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

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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 (registering DOI) - 22 Oct 2019
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
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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)
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
Viewed by 113
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
Viewed by 196
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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