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Volume 88, December

Sci. Pharm., Volume 89, Issue 1 (March 2021) – 6 articles

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Open AccessReview
Sedating Mechanically Ventilated COVID-19 Patients with Volatile Anesthetics: Insights on the Last-Minute Potential Weapons
Sci. Pharm. 2021, 89(1), 6; https://doi.org/10.3390/scipharm89010006 - 08 Jan 2021
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Abstract
Coronavirus Disease 2019 (COVID-19) has spread globally with the number of cases exceeding seventy million. Although trials on potential treatments of COVID-19 Acute Respiratory Distress Syndrome (ARDS) are promising, the introduction of an effective therapeutic intervention seems elusive. In this review, we explored [...] Read more.
Coronavirus Disease 2019 (COVID-19) has spread globally with the number of cases exceeding seventy million. Although trials on potential treatments of COVID-19 Acute Respiratory Distress Syndrome (ARDS) are promising, the introduction of an effective therapeutic intervention seems elusive. In this review, we explored the potential therapeutic role of volatile anesthetics during mechanical ventilation in the late stages of the disease. COVID-19 is thought to hit the human body via five major mechanisms: direct viral damage, immune overactivation, capillary thrombosis, loss of alveolar capillary membrane integrity, and decreased tissue oxygenation. The overproduction of pro-inflammatory cytokines will eventually lead to the accumulation of inflammatory cells in the lungs, which will lead to ARDS requiring mechanical ventilation. Respiratory failure resulting from ARDS is thought to be the most common cause of death in COVID-19. The literature suggests that these effects could be directly countered by using volatile anesthetics for sedation. These agents possess multiple properties that affect viral replication, immunity, and coagulation. They also have proven benefits at the molecular, cellular, and tissue levels. Based on the comprehensive understanding of the literature, short-term sedation with volatile anesthetics may be beneficial in severe stages of COVID-19 ARDS and trials to study their effects should be encouraged. Full article
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Open AccessReview
Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 as Potential Drugs for Type 2 Diabetes Mellitus—A Systematic Review of Clinical and In Vivo Preclinical Studies
Sci. Pharm. 2021, 89(1), 5; https://doi.org/10.3390/scipharm89010005 - 05 Jan 2021
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Abstract
Diabetes mellitus is a pathology with increasing frequency in society, being one of the main causes of death worldwide. For this reason, new therapeutic targets have been studied over the years. 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is an enzyme responsible for reducing cortisone [...] Read more.
Diabetes mellitus is a pathology with increasing frequency in society, being one of the main causes of death worldwide. For this reason, new therapeutic targets have been studied over the years. 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is an enzyme responsible for reducing cortisone to its active form cortisol, which can lead to metabolic changes such as insulin resistance and hyperglycemia. Therefore, 11β-HSD1 inhibition may offer a new therapeutic approach for type 2 diabetes mellitus. This work intends to systematically review the available scientific evidence on this subject. For this, a search was conducted in three databases and 15 clinical and in vivo preclinical studies were included in this review. Despite the high inhibitory and selectivity levels achieved with several molecules and the demonstrated clinical efficacy in diabetes treatment, no phase III clinical trials have yet been conducted. This is important because the long-term effects of 11β-HSD1 inhibitors including the consequences in hypothalamic–pituitary–adrenal axis must be evaluated. However, this enzyme remains a promising target for drug development, including due to its effectiveness in controlling various factors that constitute the metabolic syndrome and its potential for multiple indications in patients with diabetes, including wound healing and weight loss. Full article
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Open AccessArticle
Triterpenic Acid Amides as a Promising Agent for Treatment of Metabolic Syndrome
Sci. Pharm. 2021, 89(1), 4; https://doi.org/10.3390/scipharm89010004 - 29 Dec 2020
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Abstract
A series of triterpenic acid amides were synthesized incorporating a 2-ethoxy-3-phenylpropanoic acid pharmacophore fragment. The synthesized compounds were tested for their ability to improve glycemic control and to counter lipid abnormalities in C57BL/6 mice placed on a high-fat/high-cholesterol diet. Of all tested compounds, [...] Read more.
A series of triterpenic acid amides were synthesized incorporating a 2-ethoxy-3-phenylpropanoic acid pharmacophore fragment. The synthesized compounds were tested for their ability to improve glycemic control and to counter lipid abnormalities in C57BL/6 mice placed on a high-fat/high-cholesterol diet. Of all tested compounds, the dihydrobetulonic derivative (16b) had the most pronounced effect in decreasing blood glucose levels, total cholesterol (TC), and high-density lipoproteins (HDL). All the synthesized compounds displayed a relatively safe profile in the animal studies carried out in this work. Full article
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Open AccessReview
Vaginal Administration of Contraceptives
Sci. Pharm. 2021, 89(1), 3; https://doi.org/10.3390/scipharm89010003 - 25 Dec 2020
Viewed by 259
Abstract
While contraceptive drugs have enabled many people to decide when they want to have a baby, more than 100 million unintended pregnancies each year in the world may indicate the contraceptive requirement of many people has not been well addressed yet. The vagina [...] Read more.
While contraceptive drugs have enabled many people to decide when they want to have a baby, more than 100 million unintended pregnancies each year in the world may indicate the contraceptive requirement of many people has not been well addressed yet. The vagina is a well-established and practical route for the delivery of various pharmacological molecules, including contraceptives. This review aims to present an overview of different contraceptive methods focusing on the vaginal route of delivery for contraceptives, including current developments, discussing the potentials and limitations of the modern methods, designs, and how well each method performs for delivering the contraceptives and preventing pregnancy. Full article
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Open AccessHypothesis
Uniting Electroceutical and Cosmeceutical Interventions in Combating Coronavirus Using Ԑ-Poly-l-Lysine
Sci. Pharm. 2021, 89(1), 2; https://doi.org/10.3390/scipharm89010002 - 23 Dec 2020
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Abstract
Combating the COVID-19 pandemic warrants the exploitation of all the available tools and implies a major focus on both the biological and the physical properties of the causing virus (SARS-CoV2). We hereby introduce a new prophylaxis hypothesis by decreasing the viral load in [...] Read more.
Combating the COVID-19 pandemic warrants the exploitation of all the available tools and implies a major focus on both the biological and the physical properties of the causing virus (SARS-CoV2). We hereby introduce a new prophylaxis hypothesis by decreasing the viral load in the body entrances such as the nose and the mouth using pharmaceutical and cosmeceutical preparations that incorporate viral electrostatic repulsive nanofibers fabricated from an abundant marine-derived or a fermentation product polymer; Ԑ-poly-l-lysine was prepared using the electrospinning technique. Full article
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Open AccessArticle
Promising Anti-MRSA Activity of Brevibacillus sp. Isolated from Soil and Strain Improvement by UV Mutagenesis
Sci. Pharm. 2021, 89(1), 1; https://doi.org/10.3390/scipharm89010001 - 23 Dec 2020
Viewed by 340
Abstract
Antibiotic-resistant infection is a major health problem, and a limited number of drugs are currently approved as antibiotics. Soil bacteria are promising sources in the search for novel antibiotics. The aim of the present study is to isolate and assess soil bacteria with [...] Read more.
Antibiotic-resistant infection is a major health problem, and a limited number of drugs are currently approved as antibiotics. Soil bacteria are promising sources in the search for novel antibiotics. The aim of the present study is to isolate and assess soil bacteria with anti-MRSA activity and improve their capabilities by UV mutagenesis. Soil samples from the upper south of Thailand were screened for antibacterial activity using the cross-streak method. Agar well diffusion was used to examine the activity of isolates against a spectrum of human pathogens. The most active isolate was identified by 16S rRNA sequencing, and the production kinetics and stability were investigated. The most promising isolate was mutated by UV radiation, and the resulting activity and strain stability were studied. The results show that isolates from the cross-streak method could inhibit Staphylococcus aureus TISTR 517 (94 isolates) and Escherichia coli TISTR 887 (67 isolates). Nine isolates remained active against S. aureus TISTR 517 and MRSA, and eight isolates inhibited the growth of E. coli TISTR 887 as assessed using agar well diffusion. The most active strain was Brevibacillus sp. SPR-20, which had the highest activity at 24 h of incubation. The active substances in culture supernatants exhibited more than 90% activity when subjected to treatments involving various heat, enzymes, surfactants, and pH conditions. The mutant M201 showed significantly higher activity (109.88–120.22%) and strain stability compared to the wild-type strain. In conclusion, we demonstrate that soil Brevibacillus sp. is a potential resource that can be subjected to UV mutagenesis as a useful approach for improving the production of anti-MRSA in the era of antibiotic resistance. Full article
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