Scientia Pharmaceutica

14 pages, 808 KiB

Open AccessReview

Resveratrol: Extraction Techniques, Bioactivity, and Therapeutic Potential in Ocular Diseases

by Giulia Accomasso, Flavia Turku, Simona Sapino, Daniela Chirio, Elena Peira and Marina Gallarate

Sci. Pharm. 2024, 92(4), 59; https://doi.org/10.3390/scipharm92040059 - 14 Nov 2024

Abstract

Resveratrol (RV), a natural polyphenol found in various plants, exhibits a wide range of bioactive properties and mechanisms of action. Its potential therapeutic benefits in several diseases and, more specifically, in ocular diseases have garnered significant attention, with studies exploring RV properties at [...] Read more.

Resveratrol (RV), a natural polyphenol found in various plants, exhibits a wide range of bioactive properties and mechanisms of action. Its potential therapeutic benefits in several diseases and, more specifically, in ocular diseases have garnered significant attention, with studies exploring RV properties at cellular, molecular, and physiological levels. Like many natural derivatives, RV can be obtained through various extraction methods from plant sources, with a growing interest in sustainable techniques that align with recent trends in sustainability, circular economy, and green chemistry. This review begins by describing the most efficient and sustainable extraction techniques of RV from natural sources and then delves into its numerous bioactive properties and its synergistic effects with other active substances and drugs. Furthermore, an overview of the scientific literature on RV as a therapeutic agent for ocular diseases, both in its pure form and entrapped in nanoparticulate systems, is provided. Full article

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13 pages, 1001 KiB

Open AccessReview

ChatGPT in Pharmacy Practice: Disruptive or Destructive Innovation? A Scoping Review

by Tácio de Mendonça Lima, Michelle Bonafé, André Rolim Baby and Marília Berlofa Visacri

Sci. Pharm. 2024, 92(4), 58; https://doi.org/10.3390/scipharm92040058 - 21 Oct 2024

Abstract

ChatGPT has emerged as a promising tool for enhancing clinical practice. However, its implementation raises critical questions about its impact on this field. In this scoping review, we explored the utility of ChatGPT in pharmacy practice. A search was conducted in five databases [...] Read more.

ChatGPT has emerged as a promising tool for enhancing clinical practice. However, its implementation raises critical questions about its impact on this field. In this scoping review, we explored the utility of ChatGPT in pharmacy practice. A search was conducted in five databases up to 23 May 2024. Studies analyzing the use of ChatGPT with direct or potential applications in pharmacy practice were included. A total of 839 records were identified, of which 14 studies were included: six tested ChatGPT version 3.5, three tested version 4.0, three tested both versions, one used version 3.0, and one did not specify the version. Only half of the studies evaluated ChatGPT in real-world scenarios. A reasonable number of papers analyzed the use of ChatGPT in pharmacy practice, highlighting both benefits and limitations. The studies indicated that ChatGPT is not fully prepared for use in pharmacy practice due to significant limitations. However, there is great potential for its application in this context in the near future, following further improvements to the tool. Further exploration of its use in pharmacy practice is required, along with proposing its conscious and appropriate utilization. Full article

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25 pages, 1074 KiB

Open AccessReview

Passiflora By-Products: Chemical Profile and Potential Use as Cosmetic Ingredients

by Manuela Victoria Pardo Solórzano, Geison Modesti Costa and Leonardo Castellanos

Sci. Pharm. 2024, 92(4), 57; https://doi.org/10.3390/scipharm92040057 - 18 Oct 2024

Abstract

The cosmetics industry is constantly growing and occupies an important place in South American countries’ economies. Formulations increasingly incorporate ingredients from natural sources to promote sustainable and innovative productions, as well as to gain greater consumer acceptance. According to FAO, waste from post-harvest [...] Read more.

The cosmetics industry is constantly growing and occupies an important place in South American countries’ economies. Formulations increasingly incorporate ingredients from natural sources to promote sustainable and innovative productions, as well as to gain greater consumer acceptance. According to FAO, waste from post-harvest and food processing in developing countries exceeds 40%, generating significant environmental impacts and stimulating interest in adding value to these wastes, particularly in the fruit and vegetable sector in South American countries, thus contributing to the achievement of the UN Sustainable Development Goals (SDGs). By-products from harvesting and fruit processing of Passiflora species such as leaves, stems, peel, and seeds are a source of bioactive compounds; however, most of them are wasted. This study aims to compile reports on the chemical composition of cultivated Passiflora species, find evidence of the cosmetic activity of their extracts, and estimate their potential for inclusion in cosmetic formulations. Full article

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7 pages, 1069 KiB

Open AccessArticle

Evaluation of the Efficacy of Methylene Blue Administration in SARS-CoV-2-Affected Patients: A Proof-of-Concept Phase 2, Randomized, Placebo-Controlled, Single-Blind Clinical Trial

by Beatrice Barda, Bruno Di Mari, Emiliano Soldini, Claudia Di Bartolomeo, Maurizia Bissig, Adriana Baserga, Antonella Robatto, Lorenzo Magenta, Rossella Forlenza and Andreas Cerny

Sci. Pharm. 2024, 92(4), 56; https://doi.org/10.3390/scipharm92040056 - 14 Oct 2024

Abstract

The SARS-CoV-2 pandemic has revolutionized the scientific and medical world in recent years. Methylene blue (MB) is a well-known molecule. The aim of our study was to assess the efficacy of MB against early-phase SARS-CoV-2 infections. All patients with a positive swab for [...] Read more.

The SARS-CoV-2 pandemic has revolutionized the scientific and medical world in recent years. Methylene blue (MB) is a well-known molecule. The aim of our study was to assess the efficacy of MB against early-phase SARS-CoV-2 infections. All patients with a positive swab for SARS-CoV-2 were eligible for the trial. The intervention was a starting dose of 200 mg MB or placebo in the morning and 100 mg in the evening on the first day and afterwards the standard daily dose of 200 mg. Patients were followed up for safety and efficacy until day 84. We analyzed 21 patients for the safety profile and 19 for the efficacy objective: of these, there were 11 in the MB group and 8 in the placebo one. In both groups, patients had undetectable RNA from day 3 and 10 out of 11 subjects in the MB group were virus free by day 12 vs. 6 out of 8 in the placebo one. None of the patients experienced serious adverse events. MB has proved to be a safe and well-tolerated drug. We did not find superiority of efficacy or viral clearance of MB compared to the placebo. Given the good in vitro efficacy, larger studies are needed to assess MB efficacy against COVID-19 in vivo. Full article

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24 pages, 6993 KiB

Open AccessArticle

Human Target Proteins for Benzo(a)pyrene and Acetaminophen (And Its Metabolites): Insights from Inverse Molecular Docking and Molecular Dynamics Simulations

by Yina Montero-Pérez, Nerlis Pájaro-Castro, Nadia Coronado-Posada, Maicol Ahumedo-Monterrosa and Jesus Olivero-Verbel

Sci. Pharm. 2024, 92(4), 55; https://doi.org/10.3390/scipharm92040055 - 8 Oct 2024

Abstract

Acetaminophen (APAP) is a widely used analgesic and antipyretic, whereas benzo(a)pyrene (B[a]P) is a carcinogen with significant global health risks due to environmental exposure. While APAP is generally safe at therapeutic doses, co-exposure to B[a]P can exacerbate its toxicity. This study aimed to [...] Read more.

Acetaminophen (APAP) is a widely used analgesic and antipyretic, whereas benzo(a)pyrene (B[a]P) is a carcinogen with significant global health risks due to environmental exposure. While APAP is generally safe at therapeutic doses, co-exposure to B[a]P can exacerbate its toxicity. This study aimed to identify potential human target proteins for B[a]P and APAP through inverse molecular docking and molecular dynamics simulations. We performed inverse docking with B[a]P, APAP, and three APAP metabolites against 689 human proteins involved in various biological processes. Five proteins were selected based on high docking affinity and their involvement in multiple pathways. Molecular dynamics simulations revealed that B[a]P primarily interacted via hydrophobic and π-stacking interactions with proteins like LXR-β, HSP90α, HSP90β, and AKT1, while AM404 formed hydrogen bonds and hydrophobic interactions. The simulations confirmed that the complexes had high conformational stability, except for protein AKT1. These results provide insights into the potential impacts of B[a]P and AM404 on protein functions and their implications for understanding the toxic effects of combined exposure. Full article

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19 pages, 4020 KiB

Open AccessArticle

Position Matters: Effect of Nitro Group in Chalcones on Biological Activities and Correlation via Molecular Docking

by Alam Yair Hidalgo, Nancy Romero-Ceronio, Carlos Ernesto Lobato-García, Maribel Herrera-Ruiz, Romario Vázquez-Cancino, Omar Aristeo Peña-Morán, Miguel Ángel Vilchis-Reyes, Ammy Joana Gallegos-García, Eric Jaziel Medrano-Sánchez, Oswaldo Hernández-Abreu and Abraham Gómez-Rivera

Sci. Pharm. 2024, 92(4), 54; https://doi.org/10.3390/scipharm92040054 - 8 Oct 2024

Abstract

A series of nine nitro group-containing chalcones were synthesized to investigate their anti-inflammatory and vasorelaxant activities via in vivo, ex vivo, and in silico studies. The anti-inflammatory effects of the compounds were evaluated via a TPA-induced mouse ear edema model, and the vasorelaxant [...] Read more.

A series of nine nitro group-containing chalcones were synthesized to investigate their anti-inflammatory and vasorelaxant activities via in vivo, ex vivo, and in silico studies. The anti-inflammatory effects of the compounds were evaluated via a TPA-induced mouse ear edema model, and the vasorelaxant effects were evaluated via an isolated organ model in addition to molecular docking studies. The compounds with the highest anti-inflammatory activity were 2 (71.17 ± 1.66%), 5 (80.77 ± 2.82%), and 9 (61.08 ± 2.06%), where the nitro group is located at the ortho position in both rings, as confirmed by molecular docking with COX-1 and COX-2. The compounds with the highest vasorelaxant activity were 1 (81.16 ± 7.55%), lacking a nitro group, and 7 (81.94 ± 2.50%), where the nitro group is in the para position of the B ring; both of these compounds interact with the eNOS enzyme during molecular docking. These results indicate that the position of the nitro group in the chalcone plays an important role in these anti-inflammatory and vasorelaxant activities. Full article

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18 pages, 2428 KiB

Open AccessArticle

Cannabigerol Reduces Acute and Chronic Hypernociception in Animals Exposed to Prenatal Hypoxia-Ischemia

by Bismarck Rezende, Kethely Lima Marques, Filipe Eloi Alves de Carvalho, Vitória Macario de Simas Gonçalves, Barbara Conceição Costa Azeredo de Oliveira, Gabriela Guedes Nascimento, Yure Bazilio dos Santos, Fernanda Antunes, Penha Cristina Barradas, Fabrícia Lima Fontes-Dantas and Guilherme Carneiro Montes

Sci. Pharm. 2024, 92(3), 53; https://doi.org/10.3390/scipharm92030053 - 23 Sep 2024

Abstract

Cannabigerol (CBG), a phytocannabinoid, has shown promise in pain management. Previous studies by our research group identified an increase in pain sensitivity as a consequence of prenatal hypoxia-ischemia (HI) in an animal model. This study aimed to investigate the efficacy of CBG in [...] Read more.

Cannabigerol (CBG), a phytocannabinoid, has shown promise in pain management. Previous studies by our research group identified an increase in pain sensitivity as a consequence of prenatal hypoxia-ischemia (HI) in an animal model. This study aimed to investigate the efficacy of CBG in acute and chronic hyperalgesia induced by prenatal HI. A pharmacological screening was first conducted using hot plate and open-field tests to evaluate the antinociceptive and locomotor activities of animals administered with a 50 mg/kg oral dose of cannabis extract with a high CBG content. Prenatal HI was induced in pregnant rats, and the offspring were used to evaluate the acute antinociceptive effect of CBG in the formalin-induced peripheral pain model, while chronic antinociceptive effects were observed through spinal nerve ligation (SNL) surgery, a model used to induce neuropathic pain. Our results show that CBG exhibited an antinociceptive effect in the hot plate test without affecting the animals’ motor function in the open-field test. CBG significantly reduced formalin-induced reactivity in HI offspring during both the neurogenic and inflammatory phases. CBG treatment alleviated thermal and mechanical hypernociception induced by SNL. Biomolecular analysis revealed CBG’s ability to modulate expression, particularly reducing TNFα and Nav1.7 in HI male and female rats, respectively. These results highlight CBG as a potential antinociceptive agent in acute and chronic pain models, suggesting it as a promising therapeutic option without inducing motor impairment. Further research is needed to fully elucidate its mechanisms and clinical applications in pain management. Full article

(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)

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13 pages, 3538 KiB

Open AccessArticle

Natural Antioxidants from Acmella oleracea Extract as Dermatocosmetic Actives

by Claudia Maxim, Alexandra Cristina Blaga, Ramona Cimpoeșu, Inga Zinicovscaia, Alexandra Peshkova, Maricel Danu, Ana Simona Barna and Daniela Suteu

Sci. Pharm. 2024, 92(3), 52; https://doi.org/10.3390/scipharm92030052 - 19 Sep 2024

Abstract

Compounds from plant extracts make dermatocosmetic products more effective as they avoid the adaptation and resistance of the organism and achieve a synergistic effect of the molecular properties of interest. Acmella oleracea extract is considered to have great potential in preventing oxidative damage [...] Read more.

Compounds from plant extracts make dermatocosmetic products more effective as they avoid the adaptation and resistance of the organism and achieve a synergistic effect of the molecular properties of interest. Acmella oleracea extract is considered to have great potential in preventing oxidative damage and improving the appearance of the skin. The purpose of this article is to support the product formulated by preliminary studies of two types of O/W emulsions with 3% and 5% concentrations of Acmella oleracea extract. Physico-chemical methods were performed to evaluate the stability, microbiological control, rheological behavior and diffusion through the membrane. Good homogeneity, structural strength and flexibility, adequate skin diffusion, and high physico-chemical and microbiological stability were confirmed. The conclusions lead to the idea that these results require further in vivo studies as well as studies of toxicity and cytotoxicity to obtain the necessary data to place this product on the market. Full article

(This article belongs to the Topic New Compounds Discovery and Development in Medicine — Advances in Research on Potential Therapeutic Agents and Drug Candidates, 2nd Edition)

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18 pages, 2964 KiB

Open AccessArticle

Targeted Gene Delivery to Muscle Cells In Vitro and In Vivo Using Electrostatically Stabilized DNA—Peptide Complexes

by Anna Egorova, Sergei Chepanov, Sergei Selkov, Igor Kogan and Anton Kiselev

Sci. Pharm. 2024, 92(3), 51; https://doi.org/10.3390/scipharm92030051 - 14 Sep 2024

Abstract

Genetic constructs must be delivered selectively to target tissues and intracellular compartments at the necessary concentrations in order to achieve the maximum therapeutic effect in gene therapy. Development of targeted carriers for non-viral delivery of nucleic acids into cells, including those in muscle, [...] Read more.

Genetic constructs must be delivered selectively to target tissues and intracellular compartments at the necessary concentrations in order to achieve the maximum therapeutic effect in gene therapy. Development of targeted carriers for non-viral delivery of nucleic acids into cells, including those in muscle, which is one of the most challenging tissues to transfect in vivo, remains a topical issue. We have studied ternary complexes of plasmid DNA and an arginine–histidine-rich peptide-based carrier coated with a glutamate–histidine-rich polymer bearing skeletal muscle targeting peptide (SMTP) for the gene delivery to muscle tissue. The relaxation of the ternary complexes after polyanion treatment was assessed using the ethidium bromide displacement assay. The developed polyplexes were used to transfect C2C12 myoblasts in full-media conditions, followed by analysis of their toxic properties using the Alamar Blue assay and expression analysis of lacZ and GFP reporter genes. After delivering plasmids containing the GFP and lacZ genes into the femoral muscles of mdx mice, which are model of Duchenne muscular dystrophy, GFP fluorescence and β-galactosidase activity were detected. We observed that the modification of ternary polyplexes with 10 mol% of SMTP ligand resulted in a 2.3-fold increase in lacZ gene expression when compared to unmodified control polyplexes in vivo. Thus, we have demonstrated that the developed DNA/carrier complexes and SMTP-modified coating are nontoxic, are stable against polyanion-induced relaxation, and can provide targeted gene delivery to muscle cells and tissues. The results of this study are useful for a range of therapeutic applications, from immunization to amelioration of inherited neuromuscular diseases. Full article

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25 pages, 4244 KiB

Open AccessArticle

Back to Nature: Development and Optimization of Bioinspired Nanocarriers for Potential Breast Cancer Treatment

by Sally Safwat, Rania M. Hathout, Rania A. H. Ishak and Nahed D. Mortada

Sci. Pharm. 2024, 92(3), 50; https://doi.org/10.3390/scipharm92030050 - 2 Sep 2024

Abstract

This study focuses on the preparation and optimization of caffeic acid (CA)-loaded casein nanoparticles (CS NPs) via the Box–Behnken design (BBD) for potential applications in cancer treatment. CS NPs were loaded with CA as a promising anti-cancer molecule. Non-hazardous green materials were exploited [...] Read more.

This study focuses on the preparation and optimization of caffeic acid (CA)-loaded casein nanoparticles (CS NPs) via the Box–Behnken design (BBD) for potential applications in cancer treatment. CS NPs were loaded with CA as a promising anti-cancer molecule. Non-hazardous green materials were exploited for nanoparticle fabrication. The BBD was used, followed by a desirability function to select the optimum formulation. The BBD was adopted as it avoids the runs implemented in extreme conditions, hence making it suitable for proteins. CS NPs were characterized regarding particle size (PS), size distribution (PDI), zeta potential (ZP), drug entrapment, morphology using TEM, differential scanning calorimetry, molecular docking, in vitro release, and cytotoxicity studies. PS, PDI, and ZP had significant responses, while EE% was insignificant. The suggested models were quadratic with high fitting. Optimized NPs showed PS = 110.31 ± 1.02 nm, PDI = 0.331 ± 0.029, ZP = −23.94 ± 1.64 mV, and EE% = 95.4 ± 2.56%. Molecular modeling indicated hydrophobic and electrostatic interactions between CA and CS, accounting for the high EE%. Almost spherical particles were realized with a sustained CA release pattern. Optimized NPs effectively suppressed the growth of MCF-7 cell lines by scoring the lowest IC50 = 78.45 ± 1.7 µg/mL. A novel combination of bioinspired-derived materials was developed for use in breast cancer treatment. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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24 pages, 11596 KiB

Open AccessArticle

A Network Pharmacology and Molecular Docking Technology to Identify and Explore Mechanism of Bioactive Components of Fucus vesiculosus against Gut Disorders

by Varisha Anjum, Uday Bagale, Ammar Kadi and Irina Potoroko

Sci. Pharm. 2024, 92(3), 49; https://doi.org/10.3390/scipharm92030049 - 30 Aug 2024

Abstract

The gut is an intricate and diverse organ system for investigating visceral pattern generation. The gut made an early evolutionary breakthrough. There is evidence that the molecular mechanisms governing the development of gastrointestinal patterns are species-specific. Some have suggested using marine drugs to [...] Read more.

The gut is an intricate and diverse organ system for investigating visceral pattern generation. The gut made an early evolutionary breakthrough. There is evidence that the molecular mechanisms governing the development of gastrointestinal patterns are species-specific. Some have suggested using marine drugs to treat gastrointestinal disorders. The study, which used an integrated network pharmacology approach, aimed to find out how well fucoidan worked and what Fucus vesiculosus might be doing to help prevent digestive problems. Researchers gathered information on how potential bioactive components of brown seaweed and their associated targets interact with the disease gene targets of gastrointestinal disorders. We studied the signaling pathways linked to F. vesiculosus in the context of gut health treatments using a KEGG (Kyoto Encyclopedia of Genes and Genomes pathway) and GO (Gene ontology) enrichment analysis. We built and studied the protein–protein interaction (PPI) and compound-target networks using Cytoscape. PPI network analysis yielded a total of 44 important targets, including BCL2, ESR1, and STAT3. The KEGG enrichment analysis revealed a strong correlation between the signaling pathways used in the treatment and the prevention of gastrointestinal disorders. We docked significant genes with TNF, STAT3, BCL2, and ALB. Fucoxanthin and fucoidan possess beneficial properties for improving gut health by treating gastric-intestinal issues. This study showed that by controlling several targets and many pathways with multiple components, F. vesiculosus exhibited preventive effects against gastrointestinal disorders. Full article

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20 pages, 2334 KiB

Open AccessArticle

Phosal^® Curcumin-Loaded Nanoemulsions: Effect of Surfactant Concentration on Critical Physicochemical Properties

by Joanna Czerniel, Aleksandra Gostyńska, Tomasz Przybylski and Maciej Stawny

Sci. Pharm. 2024, 92(3), 48; https://doi.org/10.3390/scipharm92030048 - 30 Aug 2024

Abstract

Curcumin is a well-known and widely used substance of natural origin. It has also been found to be helpful in the treatment of liver diseases. Unfortunately, curcumin has very low bioavailability and a sensitivity to external agents. Improving these parameters is the subject [...] Read more.

Curcumin is a well-known and widely used substance of natural origin. It has also been found to be helpful in the treatment of liver diseases. Unfortunately, curcumin has very low bioavailability and a sensitivity to external agents. Improving these parameters is the subject of many studies. One way to overcome these problems may be to use Phosal^® Curcumin as a source of curcumin and encapsulate this dispersion into a nanoemulsion using different types and concentrations of surfactants and co-surfactants, thus manipulating the physicochemical parameters of the nanoemulsion. The present study aimed to develop curcumin-loaded nanoemulsions for intravenous administration and to investigate the effect of Kolliphor HS15 concentration on their critical quality attributes. Methods: Phosal^® Curcumin-loaded nanoemulsions with different concentrations of Kolliphor HS15 were prepared by high-pressure homogenization. The effect of Kolliphor HS15 on emulsion physicochemical properties such as mean droplet diameter (MDD), polydispersity index (PDI), zeta potential (ZP), osmolality (OSM), and pH, as well as encapsulation efficiency (EE) and retention rate (RR) of curcumin, were determined. Mid-term stability studies and short-term stress tests were conducted to evaluate the impact of Kolliphor HS15 on the critical quality attributes of the curcumin-loaded nanoemulsions stored under various conditions. Results: Five nanoemulsions with increasing Kolliphor HS15 concentrations were developed. Their MDD ranged from 85.2 ± 2.0 to 154.5 ± 5.1 nm, with a PDI from 0.18 ± 0.04 to 0.10 ± 0.01 and ZP from −15.6 ± 0.7 to −27.6 ± 3.4 mV. Depending on the concentration of Kolliphor HS15, the EE ranged from 58.42 ± 1.27 to 44.98 ± 0.97%. Conclusions: The studied parameters of the developed nanoemulsions meet the requirements for formulations for intravenous administration. Using the appropriate concentration of Kolliphor HS15 allows for a formulation that presents a protective effect against both curcumin and emulsion degradation. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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10 pages, 1895 KiB

Open AccessArticle

Synthesis and Catalytic Activity of Novel Complexes Based on Cyano-Substituted Phthalocyanines as Promising Drug Conversion Agents

by Dmitry Erzunov, Svetlana Tonkova, Ilya Sarvin and Arthur Vashurin

Sci. Pharm. 2024, 92(3), 47; https://doi.org/10.3390/scipharm92030047 - 28 Aug 2024

Abstract

This paper presents the results of obtaining new cobalt and zinc complexes based on dicyanophenoxy-substituted carboxypthalocyanine. The original method of synthesis and isolation of the compound is shown; its spectroscopic and photophysical characteristics are studied. Studies show the absence of aggregation processes in [...] Read more.

This paper presents the results of obtaining new cobalt and zinc complexes based on dicyanophenoxy-substituted carboxypthalocyanine. The original method of synthesis and isolation of the compound is shown; its spectroscopic and photophysical characteristics are studied. Studies show the absence of aggregation processes in organic media for solutions of complexes in working concentration ranges. This shows the possibility of the practical application of structures as catalysts. The high catalytic activity of cobalt complexes with dicyanophenoxy-substituted carboxyphthalocyanine ligand in the conversion reaction of sodium diethyldithiocarbamate to disulfiram, which is an active component of drugs for the treatment of alcohol dependence, is determined. Full article

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17 pages, 1909 KiB

Open AccessArticle

New Design and Characteristics of Probiotics Immobilized on a Clinoptilolite-Containing Tuff

by Olga Ilinskaya, Antonina Galeeva, Michael Glukhov, William Kurdy, Pavel Zelinikhin, Alexey Kolpakov, Galina Yakovleva and Oleg Lopatin

Sci. Pharm. 2024, 92(3), 46; https://doi.org/10.3390/scipharm92030046 - 19 Aug 2024

Abstract

Increasing the biological effectiveness of probiotic preparations requires the development of new stable forms in the gastrointestinal tract. Live bacteria immobilized on a sorbent belong to the latest, fourth generation of probiotics, which ensures a prolonged effect. This study is devoted to developing [...] Read more.

Increasing the biological effectiveness of probiotic preparations requires the development of new stable forms in the gastrointestinal tract. Live bacteria immobilized on a sorbent belong to the latest, fourth generation of probiotics, which ensures a prolonged effect. This study is devoted to developing a new method of preparing active lactobacilli on a natural mineral carrier, a tuff containing zeolite of the clinoptilolite group, which is among the most common authigenic silicate minerals that occur in sedimentary rocks and is known as a safe ion-exchange and adsorbing detoxicant. Among the characterized lactobacilli, strains of L. plantarum, L. acidophilus, and L. crispatus possessed a high level of acid formation and stability in gastrointestinal fluids. The protective effect of the clinoptilolite-containing tuff was registered when the samples were incubated in gastric juice. The optimal technological conditions for immobilization and lyophilization were determined, and the preservation of the viability and probiotic properties of bacteria was confirmed during 8 months of storage. The release of bacteria from the carrier occurred gradually over 12 h. The data obtained show how promising the new preparation is, combining the ability to detoxify harmful intestinal metabolites and the prolonged release of probiotics. Full article

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15 pages, 4606 KiB

Open AccessArticle

Antioxidant Activity of the Medicinal Plant Urtica dioica L.: Extraction Optimization Using Response Surface Methodology and Protective Role in Red Blood Cells

by Aleksja Suli and Eugenia Papadaki

Sci. Pharm. 2024, 92(3), 45; https://doi.org/10.3390/scipharm92030045 - 14 Aug 2024

Abstract

Free radicals are highly reactive compounds that lead to the onset of a variety of serious health conditions, known as “oxidative stress”. Antioxidants, on the other hand, act as defense mechanisms to fight the accumulation of free radicals and maintain cell homeostasis. Urtica [...] Read more.

Free radicals are highly reactive compounds that lead to the onset of a variety of serious health conditions, known as “oxidative stress”. Antioxidants, on the other hand, act as defense mechanisms to fight the accumulation of free radicals and maintain cell homeostasis. Urtica dioica L. is a medicinal plant with unique antioxidant properties, mainly attributable to the presence of polar phenolic compounds. This study aimed to optimize the combination of determinant factors toward the maximum extraction of antioxidants from U. dioica L. Furthermore, it investigated the protective role of the extract on red blood cells that were exposed to oxidative stress. The extraction optimization was performed using Response Surface Methodology and the in vitro antioxidant activity of the extract was determined with Folin–Ciocalteu, FRAP, and DPPH assays. Based on the results, the highest value of antioxidant activity and polar phenolic compounds was recorded using 34% (v/v) ethanol as a solvent in an ultrasonic process carried out at 42 °C for 87 min. In addition, UV–Vis spectrum of the extract revealed the presence of chlorophylls, carotenoids, and flavonoid glycosides. This study also provided insight into the in vitro protective effect of the plant extract on red blood cells morphology under oxidative stress conditions. The findings highlighted the good predictability of the extraction model and the potential role of the extract as an antioxidant product. Full article

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14 pages, 16172 KiB

Open AccessArticle

Topical Application of Cha-Koji, Green Tea Leaves Fermented with Aspergillus Luchuensis var Kawachii Kitahara, Promotes Acute Cutaneous Wound Healing in Mice

by Yasuhiro Katahira, Jukito Sonoda, Miu Yamagishi, Eri Horio, Natsuki Yamaguchi, Hideaki Hasegawa, Izuru Mizoguchi and Takayuki Yoshimoto

Sci. Pharm. 2024, 92(3), 44; https://doi.org/10.3390/scipharm92030044 - 12 Aug 2024

Abstract

“Koji” is one of the most well-known probiotic microorganisms in Japan that contribute to the maintenance of human health. Although the beneficial effects of some probiotics on ulcer healing have been demonstrated, there have been no reports on the wound healing effects of [...] Read more.

“Koji” is one of the most well-known probiotic microorganisms in Japan that contribute to the maintenance of human health. Although the beneficial effects of some probiotics on ulcer healing have been demonstrated, there have been no reports on the wound healing effects of koji to date. In the present study, we investigated the effects of “cha-koji”, green tea leaves fermented with Aspergillus luchuensis, on cutaneous wound healing, using a linear incision wound mouse model. Topical application of autoclave-sterilized cha-koji suspension on the dorsal incision wound area healed the wound significantly faster and, notably, with less scarring than did the green tea or the control distilled water treatment. Further in vitro experiments revealed that the accelerated effects of cha-koji could be attributed to its increased anti-bacterial activity, enhanced epidermal cell proliferation and migration, augmented expression of the anti-inflammatory cytokine transforming growth factor-β1, reduced expression of inflammatory cytokine interleukin-6 in macrophages, and decreased endoplasmic reticulum stress. In addition, we conducted a skin sensitizing potential test, which revealed that cha-koji had no adverse effects that posed a sensitizing risk. Thus, cha-koji may have a potent therapeutic effect on cutaneous wound healing, opening up a new avenue for its clinical application as a medical aid. Full article

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17 pages, 5123 KiB

Open AccessCommunication

Advances in the Production of PBCA Microparticles Using a Micromixer with HH-Geometry in a Microfluidic System

by Aline Rocha Vieira, Aline Furtado Oliveira, Fabiana Vieira Lima Solino Pessoa, Beatriz Nogueira Messias de Miranda and André Rolim Baby

Sci. Pharm. 2024, 92(3), 43; https://doi.org/10.3390/scipharm92030043 - 9 Aug 2024

Abstract

Different reaction control methods for producing nano/microstructures of poly(butyl cyanoacrylate) (PBCA) have been studied, focusing on pH and monomer-to-initiator ratios. However, these methods often require multiple steps and reagents. In the synthesis of PBCA microparticles using three versions of micromixers designed with HH [...] Read more.

Different reaction control methods for producing nano/microstructures of poly(butyl cyanoacrylate) (PBCA) have been studied, focusing on pH and monomer-to-initiator ratios. However, these methods often require multiple steps and reagents. In the synthesis of PBCA microparticles using three versions of micromixers designed with HH geometry and varying numbers of channels (4, 10, and 15), different synthesis formulations were investigated by varying monomer concentrations. PBCA microparticles synthesized with 19.2% (w/w) n-butyl cyanoacrylate (n-BCA) monomer, a residence time of 0.06 s, a flow rate of 78 mL·min⁻¹, and a phase ratio of 45/55 (W/O), exhibited an average diameter of 642.2 nm as determined by dynamic light scattering (DLS) analysis. In contrast, PBCA microparticles synthesized with 5.0% (w/w) n-BCA monomer, the same residence time of 0.06 s, a flow rate of 39 mL·min⁻¹, and a phase ratio of 20/80 (W/O), exhibited an average diameter of 74.73 µm according to laser diffraction particle size analysis. Polymer formation was confirmed by Fourier-transform infrared (FTIR) spectroscopy in both formulation and process conditions. These results indicate that the parameters for the production of microparticles with different monomer concentrations in the microfluidic system with HH geometry and 15 channels can be optimized for potential applications in cosmetics and pharmaceutical ingredients. Full article

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17 pages, 489 KiB

Open AccessArticle

Phytochemical Profiling and Biological Activities of Two Helianthemum Species Growing in Greece

by Evgenia Panou, Konstantia Graikou, Nikolaos Tsafantakis, Fanourios-Nikolaos Sakellarakis and Ioanna Chinou

Sci. Pharm. 2024, 92(3), 42; https://doi.org/10.3390/scipharm92030042 - 8 Aug 2024

Abstract

Helianthemum nummularium (HN) and Helianthemum oelanticum subsp. incanum (HO) are plant species, among Cistaceae, that are highly distributed in the Mediterranean region. In the current study, extracts of the aerial parts from both species have been analyzed phytochemically. The non-polar extract analysis resulted [...] Read more.

Helianthemum nummularium (HN) and Helianthemum oelanticum subsp. incanum (HO) are plant species, among Cistaceae, that are highly distributed in the Mediterranean region. In the current study, extracts of the aerial parts from both species have been analyzed phytochemically. The non-polar extract analysis resulted in the identification of 15 compounds in each species, mainly terpene and fatty acid derivatives, through GC–MS. The methanolic extract analysis, conducted through UHPLC–MS/MS, led to the identification of 39 metabolites in HN and 29 in HO, respectively, the majority of which were phenolics. Among the identified compounds, several have also been isolated and structurally determined (from HN: rutin, linoleic acid, gallic acid, and isoquercetin, and from HO: quercetin-3-O-(2″-O-galloyl)-galactopyranoside, methyl gallate, catechin-3-O-glucopyranoside, and astragalin, while hyperoside, and cis- and trans-tiliroside have been determined in both species). Furthermore, the methanolic extracts of HN and HO displayed a high total phenolic content (177.2 mg GA/g extract and 150.6 mg GA/g extract, respectively) and considerable free-radical scavenging activity against the DPPH radical (94.6% and 94.0% DPPH inhibition, respectively). Antimicrobial testing showed stronger inhibition of HN against Gram (+) bacterial strains (MIC values 0.07–0.15 mg/mL), while both extracts exhibited low tyrosinase-inhibitory activity. Considering the lack of studies conducted on the chemistry and biological activities of the genus Helianthemum, the chemical characterization of extracts could contribute to new sources of bioactive metabolites to be explored and exploited for further potential applications such as food and/ or the cosmetic industry. Full article

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21 pages, 3404 KiB

Open AccessArticle

Antibacterial and Wound Healing Activity In Vitro of Individual and Combined Extracts of Tagetes nelsonii Greenm, Agave americana and Aloe vera

by Karen Alejandra Olán-Jiménez, Rosa Isela Cruz-Rodríguez, Beatriz del Carmen Couder-García, Nadia Jacobo-Herrera, Nancy Ruiz-Lau, Maritza del Carmen Hernández-Cruz and Víctor Manuel Ruíz-Valdiviezo

Sci. Pharm. 2024, 92(3), 41; https://doi.org/10.3390/scipharm92030041 - 31 Jul 2024

Abstract

Currently, there are various physical and mechanical agents that can cause skin wounds, which are still traditionally treated with plant extracts. It has been reported that the genus Tagetes has a wide range of biological properties, including antibacterial and wound healing activity. Likewise, [...] Read more.

Currently, there are various physical and mechanical agents that can cause skin wounds, which are still traditionally treated with plant extracts. It has been reported that the genus Tagetes has a wide range of biological properties, including antibacterial and wound healing activity. Likewise, Agave americana extract and Aloe vera gel have shown potential in the treatment of burn wounds and other skin conditions both in vitro and in vivo. In this study, the antibacterial and wound healing activities of each of these plants were investigated, as well as the possibility of enhancing these activities by combining them. First, the secondary metabolites of the extracts were quantified, the antibacterial activity was evaluated using the Kirby-Bauer method, and their cytotoxicity was measured in 3T3 and HaCaT cells using the sulforhodamine B assay. The results revealed that Tagetes nelsonii extract had a higher amount of secondary metabolites, which is why it exhibited antibacterial activity. Finally, the scratch assay showed that the individual extracts of T. nelsonii and A. americana demonstrated greater cell migration and proliferation starting from 12 h, as well as when using the combination of A. americana extract and A. vera gel, which almost completely closed the wound compared to the control. Full article

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