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Fomentariol, a Fomes fomentarius Compound, Exhibits Anti-Diabetic Effects in Fungal Material: An In Vitro Analysis
Get PDFThe present study screened various fungal species for inhibitors of alpha-glucosidase, alpha-amylase, and DPP-4, enzymes that are crucial in carbohydrate metabolism. Ethanolic extracts exhibited superior inhibitory activity compared to water extracts, suggesting their potential as sources of anti-diabetic agents. Further fractionation revealed fomentariol from Fomes fomentarius as a potent inhibitor of alpha-glucosidase and DPP-4, with higher activity against alpha glucosidase than acarbose. Fomentariol presents a novel avenue for diabetes management, demonstrating the simultaneous inhibition of key enzymes in glucose metabolism. However, comprehensive clinical studies are needed to evaluate its safety and efficacy in humans
σ2 receptor modulation has no effect on binge eating and anxiety and reduces locomotion in a rat chronic stress model
No full textThis study aimed to investigate the effects of a novel pyrazoloquinolinone ligand (CW-02-79), which has selectivity in binding to σ2-receptors, on locomotion, anxiety and feeding behavior in rats following low-grade inflammation and chronic stress exposureRelated to poster: [https://farfar.pharmacy.bg.ac.rs/handle/123456789/5789
Geraniol in vitro and geraniol-based emulsion ex vivo potential against four-species Streptococcus spp. biofilm relevant for dentistry
No full textObjective: Concerning the importance of developing novel oral hygiene adjuncts, the aim of this study was to screen antibacterial/antibiofilm potential of geraniol and to formulate its stable nanoemulsion(s), capable to combat caries-related streptococcal multispecies biofilm. Materials and methods: Antibacterial and antibiofilm activities of geraniol were estimated in microdilution and crystal-violet assays, respectively. Five geraniol-based emulsions with Tween80 were formulated and screened for particle size diameter and stability, using dynamic light scattering measurements. The selected emulsion was characterized by TEM, and ex vivo screened against four-species biofilm settled on enamel discs, by determination of CFU. Results: The antibacterial potential of geraniol was moderate (MICs 0.55–1.11 mg/mL against S. mutans, S. sanguinis, S. gordonii and S. mutans). Geraniol significantly prevented biofilm formation and disrupted pre-formed ones (inhibition ranges against all isolates were 12.00–93.66 %, and 55.54–100 %, respectively). Emulsions (Eger:tween80) E200:200, E500:500, and E800:800 were stable and nanosized (Zavg˂200 nm). TEM of E800:800 revealed black spherical spots surrounded by grey stain. Ex vivo four-species streptococcal biofilm disruption assay showed notable inhibitory potential of E800:800 (ΔLogCFU 1.77 and 3.89, solely and in combination with chlorhexidine, respectively). Conclusion: E800:800 showed ex vivo potential against streptococcal multispecies biofilm, especially in combination with chlorhexidine. Clinical Significance: Presented results encourage further research of the examined nanoemulsions as potential part of daily oral hygiene, aiming to provide prevention of caries development
Filmovi i film-formirajući sistemi na bazi hipromeloze za topikalnu primenu: trenutni značaj i perspektiva u isporuci lekovitih supstanci
No full textFilms and film-forming systems (FFS) are increasingly recognized for their potential as
convenient carriers for precise and efficient drug delivery to or via the skin and mucous
membranes. Among them, those based on hypromellose as a film-forming polymer demonstrate
many favorable characteristics. To better understand the role of hypromellose in topical films and
film-forming drug delivery systems, this review presents physicochemical characteristics and
film-forming performances of different types of hypromellose. Furthermore, the review
encompasses relevant studies demonstrating the broad application of hypromellose as a film-
forming agent in films and FFS for dermal, oromucosal, vaginal, ocular, and nasal application,
reflecting the growing interest of researchers in this field. It also highlights the observed
advantages of hypromellose over other film-forming polymers and implies future development of
films and FFS in general.Filmovi i film-formirajući sistemi (FFS) sve više se ističu kao pogodni nosači za preciznu
i efikasnu isporuku aktivnih supstanci na ili preko kože i sluzokože. Među njima, oni koji sadrže
hipromelozu kao film-formirajući polimer pokazuju mnoge povoljne karakteristike. Kako bi se
bolje razumela uloga hipromeloze u filmovima i FFS za topikalnu primenu, ovaj pregled prikazuje
fizičko-hemijske karakteristike i sposobnost formiranja filmova različitih tipova hipromeloze. U
nastavku, pregled obuhvata relevantne studije koje prikazuju široku primenu hipromeloze kao
sredstva za formiranje filma u filmovima i FFS za dermalnu, oromukozalnu, vaginalnu, okularnu
i nazalnu primenu, odražavajući rastući interes istraživača u ovoj oblasti. Takođe, naglašava
prednosti hipromeloze u poređenju sa drugim film-formirajućim polimerima, kao i potencijal za
celokupan budući razvoj filmova i FFS
Exploring liver function effects of sulforaphane in rats: dose-dependent and sex-specific variations
No full textSulforaphane (SFN), an isothiocyanate compound, is renowned for its
significant health effects, particularly as an adjunct in chemotherapy.
Despite its promising potential, comprehensive safety data regarding
its synthesized form remain limited. Thus, this study sought to assess
the hepatotoxic effects of SFN in rats following subacute exposure to
three progressively escalating dose levels. The animals were divided
into 8 groups, each consisting of 5 rats: 2 control groups (1 male and
1 female) and 6 treated groups (3 male (SFN 1 M, SFN 2 M, SFN 3 M)
and 3 female (SFN 1 F, SFN 2 F, SFN 3 F)). The treated rats received subacute oral SFN administration at doses of 0.5, 2, and 5 mg/kg bw/
day for 28 days. The investigation included the determination of biochemical parameters in blood and inflammatory and antioxidant mediators in liver tissue homogenates. In female rats, no statistically
significant differences in liver function-related biochemical parameters
was observed. Yet, there was a slight, but non-significant rise in aspartate aminotransferase (AST) activity in the SFN 1 F group compared
to the control. Subsequent to this rise at the lowest dose, a decrease in
activity was noted in the SFN 2 F and SFN 3 F groups, while a similar
trend was noted in alanine aminotransferase (ALT) enzyme activity.
On the other hand, a statistically significant increase in albumin quantity was observed in the SFN 2 M and SFN 3 M groups compared to the
control. Analysis of heme oxygenase-1 (HO-1), nuclear factor erythroid
2-related factor 2 (Nrf2), and tumor necrosis factor alpha (TNFα) levels
revealed notable changes. In female rats, a significant increase in HO-1
quantity was observed in the SFN 2 F and SFN 3 F group compared to
the control. Additionally, SFN 3 F group exhibited significantly higher
Nrf2 levels compared to the control. Both SFN 2 F and SFN 3 F groups
showed a significant increase in TNFα compared to the control, with
the highest dose group demonstrating the most significant change. In
male rats, a statistically significant increase in HO-1 quantity was observed in the SFN 1 M group compared to the control. Furthermore,
the SFN 3 M group displayed a statistically significant increase in TNFα
quantity compared to the control. The rise in HO-1 and Nrf2 levels
noted in this study suggests activated antioxidant mechanisms in response to inflammation, indicating an adaptive response to mitigate
oxidative stress. In conclusion, the observed influence of SFN on liver
enzyme activity, inflammatory markers, and antioxidant responses,
indicating potential dose-dependent effects and sex-specific variations,
underscores the necessity for further exploration of its safety profile.Abstracts of the 58th Congress of the European Societies of Toxicology (EUROTOX 2024), "Toxicology – A Quest for safe Chemicals and Medicines.", 8-11 September 2024 • Copenhagen, Denmar
The relationship among essential oil composition, morphological and climatic diversification - the case of Teucrium montanum from the Balkan Peninsula
No full textTeucrium montanum L. (Lamiaceae) is a small, evergreen, semi-woody shrub that has a wide ecological
preference and grows in various environments. The Balkan Peninsula is characterized by a complex geological
history and very heterogeneous climatic conditions in a relatively small area. Teucrium montanum shows high
morphological and anatomical variability in the Balkan Peninsula and seven morphological groups have been
recognized (Zbiljić et al., 2023). The aim of our work was to determine whether the phytochemical variability
of essential oils follows morphological diversification and to determine the influence of climatic conditions.
Isolated essential oils from 46 populations were analysed by GC/FID/MS and multivariate statistical
analysis. The main compounds in the investigated oils were: sesquiterpenes germacrene D-4-ol, shyobunol,
cis- sesquiterpene hydrate, α-bisabolol, germacrene D and monoterpene limonene. Principal component
analysis (PCA) showed significant chemical variability in the analysed samples, with the morphological
group “montanum” showing the greatest changes, similar to the pronounced morphological variations of
this group. In addition, there were specific compounds for the morphological groups that led to a clear
separation in the discriminant analysis (CDA). Certain morphological groups (“parnassicum”, “skadarensis”
and “pannonicum”) can be easily distinguished according to both phytochemical and morphological
characteristics. The biosynthesis of various compounds was influenced by the climatic conditions. The lack
of water caused the increase of limonene content in the population influenced by arid continental climate
and of cryptomerione and (E)-nerolidol affected by arid submediterranean climate. However, it was found
that phytochemical diversification followed morphological rather than climatic variability
Composition of Essential Oils from Fruits of Peucedanum longifolium and Rhizomatophora aegopodioides (Apiaceae) with Regard to Other Related Taxa—A Chemometric Approach
Get PDFThe aim of this work was to investigate the composition of essential oils isolated from fruits of Peucedanum longifolium, and Rhizomatophora aegopodioides (a species which was previously placed in the genus Peucedanum), as well as to compare the obtained results to those available for other previously investigated related species (including taxa which are also, according to some authors, excluded from the genus Peucedanum). Essential oils were obtained via hydrodistillation in a Clevenger-type apparatus and their composition was analyzed using GC-FID and GC-MS. To compare these data to those of previously investigated taxa, a chemometric approach was applied; the data were analyzed using multivariate statistical methods: non-metric multidimensional scaling (nMDS) and hierarchical cluster analysis. The most abundant in P. longifolium essential oil were monoterpenes (79.7%), mostly α-phellandrene (26.2%), β-phellandrene + limonene (21.0%) and myrcene (9.5%), followed by sesquiterpenes (18.3%), mostly germacrene B (9.5%). On the other hand, dominant in R. aegopodioides essential oil were non-terpenic aliphatic hydrocarbons (46.1%), mainly n-undecane (16.5%) and n-nonane (11.3%). In addition, this essential oil also contained a notable quantity of sesquiterpenes (25.1%), with (E)-sesquilavandulol being the most abundant (10.0%). The results of multivariate statistics revealed a clear separation of the essential oil composition of R. aegopodioides and P. longifolium, as well as of P. longifolium and P. officinale. The clustering of the samples of most of the taxa that do not belong to the Peucedanum in the narrow sense (sensu stricto) was also observed, which is in accordance with their recent inclusion in separate genera
Metal-induced autoimmunity in neurological disorders: A review of current understanding and future directions
No full textAutoimmunity is a multifaceted disorder influenced by both genetic and environmental factors, and metal exposure has been implicated as a potential catalyst, especially in autoimmune diseases affecting the central nervous system. Notably, metals like mercury, lead, and aluminum exhibit well-established neurotoxic effects, yet the precise mechanisms by which they elicit autoimmune responses in susceptible individuals remain unclear. Recent studies propose that metal-induced autoimmunity may arise from direct toxic effects on immune cells and tissues, coupled with indirect impacts on the gut microbiome and the blood-brain barrier. These effects can activate self-reactive T cells, prompting the production of autoantibodies, inflammatory responses, and tissue damage. Diagnosing metal-induced autoimmunity proves challenging due to nonspecific symptoms and a lack of reliable biomarkers. Treatment typically involves chelation therapy to eliminate excess metals and immunomodulatory agents to suppress autoimmune responses. Prevention strategies include lifestyle adjustments to reduce metal exposure and avoiding occupational and environmental risks. Prognosis is generally favorable with proper treatment; however, untreated cases may lead to autoimmune disorder progression and irreversible organ damage, particularly in the brain. Future research aims to identify genetic and environmental risk factors, enhance diagnostic precision, and explore novel treatment approaches for improved prevention and management of this intricate and debilitating disease
Rapid Reversed-Phase High-Performance Liquid Chromatography Profiling of Serotonin Receptor Ligands and their Related Compounds
No full textAbstract: The retention profile of six serotonin receptor ligands such as arylpiperazines (aripiprazole, ziprasidone, risperidone), and benzothiazepine derivatives (olanzapine, mianserin, quetiapine), was investigated on C8 alkyl and pentafluorophenylpropyl stationary phases. The experimental design methodology was used to define their retention behavior and achieve acceptable separation results. Both phases showed satisfactory selectivity for all compounds. The optimal separation among the structurally related arylpiperazines and benzothiazepines was found with the C8 phase at 25°C, using acetonitrile (40%, v/v) and 20 mM ammonium acetate as a mobile phase modifier. The selectivity and sensitivity performances of the selected C8 system were discussed considering the separation of aripiprazole and its related compounds. In addition, the specified conditions were validated for determining aripiprazole in pharmaceutical dosage forms. The developed reversed-phase high-performance liquid chromatography method can be successfully used for the rapid chromatographic profiling of serotonin receptor ligands and related analogs, providing increased selectivity during pharmaceutical analysis
Evaluation of novel compounds as anti-bacterial or anti-virulence agents
Get PDFAntimicrobial resistance is a global threat, leading to an alarming increase in the prevalence of bacterial infections that can no longer be treated with available antibiotics. The World Health Organization estimates that by 2050 up to 10 million deaths per year could be associated with antimicrobial resistance, which would equal the annual number of cancer deaths worldwide. To overcome this emerging crisis, novel anti-bacterial compounds are urgently needed. There are two possible approaches in the fight against bacterial infections: a) targeting structures within bacterial cells, similar to existing antibiotics; and/or b) targeting virulence factors rather than bacterial growth. Here, for the first time, we provide a comprehensive overview of the key steps in the evaluation of potential new anti-bacterial and/or anti-virulence compounds. The methods described in this review include: a) in silico methods for the evaluation of novel compounds; b) anti-bacterial assays (MIC, MBC, Time-kill); b) anti-virulence assays (anti-biofilm, anti-quorum sensing, anti-adhesion); and c) evaluation of safety aspects (cytotoxicity assay and Ames test). Overall, we provide a detailed description of the methods that are an essential tool for chemists, computational chemists, microbiologists, and toxicologists in the evaluation of potential novel antimicrobial compounds. These methods are cost-effective and have high predictive value. They are widely used in preclinical studies to identify new molecular candidates, for further investigation in animal and human trials