bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis and Biological Evaluation of the Matrine Derivatives as a Novel Family of Potential Anticancer Agents
Authors: Wang Jing , Liu Hang , Zhuo Xiao-Bin , Ye Guang-Ming , Zhao Qing-Jie 
Published: October 2019

Background:
FufangKushen injection’ was a Chinese Traditional anticancer drug,
which has been widely used to treat cancer in combination with other anticancer drugs.

Objective:
Our goal is to synthesize a series of novel 13-dithiocarbamates matrine derivatives using
matrine (1) as the lead compound, and evaluate the biological activities of the obtained compounds.

Method:
The in vitro cytotoxicity of the target compounds against three human cancer cell lines
(Hep3B, LM3 and BeL-7404) was evaluated. To investigate the mechanism of biological activity,
cell cycle analysis was performed.

Result:
The results revealed that compounds 6o and 6v displayed the most significant anticancer
activity against three cancer cell lines with IC50 values in the range of 3.42-8.05 μM, which
showed better activity than the parent compound (Matrine). SAR analysis indicated that the introduction
of a substituted amino dithiocarbamate might significantly enhance the antiproliferative
activity.

Conclusion:
During the newly synthesized compounds, matrine analog 6v exhibited a potent effect
against three human tumor cell lines. The mode of action of 6v was to inhibit the G0/G1 phase
arrest. Therefore, compound 6v has been selected as a novel-scaffold lead to further structural optimizations
or as a chemical probe for exploring anticancer pathways of this kind of compounds.
Synthesis of Novel 1,2-Dihydro-1,2,4-Triazin-6(5H)-one Derivatives as Anticancer Agents
Authors: Verma Tarawanti , Sinha Manish , Bansal Nitin 
Published: October 2019

Introduction:
Cancer is still an untreatable disease and the second leading cause of death
globally. The heterocyclic compounds have always played a major role in the anticancer drug discovery
program. 1,2,4-Triazine-6-ones is a heterocyclic privileged structure with diversified activities. In the
presented study, 21 novel 2,5-disubstituted-3-phenyl-1,2-dihydro-1,2,4-triazin-6 (5H)-one derivatives
(13(a-k), 18(a-j) and 21(a1-a4, b)) have been synthesized and tested for their anticancer activity.

Methods:
The 2,5-disubstituted-3-phenyl-1,2-dihydro-1,2,4-triazin-6(5H)-one derivatives (13(a-k),
18(a-j) and 21(a1-a4, b) were synthesized by refluxing substituted-2-phenyloxazol-5(4H)-one and hydrazine
derivatives. Substituted aldehydes were synthesized via Vilsmeier-Haack reaction, while substituted-
2-phenyloxazol-5(4H)-one derivatives were synthesized by Erlenmeyer Plochl azlactone synthesis.
Twenty-one compounds were selected and screened at the National Cancer Institute (NCI), USA,
for anticancer activity at a single high dose (10-5M) in full NCI 60 cell panel assay.

Results and Conclusion:
The selected compounds (13a, 13b, 13c, 13f, 13h, 13i, 13j, 18h, 18i, 21a4)
were found to be active against different cancer cell lines. The compound, 5-((5-chloro-3-methyl-1-
phenyl-1H-pyrazol-4-yl)methylene)-2-(4-nitrobenzoyl)-3-phenyl-1,2-dihydro-1,2,4-triazin-6(5H)-one
(13a) was found to be a potent anti-cancer agent as electron-rich moiety on phenyl at position 2 of triazine
nucleus, having a great impact on anticancer activity.
Effect of Hsp90 Inhibitor KW-2478 on HepG2 Cells
Authors: Chang Xiaomin , Zhao Xuerong , Wang Jianping , Ding Shi , Xiao Lijun , Zhao Enhong , Zheng Xin 
Published: October 2019

Objective:
The objectives of this study were to investigate the effects of proliferation, apoptosis, cell
cycle, invasion, and senescence of KW-2478 on HepG2 cells, and to explore the related mechanism of apoptosis
and the cell cycle.

Methods:
HepG2 cells (hepatocellular carcinoma cells) were cultured with KW-2478, at different doses and for
different times, in vitro. The MTT assay was used to detect the effect of KW-2478 on proliferation of HepG2
cells. Flow cytometry was used to determine the effects of KW-2478 on the cell cycle and apoptosis of HepG2
cells. The Transwell assay was used to determine the effect of KW-2478 on cell invasion. The β-galactosidase
assay tested the effect of low-dose KW-2478 on the senescence of HepG2 cells. Western blotting and the quantitative
polymerase chain reaction were used respectively to assess changes in protein and mRNA levels of related
factors in HepG2 cells after the KW-2478 treatment.

Results:
KW-2478 significantly inhibited proliferation of HepG2 cells. KW-2478 induced apoptosis and cell
cycle arrest of HepG2 cells, and inhibited the invasion of HepG2 cells; low dose KW-2478 promoted HepG2
senescence.

Conclusions:
KW-2478 inhibited the proliferation of HepG2 cells, induced apoptosis and cell cycle arrest, inhibited
invasion, and promoted senescence. KW-2478 affected the expression of related factors in the mitochondrial
apoptotic signaling and cell cycle-related regulatory pathways. KW-2478 downregulated the expression of
STAT3, which is a key factor in the JAK-STAT pathway, indicating that KW-2478 may affect the function of
HepG2 cells by downregulating STAT3.
3-Benzylbenzothiazolylidene Carbene Catalyzed Isomerization of Dimethyl Maleate to Dimethyl Fumarate: Experimental and Theoretical Results
Authors: Ojha Minita , Choudhary Shweta , Bansal Raj K. 
Published: October 2019

Background:
N-Heterocyclic Carbenes (NHCs) have emerged as ubiquitous species having
applications in a broad range of fields, including organocatalysis and organometallic chemistry. Since
Arduengo and co-workers first isolated a bottlable NHC, namely imidazol-2-ylidene derivative, these
nucleophilic species have attained a prominent place in synthetic organic chemistry. The NHC-induced
non-asymmetric catalysis has turned out to be a really fruitful area of research in recent years.

Methods and Results:
The quantitative aspects of the experimental and theoretical investigation of
isomerization of dimethyl maleate to dimethyl fumarate catalyzed by an N-heterocyclic carbene
(NHC), namely 3-benzylbenzothiazolylidene are being reported for the first time. Dimethyl maleate on
treating with 3-benzylbenzothiazolylidene carbene (10 mol%), generated in situ from the reaction of 3-
benzylbenzothiazolium bromide with triethylamine in diethyl ether at room temperature under nitrogen
atmosphere isomerizes quantitatively to dimethyl fumarate. Theoretical investigation of a model reaction
scheme at the wB97XD/6-31+G(d) level reveals that initial attack of the carbene, which is the ratedetermining
step, is followed by rotation about the C-C bond in preference to a higher activation free
energy path involving proton abstraction. The species so formed splits off the carbene to yield dimethyl
fumarate. Eyring equation has been used to rationalize the effect of temperature on the isomerization
rate.

Conclusions and Perspective:
3-Benzylbenzothiazolylidene carbene catalyzes the isomerization of
dimethyl maleate to its trans-isomer. This carbene can be used in other catalytic reactions, such as
acyloin condensation and Stetter reaction.
High Thoracic Epidural Analgesia as an Adjunct to General Anesthesia in Patients Undergoing Off-Pump Coronary Artery Bypass Grafting
Authors: Cetin Erdem , Iynem Alper , Unal Celal Selcuk , Demirdas Ertan 
Published: October 2019

Aim:
To investigate the effect of high thoracic epidural analgesia combined with general anesthesia on pain management and postoperative outcomes in patients undergoing off-pump Coronary Artery Bypass Grafting (CABG).

Materials and Methods:
Patients were divided into two groups; Group 1 received general anesthesia and high thoracic epidural anesthesia whereas Group 2 received general anesthesia alone during off-pump coronary artery bypass grafting. Epidural catheters were placed at least 6 hours before transfer to the operating room. An epidural analgesic solution of 0.25% bupivacaine and 10 µg/ml fentanyl was started as continuous infusion at 5 ml/hour and maintained for at least 12 hours after completion of surgery. A 10-cm visual analog scale was used to measure pain at 4th, 6th, 9th and 12th postoperative hours.

Results:
Mean time to extubation was similar between two groups (2.45±0.88 vs. 2.59±1.31 for Groups 1 and 2, respectively, p=0.90). In all measurements, mean Visual Analogue Scale VAS scores were significantly lower in Group 1 compared to Group 2 (6.50±1.53 vs. 4.09±1.83 at 4th hour, 6.62±1.55 vs. 3.71±1.85 at 6th hour, 5.83±1.40 vs. 2.93±1.54 at 9th hour and 4.41±1.97 vs. 2.50±1.19 at 12th hour, p<0.001 in each comparison).

Conclusion:
Continuous high thoracic epidural analgesia seems to be a good adjunct to general anesthesia, as its pain relief effect becomes obvious at 4th postoperative hour and lasts at least 12th postoperative hour.
Effectiveness of an Educational Intervention in Reducing New International Postgraduates’ Acculturative Stress in Malaysian Public Universities: Protocol for a Cluster Randomized Controlled Trial
Authors: Al-Jaberi Musheer Abdulwahid , Juni Muhamad Hanafiah , Kadir Shahar Hayati , Ismail Siti Irma Fadhilah , Saeed Murad Abdu , Ying Lim Poh 
Published: October 2019

BackgroundUniversities around the world, including Malaysia, have attracted many international students from different countries. Research has reported that acculturative stress resulting from international students’ attempts to adjust to the cultures of host countries is one of the most challenging issues that affects their lives in general and academic lives in particular.ObjectiveThis study aims to examine the effectiveness of an educational intervention on acculturative stress among new postgraduate international students joining Malaysian public universities.MethodsA cluster randomized controlled trial design with Malaysian public universities as the unit of randomization will be used in this study. Public universities will be randomized in a 1:1 ratio to be either in the intervention (educational program) or control group (waiting list). Participants in the intervention group will receive 7 sessions in 9 hours delivered by an expert in psychology and the researcher. The control group will receive the intervention once the 3-month follow-up evaluation is completed.ResultsThe data will be analyzed using the generalized estimation equation with a confidence interval value of 95%; significant differences between and within groups are determined as P<.05. The results of the study underlie the effectiveness of educational program in decreasing acculturative stress of new international students and enabling them to cope with a new environment. The results of this study will contribute to previous knowledge of acculturative stress, acculturation, and adjustment of international students. Furthermore, such results are expected to play a role in raising university policy makers’ awareness of their postgraduate international students’ acculturative stress issues and how they can help them avoid such stress and perform well in their academic life.ConclusionsWe expect that the intervention group will score significantly lower than the wait-list group on the immediate and 3-month postintervention evaluation of acculturative stress and achieve a higher level of adjustment. Results will have implications for international students, policy makers at universities, the Malaysian Ministry of Higher Education, and future research.Trial RegistrationClinical Trials Registry India CTRI/2018/01/011223; http://ctri.nic.in/Clinicaltrials/showallp.php?mid1= 21978&amp;EncHid=&amp;userName=Muhamad%20Hanafiah%20JuniInternational Registered Report Identifier (IRRID)PRR1-10.2196/12950
The Effect of Smartphone Apps Versus Supervised Exercise on Physical Activity, Cardiorespiratory Fitness, and Body Composition Among Individuals With Mild-to-Moderate Mobility Disability: Randomized Controlled Trial
Authors: Berglind Daniel , Yacaman-Mendez Diego , Lavebratt Catharina , Forsell Yvonne 
Published: October 2019

Background
Adequate levels of physical activity (PA) and good cardiorespiratory fitness (CRF) are associated with profound health benefits for individuals with mobility disability (MD). Despite the vast amount of research published in the field of PA interventions, little attention has been given to individuals with MD.

Objective
The aim of this study was to examine the efficacy of an app-based versus a supervised exercise and health coaching program to support adults with MD to increase levels of PA, CRF, and improve body composition.

Methods
Participants with self-perceived MD, aged 18 to 45 years, were included in this 12-week parallel-group randomized controlled trial and allocated at random to an app-based intervention, using commercially available apps—the Swedish Military training app (FMTK), the Acupedo walking app, and the LogMyFood food photography app—or a supervised exercise and health coaching intervention, including 1 weekly supervised exercise session and healthy lifestyle coaching. The primary outcome was the level of moderate-to-vigorous PA (MVPA) measured with accelerometers. Secondary outcomes included CRF measured by a submaximal test performed on a stationary bicycle and body composition measured by bioelectrical impedance. All outcomes were measured at baseline, 6 weeks, and 12 weeks. Linear mixed-effect models were used to assess the between-group differences, as well as the within-group changes through time, in each intervention group.

Results
A total of 110 participants with MD were randomized to an app-based intervention (n=55) or a supervised exercise and health intervention (n=55). The mean age of participants was 34.9 years (SD 6.1), and 81.8% (90/110) of the participants were women. CRF showed a moderate increase in both groups after 12 weeks—1.07 (95% CI –0.14 to 2.27) mL/kg/min increase in the app-based group and 1.76 (95% CI 0.70 to 2.83) mLkg/min increase in the supervised exercise group. However, the intention-to-treat analysis showed no significant differences between the groups in MVPA or CRF after 12 weeks. Waist circumference was significantly lower in the app-based intervention group.

Conclusions
Commercially available apps increased levels of CRF and improved body composition over 12 weeks to the same extent as supervised exercise sessions, showing that both are equally effective. However, neither the app-based intervention nor the supervised exercise intervention increased MVPA.

Trial Registration
International Standard Randomized Controlled Trial Number (ISRCTN): 22387524; http://isrctn.com/ISRCTN22387524.
Dermatologists’ Adherence to the Latest Recommendations for Screening of Hydroxychloroquine Retinopathy in Saudi Arabia: Cross-Sectional Study
Authors: Mleeh Nouf Talal , Alzahrani Nujood Abdulwahed , Hariri Jehad Osama , Mortada Hatan Hisham , Algethami Mohammed Ridha 
Published: October 2019

Background
Hydroxychloroquine (HCQ) has been used to manage many inflammatory skin conditions. Nevertheless, retinopathy continues to be its most significant adverse effect. The American Academy of Ophthalmology (AAO) recommends baseline ophthalmologic screening in the first year of HCQ treatment. However, a recent study found an inadequate awareness of the recommendations. Furthermore, limited data are available regarding the implementation of the recommendations among dermatologists.

Objective
The aim of this study was to assess dermatologists’ adherence to recommendations pertaining to their current practice regarding HCQ toxicity detection.

Methods
A self-administrated questionnaire was distributed between February 2 and May 4, 2018, among members of the Saudi Society of Dermatology. The questionnaire comprised demographic-related questions and questions pertaining to each physician’s routine practice about the follow-up of HCQ-treated patients.

Results
A total of 76 dermatologists completed the questionnaire. We achieved a response rate of 62.54%. More than half (43/76, 56%) of the dermatologists were male. Furthermore, more than half (41/76, 53%) of them reported treating 1 to 3 patients with HCQ during the last year. Furthermore, two-thirds (47/76, 61%) of them reported screening patients before initiating HCQ treatment. Regarding follow-up recommendations, 59% (45/76) of dermatologists reported yearly after starting treatment for no-risk patients, whereas 94% (72/76) reported “yearly within 5 years of treatment” for at-risk patients. Data were considered significant at P<.05. All analyses were performed using SPSS, version 20 (IBM).

Conclusions
Dermatologists in Saudi Arabia are not well informed about some aspects of the latest recommendations regarding screening for HCQ toxicity in terms of tests, follow-up timing, cessation of the drug, and causative agents. Therefore, we recommend conducting more studies in Saudi Arabia to determine the adherence of more physicians to the AAO recommendations. Furthermore, patient education regarding HCQ toxicity and increased patient awareness are recommended for effective and safe HCQ use.
Feasibility, Acceptability, and Impact of a Web-Based Structured Education Program for Type 2 Diabetes: Real-World Study
Authors: Poduval Shoba , Marston Louise , Hamilton Fiona , Stevenson Fiona , Murray Elizabeth 
Published: October 2019

Background
Structured education for people with type 2 diabetes improves outcomes, but uptake is low globally. In the United Kingdom in 2016, only 8.3% of people who were referred to education programs attended the program. We have developed a Web-based structured education program named Healthy Living for People with type 2 Diabetes (HeLP-Diabetes): Starting Out (HDSO), as an alternative to face-to-face courses. A Web-based program gives people more options for accessing structured education and may help improve overall uptake.

Objective
The aim was to explore the feasibility and acceptability of delivering a Web-based structured education program (named HeLP-Diabetes: Starting Out) in routine primary health care and its potential impact on self-efficacy and diabetes-related distress.

Methods
HDSO was delivered as part of routine diabetes services in primary health care in the United Kingdom, having been commissioned by local Clinical Commissioning Groups. Quantitative data were collected on uptake, use of the program, demographic characteristics, self-reported self-efficacy, and diabetes-related distress. A subsample of people with type 2 diabetes and health care professionals were interviewed about acceptability of the program.

Results
It was feasible to deliver the program, but completion rates were low: of 791 people with type 2 diabetes registered, only 74 (9.0%) completed it. Completers improved their self-efficacy (change in median score 2.5, P=.001) and diabetes-related distress (change in median score 6.0, P=.001). Interview data suggested that the course was acceptable, and that uptake and completion may be related to nonprioritization of structured education.

Conclusions
The study provides evidence of the feasibility and acceptability of a Web-based structured education. However, uptake and completion rates were low, limiting potential population impact. Further research is needed to improve completion rates, and to determine the relative effectiveness of Web-based versus face-to-face education.
STRATEGI PENGEMBANGAN EKOWISATA MANGROVE MUARA BENGAWAN SOLO DI DESA PANGKAH WETAN, KECAMATAN UJUNGPANGKAH, KABUPATEN GRESIK
Authors: Kubro Aminah Roisatul , Ibrahim Jabal Tarik , Amir Nur Ocvanny 
Published: October 2019

Pangkah Wetan village has begun to utilize mangrove forests. At present, mangrove forests have been developed as ecotourism objects, however, the management has not developed them maximally. This study aims to determine the strengths, weaknesses, opportunities, and threats, as well as to analyze the strategies used in developing ecotourism at Muara Bengawan Solo Mangrove. Six key informants were selected as resource persons, while 30 respondents were selected by accidental sampling, they became the subject of analysis. The tool used is SWOT analysis (Strength, Weakness, Opportunity, Threat) and Quantitative Strategic Planning Matrix (QSPM). The results shows that the biggest score 1.84 was obtained at the opportunity, while the threat score was 0.84 so that this mangrove ecotourism still has many opportunities that could be used in developing ecotourism. The scores of strengths and weaknesses are 1.62 and 1.22, with a score difference of 0.4 only. The strength is only a slight difference from its weaknesses. Based on QSPM, an alternative strategy is obtained with the highest score of 5.71% at the first alternative. Application of the strategy used in developing mangrove ecotourism is the improvement of facilities provided to visitors.
Achieving Wellbeing and Prosocial Transformation Through Social Mobilisation: An Evaluation of a Gang Empowerment Strategy
Authors: Roguski Michael 
Published: October 2019

Adult gangs hold a criminalised and deviantised position in Aoteaora/New Zealand. Further, a host of strategies have been enacted to remove or obliterate the ‘gang problem’. These strategies’ lack of efficacy can be attributed to the imposition deficit-based criminogenic constructions on populations that are misunderstood and continually othered. The current study documents an evaluation of a gang-driven social mobilisation initiative. Identified outcomes are linked to the rejection of deficit and criminogenic epistemology in favour of a holistic appreciation of the socio-historical self. Criminogenic strategies have been found to entrench gang membership. In contrast, a holistic appreciation provides a foundation for social mobilisation where the membership is best placed to respond to their own needs.
Educação e Civilização
Authors: Gebara Ademir 
Published: October 2019

A Pontifícia Universidade Católica de Campinas (PUC-Campinas), é a Universidade que frequenteiem meus cursos de graduação, por isso é com muita felicidade que participo desse esforço editorial na organização desta sessão temática denominada Educação e Civilização, na qual são apresentados textos focando diferentes realidades empíricas e abordagens teóricas, em torno do tema proposto.
The Role Of Accounting Information In Enhancing The Financial Feasibility Of Economic Units
Authors: Shani Murtadha Mohammed , AL-Tameeme Layth Ali Hammadi , Sikna Swadi Wadi  
Published: October 2019

The purpose of this research is to know the effect of the future accounting information and the predictability provided by that information in enhancing the financial viability of the economic units and identifying the financial feasibility and importance of the economic units in terms of guiding the owners of capital to take the right investment decision.This research was conducted in one of the investment projects for the production of iron located in the city of Baghdad, the region of Awrig , The most important conclusion of this study is that for the financial feasibility study it is important to estimate the success of the project by determining the expected returns compared to the expected costs.
Recognition Of Revenue In Mobile Phone Companies Under IFRS 15
Authors: Al-Tamimi Layth Ali Hammadi , Sharif Abbas Alwan , Shani Murtadha Mohammed 
Published: October 2019

The aim of this research is to find out the adequacy and appropriateness of revenue recognition procedures in mobile phone companies and to know how well they comply with international financial reporting standards.
The most important conclusion reached by the researcher is the lack of experience and know-how in the accounting and administrative staff working in most mobile phone companies.
The most important recommendations of the research are the need to provide an efficient accounting and administrative staff with sufficient experience and know-how in the methods of recognizing revenues generated by mobile phone companies.