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Medicines, Volume 9, Issue 2 (February 2022) – 9 articles

Cover Story (view full-size image): In this study, we report the synthesis of several novel artemisinin derivatives and evaluate their in vitro and in silico capacity to counteract Plasmodium falciparum artemisinin resistance. The present report demonstrates, in vitro, that FM-AZ, a newly synthesized artemisinin derivative, has a lower IC50 than artemisinin in P. falciparum and a rapid action in killing parasites. The docking studies for important parasite protein targets PfATP6 and PfHDP complemented the in vitro results, explaining the superior IC50 values of FM-AZ in comparison with ART obtained for the ART-resistant strain. However, cross-resistance between FM-AZ and artemisinins was evidenced in vitro. View this paper
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16 pages, 1354 KiB  
Review
Neurogenic Dysphagia and Nutrition in Disorder of Consciousness: An Overview with Practical Advices on an “Old” but Still Actual Clinical Problem
by Loredana Raciti, Gianfranco Raciti, Grazia Pulejo, Valeria Conti-Nibali and Rocco Salvatore Calabrò
Medicines 2022, 9(2), 16; https://doi.org/10.3390/medicines9020016 - 21 Feb 2022
Cited by 3 | Viewed by 4869
Abstract
Neurogenic dysphagia is a difficulty in swallowing food caused by disease or impairment of the nervous system, including stroke and traumatic brain injury. The most clinically apparent complication of neurogenic dysphagia is pulmonary aspiration, which may manifest itself acutely as choking or coughing, [...] Read more.
Neurogenic dysphagia is a difficulty in swallowing food caused by disease or impairment of the nervous system, including stroke and traumatic brain injury. The most clinically apparent complication of neurogenic dysphagia is pulmonary aspiration, which may manifest itself acutely as choking or coughing, respiratory distress, wheezing, gasping or gurgling, and tachycardia. However, chronic symptoms, including weight loss, production of excessive oral secretions and aspiration pneumonia, may be also present, especially in patients with a disorder of consciousness (DOC). Usually, patients with dysphagia after the acute phase need to be treated with enteral nutrition using a feeding tube. This avoids patient malnutrition and supports the rehabilitation program. This narrative review aims to investigate dysphagia and its complications and management in patients with DOC. Clinical indications and practical advice on how to assess and treat this complex problem are also provided. Full article
(This article belongs to the Special Issue Frailty Syndrome in the Elderly: A Real Challenge for Our Society)
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14 pages, 2339 KiB  
Article
Early Time-Restricted Feeding Amends Circadian Clock Function and Improves Metabolic Health in Male and Female Nile Grass Rats
by Chidambaram Ramanathan, Hayden Johnson, Suman Sharma, Wangkuk Son, Melissa Puppa, Saba Neyson Rohani, Aaryani Tipirneni-Sajja, Richard J. Bloomer and Marie van der Merwe
Medicines 2022, 9(2), 15; https://doi.org/10.3390/medicines9020015 - 21 Feb 2022
Cited by 4 | Viewed by 4201
Abstract
Lengthening the daily eating period contributes to the onset of obesity and metabolic syndrome. Dietary approaches, including energy restriction and time-restricted feeding, are promising methods to combat metabolic disorders. This study explored the effect of early and late time-restricted feeding (TRF) on weight [...] Read more.
Lengthening the daily eating period contributes to the onset of obesity and metabolic syndrome. Dietary approaches, including energy restriction and time-restricted feeding, are promising methods to combat metabolic disorders. This study explored the effect of early and late time-restricted feeding (TRF) on weight and adiposity, food consumption, glycemic control, clock gene expression, and liver metabolite composition in diurnal Nile grass rats (NGRs). Adult male and female Nile grass rats were randomly assigned to one of three groups: (1) access to a 60% high-fat (HF) diet ad-libitum (HF-AD), (2) time-restricted access to the HF diet for the first 6 h of the 12 h light/active phase (HF-AM) or (3) the second 6 h of the 12 h light/active phase (HF-PM). Animals remained on their respective protocols for six weeks. TRF reduced total energy consumption and weight gain, and early TRF (HF-AM) reduced fasting blood glucose, restored Per1 expression, and reduced liver lipid levels. Although sex-dependent differences were observed for fat storage and lipid composition, TRF improved metabolic parameters in both male and female NGRs. In conclusion, this study demonstrated that early TRF protocol benefits weight management, improves lipid and glycemic control, and restores clock gene expression in NGRs. Full article
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11 pages, 682 KiB  
Article
CHRIST: CD44-Incorporated Hepatocellular Carcinoma Risk Index Scoring Tool—A Novel Prognostic Scoring System for Hepatocellular Carcinoma Development and Aggressiveness
by Ahmed Ali Khalifa, Nermeen Abdeen, Neveen L. Mikhael, Sawsan Elmalah and Ayman Elshayeb
Medicines 2022, 9(2), 14; https://doi.org/10.3390/medicines9020014 - 21 Feb 2022
Viewed by 2384
Abstract
CD44 has been demonstrated to play a pivotal role in regulating tumor cell progression, including hepatocellular carcinoma (HCC) development. Here, we aimed to establish a scoring system to evaluate the risk of developing HCC utilizing CD44-rs187115 SNP polymorphism. A prospective cohort of 120 [...] Read more.
CD44 has been demonstrated to play a pivotal role in regulating tumor cell progression, including hepatocellular carcinoma (HCC) development. Here, we aimed to establish a scoring system to evaluate the risk of developing HCC utilizing CD44-rs187115 SNP polymorphism. A prospective cohort of 120 individuals was enrolled in four groups: 19 non-metastatic HCC patients, 21 metastatic, 40 patients with hepatitis C-related cirrhosis, and 40 controls. Allelic discrimination of the CD44-rs187115 gene polymorphism was assessed using TaqMan genotyping assay. HCC patients with CT/CC genotypes were more likely to have aggressive malignancy compared to TT carriers. A significant correlation was noted between the existence of CT/CC genotypes and tumor size, multicentricity, infiltration, portal vein thrombosis, and metastasis. A CD44-incorporated Hepatocellular Carcinoma Risk Index Scoring Tool (CHRIST) was formulated utilizing clinical and genetic variables. A score > 3 for HCC development demonstrated 87.5% sensitivity, 72.5% specificity, and a 76% positive predictive value (PPV) and 85% negative predictive value (NPV). Furthermore, a score > 5 for HCC metastasis demonstrated 90.4% sensitivity, 68.4% specificity, a 76% PPV and 86% NPV. A similarly significant score was noted following a six-month re-evaluation. We conclude that CD44-rs187115 may serve as a reliable prognostic biomarker for HCC and that the CHRIST prognostic model is highly predictive of the development of HCC and metastatic HCC. Full article
(This article belongs to the Section Cancer Biology and Anticancer Therapeutics)
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10 pages, 18776 KiB  
Article
The Medial Surface of the Auricle: Historical and Recent Maps. What Are the Possible Expectations of the “Thumb-Index Technique”
by Antonello Lovato, Francesco Ceccherelli, Giuseppe Gagliardi and Marco Postiglione
Medicines 2022, 9(2), 13; https://doi.org/10.3390/medicines9020013 - 17 Feb 2022
Cited by 1 | Viewed by 5754
Abstract
Introduction: The medial surface of the auricle (MSotA), as compared to the lateral, has been less studied and has limited consensus among schools of auricular acupuncture (AA) due to its small size, greater difficulty in carrying out an adequate physical examination on it, [...] Read more.
Introduction: The medial surface of the auricle (MSotA), as compared to the lateral, has been less studied and has limited consensus among schools of auricular acupuncture (AA) due to its small size, greater difficulty in carrying out an adequate physical examination on it, and less precise and limited agreement on its anatomical references as compared to the lateral surface. The thumb-index technique TIT is performed using a guiding finger (taking advantage of the anatomical conformation of the lateral surface) to guide the explorer finger (placed on the MSotA) to project the therapeutic areas and land marks on the MSotA. TIT could be considered useful and effective in AA to make the most of diagnostic and therapeutic MSotA potential. Methods: An investigation was carried out on the impact of TIT in AA practice through a survey collected from former AA students. Results: TIT showed a high consensus, and is used and appreciated by AA practitioners. Discussion/ Conclusions: To date, in AA, there is no thoroughly shared nomenclature for MSotA. TIT is simple and quick to project on to MSotA the well-coded lateral surface auricular maps from French or Chinese AA schools. Full article
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2 pages, 170 KiB  
Editorial
Acknowledgment to Reviewers of Medicines in 2021
by Medicines Editorial Office
Medicines 2022, 9(2), 12; https://doi.org/10.3390/medicines9020012 - 02 Feb 2022
Viewed by 1388
Abstract
Rigorous peer-reviews are the basis of high-quality academic publishing [...] Full article
12 pages, 4524 KiB  
Case Report
Potential Application of Lung Ultrasound in Children with Severe Uncontrolled Asthma: Preliminary Hypothesis Based on a Case Series
by Cristina De Rose, Stefano Miceli Sopo, Piero Valentini, Rosa Morello, Daniele Biasucci and Danilo Buonsenso
Medicines 2022, 9(2), 11; https://doi.org/10.3390/medicines9020011 - 02 Feb 2022
Cited by 7 | Viewed by 2416
Abstract
In recent years, lung ultrasound (LUS) has been increasingly used for the diagnosis of respiratory diseases in both adult and pediatric patients. However, asthma is a field in which the use of LUS is not yet well defined, or is in development. In [...] Read more.
In recent years, lung ultrasound (LUS) has been increasingly used for the diagnosis of respiratory diseases in both adult and pediatric patients. However, asthma is a field in which the use of LUS is not yet well defined, or is in development. In the following case series, we describe clinical, laboratory, and radiological results, as well as detailed lung ultrasound findings of six children with asthma: some of them with acute asthma attack and with inadequately controlled allergic asthma or childhood asthma; others with acute asthma and allergic or infantile asthma adequately controlled by preventive therapy. Finally, we describe the clinical, laboratory, and imaging parameters of a child with severe allergic asthma in the absence of exacerbation. In these cases, albeit at different times, LUS played an important role in both the initial diagnostic process and follow-up. It also showed different ultrasound features depending on the severity of the individual asthma based on the type of asthmatic phenotype and control of it. Full article
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11 pages, 801 KiB  
Article
Identification of Antimycobacterial Natural Products from a Library of Marine Invertebrate Extracts
by Kojo Sekyi Acquah, Denzil R. Beukes, Ronnett Seldon, Audrey Jordaan, Suthananda N. Sunassee, Digby F. Warner and David W. Gammon
Medicines 2022, 9(2), 9; https://doi.org/10.3390/medicines9020009 - 28 Jan 2022
Cited by 2 | Viewed by 2567
Abstract
Tuberculosis (TB) remains a public health crisis, requiring the urgent identification of new anti-mycobacterial drugs. We screened several organic and aqueous marine invertebrate extracts for their in vitro inhibitory activity against the causative organism, Mycobacterium tuberculosis. Here, we report the results obtained [...] Read more.
Tuberculosis (TB) remains a public health crisis, requiring the urgent identification of new anti-mycobacterial drugs. We screened several organic and aqueous marine invertebrate extracts for their in vitro inhibitory activity against the causative organism, Mycobacterium tuberculosis. Here, we report the results obtained for 54 marine invertebrate extracts. The chemical components of two of the extracts were dereplicated, using 1H NMR and HR-LCMS with GNPS molecular networking, and these extracts were further subjected to an activity-guided isolation process to purify the bioactive components. Hyrtios reticulatus yielded heteronemin 1 and Jaspis splendens was found to produce the bengamide class of compounds, of which bengamides P 2 and Q 3 were isolated, while a new derivative, bengamide S 5, was putatively identified and its structure predicted, based on the similarity of its MS/MS fragmentation pattern to those of other bengamides. The isolated bioactive metabolites and semi-pure fractions exhibited M. tuberculosis growth inhibitory activity, in the range <0.24 to 62.50 µg/mL. This study establishes the bengamides as potent antitubercular compounds, with the first report of whole-cell antitubercular activity of bengamides P 2 and Q 3. Full article
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18 pages, 2230 KiB  
Article
Ethnobotanical and Phytochemical Profiling of Medicinal Plants from Burkina Faso Used to Increase Physical Performance
by Hemayoro Sama, Modeste Traoré, Samson Guenné, Ibrahim Séré, Adama Hilou and Mamoudou H. Dicko
Medicines 2022, 9(2), 10; https://doi.org/10.3390/medicines9020010 - 28 Jan 2022
Cited by 2 | Viewed by 2957
Abstract
Background: Some ergogenic medicinal plants are used in exercise and sport in Africa in order to increase sport performance. However, data on their composition and their possible impacts on health are limited. This study was initiated to provide ethnobotanical data on plants traditionally [...] Read more.
Background: Some ergogenic medicinal plants are used in exercise and sport in Africa in order to increase sport performance. However, data on their composition and their possible impacts on health are limited. This study was initiated to provide ethnobotanical data on plants traditionally used to optimize physical performance and to perform a qualitative characterization of their main chemical groups. Methods: Ethnobotanical surveys in two communes (Dedougou and Nouna), of the region of Boucle du Mouhoun, Burkina Faso and phytochemical analyses of the most interesting plants were conducted. Results: A total of 50 respondents including traditional hunters dozo, farmers, healers, herbalists, marabouts, etc., were interviewed. Fifty-two species used in the optimization of exercise and sports have been identified. The most cited species were Cassia sieberiana, Tamarindus indica, Annona senegalensis, Gardenia sokotensis, Securidaca longepedunculata, and Ficus tonningii. These plants are known to prevent muscle and skeletal disorders, aches and pains, and mental disorders. The study identified several types of plants including those displaying stimulation, anxiolytic, sedative, adaptogenic, or erythropoietic activities. Phytochemical screening revealed the presence of phenolic compounds, alkaloids, terpenes, and steroids, which are similar molecules families of those of doping molecules. Additionally, TLC screening allowed the characterization of numerous terpene and flavonoid compounds including rutin. Conclusions: The possible structural similarity of the characterized chemical groups of these species with those of doping families raise concerns about the consequences of their consumption. However, the identification of the active molecules of these species remains to be performed in order to predict the real risks associated with their consumption. Full article
(This article belongs to the Section New Drugs Exploration and Development)
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12 pages, 1461 KiB  
Article
In Vitro and In Silico Antimalarial Evaluation of FM-AZ, a New Artemisinin Derivative
by Ioannis Tsamesidis, Farnoush Mousavizadeh, Chinedu O. Egwu, Dionysia Amanatidou, Antonella Pantaleo, Françoise Benoit-Vical, Karine Reybier and Athanassios Giannis
Medicines 2022, 9(2), 8; https://doi.org/10.3390/medicines9020008 - 24 Jan 2022
Cited by 3 | Viewed by 2531
Abstract
Artemisinin-based Combination Therapies (ACTs) are currently the frontline treatment against Plasmodium falciparum malaria, but parasite resistance to artemisinin (ART) and its derivatives, core components of ACTs, is spreading in the Mekong countries. In this study, we report the synthesis of several novel artemisinin [...] Read more.
Artemisinin-based Combination Therapies (ACTs) are currently the frontline treatment against Plasmodium falciparum malaria, but parasite resistance to artemisinin (ART) and its derivatives, core components of ACTs, is spreading in the Mekong countries. In this study, we report the synthesis of several novel artemisinin derivatives and evaluate their in vitro and in silico capacity to counteract Plasmodium falciparum artemisinin resistance. Furthermore, recognizing that the malaria parasite devotes considerable resources to minimizing the oxidative stress that it creates during its rapid consumption of hemoglobin and the release of heme, we sought to explore whether further augmentation of this oxidative toxicity might constitute an important addition to artemisinins. The present report demonstrates, in vitro, that FM-AZ, a newly synthesized artemisinin derivative, has a lower IC50 than artemisinin in P. falciparum and a rapid action in killing the parasites. The docking studies for important parasite protein targets, PfATP6 and PfHDP, complemented the in vitro results, explaining the superior IC50 values of FM-AZ in comparison with ART obtained for the ART-resistant strain. However, cross-resistance between FM-AZ and artemisinins was evidenced in vitro. Full article
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