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Small Molecular Oligopeptides Adorned with Tryptophan Residues as Potent Antitumor Agents: Design, Synthesis, Bioactivity Assay, Computational Prediction, and Experimental Validation.
J Chem Inf Model
January 2025
Key Laboratory for Photonic and Electronic Bandgap Materials, Ministry of Education, College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin 150025, China.
Tryptophan participates in important life activities and is involved in various metabolic processes. The indole and aromatic binuclear ring structure in tryptophan can engage in diverse interactions, including π-π, π-alkyl, hydrogen bonding, cation-π, and CH-π interactions with other side chains and protein targets. These interactions offer extensive opportunities for drug development.
View Article and Find Full Text PDFExploring the Key Indicators for Off-Flavor in Industrial Osmanthus Absolute through Sensomics and Chemometric Approaches.
J Agric Food Chem
January 2025
Zhengzhou Tobacco Research Institute of CNTC, Fengyang Street #2, Zhengzhou, Henan 450001, PR China.
The occurrence of off-flavor in osmanthus absolutes has emerged as a significant concern that could hinder its broad market acceptance and associated economic development. In this study, key off-flavor molecules in industrial osmanthus absolute were identified through sensomics and chemometric approaches. A group of 10 off-flavor (OF) samples, eliciting smoky/phenolic, sweaty/sour, and spicy odors, were compared with 10 pleasant aroma (PA) samples through various analyses, including overall aroma assessment, comprehensive chemical profiling, aroma extract dilution analysis (AEDA), and orthogonal partial least-squares-discriminant analysis (OPLS-DA).
View Article and Find Full Text PDFEllagitannins from Pomegranate Flower with Whitening and Anti-skin Photoaging Effect.
Chem Biodivers
January 2025
Yatsen Global Innovation R&D Center, Yatsen Global Innovation R&D Center, No. 11 Building, No. 210, Wenshui Road, Jingan District, Shanghai, CHINA.
A new depside glucoside rosarugoside E (1), together with four known compounds punicalagin (2), corilagin (3), granatin B (4) and ellagic acid (5) were isolated from the ethanol extract of pomegranate (Punica granatum L.) flower. Their structures were identified based on careful analysis of various spectral data including UV, IR, HR-ESI-MS, 1D and 2D NMR.
View Article and Find Full Text PDFPhytosome-Enhanced Secondary Metabolites for Improved Anticancer Efficacy: Mechanisms and Bioavailability Review.
Drug Des Devel Ther
January 2025
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang, 45363, Indonesia.
Purpose: Phytosome technology, an advanced lipid-based delivery system, offers a promising solution for enhancing the bioavailability and therapeutic efficacy of secondary metabolites, particularly in cancer treatment. These metabolites, such as flavonoids, terpenoids, and alkaloids, possess significant anticancer potential but are often limited by poor solubility and low absorption. This review aims to investigate how phytosome encapsulation improves the pharmacokinetic profiles and anticancer effectiveness of these bioactive compounds.
View Article and Find Full Text PDFA 3D Model of the Human Lung Airway for Evaluating Permeability of Inhaled Drugs.
ACS Pharmacol Transl Sci
January 2025
Division of Applied Regulatory Science, Office of Clinical Pharmacology, Office of Translational Sciences, Center for Drug Evaluation and Research, United States Food and Drug Administration (FDA), Silver Spring, Maryland 20993, United States.
Current in vitro cell-based methods, relying on single cell types, have structural and functional limitations in determining lung drug permeability, which is a contributing factor affecting both local and systemic drug levels. To address this issue, we investigated a 3D human lung airway model generated using a cell culture insert, wherein primary human lung epithelial and endothelial cells were cocultured at an air-liquid interface (ALI). To ensure that the cell culture mimics the physiological and functional characteristics of airway tissue, the model was characterized by evaluating several parameters such as cellular confluency, ciliation, tight junctions, mucus-layer formation, transepithelial electrical resistance, and barrier function through assaying fluorescein isothiocyanate-dextran permeability.
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