Diabetes mellitus (DM) is counted among one of the leading challenges in the recent era, and it is a life-threatening disorder. Compound 4-hydroxy 3-methoxy phenylacetone (compound ) was previously isolated from This compound was reacted with -benzylmaleimide to synthesize the targeted compound . The purpose of this research is to exhibit our developed compound 's ability to concurrently inhibit many targets that are responsible for hyperglycemia. Compound was capable of inhibiting α-amylase, α-glucosidase, and protein tyrosine phosphatase 1 B. Even so, outstanding in vitro inhibition was shown by the compound against dipeptidyl peptidase-4 (DPP-4) with an IC value of 0.07 µM. Additionally, by using DPPH in the antioxidant activity, it exhibited good antioxidant potential. Similarly, in the in vivo activity, the experimental mice proved to be safe by treatment with compound . After 21 days of examination, the compound activity pattern was found to be effective in experimental mice. Compound decreased the excess peak of total triglycerides, total cholesterol, AST, ALT, ALP, LDL, BUN, and creatinine in the STZ-induced diabetic mice. Likewise, the histopathology of the kidneys, liver, and pancreas of the treated animals was also evaluated. Overall, the succinimde moiety, such as compound , can affect several targets simultaneously, and, finally, we were successful in synthesizing a multi-targeted preclinical therapy.
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http://dx.doi.org/10.3390/molecules28041589 | DOI Listing |
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab, India.
Neuropathic pain, a challenging condition often associated with diabetes, trauma, or chemotherapy, impairs patients' quality of life. Current treatments often provide inconsistent relief and notable adverse effects, highlighting the urgent need for safer and more effective alternatives. This review investigates marine-derived bioactive compounds as potential novel therapies for neuropathic pain management.
View Article and Find Full Text PDFMikrochim Acta
January 2025
Department of Chemistry, Sardar Vallabhbhai National Institute of Technology, Surat, Gujarat, 395 007, India.
A fluorescence "turn-off-on" nanoprobe is designed by using europium-doped strontium molybdate perovskite quantum dots (Eu:SMO PQDs) for the sequential detection of hypoxanthine (Hx) and Fe. The Eu:SMO PQDs were prepared by the sol-gel method using Sr(NO), (NH)MoO.4HO, and Eu(OCOCH) as precursors.
View Article and Find Full Text PDFMed Oncol
January 2025
Universidad Espíritu Santo, Samborondón, 092301, Ecuador.
Didemnins, a class of cyclic depsipeptides derived from marine organisms exhibit notable anticancer properties. Among them, Didemnin B has been extensively researched for its strong antitumor activity and progression to clinical trials. Nonetheless, its clinical application has been impeded by challenges like poor bioavailability and dose-limiting toxicity.
View Article and Find Full Text PDFClin Transl Oncol
January 2025
Inflammation and Cancer Biology Laboratory, Department of Molecular Biology and Biotechnology, Tezpur University, Tezpur, Assam, 784028, India.
Globally, breast and ovarian cancers are major health concerns in women and account for significantly high cancer-related mortality rates. Dysregulations and mutations in genes like TP53, BRCA1/2, KRAS and PTEN increase susceptibility towards cancer. Here, we discuss the impact of mutations in the key regulatory gene, TP53 and polymorphisms in its negative regulator MDM2 which are reported to accelerate cancer progression.
View Article and Find Full Text PDFChemistry
January 2025
Xi'an Jiaotong University, School of Chemistry, No.28, West Xianning Road, 710049, Xi'an, CHINA.
Due to the diverse chemical and physical properties of functional groups, mild and controllable ligation methods are often required to construct complex drugs and functional materials. To make diverse sets of products with tunable physicochemical properties, it is also useful to employ complimentary ligation methods that adopt the same starting materials. Here, we disclose the efficient and modular synthesis of amides or thioamides through the chemical ligation of acyl silanes with amines, simply by turning a light on or off.
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