Annona cherimola Mill., or the custard apple, is one of the species belonging to the Annonaceae family, is widely used in traditional medicine, and has been reported to be a valuable source of ...bioactive compounds. A unique class of secondary metabolites derived from this family are Annonaceous acetogenins, lipophilic polyketides considered to be amongst the most potent antitumor compounds. This review provides an overview of the chemical diversity, isolation procedures, bioactivity, modes of application and synthetic derivatives of acetogenins from A. cherimola Mill.
Naphthoquinones are a valuable source of secondary metabolites that are well known for their dye properties since ancient times. A wide range of biological activities have been described highlighting ...their cytotoxic activity, gaining the attention of researchers in recent years. In addition, it is also worth mentioning that many anticancer drugs possess a naphthoquinone backbone in their structure. Considering this background, the work described herein reports the evaluation of the cytotoxicity of different acyl and alkyl derivatives from juglone and lawsone that showed the best activity results from a etiolated wheat coleoptile bioassay. This bioassay is rapid, highly sensitive to a wide spectrum of activities, and is a powerful tool for detecting biologically active natural products. A preliminary cell viability bioassay was performed on cervix carcinoma (HeLa) cells for 24 h. The most promising compounds were further tested for apoptosis on different tumoral (IGROV-1 and SK-MEL-28) and non-tumoral (HEK-293) cell lines by flow cytometry. Results reveal that derivatives from lawsone (particularly derivative
) were more cytotoxic on tumoral than in non-tumoral cells, showing similar results to those obtained with of etoposide, which is used as a positive control for apoptotic cell death. These findings encourage further studies on the development of new anticancer drugs for more directed therapies and reduced side effects with naphthoquinone skeleton.
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•Systems synthesized enhance water solubility of β-carotene.•Supramolecular polymer micelles offer a new possibility in prodrug encapsulation.•β-carotene encapsulated reduce skin ...melanoma cells better than free carotenoid.•A control release of β-carotene is possible by pH modulation.•Gastrointestinal simulation shown bioavailability enhancement of β-carotene.
Encapsulation techniques to generate core/shell systems provide a method that improves physicochemical properties, which are very important in biological applications. β-carotene is a common carotenoid that has shown preventive effects in skin diseases and vitamin A deficiency but this compound has limited water solubility and bioavailability, which hinder its broad application. The use of polyrotaxane compounds formed from cyclodextrins has allowed supramolecular polymer micelles (SMPMs) to be synthesized to encapsulate β-carotene. The polymeric compound Pluronic F127® was also used to create core/shell nanoparticles (NPs) that contain β-carotene. Bioactive compound encapsulation was fully confirmed by nuclear magnetic resonance spectroscopy and by scanning and transmission electron microscopy. The method based on cyclodextrin and lecithin allow to release slowly when the systems were exposed to an aqueous medium by pH control, with an increase of 16 times of bioavailability comparing with free carotenoid. This allowed to potentiate the cytotoxic activity on a melanoma cell line by enhancing the water solubility to more than 28 mg/L, and present promising applications of SMPMs to provitamins.
An accurate diagnosis of β-lactam (BL) allergy improves the use of antibiotics, increases patients' safety, and reduces costs to health systems. Nevertheless, it requires skin and drug provocation ...tests, which are time-consuming and put the patient at risk. Furthermore, allergy testing is not available in circumstances such as the urgent need for antibiotic therapy.
To evaluate the usefulness of an artificial neural network (ANN) in the prediction of hypersensitivity to BLs, and compare it with logistic regression (LR) analysis.
In a single-center study, 656 patients evaluated for BL allergy between 1994 and 2000 were retrospectively analyzed, and the data were used to construct an ANN. The ANN predictive capabilities were compared with LR and then prospectively evaluated in 615 patients who underwent BL evaluation between 2011 and 2017.
A total of 1271 patients were evaluated. All patients had a definite diagnosis as allergic or nonallergic to BL. The prospective sample showed a lower percentage of patients with allergy than the retrospective sample (20.7% vs 25.8%; P = .018). In the retrospective and prospective series, the ANN reached a sensitivity of 89.5% and 81.1%, a specificity of 86.1% and 97.9%, a positive predictive value of 82.1% and 91.1%, and a negative predictive value of 92.1% and 95.2%, respectively. The ANN's performance was far superior to that of the LR, whose best performance reached a sensitivity of 31.9% and a specificity of 98.8%.
This ANN demonstrated a superior performance than the LR in predicting BL hypersensitivity without misdiagnosing severe allergic reactions. The ANN could be a helpful tool to classify the reaction risk, particularly in the identification of low-risk patients, in which an open challenge could be done to delabel patients.
Isohexenylnaphthazarins are commonly found in the root periderm of several Boraginaceous plants and are known for their broad range of biological activities. The work described herein concerns the ...biological activity of compounds from the roots of Echium plantagineum L. and Echium gaditanum Boiss (Boraginaceae) collected from field sites in southern Spain and Australia. Bioactivity was assessed using etiolated wheat coleoptile bioassay and in vitro growth inhibitory activity in HeLa and IGROV-1 cells. The quantification of four isohexenylnaphthazarins (shikonin/alkannin, deoxyshikonin/deoxyalkannin, acetylshikonin/acetylalkannin and dimethylacrylshikonin/dimethylacrylalkannin) was performed by LC-MS/MS using juglone as internal standard. Correlation coefficient values for the activities and concentrations of these four analytes were in the linear range and were greater than 0.99. Acetylshikonin/acetylalkannin and dimethylacrylshikonin/dimethylacrylalkannin were present in the highest concentrations in extracts of both species. The results reveal that greatest overall inhibition was observed in both bioassays with E. gaditanum extracts. Strong correlations between time of collection, sampling location and bioactivity were identified.
Evaluation of the biological activity and the quantification of four isohexenylnaphthazarins were carried out in two Echium spp. Correlations between surveyed locations and bioactivity were discussed. Display omitted
•The bioactivity of periderm extracts of two Echium spp. has been evaluated.•A correlation between coleoptile and cytotoxicity bioassays has been identified.•A quantitative analysis of isohexenylnaphthazarins has been performed.
Vegetarian and vegan diets are increasingly being adopted in Spain, a trend mainly driven by ethical concerns for animal welfare and the environment. This has resulted in a growing market for ...plant-based substitutes of meat products. However, available data on the nutritional value of such meat analogues in Mediterranean countries are still limited. In this study, the labelling information of four categories of plant-based meat analogues (
= 100) and the corresponding conventional meat products (
= 48) available on the Spanish market was surveyed and compared. The nutrient content of plant-based meat analogues varied significantly, due to the wide range of ingredients used in their formulation. Some of these products were found to have a low protein content, which in others was enhanced by the addition of cereals and legumes. Compared to the meat products, the plant-based analogues contained lower levels of total fat as well as saturated fat, which ranged from 30% of total fat in burgers to less than 15% in meatballs, sausages, and nuggets; in contrast, they contained higher amounts of fiber and complex carbohydrates. Overall, the meat analogues cannot be considered as nutritionally equivalent substitutes to conventional meat products due to a high variability of protein content and other nutrients.
Follicle-stellate cells are pituitary non-granular cells that are arranged between secretory cells or organized in follicles with small lumens. Cells from the follicles exhibit the typical phenotype ...of a transporting epithelium, including apical microvilli with a cilium and tight junctions. Freeze-fracture electron microscopy images show that the tight junctions consist of 5–7 anastomosing strands and that cultured follicle-stellate cells develop a trans-epithelial electrical resistance characteristic of “tight” epithelia. Here, we investigate the molecular composition of the tight junction from follicle stellate cells. We found that the rat anterior pituitary lobe expresses mRNAs for claudins 2, 4 and 5; the proteins of all these claudins are observed in the anterior lobe, whereas the intermediate lobe expresses claudins 2 and 5 and the posterior lobe contains only claudin 5. Follicle-stellate cells, identified by their protein marker S100β, expresses claudin 4 in the apical membrane, in co-localization with dipeptidyl-peptidase and near acetylated β-tubulin. Claudin 4 partially co-localizes with E-cadherin, indicating that a fraction of the protein is located in the basolateral domain. Follicle-stellate-enriched cell cultures develop patches of polygonal cells expressing claudin 4 and E-cadherin, encircled by extensive monolayers of fusiform cells. Claudin 2 stains specifically blood vessels, identified by claudin 5 and VE-cadherin labels. Thus, follicles in the anterior pituitary consist of “tight” epithelia that can carry out intense vectorial transport, together with a high cation movement in blood vessels, possibly related to the ion requirements of excitable secretory cells for hormone secretion.
In inflammatory bowel disease (IBD), chronic inflammation in the gastrointestinal tract can lead to tissue damage and remodelling, which can ultimately result in fibrosis. Prolonged injury and ...inflammation can trigger the activation of fibroblasts and extracellular matrix (ECM) components. As fibrosis progresses, the tissue becomes increasingly stiff and less functional, which can lead to complications such as intestinal strictures, obstructive symptoms, and eventually, organ dysfunction. Epithelial cells play a key role in fibrosis, as they secrete cytokines and growth factors that promote fibroblast activation and ECM deposition. Additionally, epithelial cells can undergo a process called epithelial-mesenchymal transition, in which they acquire a more mesenchymal-like phenotype and contribute directly to fibroblast activation and ECM deposition. Overall, the interactions between epithelial cells, immune cells, and fibroblasts play a critical role in the development and progression of fibrosis in IBD. Understanding these complex interactions may provide new targets for therapeutic interventions to prevent or treat fibrosis in IBD. In this review, we have collected and discussed the recent literature highlighting the contribution of epithelial cells to the pathogenesis of the fibrotic complications of IBD, including evidence of EMT, the epigenetic control of the EMT, the potential influence of the intestinal microbiome in EMT, and the possible therapeutic strategies to target EMT. Finally we discuss the pro-fibrotic interactions epithelial-immune cells and epithelial-fibroblasts cells.
Novel trans-disubstituted hexaaza-macrocyclic ligands L
1
and L
2
were successfully prepared by the alkylation of the trans secondary amines presented in L with pyridine and ethyldioxolane groups, ...respectively. The coordination properties of compounds L
1
and L
2
towards different transition, post-transition and lanthanoid metal ions were explored. Colorless crystals of NaL
1
I and L
2´
Br
2
, suitable for X-ray diffraction, were obtained by slow evaporation of an acetonitrile solution of compounds L
1
or L
2
, showing an anti conformation between the methyl groups and the pendant arms in trans positions. The ML
1
n+
(M = Ni
2+
, Cu
2+
, Zn
2+
) systems were investigated by DFT calculations (B3LYP model).
Celotno besedilo
Dostopno za:
BFBNIB, DOBA, GIS, IJS, IZUM, KILJ, KISLJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
Gadolinium-based contrast agents (GBCAs) are frequently used in magnetic resonance imaging (MRI) examinations to increase sensitivity in diagnoses. Recently, an increase in the description of ...hypersensitivity reactions to GBCAs has been detected. We performed research in PubMed, PubMed, SCOPUS, and EMBASE until September 2021, searching for studies regarding immediate and delayed hypersensitivity reactions to gadolinium-based contrast agents in which an allergy study was performed. The initial research identified 149 articles written in English. After excluding articles duplicated and articles that had irrelevant designs, 26 articles were included. Finally, 17 studies concerning immediate reactions, six studies concerning non-immediate reactions, and three concerning both that performed allergy evaluations were selected. In the review, we analyzed the characteristics of immediate and delayed reactions and the results of the allergy study and cross-reactivity. Skin tests seem to have acceptable accuracy, but drug provocation tests are still needed when skin tests are negative o to find alternative agents. Although cross-reactivity patterns are not well established, cross-reactivity seems to exist among macrocyclic agents. Notwithstanding, the number of patients analyzed is low and further studies are required. A management algorithm is suggested.
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