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Biological Activities of Natural Products, Antipsychotics, and Novel Derivatives -...
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Biological Activities of Natural Products, Antipsychotics, and Novel Derivatives - Volume II

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Biochemistry, Biophysics and Computational Biology".

Deadline for manuscript submissions: closed (28 October 2022) | Viewed by 7471

Special Issue Editors

Dr. Michał Otręba

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Guest Editor
Department of Drug Technology, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia in Katowice, St Jedności 8, 41-200 Sosnowiec, Poland
Interests: anticancer activity; cellular assays; bee products; antioxidant activity; phenothiazine derivatives
Special Issues, Collections and Topics in MDPI journals
Dr. Leon Kosmider

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Guest Editor
Department of General and Inorganic Chemistry, Faculty of Pharmaceutical Sciences, Medical University of Silesia, 41-200 Sosnowiec, Poland
Interests: electronic cigarettes; addiction; public health; toxycology
Special Issues, Collections and Topics in MDPI journals
Dr. Anna Kleczka

E-Mail Website
Guest Editor
Department of Pathology, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia in Katowice, 41-200 Sosnowiec, Poland
Interests: natural bioactive compounds; polyphenols; chemoprevention; cell cycle; ovarian cancer biology; apoptosis; cytopathology; SARS-CoV-2 research

Special Issue Information

Dear Colleagues,

In our special issue we want to focus on anti-bacteria, anti-cancer, anti-fungal, anti-viral, and other biological activities of natural compound, antipsychotic drugs and their novel derivatives. All of the activities represents major problem of human health. The viral infections still represents major problem - up to date, antiviral drugs are used only for treating less than 10 viral infections (still no effective enough drugs against Zika, Ebola, and severe acute respiratory syndrome (SARS) virus). WHO confirmed 339,000 and 13,600–20,400, cases of deaths globally caused respectively by hepatitis C virus, and Japanese encephalitis virus. In case of COVID-19 5.374,744 cases of deaths up till now.

Next problem is increasing drug-resistance in microbial infections treatment. In 2019 WHO published a report to avert a potentially disastrous drug-resistance crisis – they predict about 10 million deaths each year by 2050 caused by drug-resistant diseases, while by 2030, antimicrobial resistance could force up to 24 million people into extreme poverty.

Another problem is global increase of deaths caused by different cardiovascular diseases indicated by the WHO and Eurostat statistics data for 2016, as well as the European Heart Network data for 2017. Noteworthy, in some cases, the global death percentage is higher than the number of deaths caused by malignant neoplasm cancer (26.0%).

Finally, due to the WHO cancer is a leading cause of death worldwide (in 2020 caused about 10 million deaths worldwide). The most common in 2020 were: breast, lung, colon & rectum, prostate, skin, and stomach cancers.

Thus, to find new and more effective methods of treating above mentioned diseases drug repurposing/repositioning or natural products can be used. For example, phenothiazine derivatives can be taken into consideration for repurposing in the bacterial and viral infections as well as cancer. On the other hand, natural products such as propolis, honey, pollen, royal jelly, and wax possess anti-inflammatory, anti-bacterial, anti-fungal, anticancer, neuroprotective, cardioprotective, and chemopreventive activity.

Dr. Michał Otręba
Dr. Leon Kosmider
Dr. Anna Kleczka
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Life is an international peer-reviewed open access monthly 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 2600 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

  • in vitro assays using human and/or animal cancer and normal cell lines (viability, cell death: apoptosis, necrosis, necroptosis, autophagy
  • cellular migration & invasion
  • cell cycle
  • protein level
  • enzymes activity
  • proteins expression
  • genes expression
  • melanogenesis, antioxidant activity, and other)
  • in vivo assays
  • anticancer, antifungal, antibacterial, antiviral, and other biological activities
  • cardiovascular, brain, viral, fungal, bacterial and other human diseases treatment
  • antipsychotics and their new derivatives
  • natural products biological and protective activities
  • inhibition of bacterial growth (MIC, MBC)
  • drug-resistance / Multidrug resistance (MDR)

Related Special Issue

Published Papers (4 papers)

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Research

19 pages, 4711 KiB  
Article
Parkia speciosa Hassk. Empty Pod Extract Prevents Cardiomyocyte Hypertrophy by Inhibiting MAPK and Calcineurin-NFATC3 Signaling Pathways
by Nor Hidayah Mustafa, Juriyati Jalil, Mohammed S. M. Saleh, Satirah Zainalabidin, Ahmad Yusof Asmadi and Yusof Kamisah
Life 2023, 13(1), 43; https://doi.org/10.3390/life13010043 - 23 Dec 2022
Cited by 2 | Viewed by 1426
Abstract
Cardiac hypertrophy is an early hallmark during the clinical course of heart failure. Therapeutic strategies aiming to alleviate cardiac hypertrophy via the mitogen-activated protein kinase (MAPK)/calcineurin-nuclear factor of activated T-cells (NFAT) signaling pathway may help prevent cardiac dysfunction. Previously, empty pod ethanol crude [...] Read more.
Cardiac hypertrophy is an early hallmark during the clinical course of heart failure. Therapeutic strategies aiming to alleviate cardiac hypertrophy via the mitogen-activated protein kinase (MAPK)/calcineurin-nuclear factor of activated T-cells (NFAT) signaling pathway may help prevent cardiac dysfunction. Previously, empty pod ethanol crude extract of Parkia speciosa Hassk was shown to demonstrate protective effects against cardiomyocyte hypertrophy. Therefore, the current study aimed to investigate the effects of various fractions of the plant ethanol extract on the MAPK/NFAT signaling pathway in angiotensin II (Ang II)-induced cardiomyocyte hypertrophy. Simultaneous treatment with ethyl acetate (EA) fraction produced the most potent antihypertrophic effect evidenced by the reduced release of B-type natriuretic peptide (BNP). Subsequently, treatment with the EA fraction (6.25, 12.5, and 25 μg/mL) prevented an Ang II-induced increase in cell surface area, hypertrophic factors (atrial natriuretic peptide and BNP), reactive oxygen species, protein content, and NADPH oxidase 4 expression in the cells. Furthermore, EA treatment attenuated the activation of the MAPK pathway and calcineurin-related pathway (GATA-binding protein 4 and NFATC3), which was similar to the effects of valsartan (positive control). Our findings indicate that the EA fraction prevents Ang II-induced cardiac hypertrophy by regulating the MAPK/calcineurin-NFAT signaling pathway. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products, Antipsychotics, and Novel Derivatives - Volume II)
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20 pages, 4191 KiB  
Article
Targeting Ca2+ and Mitochondrial Homeostasis by Antipsychotic Thioridazine in Leukemia Cells
by Vivian W. R. Moraes, Vivian M. Santos, Eloah R. Suarez, Letícia S. Ferraz, Rayssa de Mello Lopes, Giuliana P. Mognol, Joana D. Campeiro, João A. Machado-Neto, Fabio D. Nascimento, Mirian A. F. Hayashi, Ivarne L. S. Tersariol, Donald D. Newmeyer and Tiago Rodrigues
Life 2022, 12(10), 1477; https://doi.org/10.3390/life12101477 - 23 Sep 2022
Cited by 5 | Viewed by 1934
Abstract
Mitochondria have pivotal roles in cellular physiology including energy metabolism, reactive oxygen species production, Ca2+ homeostasis, and apoptosis. Altered mitochondrial morphology and function is a common feature of cancer cells and the regulation of mitochondrial homeostasis has been identified as a key [...] Read more.
Mitochondria have pivotal roles in cellular physiology including energy metabolism, reactive oxygen species production, Ca2+ homeostasis, and apoptosis. Altered mitochondrial morphology and function is a common feature of cancer cells and the regulation of mitochondrial homeostasis has been identified as a key to the response to chemotherapeutic agents in human leukemias. Here, we explore the mechanistic aspects of cytotoxicity produced by thioridazine (TR), an antipsychotic drug that has been investigated for its anticancer potential in human leukemia cellular models. TR exerts selective cytotoxicity against human leukemia cells in vitro. A PCR array provided a general view of the expression of genes involved in cell death pathways. TR immediately produced a pulse of cytosolic Ca2+, followed by mitochondrial uptake, resulting in mitochondrial permeabilization, caspase 9/3 activation, endoplasmic reticulum stress, and apoptosis. Ca2+ chelators, thiol reducer dithiothreitol, or CHOP knockdown prevented TR-induced cell death. TR also exhibited potent cytotoxicity against BCL-2/BCL-xL-overexpressing leukemia cells. Additionally, previous studies have shown that TR exhibits potent antitumor activity in vivo in different solid tumor models. These findings show that TR induces a Ca2+-mediated apoptosis with involvement of mitochondrial permeabilization and ER stress in leukemia and it emphasizes the pharmacological potential of TR as an adjuvant in antitumor chemotherapy. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products, Antipsychotics, and Novel Derivatives - Volume II)
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10 pages, 1641 KiB  
Article
Biological Potential of the Main Component, Thymoquinone, of Nigella sativa in Pulp Therapy—In Vitro Study
by Rana A. Alamoudi, Soha A. Alamoudi and Ruaa A. Alamoudi
Life 2022, 12(9), 1434; https://doi.org/10.3390/life12091434 - 15 Sep 2022
Cited by 2 | Viewed by 1419
Abstract
This work is designed to assess the antimicrobial efficacy, chelating efficacy, and dissolving capability of the bioactive agent of the Nigella sativa plant (thymoquinone). Four freeze-dried microorganisms were studied. Each species was treated with either 6% sodium Hypochlorite, thymoquinone, or sterile water. The [...] Read more.
This work is designed to assess the antimicrobial efficacy, chelating efficacy, and dissolving capability of the bioactive agent of the Nigella sativa plant (thymoquinone). Four freeze-dried microorganisms were studied. Each species was treated with either 6% sodium Hypochlorite, thymoquinone, or sterile water. The zone of inhibition was measured. Thirty extracted human premolar teeth were utilized to evaluate the smear layer removal. Root canals were mechanically instrumented and then irrigated with either 6% sodium Hypochlorite, 17% ethylenediaminetetraacetic acid, or thymoquinone for 1 min and scanned under the scanning electron microscopic to evaluate the cleanliness of the root canal and the remainder of the smear layer. To evaluate the tissue dissolving effect, Bovine Pulp Tissue was utilized. Randomly treated samples included: 6% sodium Hypochlorite, thymoquinone, or isotonic saline for 30 min. The remaining pulp tissue was weighed. Thymoquinone reported the highest inhibition of microbial multiplication compared to other irrigants (p < 0.001). Thymoquinone solution had an excellent antibacterial effect on endodontic pathogen and did not affect the inorganic and organic tissue inside the root canal. Meanwhile, it reported weak chelating and dissolving effects. Tissue dissolution was statistically significant with sodium Hypochlorite solution compared to other groups (p < 0.001). Full article
(This article belongs to the Special Issue Biological Activities of Natural Products, Antipsychotics, and Novel Derivatives - Volume II)
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9 pages, 547 KiB  
Communication
Does Protocatechuic Acid Affect the Activity of Commonly Used Antibiotics and Antifungals?
by Adrian Fifere, Ioana-Andreea Turin-Moleavin and Irina Rosca
Life 2022, 12(7), 1010; https://doi.org/10.3390/life12071010 - 07 Jul 2022
Cited by 3 | Viewed by 1659
Abstract
The aim of this study is to evaluate the efficiency of protocatechuic acid (PCA) in enhancing the commonly used drugs used to fight against nosocomial infection. These drugs are represented by routinely used antibiotics, synthetic chemotherapeutic agents with an antimicrobial spectrum, and antifungals. [...] Read more.
The aim of this study is to evaluate the efficiency of protocatechuic acid (PCA) in enhancing the commonly used drugs used to fight against nosocomial infection. These drugs are represented by routinely used antibiotics, synthetic chemotherapeutic agents with an antimicrobial spectrum, and antifungals. Three concentrations of PCA were added to 12 types of commercial disks used for antibiotic and antifungal susceptibility and tested against bacterial and yeast strains represented by Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans. The results proved that PCA increased up to 50% of the antibacterial activity, especially that of levofloxacin against Staphylococcus aureus and Escherichia coli. These formulations will lead to new drug design ideas containing a smaller amount of antibiotics with the same effectiveness. Full article
(This article belongs to the Special Issue Biological Activities of Natural Products, Antipsychotics, and Novel Derivatives - Volume II)
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