Multifunctional Nanotheranostics for Overcoming the Blood–Brain Barrier

Advanced Functional Materials, Год журнала: 2024, Номер 34(19)

Опубликована: Янв. 4, 2024

Abstract The blood–brain barrier (BBB) is a tailored system of capillary endothelial cells intermixed with tight junctions and adherent that regulates the transport various materials substances between blood vasculature central nervous (CNS). However, in cases brain diseases, BBB's protective regulatory effects hamper therapeutics from reaching affected sites sufficient quantities. This has so far been leading challenge treating CNS diseases disorders. For this problem to be overcome, recent research sought develop novel modalities achieve efficient therapy alleviate associated symptoms. Therefore, numerous strategies have operated years address limitations traditional invasive methods, including poor penetration serious side effects. As desperately in‐demand technology, nanotheranostics particularly shown promising results. Herein, review reports advancements techniques nanotechnology‐based developed for neurodegenerative study provides comprehensive data on subject used future studies management disorders diseases.

Язык: Английский

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Functional Evaluation of Laminarin Butyl Esters: Antioxidant, Skin-Whitening, and Anti-Wrinkle Properties

Process Biochemistry, Год журнала: 2025, Номер unknown

Опубликована: Фев. 1, 2025

Язык: Английский

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Investigation on the inhibition mechanism and binding behavior of paeonol to tyrosinase and its anti-browning property by multi-spectroscopic and molecular docking methods

International Journal of Biological Macromolecules, Год журнала: 2023, Номер 253, С. 126962 - 126962

Опубликована: Сен. 16, 2023

Язык: Английский

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Recent progress in functionalized and targeted polymersomes and chimeric polymeric nanotheranostic platforms for cancer therapy

Progress in Materials Science, Год журнала: 2023, Номер 140, С. 101209 - 101209

Опубликована: Ноя. 3, 2023

Язык: Английский

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Inhibitory Effects of Polyphenols from Equisetum ramosissimum and Moringa peregrina Extracts on Staphylococcus aureus, Collagenase, and Tyrosinase Enzymes: In vitro Studies

Jordan Journal of Pharmaceutical Sciences, Год журнала: 2024, Номер 17(3), С. 530 - 548

Опубликована: Сен. 24, 2024

Background: Skin problems caused by oxidative stress lead to the activation of collagenase and tyrosinase enzymes, contributing skin aging, discoloration, infections. Equisetum ramosissimum Moringa peregrina were assessed for their potential uses in treating various conditions. Objective: The present research aimed investigate positive effects polyphenols extracts as cosmetic products treatment different Methods: Total phenolic flavonoid contents, antioxidants, anti-collagenase anti-tyrosinase activities plant extract mixtures (PEM) at ratios (M. peregrina: E. ramosissimum) determined using standard procedures. Inhibitory PEM against acne-causing Staphylococcus aureus (ATCC 29213) evaluated diameter (cm) inhibition zone method. A cream formulation containing was developed characterized stability irritation rats Results: a ratio (2:1) showed highest total content (150.15 ± 2.8 mg/g, equivalent gallic acid, 41.5 1.2 quercetin, respectively). Antioxidant also optimal, DPPH ABTS methods (IC50 = 7.06 0.12 µg/mL 53.29 3.3 µg/mL, Furthermore, exhibited superior inhibitory enzymes 32.4 1.19 8.4 Antimicrobial activity tested on S. largest growth (2.8 cm) concentration 60 mg/mL. Studies revealed that it remained stable under room tests no signs oedema or erythema after treatment. Conclusion: with demonstrated optimal an stress-neutralizing agent, inhibitor responsible aging hyperpigmentation, antibacterial agent. physical detectable risk throughout

Язык: Английский

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Inhibition potential of n‐hexadecanoic and oleic acids from edible insects against α‐glucosidase, α‐amylase, tyrosinase, and acetylcholinesterase: in vitro and in silico studies

Journal of the Science of Food and Agriculture, Год журнала: 2025, Номер unknown

Опубликована: Янв. 11, 2025

Abstract BACKGROUND Edible insects are used for consumption and traditional medicine due to their rich bioactive compounds. This study examined the compounds inhibitory effects of crude extracts from Bombyx mori Omphisa fuscidentalis on α ‐glucosidase, ‐amylase, acetylcholinesterase (AChE), tyrosinase. Fatty acids, including n ‐hexadecanoic acid oleic acid, were identified in evaluated potential against enzymes vitro silico . RESULTS The total phenolic content edible insect correlated with enzyme activity. quercetin kaempferol B ethyl acetate (EtOAc) extract was also closely related ‐amylase EtOAc hexane showed similar inhibition acarbose tacrine AChE, respectively. O exhibited comparable tyrosinase activity kojic acid. ‐Hexadecanoic predominant all extracts. A kinetic revealed that acted as a mixed‐type inhibitor acarbose, whereas non‐competitive unlike tacrine. Docking studies suggested these fatty acids bind active sites AChE. CONCLUSION findings suggest could be candidates treating diabetes mellitus Alzheimer's disease. An animal model might further examination confirm findings. © 2025 Society Chemical Industry.

Язык: Английский

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Small-Molecule Tyrosinase Inhibitors for Treatment of Hyperpigmentation

Molecules, Год журнала: 2025, Номер 30(4), С. 788 - 788

Опубликована: Фев. 8, 2025

Increasing attention is being focused on skin health currently, especially the excessive deposition of melanin in skin. Tyrosinase, rate-limiting enzyme biosynthesis, a crucial synthesis. However, existing tyrosinase inhibitors pose some degree toxicity to humans. Therefore, development more efficient and low-toxicity urgently needed. This review briefly depicts biosynthesis process crystal structure catalytic mechanism tyrosinase. The latest research progress regarding small-molecule also reviewed. Moreover, structure-function relationships are analyzed summarized. expected provide new scientific insights enable researchers explore safer potent inhibitors.

Язык: Английский

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Artificial Intelligence-Assisted Optimization of Antipigmentation Tyrosinase Inhibitors: De Novo Molecular Generation Based on a Low Activity Lead Compound

Journal of Medicinal Chemistry, Год журнала: 2024, Номер 67(9), С. 7260 - 7275

Опубликована: Апрель 23, 2024

Artificial intelligence (AI) de novo molecular generation is a highly promising strategy in the drug discovery, with deep reinforcement learning (RL) models emerging as powerful tools. This study introduces fragment-by-fragment growth RL forward and optimization based on low activity lead compound. process integrates fragment growth-based reaction templates, while target docking drug-likeness prediction were simultaneously performed. comprehensive approach considers similarity, internal diversity, synthesizability, effectiveness, thereby enhancing quality efficiency of generation. Finally, series tyrosinase inhibitors generated synthesized. Most compounds exhibited more improved than lead, an optimal candidate compound surpassing effects kojic acid demonstrating significant antipigmentation zebrafish model. Furthermore, metabolic stability studies indicated susceptibility to hepatic metabolism. The proposed AI structural strategies will play role accelerating discovery improving traditional efficiency.

Язык: Английский

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Elderberry Leaves with Antioxidant and Anti-Inflammatory Properties as a Valuable Plant Material for Wound Healing

Pharmaceuticals, Год журнала: 2024, Номер 17(5), С. 618 - 618

Опубликована: Май 10, 2024

Sambuci folium (elderberry leaves) have been used in traditional medicine, mainly externally, to treat skin diseases and wounds. Therefore, the aim of this study was screen biological activity elderberry leaves (antioxidant potential possibility inhibition tyrosinase hyaluronidase enzymes) combined with phytochemical analysis. For purpose, a analysis carried out. Elderberry 12 varieties (“Sampo”, “Obelisk”, “Dwubarwny”, “Haschberg”, “Haschberg 1”, “Koralowy”, “Sambo”, “Black Beauty”, Tower”, “Golden hybrid”, “Samyl”, “Samyl 1”) two growth stages. The compounds from selected groups, phenolic acids (chlorogenic acid) flavonols (quercetin), were chromatographically determined hydroalcoholic leaf extracts. All tested extracts showed antioxidant effects, but most promising potential: very high content (TPC = 61.85 mg GAE/g), (e.g., DPPH IC50 1.88 mg/mL; CUPRAC IC0.5 0.63 mg/mL) optimal anti-inflammatory (inhibition 41.28%) activities indicated for older “Sampo” variety. Additionally, extract obtained hybrid” variety facilitated treatment wounds scratch test. In summary, best multidirectional pro-health effect treating inflammation specified II (leaves during flowering period); however, wound noted as rich chlorogenic acid younger

Язык: Английский

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Span 60/Cholesterol Niosomal Formulation as a Suitable Vehicle for Gallic Acid Delivery with Potent In Vitro Antibacterial, Antimelanoma, and Anti-Tyrosinase Activity

Pharmaceuticals, Год журнала: 2023, Номер 16(12), С. 1680 - 1680

Опубликована: Дек. 2, 2023

Natural compounds such as gallic acid (GA) have attracted more attention in cosmetic and pharmaceutical skin care products. However, the low solubility poor stability of GA limited its application. This study aimed to synthesize characterize niosomal dispersion (GAN) investigate potential an optimal formulation a drug delivery system for GA. For this purpose, GAN formulations were synthesized using thin layer evaporation method with different molar ratios Tween 60/Span 60, along constant ratio polyethylene glycol 4000 (PEG-4000) cholesterol methanol chloroform solvent (1:4 v/v). The physicochemical properties nanosystems terms size, zeta potential, entrapment, release, morphology, system-drug interaction characterized methods. In addition, vitro cytotoxicity, anti-tyrosinase activity, antibacterial activity evaluated by MTT assay, spectrophotometric method, micro-well dilution assay. All revealed size 80-276 nm, polydispersity index (PDI) values below 0.35, below-9.7 mV. F2 was selected due smaller high stability. (F2) follows: 1:1 Span 60 1.5 mM release showed biphasic pattern, which fast first 12 h until 58% released. Our results against Escherichia coli Pseudomonas aeruginosa. assay that encapsulation increased effect on B6F10 cancer cells. exhibited potent inhibited melanin synthesis. These findings suggest it can be used dermatological products industries significant antibacterial, anti-melanoma, activity.

Язык: Английский

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