance the mitochondrial formation of reactive oxygen species, APPE was also characterized in terms of its free radical-scavenging capacity. APPE was found to actively scavenge O2·-, HO· and peroxyl radicals. Such free radical-scavenging activity of APPE suggests that its ability to protect mitochondria and prevent the oxidative and lytic damage induced by indometacin arises from its potent antioxidant capacity.

Conclusions
In Caco-2 cells APPE prevented mitochondrial oxidative and cell viability alterations induced by indometacin possibly through its ability to scavenge reactive oxygen species. These findings are of interest in view of the high prevalence of gastrointestinal side-effects associated with the use of conventional anti-inflammatory agents.
Cerebrospinal Fluid Biomarkers of Japanese Encephalitis
Authors: Sengupta Nabonita , Mukherjee Sriparna , Tripathi Piyush , Kumar Rashmi , Suryawanshi Amol Ratnakar , Basu Anirban 
Published: September 2015

Japanese encephalitis (JE) is the leading cause of viral encephalitis in Asia. Acute encephalitis syndrome (AES) is a group of central nervous system (CNS) disorders caused by a wide range of viruses, bacteria, fungi, chemicals and toxins. It is important to distinguish between various forms of infectious encephalitis with similar clinical manifestations in order to ensure specific and accurate diagnosis and development of subsequent therapeutic strategies. Cerebrospinal fluid (CSF) is in direct contact with the CNS and hence it is considered to be an excellent source for identifying biomarkers for various neurological disorders. With the recent advancement in proteomic methodologies, the field of biomarker research has received a remarkable boost. The present study identifies potential biomarkers for JE using a proteomics based approach. The CSF proteomes from ten patients each with JE and Non-JE acute encephalitis were analyzed by 2D gel electrophoresis followed by mass spectrometry. Vitamin D-binding protein (DBP), fibrinogen gamma chain, fibrinogen beta chain, complement C4-B, complement C3 and cytoplasmic actin were found to be significantly elevated in case of JE indicating severe disruption of the blood brain barrier and DBP can be suggested to be an important diagnostic marker.
Efficient Implementation of Collective Extended Producer Responsibility Legislation
Authors: Gui Luyi , Atasu Atalay , Ergun Özlem , Toktay L. Beril 
Published: September 2015

Extended producer responsibility (EPR) is a policy tool that holds producers financially responsible for the post-use collection, recycling, and disposal of their products. Many EPR implementations are collective—a large collection and recycling network (CRN) handles multiple producers’ products in order to benefit from scale and scope economies. The total cost is then allocated to producers based on metrics such as their return shares by weight. Such weight-based proportional allocation mechanisms are criticized in practice for not taking into account the heterogeneity in the costs imposed by different producers’ products. The consequence is cost allocations that impose higher costs on certain producer groups than they can achieve independently. This may lead some producers to break away from collective systems, resulting in fragmented systems with higher total cost. Yet cost efficiency is a key legislative and producer concern. To address this concern, this paper develops cost allocation mechanisms that induce participation in collective systems and maximize cost efficiency. The cost allocation mechanisms we propose consist of adjustments to the widely used return share method and include the weighing of return shares based on processing costs and the rewarding of capacity contributions to collective systems. We validate our theoretical results using Washington state EPR implementation data and provide insights into how these mechanisms can be implemented in practice. This paper was accepted by Serguei Netessine, operations management.
Examination of Turkish extreme athletes' personality traits in terms of gender and some demographic factors
Authors: Ceylan Merve , Altıparmak Ersin , Akçakoyun Fahri 
Published: September 2015

<p> The present study was conducted for the purpose of examining the personality traits of extreme athletes. In line with this purpose a total of 227 extreme athletes, as 86 female and 141 male athletes selected through judgment sampling, that either actively compete or trains to compete in any of the branches of snowboarding, snowkiting, kitesurfing, windsurfing, river kayaking, mountain biking, free diving, paragliding and rafting were included within the sample group of the study. Questionnaire applications were carried out in extreme sports facilities throughout the country.</p><p>Within the scope of the study, an 85-item short form of the Five Factor Personality Scale developed by Somer, Korkmaz and Tatar was used as the data collection tool. Data analysis was carried out by means of the SPSS 16.0 software and the percentages frequencies, mean, standard deviation and to find the differences between the sexes "independent t" test were calculated.</p><p>Examining the obtained results showed that the male athletes have higher extravertion level from female athletes (p &lt;0.05). This finding obtained in our study suggest that, in an essentially male-dominant society, the higher level of pressure women are subjected to in social, economic, cultural and psychological terms and the difficulties and pressure they experience in the working life are significant factors for women to be more introvert.</p><p> </p><p> </p><p><strong>Özet</strong></p><p>Bu araştırma, ekstrem sporcuların kişilik özelliklerinin incelemesi amacıyla yapılmıştır. Bu amaç doğrultusunda araştırmaya, yargısal örnekleme yöntemiyle seçilmiş, snowboard, snowkite, uçurtma sörfü, rüzgar sörfü, akarsu ve nehir kanosu, dağ bisikleti, serbest dalış, yamaç paraşütü, kaya tırmanışı ve rafting branşlarında yarışmacı olan ya da bir yarışmaya katılmak için hazırlık yapan, 86’sı kadın, 141’i erkek olmak üzere 227 ekstrem sporcu katılmıştır. Anket uygulamaları, ülke genelinde bulunan ekstrem spor tesislerinde gerçekleştirilmiştir.</p><p> Araştırmada veri toplamak amacıyla Somer, Korkmaz ve Tatar tarafından geliştirilen beş faktör kişilik envanterinin 85 sorudan oluşan kısa forumu kullanılmıştır. Elde edilen veriler SPSS programında kaydedilmiş, frekans, yüzde, aritmetik ortalama, standart sapma değerleri hesaplanmış ve cinsiyetler arası farklılığı bulmak için “independent samples t- test” kullanılarak yorumlanmıştır.</p><p>Elde edilen bulgular incelendiğinde, erkek sporcuların erkek sporcuların kadın sporculara oranla daha yüksek dışa dönük özellik gösterdiği görülmektedir (p &lt;0.05). Sonuç olarak; temelde erkek egemen bir toplumda, sosyal, ekonomik, kültürel ve psikolojik anlamda kadının daha çok baskıya maruz kalması, sosyal hayatında üstelendiği roller, iş hayatında karşılaşılan zorluk ve baskıların bir sonucu olarak, daha içe kapanık bir yapıya sahip olmalarında önemli bir etken olduğunu düşündürmektedir.</p>
Molecular Genetic Testing in Pain and Addiction: Facts, Fiction and Clinical Utility
Authors: Blum Kenneth , Hauser Mary , Fratantonio James , Badgaiyan Rajendra D. 
Published: September 2015

AbstractThe Brain Reward Cascade (BRC) is an interaction
of neurotransmitters and their respective genes to control
the amount of dopamine released within the brain.
Any variations within this pathway, whether genetic
or environmental (epigenetic), may result in addictive
behaviors as well as altered pain tolerance. While there
are many studies claiming a genetic association with
addiction and other behavioral infractions, defined
as Reward Deficiency Syndrome (RDS), not all are
scientifically accurate and in some case just wrong. Albeit
our bias, we discuss herein the facts and fictions behind
molecular genetic testing in RDS (including pain and
addiction) and the significance behind the development
of the Genetic Addiction Risk Score (GARSPREDX™), the
first test to accurately predict one’s genetic risk for RDS.
BiLipschitz Decomposition of Lipschitz Maps between Carnot Groups
Authors: Li Sean 
Published: September 2015

Abstract
Let f : G → H be a Lipschitz map between two Carnot groups. We show that if B is a ball of G,
then there exists a subset Z ⊂ B, whose image in H under f has small Hausdorff content, such that B\Z
can be decomposed into a controlled number of pieces, the restriction of f on each of which is quantitatively
biLipschitz. This extends a result of [14], which proved the same result, but with the restriction that G has an
appropriate discretization. We provide an example of a Carnot group not admitting such a discretization.