76 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, inorâ
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 applicaâ
tions, such as antimalarial, antiproliferative, analgesic, antiâinflammatory, antiviral, antipyretic, anâ
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 anaâ
lytical overview of the antibacterial and antifungal properties of SBs and chitosanâbased SBs as well
as SBsâfunctionalized nanoparticles. The most relevant and recent literature was reviewed for this
purpose
A Look at the Importance of Chirality in Drug Activity: Some Significative Examples
[EN] Chirality plays an important role in the development of many pharmaceuticals, being a general property of 'handedness'; nevertheless, a large number of pharmaceuticals are still marketed and administered as racemates. Chirality is all around and even within us; indeed, receptors and enzymes are chiral entities and interact in a specific manner with chiral drugs. Consequently, controlling enantiomeric purity and isolating the enantiomers from chiral drugs remains a crucial subject for analytical, clinical, and regulatory purposes, thus, improving the drug safety profile. The classical examples of spontaneous enantiomerization and severe toxicity related to chirality are represented by ibuprofen and thalidomide, respectively, but numerous other cases have been reported in the literature. This review intends to offer a brief overview on the most common chiral drugs used in therapy for the treatment of various diseases.Ceramella, J.; Iacopetta, D.; Franchini, A.; De Luca, M.; Saturnino, C.; Andreu, I.; Sinicropi, MS.... (2022). A Look at the Importance of Chirality in Drug Activity: Some
Significative Examples. Applied Sciences. 12(21):1-22. https://doi.org/10.3390/app122110909122122
Benzothiazole-Containing Analogues of Triclocarban with Potent Antibacterial Activity
Triclocarban (TCC) is a polychlorinated, aromatic, antimicrobial agent commercially used since the 1950s in personal care products for the prevention of spoilage and infections. Humans are frequently exposed to TCC due to its widespread use, leading to its substantial release into the aquatic environment. With the recent ban of TCC from some personal care products, implemented in 2016, many replacement antimicrobial compounds have been studied by researchers. Herein, we report the synthesis and biological activity of a series of diarylureas, analogues of TCC that bear the benzothiazole nucleus as one of the two aryl moieties. Among the studied compounds, 2bF and 2eC showed the highest antimicrobial activity against Staphylococcus aureus, being also more active than TCC, with MIC values of 8 ”g/mL versus 16 ”g/mL of TCC. Moreover, compound 2bB was much more active than TCC against Enterococcus faecalis, a Gram-positive bacterium that is, unfortunately, strongly responsible for nosocomial infections. Finally, interesting results were found for compound 2bG that, even though less active than the others, exerts an interesting bactericidal action
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
COVID-19 at a Glance: An Up-to-Date Overview on Variants, Drug Design and Therapies
Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is a member of the Coronavirus
family which caused the worldwide pandemic of human respiratory illness coronavirus
disease 2019 (COVID-19). Presumably emerging at the end of 2019, it poses a severe threat to public
health and safety, with a high incidence of transmission, predominately through aerosols and/or
direct contact with infected surfaces. In 2020, the search for vaccines began, leading to the obtaining
of, to date, about twenty COVID-19 vaccines approved for use in at least one country. However,
COVID-19 continues to spread and new genetic mutations and variants have been discovered, requiring
pharmacological treatments. The most common therapies for COVID-19 are represented by
antiviral and antimalarial agents, antibiotics, immunomodulators, angiotensin II receptor blockers,
bradykinin B2 receptor antagonists and corticosteroids. In addition, nutraceuticals, vitamins D and
C, omega-3 fatty acids and probiotics are under study. Finally, drug repositioning, which concerns
the investigation of existing drugs for new therapeutic target indications, has been widely proposed
in the literature for COVID-19 therapies. Considering the importance of this ongoing global public
health emergency, this review aims to offer a synthetic up-to-date overview regarding diagnoses,
variants and vaccines for COVID-19, with particular attention paid to the adopted treatments
NUTRACEUTICAL FUNCTIONS OF GREEN TEA
Today, the diffusion of neoplastic diseases is a widespread phenomenon. Thus, it is always
necessary to identify new molecules able to fight them. In this paper, we will deal with the interesting
antineoplastic properties of green tea. We will describe the different and plausible anticancer
mechanisms of epigallocatechin gallate (EGCG), the major polyphenol found in green tea, and in
particular the biochemical and computational discovery of a new target for the treatment of this
disease will be discussed. The bio-active substances present in tea are essentially represented by
methylxanthines, as well as by the antioxidant phenolic fraction (flavonoids). Among the other active
substances contained in lower concentrations there are vitamins (B, C and K), amino acids (L-theanine)
and minerals (aluminium and manganese). Tea extracts, particularly EGCG, could represent the starting
point for the potential emergence of new drugs for the treatment of neoplastic diseases. Other
activities of tea, as the involvement in neurodegenerative diseases prevention, as well as the
antioxidant, antibacterial, antifungal and antiviral effects, will be also briefly described
Multidrug Resistance (MDR): A Widespread Phenomenon in Pharmacological Therapies
Multidrug resistance is a leading concern in public health. It describes a complex phenotype whose predominant feature is resistance to a wide range of structurally unrelated cytotoxic compounds, many of which are anticancer agents. Multidrug resistance may be also related to antimicrobial drugs, and is known to be one of the most serious global public health threats of this century. Indeed, this phenomenon has increased both mortality and morbidity as a consequence of treatment failures and its incidence in healthcare costs. The large amounts of antibiotics used in human therapies, as well as for farm animals and even for fishes in aquaculture, resulted in the selection of pathogenic bacteria resistant to multiple drugs. It is not negligible that the ongoing COVID-19 pandemic may further contribute to antimicrobial resistance. In this paper, multidrug resistance and antimicrobial resistance are underlined, focusing on the therapeutic options to overcome these obstacles in drug treatments. Lastly, some recent studies on nanodrug delivery systems have been reviewed since they may represent a significant approach for overcoming resistance
Triclosan: A Small Molecule with Controversial Roles
Abstract: Triclosan (TCS), a broad-spectrum antimicrobial agent, has been widely used in personal
care products, medical products, plastic cutting boards, and food storage containers. Colgate TotalÂź
toothpaste, containing 10 mM TCS, is effective in controlling biofilm formation and maintaining
gingival health. Given its broad usage, TCS is present ubiquitously in the environment. Given its
strong lipophilicity and accumulation ability in organisms, it is potentially harmful to biohealth.
Several reports suggest the toxicity of this compound, which is inserted in the class of endocrine
disrupting chemicals (EDCs). In September 2016, TCS was banned by the U.S. Food and Drug
Administration (FDA) and the European Union in soap products. Despite these problems, its
application in personal care products within certain limits is still allowed. Today, it is still unclear
whether TCS is truly toxic to mammals and the adverse effects of continuous, long-term, and low
concentration exposure remain unknown. Indeed, some recent reports suggest the use of TCS as a
repositioned drug for cancer treatment and cutaneous leishmaniasis. In this scenario it is necessary
to investigate the advantages and disadvantages of TCS, to understand whether its use is advisable
or not. This review intends to highlight the pros and cons that are associated with the use of TCS
in humans
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