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Pharmaceuticals, Volume 13, Issue 4 (April 2020) – 9 articles

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Open AccessArticle
Trends in Antidepressants Use in Spain between 2015 and 2018: Analyses from a Population-Based Registry Study with Reference to Driving
Pharmaceuticals 2020, 13(4), 61; https://doi.org/10.3390/ph13040061 (registering DOI) - 03 Apr 2020
Abstract
Antidepressants are considered driving-impairing medicines (DIM). This is a population-based registry study that shows the trend in the use of antidepressants in Castile and León, Spain, from 2015 to 2018. Data on antidepressant dispensations at pharmacies and the adjusted use of these medicines [...] Read more.
Antidepressants are considered driving-impairing medicines (DIM). This is a population-based registry study that shows the trend in the use of antidepressants in Castile and León, Spain, from 2015 to 2018. Data on antidepressant dispensations at pharmacies and the adjusted use of these medicines by the driver population are presented. For the purposes of analysis, population distribution by age and gender has been taken into account, as well as the three Driving Under the Influence of Drugs, alcohol, and medicines (DRUID) categories. Antidepressants were used by 8.56% of the general population and 5.66% of drivers. Antidepressants were used more commonly by females than by males (12.12% vs. 4.87%, χ² = 1325.124, p = 0.001), and users increased as the age increased, even if women who drive used less antidepressants after turning 60 years of age. Chronic use of antidepressants was relevant (8.28%) in the same way as daily use (3.15%). Most of the consumption included SSRIs (4.99%), which are also known as “other antidepressants” (3.71%). Regardless of antidepressants consumed, users took 2.75 ± 1.19 DIMs, which are mainly anxiolytics (58.80%) and opioids (26.43%). Lastly, regarding consumption of antidepressants according to the DRUID classification, category I predominated over categories II and III. Our findings should serve as a starting point for health and traffic authorities to raise awareness of the risk for traffic accidents, especially involving SSRIs. Full article
(This article belongs to the collection Choices of the Journal)
Open AccessReview
The Treatment of Impaired Wound Healing in Diabetes: Looking among Old Drugs
Pharmaceuticals 2020, 13(4), 60; https://doi.org/10.3390/ph13040060 - 01 Apr 2020
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Abstract
Chronic wounds often occur in patients with diabetes mellitus due to the impairment of wound healing. This has negative consequences for both the patient and the medical system and considering the growing prevalence of diabetes, it will be a significant medical, social, and [...] Read more.
Chronic wounds often occur in patients with diabetes mellitus due to the impairment of wound healing. This has negative consequences for both the patient and the medical system and considering the growing prevalence of diabetes, it will be a significant medical, social, and economic burden in the near future. Hence, the need for therapeutic alternatives to the current available treatments that, although various, do not guarantee a rapid and definite reparative process, appears necessary. We here analyzed current treatments for wound healing, but mainly focused the attention on few classes of drugs that are already in the market with different indications, but that have shown in preclinical and few clinical trials the potentiality to be used in the treatment of impaired wound healing. In particular, repurposing of the antiglycemic agents dipeptidylpeptidase 4 (DPP4) inhibitors and metformin, but also, statins and phenyotin have been analyzed. All show encouraging results in the treatment of chronic wounds, but additional, well designed studies are needed to allow these drugs access to the clinics in the therapy of impaired wound healing. Full article
(This article belongs to the collection Old Pharmaceuticals with New Applications)
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Open AccessArticle
In Vitro Antibacterial and Antiproliferative Potential of Echinops lanceolatus Mattf. (Asteraceae) and Identification of Potential Bioactive Compounds
Pharmaceuticals 2020, 13(4), 59; https://doi.org/10.3390/ph13040059 - 30 Mar 2020
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Abstract
Many species belonging to the genus Echinops are widely used in traditional medicine to treat infectious diseases and cancers. The present study aimed to evaluate the antibacterial and antiproliferative properties of Echinops lanceolatus Mattf. (Asteraceae). The activity of the methanolic extract and subsequent [...] Read more.
Many species belonging to the genus Echinops are widely used in traditional medicine to treat infectious diseases and cancers. The present study aimed to evaluate the antibacterial and antiproliferative properties of Echinops lanceolatus Mattf. (Asteraceae). The activity of the methanolic extract and subsequent partition fractions was investigated against drug-resistant bacteria (Gram-negative and Gram-positive) and human tumor cell lines using broth microdilution and sulforhodamine B (SRB) assay, respectively. Our findings revealed weak to moderate antibacterial activities of tested extracts, with the recorded minimal inhibitory concentrations ranging from 256 to 1024 µg/mL. The ethyl acetate fraction (EL-EA) was found to be the most effective. Likewise, that fraction displayed strong antiproliferative potential with recorded IC50 of 8.27 µg/mL and 28.27 µg/mL on A549 and HeLa cells, respectively. An analysis based on the ultra-performance liquid chromatography–electrospray ionization tandem mass spectrometry (UPLC–ESI–MS/MS) of the EL-EA fraction allowed the identification of 32 compounds, of which quinic acid and derivatives, cinnamic acid derivatives, dihydrokaempferol, naringenin-7-O-glucoside, apigenin-7-O-d-glucoside, naringin, apigenin, rhoifolin, coniferyl aldehyde, and secoisolariciresinol are well-known compounds of biological importance. This study is first to report on the biological activity and phytochemical profile of E. lanceolatus. We provide a baseline to consider E. lanceolatus as a valuable source of anti-infective and antiproliferative agents. Full article
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Open AccessArticle
Upregulated Connexin 43 Induced by Loss-of-Functional S284L-Mutant α4 Subunit of Nicotinic ACh Receptor Contributes to Pathomechanisms of Autosomal Dominant Sleep-Related Hypermotor Epilepsy
Pharmaceuticals 2020, 13(4), 58; https://doi.org/10.3390/ph13040058 (registering DOI) - 29 Mar 2020
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Abstract
To study the pathomechanism and pathophysiology of autosomal dominant sleep-related hypermotor epilepsy (ADSHE), this study determined functional abnormalities of glutamatergic transmission in the thalamocortical motor pathway, from the reticular thalamic nucleus (RTN), motor thalamic nuclei (MoTN) tosecondary motor cortex (M2C) associated with the [...] Read more.
To study the pathomechanism and pathophysiology of autosomal dominant sleep-related hypermotor epilepsy (ADSHE), this study determined functional abnormalities of glutamatergic transmission in the thalamocortical motor pathway, from the reticular thalamic nucleus (RTN), motor thalamic nuclei (MoTN) tosecondary motor cortex (M2C) associated with the S286L-mutant α4β2-nicotinic acetylcholine receptor (nAChR) and the connexin43 (Cx43) hemichannel of transgenic rats bearing the rat S286L-mutant Chrna4 gene (S286L-TG), which corresponds to the human S284L-mutant CHRNA4 gene using multiprobe microdialysis, primary cultured astrocytes and a Simple Western system. Expression of Cx43 in the M2C plasma membrane fraction of S286L-TG was upregulated compared with wild-type rats. Subchronic nicotine administration decreased Cx43 expression of wild-type, but did not affect that of S286L-TG; however, zonisamide (ZNS) decreased Cx43 in both wild-type and S286L-TG. Primary cultured astrocytes of wild-type were not affected by subchronic administration of nicotine but was decreased by ZNS. Upregulated Cx43 enhanced glutamatergic transmission during both resting and hyperexcitable stages in S286L-TG. Furthermore, activation of glutamatergic transmission associated with upregulated Cx43 reinforced the prolonged Cx43 hemichannel activation. Subchronic administration of therapeutic-relevant doses of ZNS compensated the upregulation of Cx43 and prolonged reinforced activation of Cx43 hemichannel induced by physiological hyperexcitability during the non-rapid eye movement phase of sleep. The present results support the primary pathomechanisms and secondary pathophysiology of ADSHE seizures of patients with S284L-mutation. Full article
(This article belongs to the Special Issue Therapeutic Agents for Neurological Disorders)
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Open AccessArticle
Efficacy of Panax ginseng Meyer Herbal Preparation HRG80 in Preventing and Mitigating Stress-Induced Failure of Cognitive Functions in Healthy Subjects: A Pilot, Randomized, Double-Blind, Placebo-Controlled Crossover Trial
Pharmaceuticals 2020, 13(4), 57; https://doi.org/10.3390/ph13040057 (registering DOI) - 29 Mar 2020
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Abstract
Background: The aim of this pilot study was to compare the efficacy of hydroponically cultivated red Panax ginseng Meyer root preparation (HRG80) and traditionally harvested six-year-old white P. ginseng standard preparation (PGS) with placebo in preventing symptoms of stress. Methods: The effects of [...] Read more.
Background: The aim of this pilot study was to compare the efficacy of hydroponically cultivated red Panax ginseng Meyer root preparation (HRG80) and traditionally harvested six-year-old white P. ginseng standard preparation (PGS) with placebo in preventing symptoms of stress. Methods: The effects of HRG80, PGS, and placebo capsules were studied in 50 tired healthy subjects in a three-arm, randomized, double-blinded, placebo-controlled crossover trial. Efficacy-outcome measures included the accuracy of processing the d2 test for cognitive functions, obtained accuracy score in a computerized memory test, and the perceived-stress (PS) score. Results: A statistically significant interaction effect between time and treatment (p < 0.0001) was observed in the attention d2 and memory tests, indicating that HRG80 treatment was more beneficial than that with a placebo. The effects of PGS were better than those of the placebo, but the difference was not statistically significant. There was significant difference between the effects of HRG80 and PGS (p < 0.0001) that were observed after single (Day 1) and repeated administrations on Days 5 and 12 of treatment. Conclusion: Overall, HRG80 treatment was significantly superior compared to that with the PGS and placebo regarding attention, memory, and PS scores after single and repeated administrations for 5 and 12 days. Full article
(This article belongs to the Special Issue Medicinal Plants 2020)
Open AccessArticle
Selection of Thai Medicinal Plants with Anti-Obesogenic Potential via In Vitro Methods
Pharmaceuticals 2020, 13(4), 56; https://doi.org/10.3390/ph13040056 (registering DOI) - 29 Mar 2020
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Abstract
The prevalence of obesity is increasing globally. Despite the availability of a variety of anti-obesogenic drugs, including therapies under clinical development, these treatments are often indicated for patients with severe obesity, making them unsuitable for patients with mild obesity or for preventative use. [...] Read more.
The prevalence of obesity is increasing globally. Despite the availability of a variety of anti-obesogenic drugs, including therapies under clinical development, these treatments are often indicated for patients with severe obesity, making them unsuitable for patients with mild obesity or for preventative use. In Thailand, traditional remedies employing medicinal plants are widely used to maintain health and treat disease. These treatments are generally inexpensive and readily available at markets, making them good treatment options for preventing obesity. To evaluate the anti-obesogenic potential of Thai medicinal plants, we employed three in vitro methods: pancreatic lipase inhibition, lipolysis enhancement, and lipid accumulation reduction assays. Among 70 Thai medicinal plants, Eurycoma longifolia Jack, Tiliacora triandra Diels, and Acacia concinna (Willd.) DC. were selected as the most favorable candidates because they exhibited anti-obesogenic activity in all three assays. These medicinal plants are expected to have efficient anti-obesogenic effects, making them promising candidates for further study. Full article
(This article belongs to the Special Issue Medicinal Plants 2020)
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Open AccessArticle
Antioxidant, Anti-inflammatory Activities and Polyphenol Profile of Rhamnus prinoides
Pharmaceuticals 2020, 13(4), 55; https://doi.org/10.3390/ph13040055 (registering DOI) - 26 Mar 2020
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Abstract
Rhamnus prinoides L’Herit (R. prinoides) has long been widely consumed as folk medicine in Kenya and other Africa countries. Previous studies indicated that polyphenols were abundant in genus Rhamnus and exhibited outstanding antioxidant and anti-inflammatory activities. However, there are very few [...] Read more.
Rhamnus prinoides L’Herit (R. prinoides) has long been widely consumed as folk medicine in Kenya and other Africa countries. Previous studies indicated that polyphenols were abundant in genus Rhamnus and exhibited outstanding antioxidant and anti-inflammatory activities. However, there are very few studies on such pharmacological activities and the polyphenol profile of this plant up to now. In the present study, the antioxidant activities of the crude R. prinoides extracts (CRE) and the semi-purified R. prinoides extracts (SPRE) of polyphenol enriched fractions were evaluated to show the strong radical scavenging effects against 1,1-diphenyl-2- picrylhydrazyl radical 2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazyl (DPPH) (0.510 ± 0.046 and 0.204 ± 0.005, mg/mL), and 2,2′-azinobis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) (0.596 ± 0.005 and 0.096 ± 0.004, mg/mL), respectively. Later, the SPRE with higher contents of polyphenols and flavonoids displayed obvious anti-inflammatory activities through reducing the NO production at the dosage of 11.11 − 100 μg/mL, and the COX-2 inhibitory activity with an IC50 value at 20.61 ± 0.13 μg/mL. Meanwhile, the HPLC-UV/ESI-MS/MS analysis of polyphenol profile of R. prinoides revealed that flavonoids and their glycosides were the major ingredients, and potentially responsible for its strong antioxidant and anti-inflammatory activities. For the first time, the present study comprehensively demonstrated the chemical profile of R. prinoides, as well as noteworthy antioxidant and anti-inflammatory activities, which confirmed that R. prinoides is a good natural source of polyphenols and flavonoids, and provided valuable information on this medicinal plant as folk medicine and with good potential for future healthcare practice. Full article
(This article belongs to the Special Issue Medicinal Plants 2020)
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Open AccessArticle
Improved Surface Display of Human Hyal1 and Identification of Testosterone Propionate and Chicoric Acid as New Inhibitors
Pharmaceuticals 2020, 13(4), 54; https://doi.org/10.3390/ph13040054 - 26 Mar 2020
Viewed by 244
Abstract
Degradation of high molecular weight hyaluronic acid (HA) in humans is mainly catalyzed by hyaluronidase Hyal1. This enzyme is involved in many pathophysiological processes and therefore appears an interesting target for drug discovery. Until now, only a few inhibitors of human Hyal1 are [...] Read more.
Degradation of high molecular weight hyaluronic acid (HA) in humans is mainly catalyzed by hyaluronidase Hyal1. This enzyme is involved in many pathophysiological processes and therefore appears an interesting target for drug discovery. Until now, only a few inhibitors of human Hyal1 are known due to obstacles in obtaining active enzymes for inhibitor screening. The aim of the present work was to provide a convenient enzyme activity assay and show its feasibility by the identification of new inhibitors. By autodisplay, Escherichia coli F470 can present active Hyal1 on its surface. In this study, the inducible expression of Hyal1 on the cell surface of E. coli under the control of a rhamnose-dependent promoter (Prha) was performed and optimized. Enzyme activity per single cell was increased by a factor of 100 compared to the constitutive Hyal1 surface display, as described before. An activity of 6.8 × 10−4 mU per single cell was obtained under optimal reaction conditions. By this modified activity assay, two new inhibitors of human Hyal1 were identified. Chicoric acid, a natural compound belonging to the phenylpropanoids, showed an IC50 value of 171 µM. The steroid derivative testosterone propionate showed and IC50 value of 124 ± 1.1 µM. Both values were in the same order of magnitude as the IC50 value of glycyrrhizic acid (177 µM), one of the best known inhibitors of human Hyal1 known so far. In conclusion, we established a new enzyme activity assay for human Hyal1 and identified new inhibitors with this new assay method. Full article
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Open AccessArticle
Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
Pharmaceuticals 2020, 13(4), 53; https://doi.org/10.3390/ph13040053 (registering DOI) - 26 Mar 2020
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Abstract
In the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo release [...] Read more.
In the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo release of the model drug carbamazepine (CBZ) from two emulsified formulations with different droplet sizes (coarse and nanometric). Briefly, oil-in-water emulsions were developed using (i) Sacha inchi oil, ultrapure water, TweenTM 80, and SpanTM 80 as surfactants, (ii) methyl-paraben and propyl-paraben as preservatives, and (iii) CBZ as a nonpolar model drug. The coarse and nanometric emulsions were prepared by rotor–stator dispersion and ultra-high-pressure homogenization (UHPH), respectively. The in vitro drug release studies were conducted by dialysis, whereas the in vivo drug release was evaluated in New Zealand breed rabbits. The results showed that nanoemulsions were physically more stable than coarse emulsions, and that CBZ had a very low release for in vitro determination (<2%), and a release of 20% in the in vivo study. However, it was found that nanoemulsions could significantly increase drug absorption time from 12 h to 45 min. Full article
(This article belongs to the Section Pharmaceutical Technology)
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