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1.
Front Nutr ; 11: 1350534, 2024.
Article in English | MEDLINE | ID: mdl-38962447

ABSTRACT

Allium species are among the most widely cultivated vegetables for centuries for their positive effects on human health and their variety of uses in food preparation and cooking. Preparation and cooking processes create chemical changes that can affect the concentration and bioavailability of bioactive molecules. Understanding the changes in bioactive compounds and bioactive activities in Allium vegetables resulting from preparation and cooking processes is essential for better retention of these compounds and better utilization of their health benefits. This study aimed to investigate the effects of different preparation and cooking processes on the bioactive molecules of Allium vegetables. This review concludes that bioactive compounds in Allium vegetables are affected by each preparation and cooking process depending on variables including method, time, temperature. Owing to differences in the matrix and structure of the plant, preparation and cooking processes show different results on bioactive compounds and bioactive activities for different vegetables. Continued research is needed to help fill gaps in current knowledge, such as the optimal preparation and cooking processes for each Allium vegetable.

2.
Curr Issues Mol Biol ; 46(6): 5595-5613, 2024 Jun 03.
Article in English | MEDLINE | ID: mdl-38921006

ABSTRACT

Multiple sclerosis (MS) is a chronic autoimmune demyelinating disease of the central nervous system, the etiology of which is still unclear. Its hallmarks are inflammation and axonal damage. As a disease primarily impacting younger individuals, the social cost of MS is high. It has been proposed that environmental factors, smoking, and dietary habits acting on a genetic susceptibility play a role in MS. Recent studies indicate that diet can significantly influence the onset and progression of MS. This review delves into the impact of natural bioactive molecules on MS development and explores the dietary interventions that hold promise in managing the disease. Dietary patterns, including ketogenic and Mediterranean diets, are discussed. Theories about the potential mechanistic associations beneath the noted effects are also proposed. Several dietary components and patterns demonstrated the potential for a significant impact on MS. However, extensive prospective clinical trials are necessary to fully understand the role of natural bioactive molecules as disease modifiers in MS.

3.
Mar Drugs ; 22(6)2024 May 29.
Article in English | MEDLINE | ID: mdl-38921564

ABSTRACT

Transition metal catalysis has contributed to the discovery of novel methodologies and the preparation of natural products, as well as new chances to increase the chemical space in drug discovery programs. In the case of marine drugs, this strategy has been used to achieve selective, sustainable and efficient transformations, which cannot be obtained otherwise. In this perspective, we aim to showcase how a variety of transition metals have provided fruitful couplings in a wide variety of marine drug-like scaffolds over the past few years, by accelerating the production of these valuable molecules.


Subject(s)
Aquatic Organisms , Biological Products , Transition Elements , Catalysis , Biological Products/chemical synthesis , Biological Products/chemistry , Transition Elements/chemistry , Drug Discovery/methods , Animals
4.
Front Bioeng Biotechnol ; 12: 1351583, 2024.
Article in English | MEDLINE | ID: mdl-38807651

ABSTRACT

Bacterial natural products (BNPs) are very important sources of leads for drug development and chemical novelty. The possibility to perform late-stage diversification of BNPs using biocatalysis is an attractive alternative route other than total chemical synthesis or metal complexation reactions. Although biocatalysis is gaining popularity as a green chemistry methodology, a vast majority of orphan sequenced genomic data related to metabolic pathways for BNP biosynthesis and its tailoring enzymes are underexplored. In this review, we report a systematic overview of biotransformations of 21 molecules, which include derivatization by halogenation, esterification, reduction, oxidation, alkylation and nitration reactions, as well as degradation products as their sub-derivatives. These BNPs were grouped based on their biological activities into antibacterial (5), antifungal (5), anticancer (5), immunosuppressive (2) and quorum sensing modulating (4) compounds. This study summarized 73 derivatives and 16 degradation sub-derivatives originating from 12 BNPs. The highest number of biocatalytic reactions was observed for drugs that are already in clinical use: 28 reactions for the antibacterial drug vancomycin, followed by 18 reactions reported for the immunosuppressive drug rapamycin. The most common biocatalysts include oxidoreductases, transferases, lipases, isomerases and haloperoxidases. This review highlights biocatalytic routes for the late-stage diversification reactions of BNPs, which potentially help to recognize the structural optimizations of bioactive scaffolds for the generation of new biomolecules, eventually leading to drug development.

5.
Biosci Rep ; 44(4)2024 Apr 24.
Article in English | MEDLINE | ID: mdl-38563086

ABSTRACT

The objective of this work was to evaluate the combination of synthetic peptides based on the γ-core motif of defensin PvD1 with amphotericin B (AmB) at different concentrations against Candida albicans. We applied the checkerboard assay using different concentrations of the commercial drug AmB and the synthetic peptides γ31-45PvD1++ and γ33-41PvD1++ against C. albicans, aiming to find combinations with synergistic interactions. Between these two interactions involving γ31-45PvD1++ and AmB, an additive effect was observed. One such interaction occurred at concentrations of 0.009 µM of peptide γ31-45PvD1++ and 13.23 µM of AmB and another condition of 0.019 µM of peptide γ31-45PvD1++ and 6.61 µM of AmB. The other two concentrations of the interaction showed a synergistic effect in the combination of synthetic peptide γ31-45PvD1++ and AmB, where the concentrations were 1.40 µM peptide γ31-45PvD1++ and 0.004 µM AmB and 0.70 µM γ31-45PvD1++ peptide and 0.002 µM AmB. We proceeded with analysis of the mechanism of action involving synergistic effects. This examination unveiled a range of impactful outcomes, including the impairment of mitochondrial functionality, compromise of cell wall integrity, DNA degradation, and a consequential decline in cell viability. We also observed that both synergistic combinations were capable of causing damage to the plasma membrane and cell wall, causing leakage of intracellular components. This discovery demonstrates for the first time that the synergistic combinations found between the synthetic peptide γ31-45PvD1++ and AmB have an antifungal effect against C. albicans, acting on the integrity of the plasma membrane and cell wall.


Subject(s)
Amphotericin B , Candida albicans , Amphotericin B/pharmacology , Antifungal Agents/pharmacology , Peptides/pharmacology , Cell Membrane , Cell Wall , Microbial Sensitivity Tests
6.
Mar Drugs ; 22(4)2024 Apr 18.
Article in English | MEDLINE | ID: mdl-38667799

ABSTRACT

Techniques for extracting important bioactive molecules from seafood byproducts, viz., bones, heads, skin, frames, fins, shells, guts, and viscera, are receiving emphasis due to the need for better valorization. Employing green extraction technologies for efficient and quality production of these bioactive molecules is also strictly required. Hence, understanding the extraction process parameters to effectively design an applicable optimization strategy could enable these improvements. In this review, statistical optimization strategies applied for the extraction process parameters of obtaining bioactive molecules from seafood byproducts are focused upon. The type of experimental designs and techniques applied to criticize and validate the effects of independent variables on the extraction output are addressed. Dominant parameters studied were the enzyme/substrate ratio, pH, time, temperature, and power of extraction instruments. The yield of bioactive compounds, including long-chain polyunsaturated fatty acids, amino acids, peptides, enzymes, gelatine, collagen, chitin, vitamins, polyphenolic constituents, carotenoids, etc., were the most studied responses. Efficiency and/or economic and quality considerations and their selected optimization strategies that favor the production of potential bioactive molecules were also reviewed.


Subject(s)
Seafood , Animals , Aquatic Organisms , Humans , Biological Products/chemistry , Biological Products/isolation & purification
7.
Talanta ; 275: 126097, 2024 Aug 01.
Article in English | MEDLINE | ID: mdl-38631266

ABSTRACT

The rapid developments in the field of zeolitic imidazolate frameworks (ZIFs) in recent years have created unparalleled opportunities for the development of unique bioactive ZIFs for a range of biosensor applications. Integrating bioactive molecules such as DNA, aptamers, and antibodies into ZIFs to create bioactive ZIF composites has attracted great interest. Bioactive ZIF composites have been developed that combine the multiple functions of bioactive molecules with the superior chemical and physical properties of ZIFs. This review thoroughly summarizes the ZIFs as well as the novel strategies for incorporating bioactive molecules into ZIFs. They are used in many different applications, especially in biosensors. Finally, biosensor applications of bioactive ZIFs were investigated in optical (fluorescence and colorimetric) and electrochemical (amperometric, conductometric, and impedance) fields. The surface of ZIFs makes it easier to immobilize bioactive molecules like DNA, enzymes, or antibodies, which in turn enables the construction of cutting-edge, futuristic biosensors.


Subject(s)
Biosensing Techniques , Imidazoles , Zeolites , Zeolites/chemistry , Biosensing Techniques/methods , Imidazoles/chemistry , Metal-Organic Frameworks/chemistry , Humans , Electrochemical Techniques
8.
Adv Mater ; 36(24): e2310999, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38457626

ABSTRACT

2D materials (2DMs), such as graphene, transition metal dichalcogenides (TMDs), and black phosphorus (BP), have been proposed for different types of bioapplications, owing to their unique physicochemical, electrical, optical, and mechanical properties. Liquid phase exfoliation (LPE), as one of the most effective up-scalable and size-controllable methods, is becoming the standard process to produce high quantities of various 2DM types as it can benefit from the use of green and biocompatible conditions. The resulting exfoliated layered materials have garnered significant attention because of their biocompatibility and their potential use in biomedicine as new multimodal therapeutics, antimicrobials, and biosensors. This review focuses on the production of LPE-assisted 2DMs in aqueous solutions with or without the aid of surfactants, bioactive, or non-natural molecules, providing insights into the possibilities of applications of such materials in the biological and biomedical fields.

9.
3 Biotech ; 14(4): 94, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38444785

ABSTRACT

We analyzed here the in silico biological activities of caffeine, (+)-catechin, and theobromine. For this, the PubChem database of the NIH (National Institutes of Health) was used to obtain the SMILE canonical form of the bioactive molecules, and the free software PASS Online (Prediction of Activity Spectra for Substances) from the Way2Drug portal. Also, we conducted an in vitro experiment using a chronic myeloid leukemia (CML) cell line (K562) to confirm some results found in in silico investigation. These cells were exposed to different concentrations of caffeine, (+)-catechin, and theobromine for 72 h. The results found in this in silico study suggested that caffeine, (+)-catechin, and theobromine showed excellent biological properties, such as antioxidant, anti-inflammatory, and anticarcinogenic, as well as protection against cardiovascular, diabetes, neurological, allergic, respiratory, and other therapeutic activities. These findings can be elucidated through the modulation exerted by these bioactive molecules in many biochemical pathways involved in organism homeostasis, such as free radical scavenger action, oxidoreductase inhibitor, membrane permeability inhibitor, and lipid peroxidase inhibitor. In addition, we have found here that caffeine, (+)-catechin, and theobromine have a remarkable anti-inflammatory activity which plays an important role in the therapeutic approach of COVID-19. Moreover, our in vitro findings confirmed the in silico results regarding anticancer activity since these molecules reduce cell proliferation at all tested concentrations. Therefore, since these molecules exhibit important medicinal activities, further investigations should be conducted to reveal new therapies to improve the treatments and prevention of numerous disorders and, consequently, promote human health.

10.
Front Chem ; 12: 1356304, 2024.
Article in English | MEDLINE | ID: mdl-38469428

ABSTRACT

The advances in nanocomposites incorporating bioactive substances have the potential to transform the food packaging sector. Different nanofillers have been incorporated into polymeric matrixes to develop nanocomposite materials with improved mechanical, thermal, optical and barrier properties. Nanoclays, nanosilica, carbon nanotubes, nanocellulose, and chitosan/chitin nanoparticles have been successfully included into polymeric films, resulting in packaging materials with advanced characteristics. Nanostructured antimicrobial films have promising applications as active packaging in the food industry. Nanocomposite films containing antimicrobial substances such as essential oils, bacteriocins, antimicrobial enzymes, or metallic nanoparticles have been developed. These active nanocomposites are useful packaging materials to enhance food safety. Nanocomposites are promising materials for use in food packaging applications as practical and safe substitutes to the traditional packaging plastics.

11.
Molecules ; 29(4)2024 Feb 14.
Article in English | MEDLINE | ID: mdl-38398601

ABSTRACT

Compounds derived from natural sources continue to serve as chemical scaffolds for designing prophylactic/therapeutic options for human healthcare. In this study, we aimed to systematically unravel the chemical profile and antioxidant and anti-inflammatory activities of myrtle methanolic extract (MMEx) using in vitro, in vivo, and in silico approaches. High levels of TPC (415.85 ± 15.52 mg GAE/g) and TFC (285.80 ± 1.64 mg QE/g) were observed. Mass spectrophotometry (GC-MS) analysis revealed the presence of 1,8-cineole (33.80%), α-pinene (10.06%), linalool (4.83%), p-dimethylaminobenzophenone (4.21%), thunbergol (4%), terpineol (3.60%), cis-geranyl acetate (3.25%), and totarol (3.30%) as major compounds. MMEx induced pronounced dose-dependent inhibition in all assays, and the best antioxidant activity was found with H2O2, with an IC50 of 17.81 ± 3.67 µg.mL-1. MMEx showed a good anti-inflammatory effect in vivo by limiting the development of carrageenan-induced paw edema. The pharmacokinetic profiles of the active molecules were determined using the SwissADME website, followed by virtual screening against anti-inflammatory targets including phospholipase A2 (PLA-2), cyclooxygenase-2 (COX-2), tumor necrosis factor alpha (TNF-α), interleukin-1ß (IL-1ß), and NF-κB. A pharmacokinetic study revealed that the molecules have good absorption, distribution, and metabolism profiles, with negative organ toxicity. Among the compounds identified by GC-MS analysis, pinostrobin chalcone, cinnamyl cinnamate, hedycaryol, totarol, and p-dimethylaminobenzophenone were observed to have good binding scores, thus appreciable anti-inflammatory potential. Our study reveals that MMEx from Algerian Myrtus communis L. can be considered to be a promising candidate for alleviating many health complaints associated with oxidative stress and inflammation.


Subject(s)
Abietanes , Antioxidants , Myrtus , Humans , Antioxidants/pharmacology , Myrtus/chemistry , Molecular Docking Simulation , Hydrogen Peroxide , Anti-Inflammatory Agents/pharmacology , Plant Extracts/pharmacology
12.
Pharmaceutics ; 16(2)2024 Feb 15.
Article in English | MEDLINE | ID: mdl-38399327

ABSTRACT

Recently, nanotechnologies have become increasingly prominent in the field of bone tissue engineering (BTE), offering substantial potential to advance the field forward. These advancements manifest in two primary ways: the localized application of nanoengineered materials to enhance bone regeneration and their use as nanovehicles for delivering bioactive compounds. Despite significant progress in the development of bone substitutes over the past few decades, it is worth noting that the quest to identify the optimal biomaterial for bone regeneration remains a subject of intense debate. Ever since its initial discovery, poly(lactic-co-glycolic acid) (PLGA) has found widespread use in BTE due to its favorable biocompatibility and customizable biodegradability. This review provides an overview of contemporary advancements in the development of bone regeneration materials using PLGA polymers. The review covers some of the properties of PLGA, with a special focus on modifications of these properties towards bone regeneration. Furthermore, we delve into the techniques for synthesizing PLGA nanoparticles (NPs), the diverse forms in which these NPs can be fabricated, and the bioactive molecules that exhibit therapeutic potential for promoting bone regeneration. Additionally, we addressed some of the current concerns regarding the safety of PLGA NPs and PLGA-based products available on the market. Finally, we briefly discussed some of the current challenges and proposed some strategies to functionally enhance the fabrication of PLGA NPs towards BTE. We envisage that the utilization of PLGA NP holds significant potential as a potent tool in advancing therapies for intractable bone diseases.

13.
Int J Mol Sci ; 25(3)2024 Feb 05.
Article in English | MEDLINE | ID: mdl-38339184

ABSTRACT

The skin is the primary tissue affected by wounds and aging, significantly impacting its protective function. Natural products are widely used in cosmetics, representing a new approach to preventing age-related damage. Nanomedicine combines nanotechnology and traditional treatments to create innovative drugs. The main targets of nanotechnological approaches are wound healing, regeneration, and rejuvenation of skin tissue. The skin barrier is not easily permeable, and the creation of modern nanodevices is a way to improve the passive penetration of substances. In this study, Helichrysum italicum oil (HO) was combined with different types of electrospun nanofibers to study their protective activity on the skin and to evaluate their future application for topical treatments. In the present research, we used biodegradable polymers, including polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP), which were characterized by a scanning electron microscope (SEM). All results show a positive trend in cell proliferation and viability of human skin stem cells (SSCs) and BJ fibroblasts pre-treated with combined nanofibers and then exposed to UV stress. Gene expression analysis revealed the activation of a molecular rejuvenation program in SSCs treated with functionalized nanofibers before UV exposure. Understanding the mechanisms involved in skin changes during aging allows for the future application of nanomaterials combined with HO directly to the patients.


Subject(s)
Biological Products , Nanofibers , Skin Aging , Humans , Biological Products/pharmacology , Skin , Wound Healing , Polyvinyl Alcohol
14.
J Biomed Mater Res B Appl Biomater ; 112(1): e35358, 2024 01.
Article in English | MEDLINE | ID: mdl-38247243

ABSTRACT

Allogenic demineralized bone matrix (DBM), processed to expose bioactive proteins imbedded by calcium salts, is widely used for bone repair and regeneration as an alternative to the autologous bone graft. However, demineralized bone matrices from tissue banks vary significantly in residual calcium content and osteogenicity for clinical bone regeneration. The present study produced DBM with various residual calcium contents by partial demineralization using ethylenediaminetetraacetic acid disodium (EDTA) and hydrochloric acid. Compositional analysis reveals that, as the percent weight loss of bone materials increases from 0% to 74.9% during demineralization, the residual calcium content of DBM decreases from 24.8% to 0.2% and collagen content increases from 29.7% to 92.6%. Calorimetrical analysis and Fourier transform infrared (FTIR) analysis demonstrated that demineralization to the residual calcium content of <4% enables the complete exposure and/or release of bone collagen fibers and other bioactive molecules. In order to evaluate the relationship between the extent of demineralization and the osteogenicity of DBM, DBM particles were fabricated with the aid of acellular dermal matrix (ADM) microfibers to form flexible foam-like DBM/ADM composites. Proteomic analysis identified various type collagens and bone formation-related bioactive molecules in both ADM and DBM. Using the rat bilateral Φ = 5 mm calvarium defect repair model, the study had shown that the DBM/ADM composite with ~20% DBM residual calcium (e.g., ~40% calcium being removed) maximized the osteogenicity for bone defect repair after 4 and 8 weeks. DBM with ~40% calcium removal had the maximal osteogenicity presumably through the sustained release of bioactive molecules during the process of bone regeneration.


Subject(s)
Calcium , Osteogenesis , Animals , Rats , Calcium/pharmacology , Delayed-Action Preparations/pharmacology , Proteomics , Collagen/pharmacology
15.
J Pharm Pharmacol ; 76(3): 183-200, 2024 Mar 04.
Article in English | MEDLINE | ID: mdl-38280221

ABSTRACT

OBJECTIVES: Despite significant advancements in modern medicine, effective hepatoprotective medication with minimal side effects is still lacking. In this context. Tinospora cordifolia, an Indian Ayurvedic liana, has attracted much attention. KEY FINDINGS: Traditionally, T. cordifolia has been found to be effective in the treatment of jaundice; according to the literature, T. cordifolia is a hepatoprotective agent, and the CCl4 model is the most frequently used to evaluate its potential. Its hepatoprotective effects might be attributed to alkaloids (berberine, palmatine, and jatrorrhizine) and sinapic acid. Berberine decreases inflammation by inhibiting the proinflammatory cascade triggered by TNF-α and reduces nitrosative stress by inhibiting iNOS. T. cordifolia also exhibits anticancer, anti-inflammatory, antimicrobial, antioxidant, and other activities; it is safe at concentrations up to 2000 mg/kg. Its biological action can be attributed to polyphenols, alkaloids, steroids, terpenoids, and glycosides. T. cordifolia has also been found to be an active ingredient in several polyherbal formulations used to treat chemical-mediated hepatotoxicity. CONCLUSION: T. cordifolia's hepatoprotective effects are mediated by the inhibition of lipid peroxidation, the management of oxidative stress, and other factors. T. cordifolia can be used to manage liver disorders and as a hepatoprotective supplement in the food industry. The bioprospecting of its alkaloids can lead to the development of novel formulations against hepatic ailments.


Subject(s)
Berberine , Tinospora , Plant Extracts/pharmacology , Antioxidants/pharmacology , Dietary Supplements
16.
Toxicon X ; 21: 100182, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38226138

ABSTRACT

The Amazon biome is home to many scorpion species, with around two hundred identified in the region. Of these, forty-eight species have been reported in Brazil so far and six of them are of medical importance: Tityus apiacas, T. metuendus, T. obscurus, T. raquelae, T. silvestris, and T. strandi. Three non-medically important species have also been studied: Opisthanthuscayaporum, Brotheas amazonicus and Rhopalurus laticauda. The venom of the scorpion T. obscurus is the most studied, followed by O. cayaporum. We aim to update the study of these Amazonian scorpion species. We will explore the harmful and beneficial properties of scorpion venom toxins and how they could be applied in drug development. This systematic review will focus on collecting and analyzing venoms from scorpions in Brazil. Only papers on Amazonian scorpion venom studies published between 2001 and 2021 (scientific articles, theses, and dissertations) were selected, based on the lists of scorpions available in the literature. Species found in the Amazon but not confirmed to be Brazilian were omitted from the review. Theses and dissertations were chosen over their derived articles. We found 42 eligible studies (13 theses, 27 articles and 2 patents) out of 17,950 studies and a basic statistical analysis was performed. The literature showed that T. obscurus was the most studied venom with 28 publications, followed by O. cayaporum with seven articles, B. amazonicus with four articles, T. metuendus with two article and R. laticauda with one article. No publication on the characterization of T. silvestris and T. apiacas venoms were found during the reviewed period, only the clinical aspects were covered. There is still much to be explored despite the increasing number of studies conducted in recent years. Amazonian scorpions have promising potential for pharmaceutical and clinical applications.

17.
Microorganisms ; 12(1)2024 Jan 15.
Article in English | MEDLINE | ID: mdl-38258000

ABSTRACT

Postbiotics are gaining increasing interest among the scientific community as well as at the level of food processing enterprises. The aim of this preliminary study was to characterise the metabolic diversity of a novel Bifidobacterium longum strain, BIOCC 1719, of human origin. The change after 24 h cultivation in three media was assessed using a metabolomic approach. Milk-based substrates favoured the activity of the strain, promoting the production of B vitamins, essential amino acids, bile acids, and fatty acids. Vitamins B1, B2, B6, B7, and B12 (with an average increase of 20-30%) were produced in both whole milk and whey; the increased production in the latter was as high as 100% for B7 and 744% for B12. The essential amino acids methionine and threonine were produced (>38%) in both milk and whey, and there was an increased production of leucine (>50%) in milk and lysine (126%) in whey. Increases in the content of docosahexaenoic acid (DHA) by 20%, deoxycholic acid in milk and whey (141% and 122%, respectively), and cholic acid (52%) in milk were recorded. During the preliminary characterisation of the metabolic diversity of the novel B. longum strain, BIOCC 1719, we identified the bioactive compounds produced by the strain during fermentation. This suggests its potential use as a postbiotic ingredient to enrich the human diet.

18.
Article in English | MEDLINE | ID: mdl-38284712

ABSTRACT

Exosomes are very small (nano-sized) vesicles participating in tumor development by involvement in intercellular communication mediated by transferring biocomponents. Exosomes appear to play vital roles in various cancer development, such as ovarian cancer, a common malignancy in women. Several hallmarks of ovarian cancer are reported to be affected by the exosome-- mediated cellular cross-talk, including modulating peritoneal dissemination and chemoresistance. Since the expression of some biomolecules, such as miRNAs and mRNA, is changed in ovarian cancer, these exo-biomolecules can be applied as prognostic, diagnostic, and therapeutic biomarkers. Also, the selective loading of specific chemotherapeutic agents into exosomes highlights these biocarries as potential delivery devices. Exosomes could be artificially provided and engineered to better target the site of interest in ovarian cancer. In the present review, we summarize the notable achievement of exosome application in ovarian cancer management to gain applicable transitional insight against this cancer.

19.
CNS Neurosci Ther ; 30(4): e14528, 2024 04.
Article in English | MEDLINE | ID: mdl-38044793

ABSTRACT

BACKGROUND: Glioblastoma (GBM) is the most common primary malignant tumor in the central nervous system. Paclitaxel (PTX) is a well-established and highly effective anti-cancer drug for peripheral solid tumors. However, the application of PTX in GBM is hindered by several limitations, including poor water solubility, restricted entry across the blood-brain barrier (BBB), and enhanced excretion by efflux transporters. P-glycoprotein (P-gp) is a crucial efflux transporter that is abundantly present in cerebral vascular endothelial cells and GBM cells. It plays a significant role in the exocytosis of PTX within tumor tissues. METHODS: Recently, we have developed a novel technique for creating self-assembled nanoparticles utilizing a range of natural bioactive molecules. These nanoparticles can encapsulate insoluble drugs and effectively cross the BBB. In additional, we revealed that certain nanoparticles have the potential to act as P-gp inhibitors, thereby reducing the excretion of PTX. In this study, we conducted a screening of bioactive molecular nanoparticles to identify those that effectively inhibit the function of P-gp transporters. RESULTS: Among the candidates, we identified ursolic acid nanoparticles (UA NPs) as the P-gp inhibitors. Furthermore, we prepared co-assembled UA NPs embedded with paclitaxel, referred to as UA-PTX NPs. Our results demonstrate that UA-PTX NPs can enhance the blood concentration of PTX, facilitate its entry into the BBB, and inhibit the function of P-gp, resulting in a decrease in the excretion of PTX. This discovery effectively addressed the above three issues associated with the use of PTX in glioma treatment. CONCLUSIONS: UA-PTX NPs demonstrate strong anti-tumor effects and show great potential for treating GBM.


Subject(s)
Antineoplastic Agents , Glioblastoma , Nanoparticles , Humans , Paclitaxel/pharmacology , Paclitaxel/therapeutic use , Glioblastoma/drug therapy , Glioblastoma/pathology , Endothelial Cells , Cell Line, Tumor , Drug Delivery Systems
20.
Food Chem ; 438: 137955, 2024 Apr 16.
Article in English | MEDLINE | ID: mdl-37976873

ABSTRACT

Here we report on the occurrence of mycosporine-like amino acids (MAAs) in the Argentine shortfin squid, Illex argentinus, the second fishery resource mostly exploited in the Argentinean continental shelf. The total content of four MAAs was evaluated by reverse-phase-HPLC in different tissues (eyes, skin, liver, and gonads). Also, the antioxidant activity of crude extracts was assessed by in-vitro determinations: 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), Folin-Ciocalteu, and ferrous ion-chelating capacity assays. The content of MAAs was found to be almost ten times higher in female gonads than in other tissues (11,89 ± 0,56 mg/g dry weight). Extracts from skin, female gonads and eyes, exhibit higher antioxidant activity than the reference compounds ascorbic acid and TROLOX. Overall, Argentine squid waste is a promising potential source of MAAs with antioxidant and UV photoprotective properties, which could bear interest in food, cosmetic and pharmaceutical industries, thus encouraging maximal and sustainable use of fishing resources.


Subject(s)
Amino Acids , Antioxidants , Animals , Female , Decapodiformes , Ascorbic Acid , Skin
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