The synthesis and cytotoxic activity of new oleanolic acid derivatives (8a-c and 9a-c) are presented. The obtained compounds are hybrids of oleanolic acid oximes and carboxylic acids containing short alkyl chains linked with nitrogen atom of norbomene-2,3-dicarboximide moieties via the nitrogen atom. The structures of the obtained new compounds (8a-c and 9a-c) were confinmed by spectral data. The derivatives 8a-c and 9a-c were subjected to the MTT assay in order to evaluate their cytotoxic activity towards HeLa, KB, MCF-7, HepG2 and HDF cell lines in comparison to mother compound (oleanolic acid, 1). Among the tested oximes acylated with carboxylic acids containing norbomene-imide moieties, the derivative 8b, with a propionoxyimino linker, exhibited the most advantageous level of cytotoxicity, with IC50 values from 2.75 pM (for MCF-7 cells) to 4.36 pM (for HDF cells).
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Pharmaceutics
December 2024
Division of Pulmonology, Department of Internal Medicine, Pusan National University Yangsan Hospital, Pusan National University School of Medicine, Yangsan 50612, Republic of Korea.
Lung cancer remains a major global health problem because of its high cancer-related mortality rate despite advances in therapeutic approaches. Non-small cell lung cancer (NSCLC), a major subtype of lung cancer, is more amenable to surgical intervention in its early stages. However, the prognosis for advanced NSCLC remains poor, owing to limited treatment options.
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January 2025
Laboratory of Food Chemistry and Technology, School of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
Virgin avocado oil (VAO), treasured for its nutritional and sensory properties, is susceptible to oxidation. To improve its oxidative stability, the feasibility of enrichment with antioxidants from avocado or olive-processing by-products via ultrasound-assisted maceration was explored. Dried, milled avocado (AL), olive leaves (OL), or olive pomace (OP) were ultrasound-macerated with laboratory-extracted VAO at 5, 10, and 20% levels.
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January 2025
Department of Chemistry, Wayne State University, Detroit, Michigan 48202, United States.
Alzheimer's disease (AD) is the most common form of dementia, marked by progressive brain degeneration and cognitive decline. A major pathological feature of AD is the accumulation of hyperphosphorylated tau (p-tau) in the form of neurofibrillary tangles (NFTs), which leads to neuronal death and neurodegeneration. P-tau also induces endoplasmic reticulum (ER) stress and activates the unfolded protein response, causing inflammation and apoptosis.
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Key Laboratory for Animal Disease-Resistance Nutrition of China Ministry of Education, Institute of Animal Nutrition, Sichuan Agricultural University, Chengdu, Sichuan 611130, P. R. China. Electronic address:
Inhibition of appetite is an effective approach to fight obesity. Recently, bile acids have been reported to suppress appetite and alleviate obesity via the Takeda G protein-coupled receptor 5 (TGR5). However, whether the downstream signaling molecule cyclic adenosine monophosphate (cAMP) of TGR5 is involved in this process remains unclear.
View Article and Find Full Text PDFNat Prod Res
January 2025
The College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, China.
An endophytic actinomycetes, , was -isolated from the leaves of Hook. et Arn. Five compounds were separated from the ethyl acetate extract of the fermentation broth of endophytic actinomycetes, and their structures were confirmed by utilising methods such as nuclear magnetic resonance, mass spectrometry, and literature references.
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