A new series of 2-imino or 2-oxo-2-chromene-6-sulfonamide derivatives 2-9 with potential anti-diabetic activity were designed and synthesized. The new 6-sulfonamide chromenes were synthesized by reacting 3-formyl-4-hydroxybenzenesulfonyl chloride with activated methylene derivatives in the presence of ammonium acetate as a catalyst. The structure of the products was confirmed by spectroscopic analysis. All the designed derivatives 2-9 were evaluated for their activity against α-amylase and exhibited inhibitory percentage values higher than 93% at 100 μg mL. Additionally, the IC values represented a variable degree of activity with two derivatives 2 and 9 exhibiting the most promising derivative results with IC values of 1.76 ± 0.01 and 1.08 ± 0.02 μM, respectively, compared to Acarbose (IC = 0.43 ± 0.01 μM). Additionally, these derivatives showed potency against the α-glucosidase enzyme with IC values of 0.548 ± 0.02 and 2.44 ± 0.09 μg mL, compared to Acarbose (0.604 ± 0.02 μg mL). Moreover, the PPAR-γ transactivation assay revealed that chromene-6-sulfonamide derivatives 2 and 9 exhibited potential PPAR-γ activity with IC values of 3.152 ± 0.03 and 3.706 ± 0.32 μg mL, respectively, compared to Pioglitazone (4.884 ± 0.29 μg mL). This indicates that these derivatives have insulin sensitivity and glucose metabolism activity. The ADMET prediction showed that these derivatives have an acceptable range of oral bioavailability, drug-likeness, and a safe toxicity profile, including being non-cytotoxic, non-mutagenic, non-immunotoxic, and non-carcinogenic. Finally, computational docking analysis demonstrated the ability of these derivatives to interact with α-amylase, α-glucosidase, and PPAR-γ enzymes, with confirmed successful placement due to good binding energy values and various interactions within the pocket.
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http://dx.doi.org/10.1039/d4ra02143f | DOI Listing |
Anal Methods
January 2025
Department of Food Science and Postharvest Technology, School of Applied Sciences and Technology, Cape Coast Technical University, Cape Coast, Ghana.
This research examined the distinction between organic and conventional mango fruits, chips, and juice using portable near-infrared (NIR) spectroscopy. A comprehensive analysis was conducted on a sample of 100 mangoes (comprising 50 organic and 50 conventional) utilising a portable NIR spectrometer that spans a wavelength range from 900 to 1700 nm. The mangoes were assessed in their entirety and their juice and chip forms.
View Article and Find Full Text PDFEmerg Microbes Infect
January 2025
Key Laboratory of Jiangxi Province for Transfusion Medicine, Department of Blood Transfusion, The First Affiliated Hospital, Jiangxi Medical College, Nanchang University, Nanchang, Jiangxi 330006, China.
The tRNA-derived small RNAs (tsRNAs) are a new class of non coding RNAs, which are stable in body fluids and can be used as potential biomarkers for disease diagnosis. However, the exact value of tsRNAs in the diagnosis of tuberculosis (TB) is still unclear. The objective of the present study was to evaluate the performance of the serum tsRNAs biosignature to distinguish between active TB, healthy controls, latent TB infection, and other respiratory diseases.
View Article and Find Full Text PDFCirc Genom Precis Med
January 2025
Centre for Heart Lung Innovation, University of British Columbia, Vancouver. (K.H., M.A., L.R., Y.L., A.S., H.H., L.R.B., Z.W.L.).
Background: Protein-truncating mutations in the titin gene are associated with increased risk of atrial fibrillation. However, little is known about the underlying pathophysiology.
Methods: We identified a heterozygous titin truncating variant (TTNtv) in a patient with unexplained early onset atrial fibrillation and normal ventricular function.
J Mater Chem B
January 2025
State Key Laboratory of Biopharmaceutical Preparation and Delivery, Chinese Academy of Sciences, Beijing 100190, P. R. China.
Adjuvants can enhance an immunological response, which is an important part of vaccine research. Pickering bubbles have been a mega-hit for biomedical applications, including visualization and targeted drug delivery. However, there have been no studies on Pickering bubbles as an immunological adjuvant, and the special properties and structures of Pickering bubbles may play an important role in immunization.
View Article and Find Full Text PDFInt Health
January 2025
Department of Public Health, Torbat Jam Faculty of Medical Sciences, Torbat Jam, Iran.
Background: Aflatoxin M1 (AFM1) is a derivative of aflatoxin B1 and a significant contaminant of milk and dairy products. In this study, we implemented an umbrella review of all existing systematic reviews and meta-analyzing studies to apprise and summarize the worldwide prevalence and level of AFM1 in milk and dairy products.
Methods: We conducted a systematic review of structured review and meta-analysis articles published in English until January 2024, with no time limit.
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