Search Results (36)

To overcome the limitations of traditional motion sickness medications—slow onset of action, short duration of efficacy, and poor patient compliance—this study employed coaxial electrospinning technology. Poly(lactic acid) (PLA) and polyvinylpyrrolidone K90 (PVP K90) were used as composite carrier materials. The sheath layer is composed of highly hydrophilic PVP K90, loaded with the antihistamine diphenhydramine (DPH). The core layer, composed of biodegradable PLA with excellent sustained-release properties, carries the anticholinergic drug scopolamine hydrobromide (SH). This core–sheath nanostructured nanofiber sublingual film delivers dual anti-motion sickness drugs. A series of characterization tests revealed that the sublingual membrane exhibits a linear morphology with a distinct core–shell nanostructure. The drugs DPH and SH are distributed in an amorphous state within the sheath and core layers, respectively. Wetting performance tests indicate that the membrane’s wettability falls between those of monofilament membranes. In vitro drug release experiments revealed that DPH exhibited a “rapid onset + sustained release” biphasic profile, with cumulative release reaching 60% within 2 h and approaching complete release by 10 h, primarily via Fickian diffusion (n = 0.30). SH exhibited prolonged sustained release, approaching complete release at 12 h via non-Fickian diffusion (n = 0.55). Cytotoxicity and vital/necrotic staining experiments mutually corroborated that cell viability remained above 80%, further validating the safety and efficacy of PLA/PVP as a combined drug delivery carrier. This study provides a novel delivery system for motion sickness treatment, offering significant theoretical value and broad clinical application prospects. Full article

The increasing use of multiple medications among older adults raises concerns about potentially inappropriate medications (PIMs), which are associated with adverse health outcomes and increased healthcare costs. This study aimed to assess the prevalence and types of PIMs dispensed to older adults living in Northwest Italy using real-world pharmacy claims data. An observational, retrospective analysis was conducted on anonymized drug dispensing datasets from two local health authorities, covering individuals aged 65 years or older between 2018 and 2021. PIMs were identified according to the 2019 American Geriatrics Society Beers Criteria, focusing on drugs that are inappropriate or should be used with caution in older adults or have anticholinergic properties. Over half of older adults who received medications during the study period were dispensed at least one PIM, with stable or slight increased prevalence over time with no differences by sex or region. Proton-pump inhibitors used for more than 8 weeks and paroxetine were the most common PIMs, while furosemide and sulfonylureas were also frequently reported PIMs. These findings indicate a persistently high burden of inappropriate prescribing in older adults and highlight the need for coordinated deprescribing interventions and prescriber education to promote safer, evidence-based pharmacotherapy in aging populations. Full article

Actinidia arguta, also known as mini kiwi (due to its small size) or hardy kiwi (due to its frost resistance), is becoming an increasingly popular fruit alongside its commercially older siblings, i.e., A. deliciosa (green kiwi fruit) and A. chinensis (golden kiwifruit), from the Actinidiaceae family. This review paper discusses the biological and pharmacological properties of A. arguta fruits, with a special focus on methods of the bioactive component analysis. Mini kiwi is a valuable source of bioactive compounds, which contribute to its health-promoting properties, among others: antioxidant, neuroprotective, anticholinergic, antitumor, anti-inflammatory, antidiabetic, antiobesity as well as antiatherosclerotic ones. They are briefly discussed, illustrating the action of bioactive ingredients and the methods of analysis, which are presented in the tables. This review includes a concise characterization of A. arguta and updates the current field of knowledge about its diverse biological activities, which are undoubtedly related to the content of bioactive components and the methods used for their isolation and analysis. The information included in this review paper will be helpful in perceiving mini kiwi not only as a tasty fruit but also as a source of bioactive ingredients with beneficial, health-promoting effects on the body. Effective isolation of these components can contribute to the future development of antiaging and anticancer drugs, which undoubtedly will lead to further research and promote this species. Full article

Arctium lappa L., commonly known as burdock, is a biennial plant whose roots are a valuable source of bioactive phenolic compounds with notable health-promoting properties. However, the bioactivity of these compounds is influenced by both extraction parameters and plant growth conditions. This study investigated the combined effect of extraction temperature, land management, and cultivation altitude on the antioxidant and anticholinergic potential of burdock root extracts obtained through pressurized liquid extraction (PLE). Extractions were performed at 50 °C, 100 °C, and 150 °C, with 50 °C being the temperature that best preserved phenolic content and bioactivity. Remarkably, root extracts obtained at 50 °C and collected from an untreated organic field at 150 m altitude yielded higher phenolic levels (42 mg gallic acid/g extract) than conventional solid–liquid extraction (38 mg gallic acid/g extract). A comparative analysis of three ecotypes, including Organic Land Ecotype (OLE) and Spontaneous Land Ecotype (SPLE), both collected at 150 m altitude, and Spontaneous Mountain Ecotype (SPME), collected at 800 m (over sea level), revealed that a higher altitude significantly increased phenolic content and anticholinergic potential. Furthermore, roots from non-weeded soils exhibited superior bioactivity compared to those from weeded areas. These findings underline that the successful obtention of highly bioactive burdock root extracts depends not only on extraction conditions, but also critically on cultivation altitude and land management strategies. Full article

Fermentation processes, which occur under the influence of multiplying microorganisms, lead to the creation of products with beneficial health properties. Due to the growing interest of consumers in beverages with health-promoting properties, new raw materials and their processing methods are being intensively studied to obtain products with improved functional values. The purpose of the study is to determine the effect of fermentation using SCOBY (Symbiotic Culture of Bacteria and Yeast) on the chemical composition, polyphenolic profile, and biological activity of apple and pear juices. The fermentation process caused a decrease in the content of polyphenols in apple juice from 1568.8 to 1269.0 mg/L, while in pears, an increase was observed from 492.9 to 576.7 mg/L. Statistically significant changes were observed in the content of individual groups of polyphenolic compounds. The fermentation process also influenced the increase in the value of anti-inflammatory, antioxidant, antidiabetic, and anticholinergic activity. This indicates that fermentation can be an effective process in increasing the biological properties of fruit juices. This fact can be used in the prevention of lifestyle diseases and in the production of functional foods with targeted health-promoting properties. Full article

Background: Aging-related comorbidities such as cardiovascular disease and neurocognitive impairment are more common among people with HIV (PWH). Hypertension (HTN) has been implicated in cognitive decline, and antihypertensives with anticholinergic properties may exacerbate this decline. Our research probed the relationship between neurocognitive performance and antihypertensives in hypertensive PWH and in those without HIV (PWoH), examining whether increased antihypertensives followed the worsening in neurocognitive performance. Methods: This longitudinal analysis encompassed seven visits over five years, enrolled between 1999 and 2022. Participants were included if they reported HTN or used antihypertensives. All participants underwent comprehensive cognitive assessments, and their global cognitive performance was evaluated using summary, demographically corrected T-scores. The association between the global T-score and the number of antihypertensives was evaluated using generalized linear mixed-effects models. Summary regression-based change score (sRCS) was analyzed as an indicator of global performance over time. Results: Among 1158 hypertensive PWH (79.9% were on ART), worsening cognitive performance was associated with an increased number of antihypertensives (p = 0.012) but not in PWoH (p = 0.58). PWH had lower mean arterial pressure (MAP) than PWoH after adjusting for demographics (β = −5.05, p = 2.3 × 10⁻¹¹). In PWH, an association between mean arterial pressure (MAP) and sRCS suggested that those with cognitive improvement had lower MAP (p = 0.027). PWH taking more anticholinergics were more likely to have worse cognitive performance over time (p < 0.001). Conclusions: PWH with declining neurocognitive performance over time used increasing numbers of antihypertensives, suggesting that their providers prescribed more antihypertensives because of either treatment refractory HTN or poor adherence. Prescribers should avoid using antihypertensives with anticholinergic properties when possible. Full article

This study introduces a novel pressurized liquid extraction (PLE) strategy utilizing biobased solvents to simultaneously extract non-polar and polar compounds with antioxidant and anticholinergic properties from burdock roots. The influence of altitude and weeding on the bioactive composition of three burdock root ecotypes was evaluated: two from 150 m (one subjected to weeding during growth and another not subjected to weeding) and one from 800 m without weeding. A simplex-centroid mixture design identified 100% 2-methyltetrahydrofuran as the optimal solvent for PLE, offering superior extraction of bioactive compounds due to its ability to form strong hydrogen bonds with phenolic groups. Extraction at 100 °C was found to be optimal, avoiding the low yields and undesirable reactions observed at 40 °C and 160 °C, respectively. Altitude emerged as the most significant factor influencing bioactivity and composition, with roots from 800 m exhibiting the highest bioactivity. Key bioactive compounds included caffeoylquinic acids, caryophyllene oxide, spathulenol, and bisnorallocholanic acid. At 150 m, weeding reduced anticholinergic capacity but increased antioxidant synthesis, though the levels were lower than those observed at higher altitudes. These findings highlight that burdock roots grown at high altitudes without weeding produce extracts rich in antioxidant and neuroprotective compounds, offering significant potential for functional ingredient development. Full article

Multimorbidity and polypharmacy are prevalent among Long-Term Care (LTC) users. Older people, who most use LTC services, are more prone to drug-related problems, which polypharmacy aggravates. Deprescribing is a key intervention to address polypharmacy and inappropriate medication. Evidence shows that pharmacists’ expertise in medicines and their growing involvement in clinical-oriented activities have proven to play an essential role across many healthcare settings, including LTC. Thus, this study aimed to identify and assess LTC pharmacist-mediated deprescribing. A systematic review was undertaken following the PRISMA checklist, using three literature databases (PubMed, Scopus, and Web of Knowledge). A set of 18 keywords, divided into three domains (professional, type of care, and type of setting), were combined into search equations. The studies selected were assessed through the Quality Assessment Tool for Quantitative Studies. Fifteen studies met the inclusion criteria out of 288 initial hits. Pharmacist-mediated deprescribing was divided into specific (targeted to a medicine group) and non-specific. Half of the studies were graded as low quality (53%). In total, the studies enrolled 6928 patients and 45 pharmacists. The ATC groups A, C, M, and N, as well as medicines with anticholinergic properties, were the most addressed medicines groups. Acceptance rates of pharmacists’ recommendations ranged between 30% and 100%. Generically, the number of medicines was reduced after the intervention. Mixed results were found for falls and quality of life outcomes. Cost savings associated with the interventions ranged from neutral to as high as 3800 €/patient/year. Barriers to deprescribing were mainly linked to patients’ or family members’ refusal to change. In conclusion, pharmacist-mediated deprescribing seems feasible in LTC. The studies’ methodological heterogeneity hampers robust comparisons and conclusions. The medicine groups targeted by deprescribing can help tailor interventions to optimize the use of medicines in LTC. A detailed understanding of barriers and enablers to deprescribing would support developing and implementing these interventions. Full article

Atropa belladonna is a medicinal plant and an important source for the commercial production of tropane alkaloids (TAs), such as scopolamine and hyoscyamine, which are used clinically for their anticholinergic properties. In this study, we identified 16 metallocarboxypeptidase inhibitor (MCPI) genes from A. belladonna (AbMCPIs), which are grouped into three subgroups based on phylogenetic relationships and are distributed across 10 chromosomes. Promoter analysis showed that most cis-regulatory elements were related to defense and stress responses, such as drought, low-temperature, ABA (abscisic acid), GA (gibberellin), auxin, light and MeJA responsiveness. A gene encoding a putative metallocarboxypeptidase inhibitor (AbMCPI8) is cloned from A. belladonna and characterized. AbMCPI8 shows similar tissue expression pattern to TA biosynthesis genes such as AbPMT, AbAT4, AbTRI, etc., with exclusive expression in the roots. When AbMCPI8 is silenced by virus-induced gene silencing (VIGS), the root growth is markedly inhibited and the production of hyoscyamine and scopolamine is significantly reduced. Our findings indicate a positive role of AbMCPI8 in root development, which could positively affect TA production in A. belladonna. Full article

Propolis is very significant in terms of its phytochemical content and biological activity among bee products. In this study, the antioxidant activities (total phenolic and flavonoid, Fe³⁺, Cu²⁺ (CUPRAC), Fe³⁺-TPTZ (FRAP) reducing, and DPPH^•, ABTS^•+ scavenging assays) of propolis collected from the Bitlis province of Türkiye were determined. In addition, the carbonic anhydrase I and II isoenzymes (hCA I and hCA II), α-glycosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) inhibition activity and phytochemical profile of propolis and mineral content were determined by LC-MS/MS and ICP-MS, respectively. In propolis, 31 phytochemicals were found, and the highest concentration of acacetin (23.604 mg/g) was detected. It is seen that the phytochemicals in propolis provide antioxidant properties. The mineral content was screened for 18 elements and determined to be rich in the elements that make up the salt content. Total phenolic content was 215.14 mg GAE/g, and total flavonoid content was 79.11 mg QE/g. The Fe³⁺ reduction result was 0.940 (µg/mL), CUPRAC 1.183 (µg/mL), FRAP 0.963 (µg/mL), DPPH^• scavenging IC₅₀: 16.7 (µg/mL), and ABTS IC₅₀: 8.01 (µg/mL). hCA I enzyme inhibition results in IC₅₀: 7.19 (µg/mL), hCA II 8.15, AChE 5.17, BChE 7.50, and α-Glycosidase 5.72. As a result of this study, it was determined that Bitlis propolis has high antioxidant properties and a rich phytochemical content. It was also observed that it is an effective enzyme inhibitor against epilepsy, glaucoma, Alzheimer’s, and diabetes, which are important diseases, and it can be evaluated in the treatment of these diseases and drug production. Full article

Fenpiverinium is an agent which, from a medical perspective, has anticholinergic and antispasmodic properties, with applications in the treatment of smooth muscle spasm. The crystal and molecular structures of two fenpiverinium-based crystals, namely fenpiverinium bromide and fenpiverinium bromide hemihydrate, were elucidated and explored by single-crystal X-ray diffraction. Full article

Background: Plants have long been recognized for their potential to influence neurological health, with both neuroprotective and neurotoxic properties. This review explores the dual nature of plant-derived compounds and their impact on the human brain. Discussion: Numerous studies have highlighted the neuroprotective effects of various phytoconstituents, such as those found in Ginkgo biloba, Centella asiatica, Panax ginseng, Withania somnifera, and Curcuma longa. The neuroprotective compounds have demonstrated antioxidant, anti-inflammatory, and cognitive-enhancing properties, making them promising candidates for combating neurodegenerative diseases and improving brain function. Polyphenolic compounds, triterpenic acids, and specific phytocompounds like the ones from EGb 761 extract have shown interactions with key enzymes and receptors in the brain, leading to neuroprotective outcomes. However, this review also acknowledges the neurotoxic potential of certain plants, such as the Veratrum species, which contains steroidal alkaloids that can cause DNA damage and disrupt neurological function, or Atropa belladonna, which interfere with the normal functioning of the cholinergic system in the body, leading to a range of symptoms associated with anticholinergic toxicity. Conslusions: This review also emphasizes the need for further research to elucidate the complex mechanisms underlying the neuroprotective and neurotoxic effects of plant-derived compounds, as well as to identify novel phytoconstituents with therapeutic potential. Understanding the complex relationship between plants and the human brain is crucial for harnessing the benefits of neuroprotective compounds while mitigating the risks associated with neurotoxic substances. This review provides a comprehensive overview of the knowledge on the neurological properties of plants and highlights the importance of continued research in this field for the development of novel therapeutic strategies targeting brain health and neurological disorders. Full article

Increasing demand for functional beverages is attracting consumers’ attention and driving research to expand our knowledge of fermentation using symbiotic culture of bacteria and yeast (SCOBY) and demonstrate the health effects of consuming kombucha. The objective of this study was to develop innovative recipes for unpasteurized mint/nettle kombucha analogs, and to compare the products obtained under varying conditions in terms of chemical composition, bioactive polyphenols and health-promoting activity. Four variants of kombucha beverages (K1–K4), differing in the addition of sucrose and fermentation temperature, were formulated. The fermentation process provided data indicating the increase of antidiabetic, anti-inflammatory and anticholinergic properties, while a decrease in antioxidant capacity was observed. The content of polyphenolics was the highest on the seventh day of fermentation. A higher fermentation temperature and a larger amount of sucrose accelerated the fermentation process, which may be crucial for shortening the production time of kombucha drinks. Full article

Since its first approval by the Food and Drug Administration in 1989 for strabismus, botulinum toxin indications of use have been widely expanded. Due to its anticholinergic properties, this toxin is currently approved in adult patients for the treatment of a wide range of neuromuscular, otolaryngologic, orthopedic, gastrointestinal, and urologic disorders. Approved pediatric indications of use include the treatment of blepharospasm associated with dystonia, strabismus, lower-limb spasticity, focal spasticity in patients with cerebral palsy, and neurogenic detrusor overactivity. Alongside these approved indications, botulinum toxin is extensively used off-label. Although several clinical studies have shown that botulinum toxin is effective and well-tolerated in children, uncertainties persist regarding its long-term effects on growth and appropriate dosing in this population. As such, further research is needed to better define the botulinum toxin risk–benefit profile and expand approved uses in pediatrics. This narrative review aimed to provide a broad overview of the evidence concerning the clinical effectiveness and safety of BoNT with respect to its principal authorized and non-authorized pediatric therapeutic indications, as well as to describe perspectives on its future use in children. Full article

Scopolamine and atropine are two medicinal alkaloids derived from Datura stramonium L. with anticholinergic properties. This study explored how methyl jasmonate (MJ), a plant growth regulator, affects the biosynthesis and accumulation of these alkaloids in different plant tissues. The expression levels of putrescine N-methyltransferase (PMT), tropinone reductase I (TR1), and hyoscyamine 6β-hydroxylase (h6h), three critical enzymes in the biosynthetic pathway, were also analyzed. The results indicated that MJ at 150 µM increased the production of scopolamine and atropine in both leaves and roots, while MJ at 300 µM had an adverse effect. Furthermore, MJ enhanced the expression of PMT, TR1, and h6h genes in the roots, the primary site of alkaloid synthesis, but not in the leaves, the primary site of alkaloid storage. These results imply that MJ can be applied to regulate the biosynthesis and accumulation of scopolamine and atropine in D. stramonium, thereby improving their production efficiency. Full article