214 research outputs found
A Review on the Antimicrobial Activity of Schiff Bases: Data Collection and Recent Studies
Schiff bases (SBs) have extensive applications in different fields such as analytical, inor‐
ganic and organic chemistry. They are used as dyes, catalysts, polymer stabilizers, luminescence
chemosensors, catalyzers in the fixation of CO2 biolubricant additives and have been suggested for
solar energy applications as well. Further, a wide range of pharmacological and biological applica‐
tions, such as antimalarial, antiproliferative, analgesic, anti‐inflammatory, antiviral, antipyretic, an‐
tibacterial and antifungal uses, emphasize the need for SB synthesis. Several SBs conjugated with
chitosan have been studied in order to enhance the antibacterial activity of chitosan. Moreover, the
use of the nanoparticles of SBs may improve their antimicrobial effects. Herein, we provide an ana‐
lytical overview of the antibacterial and antifungal properties of SBs and chitosan‐based SBs as well
as SBs‐functionalized nanoparticles. The most relevant and recent literature was reviewed for this
purpose
Antimicrobial and antioxidant properties and quantitative screening of phytochemicals of Fraxinus excelsior L. and Eschscholtzia californica Cham. mother tinctures
The antioxidant and antimicrobial activities of Fraxinus excelsior L.
and Eschscholtzia californica Cham. mother tinctures against a
range of foodborne bacteria were investigated to determine the
major components and to analyse the action spectrum and antimicrobial effectiveness of the extracts. Results demonstrated a significant antioxidant activity of Fraxinus excelsior L. and a lower
activity of Eschscholtzia californica Cham. and a good chemical
phenolic composition with the highest content of flavonoids. The
Fraxinus excelsior L. and Eschscholtzia californica Cham. mother
tinctures demonstrated a middle-high antimicrobial activity
against, respectively, 66.67% and 43.33% of all tested bacteria.
The inhibitory activity showed a moderate effect on the growth
of the sensitive strains in presence of extracts minimum inhibitory
concentration. The synergistic actions of bioactive compounds
detected in the extracts might be on the basis of antioxidant and
biological activities observed and should be used in pharmaceutical, food preservation, alternative medicine and natural therapies
fields
An Update of Carbazole Treatment Strategies for COVID-19 Infection
The Coronavirus disease 2019 (COVID-19) outbreak was declared by the World Health
Organization (WHO) in March 2020 to be a pandemic and many drugs used at the beginning proved
useless in fighting the infection. Lately, there has been approval of some new generation drugs for the
clinical treatment of severe or critical COVID-19 infections. Nevertheless, more drugs are required to
reduce the pandemic’s impact. Several treatment approaches for COVID-19 were employed since the
beginning of the pandemic, such as immunomodulatory, antiviral, anti-inflammatory, antimicrobial
agents, and again corticosteroids, angiotensin II receptor blockers, and bradykinin B2 receptor
antagonists, but many of them were proven ineffective in targeting the virus. So, the identification of
drugs to be used effectively for treatment of COVID-19 is strongly needed. It is aimed in this review
to collect the information so far known about the COVID-19 studies and treatments. Moreover, the
observations reported in this review about carbazoles as a treatment can signify a potentially useful
clinical application; various drugs that can be introduced into the therapeutic equipment to fight
COVID-19 or their molecules can be used as the basis for designing new antivirals
Carbazoles: Role and Functions in Fighting Diabetes
Carbazole derivatives have gained a lot of attention in medicinal chemistry over the
last few decades due to their wide range of biological and pharmacological properties, including
antibacterial, antitumor, antioxidant, and anti-inflammatory activities. The therapeutic potential of
natural, semi-synthetic or synthetic carbazole-containing molecules has expanded considerably owing
to their role in the pathogenesis and development of diabetes. Several studies have demonstrated
the ability of carbazole derivatives to reduce oxidative stress, block adrenergic hyperactivation,
prevent damage to pancreatic cells and modulate carbohydrate metabolism. In this survey, we
summarize the latest advances in the synthetic and natural carbazole-containing compounds involved
in diabetes pathways
Synthesis of sericin-based conjugates by click chemistry: enhancement of sunitinib bioavailability and cell membrane permeation
Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw material for polypeptide-based drug delivery systems (DDSs). In this paper, it has been employed as pharmaceutical biopolymer for the production of sunitinib–polypeptide conjugate. The synthesis has been carried out by simple click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide as a free radical grafting initiator. The bioconjugate molecular weight (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic characteristics have been studied in order to reveal the presence of grafted sunitinib. In both FT-IR and UV/Vis spectra, signals corresponding to sunitinib functional groups have been identified. Since sunitinib is an anticancer drug characterized by low bioavailability and low permeability, the bioconjugation aimed at their enhancement. In vitro studies demonstrated that bioavailability has been increased to almost 74%, compared with commercial formulation. Also cell membrane permeability has been augmented in in vitro tests, in which membrane models have been used to determine the lipid membrane/physiological fluid partition coefficient (Kp). The log(Kp) value of the bioconjugate was increased to over 4. This effect resulted in a three-fold decrease of IC50 value against MCF-7 cells
Target Therapy in Cancer Treatment: mPGES-1 and PARP
Target therapy is an approach focusing on specific protein or signaling pathways. This therapy is
directly aimed to a molecular target such as a receptor, growth factor or enzyme in cancer cells. These
targets are used by the tumor cells themselves to obtain uncontrolled proliferation, resistance to
traditional therapies and to increase the number of blood vessels in the tissue of origin (neoangiogenesis). A purpose of target therapy may be to counteract the growth and proliferation of
cancer cells through the use of drugs or monoclonal antibodies capable of inhibiting the receptor for
the epidermal growth factor (EGFR), that is crucial in the process of neo-angiogenesis, protein kinases
(PKs), as regulators of cell growth signals and human epidermal growth factor type 2 (HER2), which is
essential in stimulating growth and proliferation of cancer cells. Among anticancer drugs,
Bevacizumab, a humanised monoclonal antibody produced by recombinant DNA technique, is used for
the first-line treatment of metastatic breast cancer, as it inhibits EGFR and the vascular endothelial cell
growth factor (VEGF). Abemaciclib, a protein kinase inhibitor drug, is also used for the treatment of the
same cancer. In 20-30% of primary breast tumors, the excessive expression of HER2 is observed; thus,
HER2 inhibitors may represent another plausible therapy. A potent HER2 inhibitor is the recombinant
humanized igG1 monoclonal antibody Trastuzumab, which was first tested in 1992 and is currently used
for the treatment of HER2 positive breast cancer. Unfortunately, despite the numerous advances in
finding new therapies, patients treated with these drugs often suffer from severe undesirable side
effects. Therefore, the search for new therapeutic targets may be desirable. In this paper we analyse
particularly two targets studied quite recently: the microsomal prostaglandin E2 synthase type 1
(mPGES-1) and poly (ADP-ribose) polymerase (PARP) proteins
Target Therapy in Cancer Treatment: mPGES-1 and PARP
Target therapy is an approach focusing on specific protein or signaling pathways. This therapy is
directly aimed to a molecular target such as a receptor, growth factor or enzyme in cancer cells. These
targets are used by the tumor cells themselves to obtain uncontrolled proliferation, resistance to
traditional therapies and to increase the number of blood vessels in the tissue of origin (neoangiogenesis). A purpose of target therapy may be to counteract the growth and proliferation of
cancer cells through the use of drugs or monoclonal antibodies capable of inhibiting the receptor for
the epidermal growth factor (EGFR), that is crucial in the process of neo-angiogenesis, protein kinases
(PKs), as regulators of cell growth signals and human epidermal growth factor type 2 (HER2), which is
essential in stimulating growth and proliferation of cancer cells. Among anticancer drugs,
Bevacizumab, a humanised monoclonal antibody produced by recombinant DNA technique, is used for
the first-line treatment of metastatic breast cancer, as it inhibits EGFR and the vascular endothelial cell
growth factor (VEGF). Abemaciclib, a protein kinase inhibitor drug, is also used for the treatment of the
same cancer. In 20-30% of primary breast tumors, the excessive expression of HER2 is observed; thus,
HER2 inhibitors may represent another plausible therapy. A potent HER2 inhibitor is the recombinant
humanized igG1 monoclonal antibody Trastuzumab, which was first tested in 1992 and is currently used
for the treatment of HER2 positive breast cancer. Unfortunately, despite the numerous advances in
finding new therapies, patients treated with these drugs often suffer from severe undesirable side
effects. Therefore, the search for new therapeutic targets may be desirable. In this paper we analyse
particularly two targets studied quite recently: the microsomal prostaglandin E2 synthase type 1
(mPGES-1) and poly (ADP-ribose) polymerase (PARP) proteins
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