37 research outputs found
Telemedicine in inflammatory bowel disease from its origin to the post pandemic golden age: A narrative review
: Inflammatory bowel disease (IBD), a chronic intestinal inflammatory disorder encompassing ulcerative colitis and Crohn's disease can be disabling and often requires lifelong treatment and follow-up. Digital health technologies and distance-management tools are less costly alternatives for IBD management and clinical monitoring. This review discusses how telephone/videoconference appointments enable treatment optimization from an early disease stage, provide complementary value-based patient care and educational resources, and allow consistent follow-up with a high standard of care. Replacing/supplementing traditional clinical consultations with telemedicine reduces healthcare utilization costs and the need for in-person consultations. The COVID-19 pandemic has accelerated the evolution of telemedicine in IBD, with several studies conducted since 2020 reporting high levels of patient satisfaction. Home-based injectable formulations coupled with telemedicine may become permanently embedded in healthcare systems in the post-pandemic period. While telemedicine consultations are well-accepted by many patients with IBD, they do not suit all patients or are not preferred (e.g., by elderly who do not have the means or ability to understand the associated technology). Ultimately, use of telemedicine should be decided by the patient and careful consideration is required to ensure that the patient is willing and capable of a successful remote visit
Corrigendum to "Telemedicine in inflammatory bowel disease from its origin to the post pandemic golden age: A narrative review" [Digestive and Liver Disease, Volume 56, Issue 1, January 2024, Pages 1-6]
Pistacia lentiscus: phytochemistry and anti-diabetic properties
Pistacia lentiscus L. (P. lentiscus) is an evergreen shrub (Anacardiaceae family) primarily found in the Mediterranean region. The plant has been thoroughly characterized, resulting in a high concentration of bioactive compounds as flavonoids and phenolics. Moreover, P. lentiscus was revealed to possess a great nutritional and industrial importance because of its variety of biological activities, including antibacterial, anti-inflammatory, anti-atherogenic and antioxidant properties. Many of its beneficial health properties and applications date back to antiquity, and the European Medicines Agency officially acknowledged it as an herbal medicinal product. Indeed, it is widely employed in conventional medicine to treat several diseases, including type 2 diabetes (T2D). On this basis, this review aims to summarize and describe the chemical composition of different parts of the plant and highlight the potential of P. lentiscus, focusing on its antidiabetic activities. The plant kingdom is drawing increasing attention because of its complexity of natural molecules in the research of novel bioactive compounds for drug development. In this context, P. lentiscus demonstrated several in vitro and in vivo antidiabetic effects, acting upon many therapeutic T2D targets. Therefore, the information available in this review highlighted the multitarget effects of P. lentiscus and its great potential in T2D treatment
Butyrylcholinesterase Inhibitors: Structure-Activity Relationships of 2-Phenylbenzofuran derivatives.
Butyrylcholinesterase Inhibitors: Structure-Activity
Relationships of 2-Phenylbenzofuran derivatives
Antonella Fais1*, Giovanna L. Delogu 1, Benedetta Era 1, Amalia Di Petrillo1,
Amit Kumar2,3, Paola Caria4, Sonia Floris1, Francesca Pintus1
1Department of Life and Environmental Sciences, University of Cagliari , Cagliari , Italy;
2Department of Mech., Chem. and Material Engineering , University of Cagliari , Cagliari , Italy;
3Biosciences Sector, CRS4 ,Pula , Italy
4Department of Biomedical Sciences, University of Cagliari, Cagliari, Italy
*Corresponding author: [email protected]
Alzheimer’s disease (AD) is an irreversible and progressive brain disorder which is characterized by
progressive memory loss and a wide range of cognitive impairments.1 Although the precise cause of AD is
not completely known, there are some factors that seem to play a significant role in the pathogenesis of AD.
Since AD is characterized by a forebrain cholinergic neuron loss and a progressive decline in acetylcholine, a
possible therapeutic strategy involves the use of cholinesterase (ChE) inhibitors to restore the
neurotransmitter level and thus alleviate AD symptoms.2
Benzofuran scaffold has drawn considerable attention over the last few years due to its profound
physiological and chemotherapeutic properties. Recent studies have also investigated their inhibitory activity
towards ChEs.3,4
In this study, a series of 2-phenylbezonfurans compounds were synthesized and their inhibition
activity towards the ChE enzymes were investigated. We further combined biochemical analysis and
molecular modelling studies to identify selective butyrylcholinesterase (BChE) inhibition by benzofuran
scaffold. In particular, two compounds exhibited the highest BChE inhibition with IC50 values better than the
standard cholinesterase inhibitor compound. Molecular modelling studies highlighted the importance of
catalytic and peripheral site residues in BChE inhibition. Subsequently, the biosafety of the two promising
compounds was evaluated, in NSC-34 cells at the concentration in which BChE activity is inhibited, and no
considerable cytotoxic effect was found.
References
1. Schuster et al. Bioorg. Med. Chem. (2010) 18, 5071.
2. Zemek et al. Expert Opin Drug Saf (2014) 13, 759.
3. Mostofi et al. Eur. J. Med. Chem. (2015) 103, 361.
4. Delogu et al. Bioorg. Med. Chem. (2016) 26, 2308
GPR120/FFAR4: A Potential New Therapeutic Target for Inflammatory Bowel Disease
Inflammatory bowel disease, whose major forms are Crohn's disease and ulcerative colitis, is characterized by chronic inflammation of the gut due to the loss of tolerance toward antigens normally contained in the gut lumen. G protein-coupled receptor (GPR) 120 has gained considerable attention as a potential therapeutic target for metabolic disorders due to its implication in the production of the incretin hormone glucagon-like peptide 1 and the secretion of cholecystokinin. Recent studies have also highlighted the role of GPR120 in regulating immune system activity and inflammation. GPR120, expressed by intestinal epithelial cells, proinflammatory macrophages, enteroendocrine L cells, and CD4(+) T cells, suppresses proinflammatory and enhances anti-inflammatory cytokine production, suggesting that GPR120 might have a pivotal role in intestinal inflammation and represent a possible therapeutic target in inflammatory bowel disease. This narrative review aims at summarizing the role of GPR120 in the maintenance of intestinal homeostasis through the analysis of the most recent studies
Interplay Between Depression and Inflammatory Bowel Disease: Shared Pathogenetic Mechanisms and Reciprocal Therapeutic Impacts-A Comprehensive Review
Inflammatory bowel disease (IBD) is characterized by chronic inflammation of the gastrointestinal tract. Although the aetiology of IBD remains largely unknown, several studies suggest that an individual’s genetic susceptibility, external environmental factors, intestinal microbial flora, and immune responses are all factors involved in and functionally linked to the pathogenesis of IBD. Beyond the gastrointestinal manifestations, IBD patients frequently suffer from psychiatric comorbidities, particularly depression and anxiety. It remains unclear whether these disorders arise solely from reduced quality of life or whether they share overlapping biological mechanisms with IBD. This review aims to explore the bidirectional relationship between IBD and depressive disorders (DDs), with a focus on four key shared mechanisms: immune dysregulation, genetic susceptibility, alterations in gut microbiota composition, and dysfunction of the hypothalamic–pituitary–adrenal (HPA) axis. By examining recent literature, we highlight how these interconnected systems may contribute to both intestinal inflammation and mood disturbances. Furthermore, we discuss the reciprocal pharmacologic interactions between IBD and DDs: treatments for IBD, such as TNF-alpha and integrin inhibitors, have demonstrated effects on mood and anxiety symptoms, while certain antidepressants appear to exert independent anti-inflammatory properties, potentially reducing the risk or severity of IBD. Overall, this review underscores the need for a multidisciplinary approach to the care of IBD patients, integrating psychological and gastroenterological assessment. A better understanding of the shared pathophysiology may help refine therapeutic strategies and support the development of personalized, gut–brain-targeted interventions
Evaluation of antioxidant activities and tyrosinase inhibitory property of Sarcopoterium spinosum extracts.
Natural and Synthetic Sources as Antioxidant and Inhibitors of Tyrosinase
Melanogenesis is a physiological pathway for the formation of melanin, a pigment which plays an important role in the protection against UV damage and represents an important defense system of the skin against harmful factors.
Overproduction and accumulation of melanin occur in several skin disorders including solar melanosis, ephelides, melasma, senile lentigos and postinflammatory hyperpigmentation. Since tyrosinase is the limiting step enzyme in melanogenesis, its inhibitors have become increasingly important as depigmenting agents in hyperpigmentation disorders.
Since (or considering that) many known whitening agents have been proven to be toxic, there has been increasing impetus to identify alternative tyrosinase inhibitors, especially from natural sources. In this thesis has been investigated the inhibitory activity on tyrosinase of different natural extracts (Asphodelus. microcarpus, Sarcopoterium spinosum, Phytolacca dioica and several honeys) and of synthetic heteroarylcoumarins. It has been also evaluated the antioxidant activity and the citotoxicity of several compounds and extracts.
The results showed that all extracts have a direct inhibitory anti-tyrosinase activity with flowers ethanol extract of Asphodelus microcarpus and ethylacetate extract of Phytolacca dioica exhibiting the stronger effect. The same extracts showed the highest antioxidant activity and an elevated levels of total phenolics and flavonoid content.
As for the neo-synthesized compounds, two of them have shown inhibitory activity on tyrosinase even on B16F10 cells. These results encourage the the further deepening of research both on synthetic compounds derived from coumarins and on the extracts, that could be a good source of bioactive compounds useful as depigmenting agents in skin disorders
Tyrosinase inhibition and antioxidant properties of Asphodelus microcarpus extracts
Asphodelus microcarpus belongs to the family Liliaceae that include several medicinal plants. In the traditional medicine plants of the genus Asphodelus are used to treat skin disorders such as ectodermal parasites, psoriasis, microbial infection and for lightening freckles. In order to find novel skin depigmenting agents, the present work was carry out to evaluate antioxidant activity and tyrosinase inhibitory potential of leaves, flowers and tubers extracts of A. microcarpus. The phytochemical composition of the active extract was also evaluated
Exploring Asphodelus microcarpus as a source of xanthine oxidase inhibitors: Insights from in silico and in vitro studies
Xanthine oxidase (XO) plays a critical role in purine catabolism, catalyzing the conversion of hypoxanthine to
xanthine and xanthine to uric acid, contributing to superoxide anion production. This process is implicated in
various human diseases, particularly gout. Traditional XO inhibitors, such as allopurinol and febuxostat, while
effective, may present side effects.
Our study focuses on Asphodelus microcarpus, a plant renowned for traditional anti-inflammatory uses. Recent
investigations into its phenolic-rich flowers, notably abundant in luteolin derivatives, reveal its potential as a
natural source of XO inhibitors. In the present research, XO inhibition by an ethanolic flowers extract from
A. microcarpus is reported. In silico docking studies have highlighted luteolin derivatives as potential XO inhibitors,
and molecular dynamics support that luteolin 7-O-glucoside has the highest binding stability compared
to other compounds and controls. In vitro studies confirm that luteolin 7-O-glucoside inhibits XO more effectively
than the standard inhibitor allopurinol, with an IC50 value of 4.8 μg/mL compared to 11.5 μg/mL, respectively.
These findings underscore the potential therapeutic significance of A. microcarpus in managing conditions related
to XO activity. The research contributes valuable insights into the health-promoting properties of A. microcarpus
and its potential application in natural medicine, presenting a promising avenue for further exploration in disease
management
