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Sci. Pharm., Volume 87, Issue 4 (December 2019) – 11 articles

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Open AccessObituary
Obituary for Prof. Dr. Gottfried Heinisch
Sci. Pharm. 2019, 87(4), 35; https://doi.org/10.3390/scipharm87040035 - 06 Dec 2019
Viewed by 770
Abstract
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Open AccessReview
Multifaceted Protective Role of Glucosamine against Osteoarthritis: Review of Its Molecular Mechanisms
Sci. Pharm. 2019, 87(4), 34; https://doi.org/10.3390/scipharm87040034 - 05 Dec 2019
Cited by 3 | Viewed by 1150
Abstract
Osteoarthritis (OA) is a joint disease resulting from cartilage degeneration and causing joint pain and stiffness. Glucosamine exerts chondroprotective effects and effectively reduces OA pain and stiffness. This review aims to summarise the mechanism of glucosamine in protecting joint health and preventing OA [...] Read more.
Osteoarthritis (OA) is a joint disease resulting from cartilage degeneration and causing joint pain and stiffness. Glucosamine exerts chondroprotective effects and effectively reduces OA pain and stiffness. This review aims to summarise the mechanism of glucosamine in protecting joint health and preventing OA by conducting a literature search on original articles. Current evidence has revealed that glucosamine exhibits anti-inflammatory effects by reducing the levels of pro-inflammatory factors (such as tumour necrosis factor-alpha, interleukin-1, and interleukin-6) and enhancing the synthesis of proteoglycans that retard cartilage degradation and improve joint function. Additionally, glucosamine improves cellular redox status, reduces OA-mediated oxidative damages, scavenges free radicals, upregulates antioxidant proteins and enzyme levels, inhibits the production of reactive oxygen species, and induces autophagy to delay OA pathogenesis. In conclusion, glucosamine prevents OA and maintains joint health by reducing inflammation, improving the redox status, and inducing autophagy in joints. Further studies are warranted to determine the synergistic effect of glucosamine with other anti-inflammatory and/or antioxidative agents on joint health in humans. Full article
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Open AccessReview
Cyclodextrins in Drug Delivery Systems and Their Effects on Biological Barriers
Sci. Pharm. 2019, 87(4), 33; https://doi.org/10.3390/scipharm87040033 - 20 Nov 2019
Cited by 17 | Viewed by 1438
Abstract
Cyclodextrins are widely used excipients, composed of glucopyranose units with a cyclic structure. One of their most important properties, is that their inner cavity is hydrophobic, while their surface is hydrophilic. This enables them for the complex formation with lipophilic molecules. They have [...] Read more.
Cyclodextrins are widely used excipients, composed of glucopyranose units with a cyclic structure. One of their most important properties, is that their inner cavity is hydrophobic, while their surface is hydrophilic. This enables them for the complex formation with lipophilic molecules. They have several applications in the pharmaceutical field like solubility enhancers or the building blocks of larger drug delivery systems. On the other hand, they have numerous effects on cells or biological barriers. In this review the most important properties of cyclodextrins and cyclodextrin-based drug delivery systems are summarized with special focus on their biological activity. Full article
(This article belongs to the Special Issue New Insights into Drug Delivery and Absorption)
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Open AccessArticle
The Optimization of Gel Preparations Using the Active Compounds of Arabica Coffee Ground Nanoparticles
Sci. Pharm. 2019, 87(4), 32; https://doi.org/10.3390/scipharm87040032 - 19 Nov 2019
Cited by 1 | Viewed by 1032
Abstract
Arabica coffee (Coffea arabica L.) ground nanoparticles contain phenolics compounds that have anti-inflammatory effects, so they can be used as sources of active compounds in anti-inflammatory gel preparations. This study aims to determine the optimum formulation of anti-inflammatory gel preparations using Arabica [...] Read more.
Arabica coffee (Coffea arabica L.) ground nanoparticles contain phenolics compounds that have anti-inflammatory effects, so they can be used as sources of active compounds in anti-inflammatory gel preparations. This study aims to determine the optimum formulation of anti-inflammatory gel preparations using Arabica coffee ground nanoparticles as active compounds. Treatment optimization was performed using a Response Surface Methodology according to the Box-Behnken Design with a quadratic model in the Design Expert Version 10.0.3.0 software. In this study we used three factors (x): carbopol 940, triethanolamine (TEA), and nanoparticles, each of which consists of three levels, the response (y) observed including the acidity degree (pH), spreadability, viscosity and total phenolic content. ANOVA analysis results show that the quadratic model is very appropriate since it produces a high R2 value and a low PRESS value for all responses, as well as significant p-values (<0.0500) and an insignificant lack of Fit values (p-value> 5%). The optimum formulations for the gel preparations of the Arabica coffee ground nanoparticles obtained in this study are carbopol 940 (0.569%), TEA (0.468%), and nanoparticles (3.000%), which have values w/o an interval (0.994) and a desirable (0.981) response to acidity (5.212), spreadability (5.850 cm), viscosity (3734.244 cps) and total phenolic content (669.227 µgGAE/g). Full article
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Open AccessArticle
Stability Indicating HPLC-ECD Method for the Analysis of Clarithromycin in Pharmaceutical Dosage Forms: Method Scaling versus Re-Validation
Sci. Pharm. 2019, 87(4), 31; https://doi.org/10.3390/scipharm87040031 - 16 Nov 2019
Cited by 3 | Viewed by 1328
Abstract
An isocratic high-performance liquid chromatographic method using electrochemical detection (HPLC-ECD) for the quantitation of clarithromycin (CLA) was developed using Response Surface Methodology (RSM) based on a Central Composite Design (CCD). The method was validated using International Conference on Harmonization (ICH) guidelines with an [...] Read more.
An isocratic high-performance liquid chromatographic method using electrochemical detection (HPLC-ECD) for the quantitation of clarithromycin (CLA) was developed using Response Surface Methodology (RSM) based on a Central Composite Design (CCD). The method was validated using International Conference on Harmonization (ICH) guidelines with an analytical run time of 20 min. Method re-validation following a change in analytical column was successful in reducing the analytical run time to 13 min, decreasing solvent consumption thus facilitating environmental and financial sustainability. The applicability of using the United States Pharmacopeia (USP) method scaling approach in place of method re-validation using a column with a different L–designation to the original analytical column, was investigated. The scaled method met all USP system suitability requirements for resolution, tailing factor and % relative standard deviation (RSD). The re-validated and scaled method was successfully used to resolve CLA from manufacturing excipients in commercially available dosage forms. Although USP method scaling is only permitted for columns within the same L-designation, these data suggest that it may also be applicable to columns of different designation. Full article
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Open AccessArticle
4-Hydroxyderricin Isolated from the Sap of Angelica keiskei Koidzumi: Evaluation of Its Inhibitory Activity towards Dipeptidyl Peptidase-IV
Sci. Pharm. 2019, 87(4), 30; https://doi.org/10.3390/scipharm87040030 - 15 Nov 2019
Cited by 1 | Viewed by 1020
Abstract
Angelica keiskei sap is used as a blood-sugar reducer in Indonesia, however its molecular mechanism has not yet been explored. 4-hydroxyderricin (4-HD) is one of the major components extracted from A. keiskei sap. The aim of this work was to isolate 4-HD from [...] Read more.
Angelica keiskei sap is used as a blood-sugar reducer in Indonesia, however its molecular mechanism has not yet been explored. 4-hydroxyderricin (4-HD) is one of the major components extracted from A. keiskei sap. The aim of this work was to isolate 4-HD from the sap of A. keiskei planted in Lombok, Indonesia, and to study in silico and in vitro mechanisms against dipeptidyl peptidase-IV (DPP-IV). The dried sap was submitted to liquid–liquid extraction using solvents with different polarity. Further purification processing was conducted using gradient elution column chromatography. The isolated compound was a yellowish powder, m/z 339.2215 [M + H]+, which was confirmed as 4-HD. Sitagliptin, a DPP-IV inhibitor, was employed as the positive control for both the in silico and in vitro studies. It was indicated that 4-HD interacts with Glu206 and Phe357, important amino acid residues in the DPP-IV binding pocket. These interactions are similar to that of sitagliptin. The affinity of 4-HD (inhibition constant (Ki) = 3.99 μM) to DPP-IV is lower than that of sitagliptin (inhibition constant (Ki) = 0.17 μM). Furthermore, in vitro study showed that 4-HD inhibits DPP-IV (IC50 = 81.44 μM) weaker than for sitagliptin (IC50 = 0.87 μM). We concluded that 4- HD might have potential in inhibiting DPP-IV. However, by considering the polar interaction of sitagliptin with DPP-IV, a further structure modification of 4-HD, e.g., by introducing a polar moiety such as a hydroxyl group, might be needed to obtain stronger activity as a DPP-IV inhibitor. Full article
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Open AccessArticle
In Silico Mapping of Essential Residues in the Catalytic Domain of PDE5 Responsible for Stabilization of Its Commercial Inhibitors
Sci. Pharm. 2019, 87(4), 29; https://doi.org/10.3390/scipharm87040029 - 01 Nov 2019
Viewed by 1042
Abstract
Phosphodiesterase type 5 (PDE5) is an important enzyme associated with the hydrolysis of cyclic guanosine monophosphate (cGMP) to guanosine monophosphate (GMP). Due to the relevant role of second messenger cGMP as a mediator in many physiological processes, efforts have been converged to find [...] Read more.
Phosphodiesterase type 5 (PDE5) is an important enzyme associated with the hydrolysis of cyclic guanosine monophosphate (cGMP) to guanosine monophosphate (GMP). Due to the relevant role of second messenger cGMP as a mediator in many physiological processes, efforts have been converged to find a safe pharmacological approach, seeking a specific, selective and potent inhibitor of the PDE5 enzyme. There are five commercial drugs with potential for clinical use: tadalafil, sildenafil, avanafil, udenafil and vardenafil. Here, we applied molecular modeling to obtain different profiles of protein–ligand interactions by adopting distinct PDE5 structures, specifically PDBid:1XOZ and two extracted from molecular dynamics (MD) simulations. The results generated by molecular docking showed several possibilities for inhibitor interactions with the catalytic pocket. Tadalafil, sildenafil and vardenafil were clearly stabilized by Gln817 via a well-oriented hydrogen bond. Another set of different interactions, such as polar, hydrophobic, π-stacking, metal–ligand and electrostatic, were responsible for accommodating avanafil and udenafil. All of the ligands are discussed in detail with consideration of the distinct protein structures, and a profile of the probability of residue–ligand contact is suggested, with the most frequently observed being: Tyr612, His613, Ser661, Thr723, Asp724, Asp764, Leu765, Val782 and Phe786. The molecular interactions displayed herein confirm findings achieved by previous authors and also present new contacts. In addition, the discussion can help researchers obtain a molecular basis for planning new selective PDE5 inhibitors, as well as explain an inhibitor’s experimental assays by considering the specific interactions occurring at the catalytic site. Full article
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Open AccessArticle
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
Sci. Pharm. 2019, 87(4), 28; https://doi.org/10.3390/scipharm87040028 - 22 Oct 2019
Cited by 2 | Viewed by 1215
Abstract
Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with [...] Read more.
Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors. Full article
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Open AccessReview
Recent Approaches for Solid Dose Vaccine Delivery
Sci. Pharm. 2019, 87(4), 27; https://doi.org/10.3390/scipharm87040027 - 14 Oct 2019
Cited by 3 | Viewed by 1383
Abstract
Recent studies on vaccine delivery systems are exploring the possibility of replacing liquid vaccines with solid dose vaccines due to the many advantages that solid dose vaccines can offer. These include the prospect of a needle-free vaccine delivery system leading to better patient [...] Read more.
Recent studies on vaccine delivery systems are exploring the possibility of replacing liquid vaccines with solid dose vaccines due to the many advantages that solid dose vaccines can offer. These include the prospect of a needle-free vaccine delivery system leading to better patient compliance, cold chain storage, less-trained vaccinators and fewer chances for needle stick injury hazards. Some studies also indicate that vaccines in a solid dosage form can result in a higher level of immunogenicity compared to the liquid form, thus providing a dose-sparing effect. This review outlines the different approaches in solid vaccine delivery using various routes of administration including, oral, pulmonary, intranasal, buccal, sublingual, and transdermal routes. The various techniques and their current advancements will provide a knowledge base for future work to be carried out in this arena. Full article
(This article belongs to the Special Issue New Insights into Drug Delivery and Absorption)
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Open AccessReview
A Mini-Review of Human Studies on Cholesterol-Lowering Properties of Probiotics
Sci. Pharm. 2019, 87(4), 26; https://doi.org/10.3390/scipharm87040026 - 14 Oct 2019
Cited by 5 | Viewed by 1240
Abstract
Cardiovascular diseases (CVD) are the major health issue of modernized society with a high mortality rate. Lifestyle, genetic makeup, and diet are some of the major influencing factors associated with CVD. The dyslipidemia is one such factor related to the development of several [...] Read more.
Cardiovascular diseases (CVD) are the major health issue of modernized society with a high mortality rate. Lifestyle, genetic makeup, and diet are some of the major influencing factors associated with CVD. The dyslipidemia is one such factor related to the development of several CVD. Many studies proved that the consumption of probiotics confers several health benefits. Several studies reported the evaluation of the cholesterol-lowering ability of probiotics (probiotics that showed positive effect in vitro and in vivo studies) in human volunteers. The current review summarizes the outcomes of human studies on the cholesterol-lowering property of probiotics. Probiotic consumption significantly improved the health status of hypercholesteremic patients by reducing the low-density lipoprotein cholesterol, total cholesterol, triglyceride levels, and increased the high-density lipoprotein cholesterol. The probiotic supplementation improved the lipid profile of diabetic patients, and obese people as well. However, not all probiotic interventions are effective against dyslipidemia. The results are controversial and depend on several factors such as probiotic strain, dose, duration of the treatment, lifestyle changes, etc. This literature survey indorses additional studies on the cholesterol-lowering property of probiotics, which could help to reduce the risk of CVD and other dyslipidemia associated health issues. Full article
Open AccessCommunication
A New DNA Repair-Related Platform for Pharmaceutical Outlook in Cancer Therapies: Ultrashort Single-Stranded Polynucleotides
Sci. Pharm. 2019, 87(4), 25; https://doi.org/10.3390/scipharm87040025 - 05 Oct 2019
Cited by 1 | Viewed by 994
Abstract
Thio- and cyano- modified single-stranded poly(dNTP) sequences of different molecular sizes (20–200 n) and the same lengths routine poly(dNTP) and poly(NTP) species were tested for their impact on catalytic activities of β-like DNA polymerases from chromatin of HL-60, WERI-1A and Y-79 cells [...] Read more.
Thio- and cyano- modified single-stranded poly(dNTP) sequences of different molecular sizes (20–200 n) and the same lengths routine poly(dNTP) and poly(NTP) species were tested for their impact on catalytic activities of β-like DNA polymerases from chromatin of HL-60, WERI-1A and Y-79 cells as well as for the affinity patterns in DNApolβ-poly(dNTP)/(NTP) pairs, respectively. An essential link between the lengths of ultrashort (50–100 n) single-stranded poly(dNTP) sequences of different structures and their inhibitory effects towards the cancer-specific DNA polymerases β was found. A possible significance of this phenomenon for both DNA repair suppression in tumors and a consequent anti-cancer activity of the DNA repair related short poly(dNTP) fragments is under discussion. Full article
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