Women have been found to be at a higher risk of morbidity and mortality from type 2 diabetes mellitus (T2DM) and asthma. α-Glucosidase inhibitors have been used to treat T2DM, and arachidonic acid 15-lipoxygenase (ALOX15) inhibitors have been suggested to be used as treatments for asthma and T2DM. Compounds that inhibit both enzymes may be studied as potential treatments for people with both T2DM and asthma. This study aimed to determine potential anti-diabetic and anti-inflammatory bioactive hits from Matsum. stem and (Blanco) Merr. & Rolfe bark. A bioassay-guided fractionation framework was used to generate bioactive fractions from stem and bark. Subsequently, dereplication through ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) and database searching was performed to putatively identify the components of one bioactive fraction from each plant. Seven compounds were putatively identified from the stem active fraction, and six of these compounds were putatively identified from this plant for the first time. Nine compounds were putatively identified from the bark active fraction, and seven of these compounds were putatively identified from this plant for the first time. One putative compound from the stem active fraction (corilagin) has been previously reported to have inhibitory activity against both α-glucosidase and 15-lipoxygenase-1. It is suggested that further studies on the potential of corilagin as an anti-diabetic and anti-inflammatory treatment should be pursued based on its several beneficial pharmacological activities and its low reported toxicity.
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http://dx.doi.org/10.3389/fphar.2024.1349725 | DOI Listing |
Chem Biodivers
January 2025
University of Lille: Universite de Lille, UMR BioEcoAgro, 3 rue du Professeur Laguesse, 59800, LILLE, FRANCE.
Parasitic diseases such as trypanosomiasis and leishmaniasis pose significant health challenges in Africa. The Senegalese Pharmacopoeia, known for its many medicinal plants with anti-infectious properties, can be a source of antiparasitic natural products. This study aimed to evaluate the in vitro antiparasitic activities of 33 methanolic extracts from 24 ethnopharmacologically selected plants against Trypanosoma brucei brucei and Leishmania mexicana mexicana, as well as their cytotoxic activities on WI-38 cells.
View Article and Find Full Text PDFCurr Nutr Rep
January 2025
School of Medical Sciences, University of Hyderabad, Hyderabad, Telangana, India.
Purpose Of Review: This review evaluates current research on grape-based interventions and their impact on cognitive and mental health. It also explores the putative mechanisms by which the grape-derived compounds might modulate cognitive function. The growing prevalence of cognitive decline and mental health disorders necessitates exploring novel dietary approaches.
View Article and Find Full Text PDFMetab Brain Dis
January 2025
Department of Pharmacy, Jiangbei Campus of The First Affiliated Hospital of Army Medical University (No. 958 Hospital of PLA Army), Chongqing, 400020, China.
To explore the pharmacological mechanism of Changpu-Yizhi-Wan (CYW) in the treatment of Alzheimer's disease (AD) from the perspective of ferroptosis based on network pharmacology and experimental verification. The Encyclopedia of Traditional Chinese Medicine 2.0 (ETCM2.
View Article and Find Full Text PDFAntimicrob Agents Chemother
January 2025
Department of Pharmacy Practice, College of Pharmacy, Midwestern University, Downers Grove, Illinois, USA.
Vancomycin causes kidney injury by accumulating in the proximal tubule, likely mediated by megalin uptake. Protamine is a putative megalin inhibitor that shares binding sites with heparin and is approved for the treatment of heparin overdose. We employed a well-characterized Sprague-Dawley rat model to assess kidney injury and function in animals that received vancomycin, protamine alone, or vancomycin plus protamine over 5 days.
View Article and Find Full Text PDFJ Med Chem
January 2025
Laboratory of Medicinal Chemistry (Associated Unit to CSIC), Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
Imidazoline receptors (I-IRs) are altered in Alzheimer's disease (AD) patients and are associated with analgesia. I-IRs are not structurally described, and their pharmacological characterization relies on their modulation by highly affine ligands. Herein, we describe the synthesis of (3-phenylcarbamoyl-3,4-dihydro-2-pyrrol-2-yl)phosphonates endowed with relevant affinities for I-IRs in human brain tissues.
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