A lipophilic oxygen radical absorbance capacity (L-ORAC) assay is an evaluation of the antioxidant capacity of solutions of lipophilic compounds. The concentrations of fluorescein, radical generator, and Trolox standard solutions were optimized to improve the precision of the assay. An interlaboratory study using two antioxidant solutions and three food extracts as test samples conducted in accordance with harmonized protocol demonstrated satisfactory L-ORAC measurements; the intermediate precision relative standard deviations (RSD(int)) ranged from 7.0 to 16.7%, the reproducibility relative standard deviations (RSD(R)) ranged from 14.8 to 19.4%, and the HorRat values ranged from 1.35 to 1.78.
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http://dx.doi.org/10.2116/analsci.32.171 | DOI Listing |
Bioorg Med Chem Lett
January 2025
Department of Natural Medicinal Chemistry, School of Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009 China. Electronic address:
Novel lipophilic cationic derivatives including quaternary ammonium salt and triphenylphosphine series were designed and synthesized using diosgenin (1) and sarsasapogenin (2) as substrates to improve the cytotoxicity and selectivity. Most of the derivatives showed higher cytotoxicity against all cancer cell lines tested, compound 13 exhibited the most superior activity against A549 cells with an IC value of 0.95 μM, which was 34-fold of diosgenin.
View Article and Find Full Text PDFBioorg Chem
December 2024
Pharmacology Division, CSIR- Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Ursolic acid (3-hydroxy-urs-12-ene-28-oic acid, UA) is a pentacyclic triterpene present in numerous plants, fruits and herbs and exhibits various pharmacological effects. However, UA has limited clinical applicability since it is classified as BCS class IV molecule, characterized by low solubility, low oral bioavailability and low permeability. In the present study, UA was isolated from the biomass marc of Lavandula angustifolia and was structurally modified by an induction of indole ring at the C-3 position and amide group at the C-17 position with the aim to enhance its pharmacological potential.
View Article and Find Full Text PDFAdv Healthc Mater
December 2024
Department of Biomedical Sciences, Chonnam National University Medical School, Hwasun, 58128, South Korea.
One of the most significant challenges for image-guided cancer-targeted therapy is to develop multifunctional optical contrast agents enabling simultaneous targeting and therapy. Herein, a feasible strategy is based on the incorporation of therapeutic moieties into the non-delocalized structure of polymethine indocyanines, known as the "structure-inherent targeting" concept. By possessing a rigid chloro-cyclohexenyl ring in the heptamethine cyanine backbone, a new type of multifunctional near-infrared fluorescent dye, Ph790H, that targets tumor without the need for additional targeting ligands is synthesized.
View Article and Find Full Text PDFRedox Biol
December 2024
Radiation Immuno-Oncology Group, Central Institute for Translational Cancer Research (TranslaTUM), TUM School of Medicine and Health, Klinikum rechts der Isar, Technical University of Munich (TUM), Munich, Germany; Department of Radiation Oncology, TUM School of Medicine and Health, Klinikum rechts der Isar, Technical University of Munich (TUM), Munich, Germany. Electronic address:
Despite advances in multimodal therapy approaches such as resection, chemotherapy and radiotherapy, the overall survival of patients with grade 4 glioblastoma (GBM) remains extremely poor (average survival time <2 years). Altered lipid metabolism, which increases fatty acid synthesis and thereby contributes to radioresistance in GBM, is a hallmark of cancer. Therefore, we explored the radiosensitizing effect of the clinically approved, lipid-lowering drug fenofibrate (FF) in different GBM cell lines (U87, LN18).
View Article and Find Full Text PDFChemistry
December 2024
Enamine Ltd., Winston Churchill Street 78, 02094, Kyїv, Ukraine.
A comprehensive study on the physicochemical properties of gem-fluorinated O-heterocyclic substituents is reported. Systematic additive effects of introducing O- and gem-CF group introduction on acidic properties (pK) of the corresponding carboxylic acids/protonated primary amines were demonstrated. The impact of the O/CF moieties on lipophilicity (LogP) was found to be complex; significant mutual influence of the corresponding polar moieties governed the compound's overall properties in this case.
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