bluuebunny/crossref_metadata_2025_split huggingface dataset:
Bioactive Compounds with Significant Anti-Rheumatoid Arthritis Effect Isolated for the First time from Leaves of Bougainvillea spectabilis
Authors: Ahmed Amal H. , Abd Elkarim Asmaa S. 
Published: December 2020

Objective:
The aim of this work is to identify and purify bioactive compounds from
70℅ aqueous methanolic extract (AME) of B. spectabilis leaves collected in Cairo, Egypt and assessed
their rheumatoid arthritis activity.

Methods:
The methanolic extract of B. spectabilis leaves was fractionated and subjected to different
chromatographic techniques to isolate pure new compounds which were identified by one dimensional
and two dimensional nuclear magnetic resonance (NMR) spectroscopic analyses and
mass spectrometric methods. The isolated compounds were evaluated for their anti-inflammatory
activity on adjuvant induced chronic rheumatoid arthritis.

Results & Discussion:
Seven bioactive compounds were purified and identified for the first time
from the methanolic extract of Bougainvillea spectabilis leaves; secologanin dimethyl acetal,
α- and β-amyrin, α- and β-amyrin acetate, Kaempferol and kaempferol-3-O-rhamnoside. The previously
mentioned compounds had a significant effect against rheumatoid arthritis.

Conclusion:
The seven compounds isolated from the methanolic extract of B. spectabilis leaves
showed strong anti-rheumatoid arthritis activity.
Aerosolized Liposomal Formulation Prevents Enhanced Drug Transfer from Fibrotic Lungs to the Systemic Circulation
Authors: Togami Kohei , Kurasho Kaede , Kanehira Yukimune , Tada Hitoshi , Chono Sumio 
Published: December 2020

Background:
Idiopathic Pulmonary Fibrosis (IPF) is a chronic and progressive respiratory
disease characterized by the destruction of the alveolar structure. In pulmonary fibrosis, aerosolized
drugs are easily transferred to the systemic circulation via leakage through the injured alveolar
epithelium. Therefore, pulmonary drug delivery systems for sustained distribution in fibrotic lungs
are needed.

Objective:
We evaluated the intrapulmonary pharmacokinetics of aerosolized liposomes as pulmonary
drug delivery systems in mice with bleomycin-induced pulmonary fibrosis.

Methods:
The aerosolized liposomal formulations and solutions of model compounds, including indocyanine
green and 6-carboxyfluorescein (6-CF), were intrapulmonary administered to mice with
bleomycin-induced pulmonary fibrosis. In vivo imaging for indocyanine green and 6-CF measurements
in lung tissues and plasma were performed. Additionally, in vitro permeation experiments using
NCI-H441 cell monolayers as a model of alveolar epithelial cells were performed.

Results:
The fluorescence signals of indocyanine green following the administration of liposomal
formulations were observed longer in the lungs than those in solution-treated mice. Compared with
the solution, the 6-CF concentrations in lung tissues after the administration of liposomal formulations
were determined higher, whereas those in the plasma were lower. 6-CF permeability was significantly
increased by transforming growth factor-β1 in NCI-H441 cell monolayers treated with
the solution but unchanged in the presence of the liposomal formulation.

Conclusion:
The aerosolized liposomal formulation can prevent enhanced drug transfer from fibrotic
lungs into the systemic circulation via the injured alveolar epithelium. This system may be useful
for the sustained distribution of anti-fibrotic agents in fibrotic lungs and the optimization of IPF
therapy.
Design, Synthesis and Biological Evaluation of Cyanopyridines, Pyridopyrazolopyrimidines and Pyridopyrazolotriazines as Potential Anticancer Agents
Authors: Keshk Reda Mohammed , Izzularab Batoul Mohamed 
Published: December 2020

Background:
The continuous need for new anticancer drugs is never-ending task due to cancer resistance
to the existing drugs.

Objective:
This article aimed to design, synthesis, characterization, and anticancer evaluation of cyanopyridines,
pyridopyrazolopyrimidines and pyridopyrazolotriazines.

Methods:
Anticancer activity of the synthesized compounds was determined using MTT assay against three cancer
cell lines, namely liver cancer cell line (HepG-2), pancreatic cancer cell line (PANC-1), non-small lung cancer
cell line (A-549) and normal fibroblast.

Results and Discussion:
A series of 3-cyanopyridines (2a,b, 4, 5, 9), pyridopyrimidine (10), pyridopyrazolopyrimidines
(11a-c, 12a,b, 18), pyrazolopyridine salt (13) and pyridopyrazolotriazines (16a,b) were synthesized
from 3-cyano-4,6-dimethyl-2-pyridone. The synthesized compounds were evaluated in vitro for their anticancer
activity and their chemical structures were determined by elemental analysis and spectroscopic data.

Conclusion:
Some of the synthesized compounds showed remarkable anticancer activities, especially 11a exhibited
superior potency to the reference drug cisplatin against A-549 (IC50 = 9.24 μg mL-1 compared to 11.76 μg
mL-1 for reference drug) and was found to be safe (IC50 = 66 μg mL-1) for normal fibroblast. Furthermore, compound
16a displayed the highest activity among the tested compounds against HepG-2 (IC50 = 6.45 μg mL-1
equipotent to cisplatin) with the highest safety profile for normal fibroblast (IC50=113.97 μg mL-1).
Effect of Lipid Emulsion on the Improvement of Renal Damage in Colistin- Induced Nephrotoxicity
Authors: Senkal Naci , Atasoy Ozum , Caparali Emine Bilge , Erdogan Mumin Alper , Erbas Oytun 
Published: December 2020

Background:
Colistin utilization has gradually increased worldwide with the rising of
multidrug-resistant (MDR) gram-negative bacilli despite its nephrotoxicity. Lipid emulsion (LE) is
widely used for the toxic overdose treatment of various drugs.

Objective:
The aim of the present study is to evaluate the effect of lipid emulsion on the improvement
of renal damage in colistin-induced nephrotoxicity with an experimental Sprague Dawley rat
model.

Methods:
Twenty-four male Sprague Dawley rats were initially assigned to 2 random groups. Sixteen
rats were given a single dose of 20 mg/kg colistin, and eight rats received no medication (control
group). Sixteen rats that were administered colistin were sub-divided into 2 groups. Group
1/LE rats (n = 8) were given 20 ml/kg solution of lipid emulsion, and group 2/S rats (n = 8) were
given 20 ml/kg/day (i.p.) of 0.9% NaCl saline; both were administered for 10 days. Then tubular injury
was evaluated histopathologically. Serum levels of blood urea nitrogen (BUN), Kidney Injury
Molecule-1 (KIM-1), and creatinine were measured. Besides, malondialdehyde (MDA) levels were
determined in tissue samples for the assessment of lipid peroxidation.

Results:
The mean percent of tubular epithelial cell injury and tubular dilatation was found significantly
higher in group 2/S than in control and group 1/LE (p < 0.0001 and < 0.001; respectively).
KIM-1 and MDA levels were also statistically higher in group 2/S than in control and group 1/LE.
(p < 0.0001 and < 0.0001; respectively). Additionally, serum BUN and creatinine levels of group
2/S were significantly greater than control and group 1/LE (p < 0.0001 and < 0.0001; respectively).

Conclusion:
In this present study, we determined that colistin-induced proximal tubular damage
was decreased histopathologically and serologically by the effect of lipid emulsion. Thus, our findings
may guide future studies on the clinical use of colistin, particularly in MDR positive intensive
care infections.
A Fluoro Derivative of Embelin, as Potent B-RAF Inhibitor in Melanoma
Authors: Babu Arunkumar , Laila Shiny P. , Fernandez Annette 
Published: December 2020

Background:
Melanoma is one of the most common forms of skin cancer, and B-RAF is a mutated
protein found in most melanomas. The important function of B-RAF is normal cell growth and survival. Most of
the known B-RAF mutations are V600E mutations. Vemurafenib is the fluorine-based drug currently used for
V600E mutations. However, this drug has side effects, therefore, more potent drugs with fewer side effects are
required.

Objective:
This study aims to develop a more effective lead compound as a B-RAF inhibitor from
hydroxyquinone by structural modification of embelin, a naturally occurring hydroxybenzoquinone. It has the
potency of detoxifying blood and is hence useful in a wide range of skin diseases. Thus, a fluorine substituted
semisynthetic derivative of embelin, 5-(3-chloro-4-trifluoromethoxy phenyl amino)-2-hydroxy-3-undecyl- [1, 4]
benzoquinone to fight against skin cancer was prepared.

Methods:
Fluoro derivative of embelin was synthesized by the direct condensation of embelin with 3-chloro-4-
trifluoromethoxy aniline. The structure of the product was characterized using various spectral data obtained
from IR, 1H NMR, 19F NMR, 13C NMR, and mass spectrum. Various in vitro studies like antiproliferative study
in A375 Cell Lines (B-RAF Elisa), western blotting analysis, gene expression study by reverse transcriptase
PCR, caspase assay, flow cytometry analysis, clonogenic assay, and transwell migration assay were carried out to
find its biological activity.

Results:
A semisynthetic derivative of Embelin 5-(3-Chloro-4-trifluoromethoxy phenyl amino)-2-hydroxy-3-
undecyl- [1, 4] benzoquinone (EOCF) was prepared, and the structure of the derivative was confirmed by
spectral analysis. The MTT assay proves that the fluoro derivative of embelin exhibited better anti-cancer activity
in melanoma cell lines than the parent compound, embelin. Western blot analysis showed that B-RAF expression
level was reduced by the addition of derivative than the parent compound embelin. The Caspase ELISA analysis
indicated that the derivative was found to be a good apoptotic marker. From the flow cytometry analysis, it was
observed that cell arrest occurs at the G0/G1 phase. Its antimetastatic activity was determined using clonogenic
assay. It indicated that the derivative EOCF inhibits the metastatic effects in melanoma cell lines. The migratory
potential of melanoma cells was significantly reduced in the presence of EOCF when the transwell migration
assay was conducted.

Conclusion:
This work established that the potency of the synthesized compound was more than the parent
compound, embelin, when it was structurally modified with 3-chloro-4-trifluoromethoxy aniline. The derivative
can be used as a lead molecule for further drug discovery.
An Overview on COVID-19 and its Effect on Cardiovascular Diseases
Authors: Hamadi Abdullah , Mahzari Ali , Hakami Abdulrahim , Hindawi Salwa , Dobie Gasim , Sayyed M. I , Hamdi Fawaz , Nahari Mohammed , Jackson Denise E. 
Published: December 2020

Abstract::
COVID-19 (Virus named as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)) is a pandemic
disease characterized with respiratory infection caused by coronavirus. It has worldwide after an outbreak began in Wuhan,
China, in December 2019. SARS-CoV-2 has infected more than 15 million people globally. The disease severity and
mortality increased in patients with heart-related comorbidities. Cardiovascular disease patients are more susceptible and
infected with SARS-CoV-2. Early screening and managements these patients prevent or ameliorate adverse outcomes.
Several treatments have been used to combat these effects as previously seen in MERS and SARS. This review will cover
the association of cardiovascular diseases with COVID 19. It showed that cardiovascular diseases are common in patients
with COVID- 19. Increased attention to highlight the gaps should be paid to the care of this unique group of patients.
Curcumin Loaded and Co-loaded Nanosystems: A Review from a Biological Activity Enhancement Perspective
Authors: Araya-Sibaja Andrea M. , Wilhelm Krissia , González-Aguilar Gustavo A. , Vega-Baudrit José R. , Salazar-López Norma J. , Domínguez-Avila Jesús A. , Navarro-Hoyos Mirtha 
Published: December 2020

Background:
Curcumin is a natural phenolic compound exhibiting multiple bioactivities
that have been evaluated in vitro, in vivo as well as through clinical studies in humans. Some
of them include antimicrobial, antioxidant, anti-inflammatory, and central nervous system protective
effects. Further, curcumin is generally recognized as a safe substance because of its low toxicity.
However, its molecular structure is susceptible to changes in pH, oxidation, photodegradation,
low aqueous solubility, and biotransformation compromising its bioavailability; these drawbacks
are successfully addressed through nanotechnology.

Objective:
The present review systematizes findings on the enhancement of curcumin’s beneficial
effects when it is loaded and co-loaded into different types of nanosystems covering liposomes, polymeric
and solid-lipid nanoparticles, nanostructured lipid carrier, lipid-polymeric hybrids, self-
-assembled and protein-based core-shell systems in relation to its antimicrobial, antioxidant, anti-inflammatory
and central nervous system protective bioactivities.

Conclusion:
Curcumin is a versatile molecule capable of exerting antimicrobial, antioxidant, anti-
inflammatory, and central nervous system protective effects in an enhanced manner using the
possibilities offered by the nanotechnology-based approach. Its enhanced bioactivities are associated
with increments in solubility, stability, bioavailability, as well as in improved intracellular uptake
and cell internalization. These advantages, in addition to curcumin’s low toxicity, indicate the
potential of curcumin to be loaded and co-loaded into nanosystems capable of providing a controlled
release and targeted administration.
Design and Dynamic Simulation Research of a Bionic Three-Link Tube Shock Absorber
Authors: Song Yong , Li Yue , Li Zhanlong , Lian Jinyi , Shi Qinglu , Meng Jie 
Published: December 2020

Background::
Shock absorbers are the main damping component of vehicle suspension system, whose excellent passive characteristics can greatly improve and guarantee the ride comfort and handling stability of vehicles. Therefore, it is of great significance to research and develop a shock absorber with excellent passive characteristics.

Objective::
The purpose of this paper is to propose and design a bionic three-link tube shock absorber with good buffering and vibration reduction performance and bionic adaptive characteristics. In addition, the passive characteristics of the purposed shock absorber are studied.

Methods::
The bionics idea is applied to the development of vehicle shock absorbers. A three-link mechanism with dampers and springs is abstracted and designed according to the structure and the function of kangaroo legs. A bionic three-link tube shock absorber is constructed based on the traditional tube shock absorber structures and the three-link mechanism. Three-dimensional modeling and three-dimensional dynamic simulation of the shock absorber are carried out by CATIA and ADAMS.

Results::
The body acceleration are greatly reduced relative to excitations; the dynamic displacement decreases sharply under greater excitation, but there is slight increase under smaller excitation; the motion function and joint change characteristics of the proposed shock absorber are similar to those of kangaroo legs to a certain degree.

Conclusion::
The results show that the structure design of the bionic three-link tube shock absorber is reasonable and workable, the shock absorber presents good buffering and damping performance and some bionic adaptive characteristics, however, there is still room for further optimization of the structure design.
Aloe vera Compositions Used for Medicinal Applications: A Patent Review (2013-till 2020)
Authors: Varpe Bhushan D. , kulkarni Amol A. , Mali Anil S. 
Published: December 2020

Background::
Aloe vera is a traditionally used plant for medicinal purposes, mostly as a cosmetic. The Aloe vera gel/extract/juice is being used in hair care, moisturizing, cleansing, and thickening agent in formulations. The Aloe vera gel is rarely used on burns, wounds, infections, and gastric diseases.

Objectives::
To study the patents filed recently to understand the trend in the application of Aloe vera for therapeutic purposes.

Methods::
This patent review focuses on granted patents during the year 2013-till 2020. The patents were analyzed and their therapeutic use was studied to assess the recent trends in Aloe vera formulations.

Results::
Most of the patents of this article on skincare products and out of those maximum patents are on moisturizing compositions. Most of the patents are found in US jurisdiction and few in Europe and China. As there are certain restrictions on patenting inventions related to composition and natural products in various jurisdictions, patents are found in only a few jurisdictions.

Conclusion::
The trend of use of Aloe vera is still towards cosmetic products also the Aloe vera is used in oral care composition, deodorant compositions, anti-inflammatory composition, vitamin compositions, antibiotic compositions, etc.
Efficacy of Topical Formulations in Healing of Caesarean Scars Using Non-Invasive Devices: A Controlled Trial
Authors: Abdullah Alia , Al Kredly Rawya , Baguneid Mohamed 
Published: December 2020

Background:
Despite the availability of many topical formulations for scar treatment, an objective evaluation of
their effect is lacking.

Objective:
To assess the physiological, structural, and mechanical parameters of scar healing by a scar ointment (MEBOScar).

Methods:
45 patients from the Department of Obstetrics at Al Ain Hospital, UAE, with recently acquired Pfannenstiel scars
were recruited into this prospective, open-label, controlled study. Scar ointment was applied to a lateral third of the scar;
positive control (silicone gel based topical) to the other lateral third; the middle third was left untreated (negative control).
The scars were evaluated at 4 time points up to 12 weeks using non-invasive devices and a scar questionnaire.

Results:
In comparison with silicone gel, there was a significant reduction in trans epithelial water loss at weeks 2,4,8, and
12 (p<0.001) and scar area at weeks 4, 8 and 12 (p<0.001) with scar ointment. The skin elasticity at week 4 was significantly
increased by scar ointment (p=0.007). By week 12, gross colour mismatch of the scar was described by 9% patients with
scar ointment (24% with silicone gel, 42% with no treatment; p<0.001). There was significant improvement in scar texture
with scar ointment by week 12 (p<0.001).

Conclusions:
Scar ointment has beneficial effects on objective and subjective patient-reported parameters of Pfannenstiel
scars.
A Conceptual Framework of Designer Responses in Designing Furniture Application from Upcycled Plastic Materials
Authors: Ahmad Fahmi , Ahmad Azroll , Saharudin Haszlin , Khairi Hanif 
Published: December 2020

Understanding the design should be an emotion's role in various aspects of design, represent not only this research goal for research purpose but also for the successfulness of any design that has good philosophy. However, upcycling the solid waste plastic material to create another creative object could reduce the pollution issue and at the same time, support the awareness sustainability campaign. An underlying objective of this research understudy is to investigate and develop furniture application design, which will respond from designer and their experience. This is to contribute guidelines for the future development of new alternative material for furniture applications.
Keywords: Application, Furniture design, Designer response, Upcycling.
eISSN: 2398-4287© 2020. The Authors. Published for AMER ABRA cE-Bsby e-International Publishing House, Ltd., UK. This is an open access article under the CC BYNC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). Peer–review under responsibility of AMER (Association of Malaysian Environment-Behaviour Researchers), ABRA (Association of Behavioural Researchers on Asians) and cE-Bs (Centre for Environment-Behaviour Studies), Faculty of Architecture, Planning & Surveying, Universiti Teknologi MARA, Malaysia.
DOI: https://doi.org/10.21834/ebpj.v5iSI3.2532
Сучасні підходи до вибору базисної терапії легкої персистуючої бронхіальної астми у дітей
Authors: Nedelska S.M. , Kuznietsova O.D. , Raskina K.V. 
Published: December 2020

Мета роботи: удосконалення лікування легкої персистуючої бронхіальної астми на підставі розроблення диференційної програми протизапальної терапії. Зі 120 дітей сформовані 3 групи залежно від ефективної базисної терапії (антилейкотрієновий препарат, флутиказону пропіонат або їх комбінація), яка дозволила досягти контролю над захворюванням. Результати. Найбільш високі концентрації лейкотрієнів C4/D4/E4 у сироватці крові спостерігалися у дітей 3-ї групи, навіть після лікування вони залишалися вищими, ніж у дітей контрольної групи. При рівні лейкотрієнів від 500 до 1000 пг/мл шанси досягти контролю над бронхіальною астмою за допомогою антилейкотрієнового препарату у 5,9 раза вищі порівняно з інгаляційними глюкокортикостероїдами (95% довірчий інтервал 2,01–18,2). А коли рівень лейкотрієнів (C4/D4/E4) перевищував 1000 пг/мл, комбіноване лікування є ефективнішим, ніж терапія антилейкотрієновим препаратом (відношення шансів (OR) = 6,7; СІ95% 2,5–17,8) та флутиказону пропіонатом (OR = 83,3; СІ95% 9,9– 667,9).Висновки. Антилейкотрієновий препарат як монотерапія показаний дітям 6–7 років з легкою персистуючою бронхіальною астмою при сироваткових рівнях лейкотрієнів від 500 до 1000 пг/мл. При рівні лейкотрієнів нижче від 500 пг/мл доцільно призначати флутиказону пропіонат, вище від 1000 пг/мл — комбінацію антилейкотрієнового препарату та інгаляційного глюкокортикостероїду.
Вплив базисної фармакотерапії на стан мозкової гемодинаміки у хворих на бронхіальну астму дітей
Authors: Akulova O.Yu. , Nedelska S.M. 
Published: December 2020

У статті проаналізовано вплив базисної фармакотерапії на стан екстра- та інтракраніальної церебральної гемодинаміки у хворих на бронхіальну астму (БА) дітей. Монотерапія антилейкотрієновими препаратами нормалізує найбільшу кількість показників церебральної гемодинаміки, на другому місці — комбіноване лікування глюкокортикостероїдами та антилейкотрієновими препаратами, найменш ефективна базисна інгаляційна глюкокортикостероїдна терапія. Жодна проаналізована схема не усуває явища гіпоперфузії у вертебробазилярній зоні у хворих на БА дітей. У період ремісії декілька показників церебральної гемодинаміки, щодо яких усі перелічені схеми базисної фармакотерапії БА були ефективними, погіршилися та статистично не відрізнялись від аналогічних показників хворих із неконтрольованим перебігом БА. Хворі на БА діти повинні перебувати під наглядом дитячого невролога та потребують планового допплерографічного дослідження магістральних судин голови та шиї незалежно від ступеня контролю основного захворювання.