bluuebunny/crossref_metadata_2025_split huggingface dataset:
Identification of In Vivo Metabolites of a Potential Anti-tumor Drug Candidate AMAC, in Rat Plasma, Urine and Feces Samples Using UHPLC/QTOF /MS/MS
Authors: Dou Caixia , Tang Minghai , Xia Yuanyuan , Yang Linyu , Qiu Xiang , Li Yong , Ye Haoyu , Wan Li 
Published: December 2019

Background:
Drugs based on natural products targeting the microtubule system remain an
important component in cancer therapy. Compound 10, 4-((3-amino-4-methoxyphenyl) amino)-2Hcoumarin,
derived from coumarin, showed excellent anti-proliferative activity through directly binding
to the colchicine-binding site in β-tubulin, suggesting that it could be a perfect drug candidate for antitumor
drug research and development. Identification and structural characterization of metabolites is a
critical step of both drug discovery and development research.

Objective:
Compound 10, 4-((3-amino-4-methoxyphenyl) amino)-2H-coumarin, derived from coumarin.

Method:
In this study, an efficient and sensitive method using Ultra High-Performance Liquid Chromatography
couple with Quadrupole Time of Flight tandem Mass Spectrometry (UHPLC/QTOF/
MS/MS) was successfully established and applied to identify the in vivo metabolites in plasma,
urine and feces samples of rats after intravenous administration of Compound 10 with a single dose of
10 mg/kg.

Result:
A total of eight metabolites (including two phase I and six phase II metabolites) had been detected
or tentatively identified in plasma, urine and feces, indicating the prominent metabolic pathways
were glucuronidation, demethylation and hydroxylation. In addition, in order to understand the structure
of metabolites more accurately, synthesis strategy was used to confirm the metabolite M3.

Conclusion:
The present study provides important information on the metabolism of Compound 10 in
vivo for the first time, which would be helpful for understanding the potential metabolic processes of
Compound 10 and paving the way for pharmacology and toxicology research.
Applicability of Monocyte Activation Test for Pyrogen Detection in Succinylated Gelatin Injection
Authors: Zheng Luxia , Wang Mingren , Shen Xiong , Wang Can , Wan Liqing , Tang Liming , Chen Guiliang , Chen Gang 
Published: December 2019

Background::
Pyrogens are fever-inducing substances and pyrogen detection is mandatory in
parenteral pharmaceuticals. Succinylated Gelatin Injection (SGI) is a biopharmaceutical product, containing
multi-component, and it is administered parenterally.

Objective:
The study aimed to assess pyrogen in SGI and to evaluate the feasibility of the Monocyte
Activation Test (MAT) for pyrogen detection in a multi-component pharmaceutical product.

Method:
In the present study, the Bacterial Endotoxin Test (BET) and the Monocyte Activation Test
(MAT) were employed to assess pyrogen in SGI. The MAT method was developed on the basis of the
HL-60/IL-6 assay. HL-60 cells were incubated with lipopolysaccharide (LPS) standards and sample
solutions. The endotoxin produced by the incubation, interleukin-6 (IL-6), was measured by ELISA.
The MAT method was validated and main parameters were investigated. Finally, the pyrogenicity of
SGIs from two different enterprises was determined by the developed MAT method.

Results:
The BET failed in the test for interfering factors and the MAT was proved suitable for the pyrogen
detection of SGI. All the products examined showed negative results in the pyrogen detection
test.

Conclusion:
The MAT method is feasible in pyrogen detection of SGI. It can be applied in pyrogen
detection for quality and safety control of multi-component biological products.
Chemical Composition of Essential Oil and In Vitro Biological Activities of Dryopteris marginalis L.
Authors: Islam Mohammad Zahidul , Shahinuzzaman Mohammad , Yilmaz Raşit Fikret , Rahman Hafizur , Derin Yavuz , Tutar Omer Faruk , Tutar Ahmet 
Published: December 2019

Introduction:
Dryopteris marginalis L. is a local plant in Bangladesh which is widely
used as folk medicine.

Materials and Methods:
In this study, the chemical composition of essential oil of D. marginalis L.
as well as the antioxidant activity, antibacterial activity and total phenolic content of various organic
extracts were analyzed. The gas chromatography mass spectrometry analysis was used to identify
the chemical compositions. The antibacterial activity of different extracts of Dryopteris marginalis
was examined against three gram-negative bacteria and two gram-positive bacteria. The antibacterial
activity of different extracts was investigated using the disc diffusion method and minimum inhibitory
concentration showing important antibacterial activity and was measured by using the broth
dilution method.

Results:
The antioxidant activity was determined by using 2,2-diphenyl-1-picrylhydrazyl (DPPH)
assay and superoxide radical scavenging assay. The total phenolic portion of the extracts was ascertained
by Folin-Ciocalteu in an alkaline medium. Twenty-two volatile compounds were identified
from the essential oil. The methanol extract exhibited a significant inhibitory effect which was close
to the value of standard antibiotic (Streptomycin). The zones of inhibition of different organic extracts
against the tested bacteria were found in the range of (7-15) mm and the Minimum Inhibitory
Concentrations (MIC) were recorded (15.62-1000) μg/ml. The antioxidant activity of D. marginalis
was (82.13+1.2) % and (59.21+0.45) % highest activity with DPPH and superoxide radical scavenging
assay, respectively.

Conclusion:
The methanol extract showed the highest (147.43+3.1) mg/g GAE of total phenolic content.
The extracts and essential oil of D. marginalis showing strong antibacterial activity can be considered
as a potential source of natural medicine and the ingredient of modern therapeutic agents.
Evaluation of Anticancer and Anti-Mitotic Properties of Quinazoline and Quinazolino-Benzothiadiazine Derivatives
Authors: Shaik Thoukhir B. , Malik M. Shaheer , Routhu Sunitha R. , Seddigi Zaki S. , Althagafi Ismail I. , Kamal Ahmed 
Published: December 2019

Background:
Cancer is one of the major health and social-economic problems despite considerable
progress in its early diagnosis and treatment. Owing to the emergence and increase of multidrug resistance to
various conventional drugs, and the continuing importance of health-care expenditure, many researchers have
focused on developing novel and effective anticancer compounds.

Objective:
Chemical repositories provide a good platform to evaluate and exploit known chemical entities for
the identification of other biological activities. In the present study, we have selected an in-house library of
synthesized compounds based on two different pharmacophoric scaffolds to evaluate their cytotoxic potency on
various cancer cell lines and mechanisms of action.

Methods:
A series of in-house synthesized quinazoline and quinazolino-benzothiadiazine derivatives were investigated
for their anticancer efficacy against a panel of five cancer (DU145, MCF7, HepG2, SKOV3 and
MDA-MB-231) and one normal (MRC5) cell lines. Furthermore, the active compound of the study was investigated
to elucidate the mechanism of cytotoxicity by performing series of experiments such as cell cycle analysis,
inhibition of tubulin polymerization, alteration of mitochondrial membrane potential, determination of endocytic
pathway for drug uptake pathway and combination drug treatment.

Results:
Among all the tested compounds, fifteen of them exhibited promising growth-inhibitory effect (0.15-
5.0μM) and induced cell cycle arrest in the G2/M phase. In addition, the selected compounds inhibited the microtubule
assembly; altered mitochondrial membrane potential and enhanced the levels of caspase-9 in MCF-7
cells. Furthermore, the active compound with a combination of drugs showed a synergistic effect at lower concentrations,
and the drug uptake was mediated through clathrin-mediated endocytic pathway.

Conclusion:
Our results indicated that quinazoline and quinazolino-benzothiadiazine conjugates could serve as
potential leads in the development of new anticancer agents.
Conceptual Design, Kinematics and Dynamics of Vector Thruster for Underwater Vehicle Based on Screw Theory
Authors: Chen Yuan , Tang Liang , Han Lingyun , Xu Han 
Published: December 2019

Background:
The vector propulsion device can significantly improve the sensitivity and
mobility of the mechanism. Furthermore, thrust vectoring technology with single manipulator and multidimensional
attitude is a novel thrust vectoring technique in industry, especially in aviation fields.
Numerous progresses made by various research groups and the newest patents in these aspects will be
cited in this paper.

Objective:
To apply the thrust vectoring technology to Autonomous Underwater Vehicles (AUVs), a
spherical parallel vectored thruster with three Degree-Of-Freedom (DOF) was proposed based on vector
deflection constrained screw method.

Methods:
Firstly, in the framework of screw theory, the topological structure of the spherical parallel
mechanism was modeled to analyze the motion characteristics. Secondly, in terms of closed chain constraint
equations, the vectored algebra method was employed to derive the Jacobian matrix of the
mechanism. Thirdly, the decoupling structure configuration method was adopted to establish the analytical
model of velocity and acceleration. Finally, the dynamic model was established by means of
virtual work principle.

Results:
The forward and inverse solutions of the mechanism was calculated; the Jacobian matrix of the
mechanism was derived; the kinematic characters including singularity and dexterity were analyzed;
the performance analysis was carried out.

Conclusion:
This new type of underwater vehicle oriented power plant, which is characterized by simple
decoupling structure, strong steering capability, and high cost-efficiency, has broad prospects in the
field of AUV.
Design of Multi-function Power Factor Instrument with STM32
Authors: Qi Wenjuan , Gao Jixuan , Wang Zhongxian 
Published: December 2019

Background:
A multifunctional power factor device based on the FFT algorithm has
been designed. The digital panel can display power factor, voltage, current, frequency, phase angle,
active power and reactive power.

Objective:
To solve the influence of the harmonic interference and the aperiodic component on the
accuracy of power factor measurement.

Methods:
In this paper, by combining a fixed-point 256-point FFT algorithm and taking STM32 as
the core microcontroller, the hardware circuit and the software program are designed respectively.
The hardware circuit is tested and analyzed in practice. Among them, the hardware circuit mainly
includes the main circuit design, STM32 control circuit design, EMI and second-order RC filter
circuit design, sampling circuit design, and signal conditioning circuit design. The software program
mainly includes the main program, AD conversion subroutine, voltage and current acquisition
subroutine, LCD display subroutine and twirl factor array. FFT algorithm is achieved by the
table look-up method.

Results:
Finally, the hardware circuit is built and the software program is debugged to test the designed
device. The experimental results show that the designed power factor instrument meets the
task requirements under the different types of loads.

Conclusion:
After processing and analyzing the measurement results, it can be concluded that: under
the pure resistive load, the maximal relative error of electrical parameters is 4.49%; and under
the resistive inductive load, the maximal relative error of electrical parameters is 2.86%. Both results
meet the design requirements.
Heat engineering properties of energy-efficient material based on plant additives (dried hogweed)
Authors: Musorina Тatiana А. , Naumova Elizaveta A. , Shonina Ekaterina V. , Petrichenko Mikhail R. , Kukolev Maksim I. 
Published: December 2019

Introduction. The articlecompares the heat engineering properties of construction materials: high-strength concrete, ordinary concrete, and two concrete samples containing a vegetable additive, dried stem fragments of hogweed (Heracleum sosnowskyi). The first sample contains the additive in the crushed form, while the second contains the additive in the form of tubes. The research to estimate heat conduction in the four samples under unsteady conditions.
Materials and methods. The thermal diffusivity of two samples with plant additive is determined using a comparative physical experiment. When determining the thermal properties, the accumulating component of the enclosure is taken into account what leads to a long delay in the temperature variation over time. DS18B20 digital temperature sensors connected to an Arduino Uno board were used to measure the temperature. The experiment was carried out in the Challenge 250 chamber at an initial temperature of 20 ºС. Then the chamber temperature was lowered to 0 ºС within 30 minutes. In the next period, the temperature dropped from 0 ºС to –10 ºС. The data obtained are of interest for improving the energy efficiency of buildings.
Results. The experiments showed that the tubular-hogweed sample is close to high-strength concrete by its heat engineering properties. The material thermal diffusivity affects the amplitude of temperature fluctuations and the accumulating capacity of the wall.
Conclusions. It is established experimentally that at lower thermal diffusivity of a hogweed-containing sample, the amplitude of temperature fluctuations increases. This indicates a greater time lag, just as in the case of a high-strength concrete sample. When using the hogweed as an additive, we obtain a heat-resistant minimum-cost material for enclosures. Considering an issue of the energy efficiency in construction and existing additives to concrete, the researchers have reached the conclusion that it is efficient to use the dried hogweed as the plant additive.
Ethical Invention in Sartre and Foucault: Courage, Freedom, Transformation
Authors: Engels Kimberly 
Published: December 2019

This article explores the concept of ethical invention in both Jean-Paul Sartre’s and Michel Foucault’s later lectures and interviews, showing that a courageous disposition to invent or transform plays a key role in both thinkers’ visions of ethics. Three of Sartre’s post-Critique of Dialectical Reason lectures on ethics are examined: Morality and History, The Rome Lecture, and A Plea for Intellectuals. It is shown that ethical invention for Sartre requires the use of our freedom to transcend our current circumstances, a willingness to break away from harmful ideologies, and directing our free praxis towards the goal of universal humanism. Examining several of Foucault’s interviews alongside his lecture series The Government of Self and Others and The Courage of Truth, it is shown that ethical invention for Foucault requires a rejection of necessities or inevitabilities in our current landscape, a willingness to reshape our current beliefs, and a philosophical way of life that results in an alteration of the relationship to self and others. For both thinkers, ethical invention should be preceded by a critical reflection on ourselves in our historical moment. Both argue that ethical invention requires a rejection of the inherent value of our world and realization that the conditions of possibility for being subjects are malleable. Last, it is shown that both philosophers specifically call philosophers or intellectuals to invent.
KEPEMIMPINAN KETUA KELOMPOK TANI DALAM MENINGKATKAN DINAMIKA KELOMPOK DI KECAMATAN NATAR KABUPATEN LAMPUNG SELATAN
Authors: Hutomo Fernaldi Shidi , Effendi Irwan , Silviyanti Serly 
Published: December 2019

This study aimed to analyze the leadership level of the farmer group chairman, the dynamism level of the farmer group, the relation between farmer grup chairman’s leadership and group dynamics, in addition to the relation of group dynamics and rice productivity in Natar Sub-Distict of South Lampung Regency. This study was conducted purposively in Natar Sub-District of South Lampung Regency by survey method, in which respondents consist of 69 farmer groups. The data was collected in September - December 2016. The data was analyzed descriptively and statistically, in which the relation between variables of this study were tested by Rank-Sperman Correlation Test. The results showed that: the leadership level of the farmer group chairman in Natar Sub-District of South Lampung Regency was in good classification, the dynamics level of the group was in quite good classification. The leadership of the farmer group’s chairman in Natar Sub-District was significantly related to the group dynamics, whereas group dynamics was not correlated significantly to productivity of rice in Natar Sub-Distric of South Lampung Regency.Key words : group dynamics, leadership, productivity of rice
EFISIENSI TEKNIS USAHATANI BAWANG MERAH DI KECAMATAN KETAPANG KABUPATEN LAMPUNG SELATAN
Authors: Tristya Hardini , Murniati Ktut , Affandi Muhammad Irfan 
Published: December 2019

This study aims to analyze technical efficiency of onion farming and the factors that influence the technical inefficiency of onion farming. This research is conducted purposely in Ketapang Sub-district. The respondents are 49 farmers collected by sensus method. He research data is taken in September to November 2016. The technical efficiency is measured by frontier production function and estimated by Maximum Likelihood Estimation (MLE) method with Frontier 4.1c computer program. The estimation of factor that influences the technical inefficiency is applied by linear regression model simultaneously obtained by using the frontier production function. The results showed that the average of technical efficiency of onion farming in Ketapang Sub-district was 0.93 which meant very efficient. Furthermore, the factors that significantly influenced the technical inefficiency of onion farm in Ketapang Sub-district were the farming experience and counseling frequency.Key words: frontier, onion farming, technical efficiency
ANALISIS BIAYA DAN PENDAPATAN USAHA PEDAGANG SAYURAN DI PASAR TAMIN KOTA BANDAR LAMPUNG
Authors: Astuti Romidah , Zakaria Wan Abbas , Endaryanto Teguh 
Published: December 2019

This study aims to analyze the cost structure and the income level of vegetable traders in Tamin Market Bandar Lampung City. This research is conducted in purposively chosen Tamin Market with the consideration that Tamin Market is a center of vegetable trade and the main market in Bandar Lampung City. The data were collected in March 2017 and respondents were 15 vegetable traders who are willing to be interviewed, consisting of five stall traders, five los traders, and five street traders. Data are analyzed descriptively using qualitative and quantitative of cost and income analysis. The result showed that the traders' business cost structure consists of fixed cost and variable cost. The propotion of variable cost is higher than the fixed cost, which is 99 percent of total cost. Variable costs include plastic cost, vegetable purchase, transport, labor, and information. And fixed costs include rent cost, electricity and market facility fees. The average income of stall traders is higher than the loser traders and the street traders. The average income of stall traders is Rp817,055.00 per day, los traders is Rp737,604.00 per day, and street traders is Rp183,455.00 per day.Key words: cost structure, the level of income, vegetable traders
PARTISIPASI PETANI DALAM PROGRAM PENGEMBANGAN USAHA AGRIBISNIS PEDESAAN (PUAP) DI KECAMATAN ADILUWIH KABUPATEN PRINGSEWU
Authors: Sitompul Rika ES , Rangga Kordiyana K , Viantimala Begem 
Published: December 2019

The objectives of this research are to know the participation of farmers in PUAP program, factors related to farmers’ participation in PUAP program, and farmers’ income. This research was conducted in Bandung Baru Village of Adiluwih District, Pringsewu Regency. The sampling used was proportional random sampling with total of 81 farmers. The research was conducted in October - December 2016. The research method is a survey. The relationship between the variables was tested using Rank Spearman correlation test. The results showed that farmers' participation in the PUAP program was quite active, factors related to farmers’ participation were age, education level, length of farming experience, and cultivated land area. Average household income of farmers in Bandung Baru Village Adiluwih District Pringsewu Regency each year is Rp67.633.851. Key words: income, participation, PUAP program
KINERJA PENYULUH PERTANIAN LAPANGAN DAN PRODUKTIVITAS USAHATANI PADI SAWAH (KASUS PETANI PADI DI KECAMATAN KALIREJO KABUPATEN LAMPUNG TENGAH)
Authors: Pujiana Tri , Hasanuddin Tubagus , Gitosaputro Sumaryo 
Published: December 2019

The objectives of this study were to analyze the performance of agricultural extension agents (PPL), factors related to PPL performance, the relationship between PPL performance and productivity of the rice and the relationship between the productivity and paddy rice income in Kalirejo. This study uses a survey method on rice farming in Kalirejo, Central Lampung. The data was collected in October 2017 by interviewing 53 respondents consist of 8 PPLs and 45 rice farmer who were drawn by purposive sampling method. The data was analyzed by qualitative-descriptive analysis, tabulation and Rank Spearman correlation. The study showed that the performance of PPL in BPP Kalirejo was considered high. The competence, work environment, motivation and leadership PPL are related to the performance of PPL. The performance of PPL was related to the productivity of rice. However the productivity was not related to the income of rice farming. Although, the productivity of the rice was increasing, income of the rice farmer was considered low due to low price of rice. Key words: income, performance, productivity
ANALISIS DAMPAK EL NINO TAHUN 2015 TERHADAP PENDAPATAN PETANI PISANG DI KECAMATAN KETAPANG KABUPATEN LAMPUNG SELATAN
Authors: Syafe’i Ahmad , Abidin Zainal , Soelaiman Achdiansyah 
Published: December 2019

This study aims to determine the impact of El Nino on income of banana farmers and identifying mitigation of banana farmers to reduce the impact of El Nino. The research is conducted in Ketapang Sub District, Southern Lampung. The respondents are 49 banana farmers. The first objective was analyzed by income, and t-test indicators. The second objective is analyzed descriptively by mitigation undertook by farmers. The results showed that El Nino had significant impact on income of banana farmer in Ketapang Sub District of South Lampung in which income of banana farmers decreased by 37.85 percent. The mitigation done by banana farmers during El Nino were to reduce the banana seedlings, cut the banana leaves and not to use pesticides. Key words: Banana farming, El Nino, impact, welfare analysis