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Pegylation of phenothiazine - A synthetic route towards potent anticancer drugs
No full textIntroduction: Cancer is a big challenge of the 21 century, whose defeat requires efficient antitumor drugs.
Objectives: The paper aims to investigate the synergistic effect of two structural building blocks, phenothiazine
and poly(ethylene glycol), towards efficient antitumor drugs.
Methods: Two PEGylated phenothiazine derivatives were synthetized by attaching poly(ethylene glycol)
of 550 Da to the nitrogen atom of phenothiazine by ether or ester linkage. Their antitumor activity has
been investigated on five human tumour lines and a mouse tumor line as well, by determination of
IC50. The in vivo toxicity was determined by measuring the LD50 in BALB/c mice by the sequential
method and the in vivo antitumor potential was measured by the tumours growth test. The antitumor
mechanism was investigated by complexation studies of zinc and magnesium ions characteristic to the
farnesyltransferase enzyme, by studies of self-aggregation in the cells proximity and by investigation
of the antitumor properties of the acid species resulted by enzymatic cleavage of the PEGylated derivatives.
Results: The two compounds showed antitumor activity, with IC50 against mouse colon carcinoma cell
line comparable with that of the traditional antitumor drugs 5-Fluorouracil and doxorubicin. The phenothiazine
PEGylation resulted in a significant toxicity diminishing, the LD50 in BALB/c mice increasing
from 952.38 up to 1450 mg/kg, in phenothiazine equivalents. Both compounds inflicted a 92% inhibition of the tumour growth for doses much smaller than LD50. The investigation of the possible tumour inhibition
mechanism suggested the nanoaggregate formation and the cleavage of ester bonds as key factors
for the inhibition of cancer cell proliferation and biocompatibility improvement.
Conclusion: Phenothiazine and PEG building blocks have a synergetic effect working for both tumour
growth inhibition and biocompatibility improvement. All these findings recommend the PEGylated phenothiazine
derivatives as a valuable workbench for a next generation of antitumor drugs
Elaboration of biodegradable whey isolate film incorporated with green synthesized silver nanoparticles
No full textFinding a feasible alternative to reduce the use of conventional polymers in the plastic sector has become a top priority,
since industrially generated plastic waste, mostly traditional food packaging, has turned into a global environmental
disaster. The aim of the study was the preparation and characterization of biodegradable films based on whey protein
isolate, functionalized with green synthesized nanoparticles. Green silver nanoparticles (AgNPs) were synthesized using
cinnamon extract as both capping and reducing agent. Biodegradable nanocomposite blend films based on silver
nanoparticles and whey protein isolate (WPI) were made by casting denatured WPI film solutions incorporated with
green synthesized silver nanoparticles. The film thickness and water vapor permeability (WVP) of both control and
AgNPs were determined. The biodegradable films based on whey and (1%) green synthesized nanoparticles have
potential application as active food packaging in the cheese industry
Research concerning the behavior of smooth bromegrass (Bromus inermis Leyss.) and common sainfoin (Onobrychis viciifolia Scop.) alone and in simple mixtures under the conditions of Jiji-Bahlui depression
No full textStudy regarding the changes in some hepatic parameters during general anesthesia in a group of dogs
Get PDFThe main organ involved in the biotransformation of the anesthetic drugs used for general anesthesia is the liver. Drugs
will be at this level transformed into more easily excreted substances known as metabolites.The evaluation of the
hepatic function before general anesthesia is essential for a safe and individualized protocol.Comprehensive
understanding of the anesthetic drugs and their effects on hepatic functions during anesthesia remains
fundamental.Techniques and protocols used for anesthesia and intensive care in the recovery phase will be designed
taking into account the trend of the hepatic parameters.This study will focus on how the general anesthesia influences
hepatic parameters measured before premedication and in the early recovery phase: alanine aminotransferase (ALT),
alkaline phosphatase (ALP),total proteins (TP) and albumin (ALB). Following the result of the study,we discovered
that ALP increased with 11% and ALT decresed with 12% after general anesthesia in comparison with the value before
premedication
Study of phenolic and volatile compounds from Busuioaca de Bohotin wine in order to establish the typicity of the variety
No full textResearches regarding the fauna of Coccinellide (Coleoptera- Coccinellidae) within some agricultural crops from NE part of Moldova
No full textStudy of the urban heat island in Iasi municipality using remote sensing and GIS
No full textCurrent climate change in urban areas is manifested due to the rapid urbanization of cities around the world. The island
of urban heat is represented by a metropolitan area significantly warmer than the environment. It is important to find a
balance between urban expansion and the temperatures recorded in these areas to guarantee sustainable urban
development. This paper is a study to highlight the temperature of the ground surface (LST values) both during the day
and at night, for the area of Iasi municipality. Remote sensing and GIS techniques were used for the case study. In order
to make LST maps, MODIS images, taken daily by the Terra and Aqua satellites between 2013-2018, were used as
primary data. Also, a number of 8 sensors were installed on the ground in the study area in order to monitor the
temperature in the 2013-2018 period. The conslusion
Review: the epidemiology and zoonotic risks of coronaviroses
Get PDFThe following paper includes a synthesis of bibliographical information regarding the main diseases caused by
coronaviruses, both in animals (companion and domestic) as well as in humans, observing the imprevisible tendencies
of this viral family. These data are completed by an epidemiological analysis of the main events caused by
coronaviruses in humans, using the available databases.
Coronaviruses are worldspread entities, producing, in humans and animals, the most diverse diseases, with digestive,
respiratory or nervous symptoms in animals, some forms being very serious and with special economic implications and
others mild or even clinically unexpressed; in humans, the symptoms are predominantly respiratory, in some cases
beginning with digestive signs and the complications that occur may be neurological in nature. Over the years,
especially since 2002 (SARS-CoV), continuing with 2012 (MERS) and more recently, from 2019, culminating with
SARS-CoV-2, it has been possible to identify the trend of zoonotic transmission (from animal to human), with a
particularly high pathogenic potential of these viruses, which have different rates of morbidity and mortality. Another
interesting aspect is the fact that cases of anthropozoonotic transmission (from human to animal) have been reported, in
the case of pets, but also of fur animals (minks)
Appreciation of changing climatic conditions, hydrography and soil distribution in Costuleni village
No full textThe climate of the Republic of Moldova and its Central Region is temperate continental with a transitional character
and is formed under the influence of three groups of climatogenesis factors: radiative, dynamic and physicogeographical. Also, the climate of our Republic is characterized by mild and short winters, with little snow, long, hot
summers, but with an insufficient amount of atmospheric precipitation, which fall predominantly in the warm period of
the year in the form of showers. In this paper will be examined the ecological status of Costuleni locality, Ungheni
district. The evaluation and study were carried out according to the standards and normative acts in force for the
Republic of Moldova. The research consists in identifying the ecological status of the locality, through observations,
comparisons, as well as, data collection, organization and evaluation. Environmental impact assessment - represents the
assessment (quantification) of the effects of human activities and negative natural processes on natural elements and
factors, ecosystems, human health and safety, as well as on material goods. Various specialized publications, scientific
papers, legislative and normative acts, plans and strategies for sustainable development, statistical and activity reports
of the Ministry of Environment and State Ecological Inspectorate, as well as those of the Ungheni Ecological Inspection
were studied. Ensuring the long-term survival of ecological systems, the main provider of resources on which
development and human well-being depend, can only be achieved in the case of sustainable development. Equally
important is the role of biodiversity in providing services provided by ecological systems, such as determining soil and
climate conditions, water purification, mitigating the effects of natural disasters, etc
