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Antiproliferative and Anti-inflammatory Drugs

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (23 September 2022) | Viewed by 7274

Special Issue Editors


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Guest Editor
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampl. Polifunzionale, Via P. Bucci, 87036 Arcavacata di Rende, Italy
Interests: drug design; small molecules; natural compounds; protein targeting; anticancer; antiviral; metabolic disorders
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Pharmacy, Health and Nutritional Science, University of Calabria, 87036 Rende, CS, Italy
Interests: drug stability; photodegradation; light-stable formulations
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Inflammation is a physiological response of the immune system to damaging stimuli, including pathogens, toxic compounds, irradiation, or altered cells. Uncontrolled inflammation may turn into a variety of more severe diseases involving several mediators of regulatory pathways. Several studies suggest that inflammation conditions could predispose individuals to develop cancer by promoting key stages of tumorigenesis.

Despite the recent progress in cancer research, there are still many concerns that need to be addressed in order to develop new and efficient therapeutics overcoming the side effects caused by conventional antineoplastic drugs.

New active molecules and handy drug-releasing devices are currently compelling research goals in medicinal chemistry. The definition of innovative and stable pharmaceutical formulations, able of optimize pharmacokinetic properties and protect drugs from degradation, represent new aspects being widely investigated. The monitoring system is nowadays regulated by the international guidelines from ICH (International Conference on Harmonization), which arranges the stability study of both a drug and its pharmaceutical forms.

This Special Issue aims to highlight current efforts in pharmaceutical chemistry and pharmacology towards innovative strategies against cancer and inflammation. Its content will focus on advanced drug discovery approaches by in silico identification of alternative natural and synthetic therapeutic agents, structure–activity relationships definition, and design of convenient synthetic strategies of new effective agents. Reports on the application of nanotechnologies and the biological and computational evaluation of newly synthesized or current drugs will be considered as well.

Dr. Fedora Grande
Dr. Giuseppina Ioele
Guest Editors

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • natural and synthetic compounds
  • drug design and synthesis
  • pharmacophore modelling and dynamic simulations
  • structure–activity relationships
  • target validation
  • biological evaluation
  • drug Stability
  • protective systems

Published Papers (2 papers)

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Research

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18 pages, 3991 KiB  
Article
The Assessment of Meloxicam Phototoxicity in Human Normal Skin Cells: In Vitro Studies on Dermal Fibroblasts and Epidermal Melanocytes
by Marta Karkoszka, Jakub Rok, Klaudia Banach, Justyna Kowalska, Zuzanna Rzepka and Dorota Wrześniok
Molecules 2022, 27(13), 4215; https://doi.org/10.3390/molecules27134215 - 30 Jun 2022
Cited by 3 | Viewed by 1491
Abstract
Meloxicam (MLX), which belongs to the oxicam nonsteroidal anti-inflammatory drug derivatives, is an inhibitor of the cyclooxygenase-2 (COX-2) enzyme. Cutaneous adverse effects caused by interaction between UVA radiation and exogenous factors can manifest as phototoxic reactions. Phototoxicity may be a reason for the [...] Read more.
Meloxicam (MLX), which belongs to the oxicam nonsteroidal anti-inflammatory drug derivatives, is an inhibitor of the cyclooxygenase-2 (COX-2) enzyme. Cutaneous adverse effects caused by interaction between UVA radiation and exogenous factors can manifest as phototoxic reactions. Phototoxicity may be a reason for the accumulation of genetic and molecular changes in long-lived cells with low proliferation potential, leading to tumor development. There are several potentially phototoxic drugs, the active component of which is meloxicam. The research aimed to evaluate the influence of MLX and UVAR on skin cells—fibroblasts and melanocytes homeostasis. The obtained results indicated that co-treatment with MLX and UVAR inhibited skin cell proliferation, proportionally to the drug concentration. The observation was confirmed by cytometric analysis of the cell number and viability. The phototoxic effect of MLX was revealed in morphological changes. It was stated that MLX with UVAR lowered the mitochondrial transmembrane potential and changed the cell cycle profile. Additionally, MLX and UVAR caused the disruption of redox homeostasis by lowering the intracellular level of reduced thiols. The presented study revealed that the phototoxic activity of MLX is associated with oxidative stress induction and disruptions in cell homeostasis. The differences in the phototoxic effects of MLX at the cellular level may be related to the different content of melanin pigments. Full article
(This article belongs to the Special Issue Antiproliferative and Anti-inflammatory Drugs)
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Review

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23 pages, 727 KiB  
Review
Anticancer Drugs: Recent Strategies to Improve Stability Profile, Pharmacokinetic and Pharmacodynamic Properties
by Giuseppina Ioele, Martina Chieffallo, Maria Antonietta Occhiuzzi, Michele De Luca, Antonio Garofalo, Gaetano Ragno and Fedora Grande
Molecules 2022, 27(17), 5436; https://doi.org/10.3390/molecules27175436 - 25 Aug 2022
Cited by 35 | Viewed by 5219
Abstract
In past decades, anticancer research has led to remarkable results despite many of the approved drugs still being characterized by high systemic toxicity mainly due to the lack of tumor selectivity and present pharmacokinetic drawbacks, including low water solubility, that negatively affect the [...] Read more.
In past decades, anticancer research has led to remarkable results despite many of the approved drugs still being characterized by high systemic toxicity mainly due to the lack of tumor selectivity and present pharmacokinetic drawbacks, including low water solubility, that negatively affect the drug circulation time and bioavailability. The stability studies, performed in mild conditions during their development or under stressing exposure to high temperature, hydrolytic medium or light source, have demonstrated the sensitivity of anticancer drugs to many parameters. For this reason, the formation of degradation products is assessed both in pharmaceutical formulations and in the environment as hospital waste. To date, numerous formulations have been developed for achieving tissue-specific drug targeting and reducing toxic side effects, as well as for improving drug stability. The development of prodrugs represents a promising strategy in targeted cancer therapy for improving the selectivity, efficacy and stability of active compounds. Recent studies show that the incorporation of anticancer drugs into vesicular systems, such as polymeric micelles or cyclodextrins, or the use of nanocarriers containing chemotherapeutics that conjugate to monoclonal antibodies can improve solubility, pharmacokinetics, cellular absorption and stability. In this study, we summarize the latest advances in knowledge regarding the development of effective highly stable anticancer drugs formulated as stable prodrugs or entrapped in nanosystems. Full article
(This article belongs to the Special Issue Antiproliferative and Anti-inflammatory Drugs)
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