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Medicines, Volume 9, Issue 6 (June 2022) – 4 articles

Cover Story (view full-size image): In this investigation, hybrid molecules were formed which include the structural features of cytotoxic 3.5-bis(benzylidene)-4-piperidones (considered to be alkylators) and dichloroacetic acid, which inhibits pyruvate dehydrogenase kinase 1. The compounds are highly toxic to several neoplasms (CC50 values less than 1 µM) and much less toxic to three non-malignant cell lines. These observations reveal that these hybrid molecules demonstrate tumor-selective toxicity. The mode of action of representative compounds using Ca9-22 cells includes G2/M arrest, causing cells to undergo mitosis and cleavage of both PARP and procaspase-3. View this paper
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9 pages, 353 KiB  
Commentary
The Sweet Side of Fungal Infections: Structural Glycan Diversity and Its Importance for Pathogenic Adaptation
by Israel Diniz-Lima, Leonardo Marques da Fonseca, Jhenifer Santos dos Reis, Marcos André Rodrigues da Costa Santos, Kelli Monteiro da Costa, Carlos Antonio do Nascimento Santos, Pedro Marçal Barcelos, Kamila Guimarães-Pinto, Alessandra Almeida Filardy, Marco Edilson Freire-de-Lima, Debora Decote-Ricardo, Alexandre Morrot, Celio Geraldo Freire-de-Lima and Leonardo Freire-de-Lima
Medicines 2022, 9(6), 37; https://doi.org/10.3390/medicines9060037 - 16 Jun 2022
Cited by 4 | Viewed by 2157
Abstract
Fungal infections are the most common secondary infections in debilitated individuals in a state of chronic disease or immunosuppression. Despite this, most fungal infections are neglected, mainly due to the lower frequency of their more severe clinical forms in immunocompetent individuals with a [...] Read more.
Fungal infections are the most common secondary infections in debilitated individuals in a state of chronic disease or immunosuppression. Despite this, most fungal infections are neglected, mainly due to the lower frequency of their more severe clinical forms in immunocompetent individuals with a healthy background. However, over the past few years, several cases of severe fungal infections in healthy individuals have provoked a change in the epidemiological dynamics of fungal infections around the world, both due to recurrent outbreaks in previously infrequent regions and the greater emergence of more pathogenic fungal variants affecting healthy individuals, such as in the Cryptococcus genus. Therefore, before the arrival of a scenario of prevalent severe fungal infections, it is necessary to assess more carefully what are the real reasons for the increased incidence of fungal infection globally. What are the factors that are currently contributing to this new possible epidemiological dynamic? Could these be of a structural nature? Herein, we propose a discussion based on the importance of the virulence factors of glycoconjugate composition in the adaptation of pathogenic fungal species into the current scenario of increasing severity of these infections. Full article
15 pages, 328 KiB  
Article
Potential Role of Certain Biomarkers Such as Vitamin B12, ROS, Albumin, as Early Predictors for Prognosis of COVID-19 Outcomes
by Evgenia Lymperaki, Konstantina Kazeli, Georgia Variti, Magda Gerothanasi, Argyrios Gkinoudis, Ioannis Tsamesidis and Eleni Vagdatli
Medicines 2022, 9(6), 36; https://doi.org/10.3390/medicines9060036 - 15 Jun 2022
Cited by 1 | Viewed by 1820
Abstract
COVID-19 disease is still a major global concern because of its morbidity and its mortality in severe disease. Certain biomarkers including Reactive Oxygen Species (ROS), vitamins, and trace elements are known to play a crucial role in the pathophysiology of the disease. The [...] Read more.
COVID-19 disease is still a major global concern because of its morbidity and its mortality in severe disease. Certain biomarkers including Reactive Oxygen Species (ROS), vitamins, and trace elements are known to play a crucial role in the pathophysiology of the disease. The aim of our study was to evaluate how certain biomarkers, such as ROS, biochemical indicators, trace elements in serum blood of 139 COVID-19 hospitalized patients, and 60 non-COVID cases according to age and sex variations, can serve as the predictors for prognosis of COVID-19 outcome. An attempt of correlating these biomarkers with the severity of the disease as well as with each other is represented. All subjects were hospitalized from April 2021 until June 2021. A statistically significant increase of B12 levels (p = 0.0029) and ROS levels (p < 0.0001) as well as a decrease in albumin and Total Protein (T.P.) levels (p < 0.001) was observed especially in the early stage of the disease before CRP and ferritin elevation. Additionally, a statistically significant increase in ferritin (p = 0.007), B12 (p = 0.035, sALT p = 0.069, Glucose p = 0.012 and urea p = 0.096 and a decrease in Ca p = 0.005, T.P p = 0.052 albumin p = 0.046 between stage B (CRP values 6–30 mg/L) and C (CRP values 30–100 mg/L) was evident. Thus, this study concludes that clinicians could successfully employ biomarkers such as vitamin B12, ROS and albumin as possible prognosis tools for an early diagnosis. In addition, the total biochemical profile can assist in the understanding of the severity of COVID-19 disease, and could potentially lead to a better diet or early pharmaceutical treatment to prevent some of the more acute symptoms. Full article
11 pages, 2913 KiB  
Article
Dichloroacetyl Amides of 3,5-Bis(benzylidene)-4-piperidones Displaying Greater Toxicity to Neoplasms than to Non-Malignant Cells
by Mohammad Hossain, Praveen K. Roayapalley, Hiroshi Sakagami, Keitaro Satoh, Kenjiro Bandow, Umashankar Das and Jonathan R. Dimmock
Medicines 2022, 9(6), 35; https://doi.org/10.3390/medicines9060035 - 08 Jun 2022
Viewed by 1948
Abstract
A series of 3,5-bis(benzylidene)-1-dichloroacetyl-4-piperidones 1al was evaluated against Ca9-22, HSC-2, HSC-3, and HSC-4 squamous cell carcinomas. Virtually all of the compounds displayed potent cytotoxicity, with 83% of the CC50 values being submicromolar and several CC50 values being in the [...] Read more.
A series of 3,5-bis(benzylidene)-1-dichloroacetyl-4-piperidones 1al was evaluated against Ca9-22, HSC-2, HSC-3, and HSC-4 squamous cell carcinomas. Virtually all of the compounds displayed potent cytotoxicity, with 83% of the CC50 values being submicromolar and several CC50 values being in the double digit nanomolar range. The compounds were appreciably less toxic to human HGF, HPLF, and HPC non-malignant cells, which led to some noteworthy selectivity index (SI) figures. From these studies, 1d,g,k emerged as the lead molecules in terms of their potencies and SI values. A Quantitative Structure-Activity Relationship (QSAR) study revealed that cytotoxic potencies and potency–selectivity expression figures increased when the magnitude of the sigma values in the aryl rings was elevated. The modes of action of the representative cytotoxins in Ca9-22 cells were found to include G2/M arrest and stimulation of the cells to undergo mitosis and cause poly(ADP-ribose) polymerase (PARP) and procaspase 3 cleavage. Full article
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5 pages, 275 KiB  
Opinion
Glycobiology of Cancer: Sugar Drives the Show
by Jhenifer Santos dos Reis, Marcos André Rodrigues da Costa Santos, Daniella Pereira Mendonça, Stefani Ingrid Martins do Nascimento, Pedro Marçal Barcelos, Rafaela Gomes Correia de Lima, Kelli Monteiro da Costa, Celio Geraldo Freire-de-Lima, Alexandre Morrot, Jose Osvaldo Previato, Lucia Mendonça Previato, Leonardo Marques da Fonseca and Leonardo Freire-de-Lima
Medicines 2022, 9(6), 34; https://doi.org/10.3390/medicines9060034 - 24 May 2022
Cited by 5 | Viewed by 2259
Abstract
Cancer development and progression is associated with aberrant changes in cellular glycosylation. Cells expressing altered glycan-structures are recognized by cells of the immune system, favoring the induction of inhibitory immune processes which subsequently promote tumor growth and spreading. Here, we discuss about the [...] Read more.
Cancer development and progression is associated with aberrant changes in cellular glycosylation. Cells expressing altered glycan-structures are recognized by cells of the immune system, favoring the induction of inhibitory immune processes which subsequently promote tumor growth and spreading. Here, we discuss about the importance of glycobiology in modern medicine, taking into account the impact of altered glycan structures expressed in cancer cells as potential glycobiomarkers of disease, as well as on cancer development and progression. Full article
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