Glioblastoma (GB) is an aggressive brain malignancy characterized by its invasive nature. Current treatment has limited effectiveness, resulting in poor patients' prognoses. β-Amino carbonyl (β-AC) compounds have gained attention due to their potential anticancerous properties. assays were performed to evaluate the effects of an in-house synthesized β-AC compound, named SHG-8, upon GB cells. Small RNA sequencing (sRNA-seq) and biocomputational analyses investigated the effects of SHG-8 upon the miRNome and its bioavailability within the human body. SHG-8 exhibited significant cytotoxicity and inhibition of cell migration and proliferation in U87MG and U251MG GB cells. GB cells treated with the compound released significant amounts of reactive oxygen species (ROS). Annexin V and acridine orange/ethidium bromide staining also demonstrated that the compound led to apoptosis. sRNA-seq revealed a shift in microRNA (miRNA) expression profiles upon SHG-8 treatment and significant upregulation of miR-3648 and downregulation of miR-7973. Real-time polymerase chain reaction (RT-qPCR) demonstrated a significant downregulation of , an oncogene and a player in the Wnt/β-catenin pathway. analysis indicated SHG-8's potential to cross the blood-brain barrier. We concluded that SHG-8's inhibitory effects on GB cells may involve the deregulation of various miRNAs and the inhibition of .
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http://dx.doi.org/10.1021/acsomega.4c02991 | DOI Listing |
Nat Prod Bioprospect
January 2025
Consejo Nacional de Investigaciones Científicas y Técnicas, Suipacha 531, S2002LRK, Rosario, Argentina.
Chemically engineered extracts represent a promising source of new bioactive semi-synthetic molecules. Prepared through direct derivatization of natural extracts, they can include constituents enriched with elements and sub-structures that are less common in natural products compared to drugs. Fourteen such extracts were prepared through sequential reactions with hydrazine and a fluorinating reagent, and their α-glucosidase inhibition properties were compared.
View Article and Find Full Text PDFSci Bull (Beijing)
December 2024
State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200032, China. Electronic address:
Divergent synthesis of valuable molecules through common starting materials and metal catalysis represents a longstanding challenge and a significant research goal. We here describe chemodivergent, highly enantio- and regioselective nickel-catalyzed reductive and dehydrogenative coupling reactions of alkynes, aldehydes, and silanes. A single chiral Ni-based catalyst is leveraged to directly prepare three distinct enantioenriched products (silyl-protected trisubstituted chiral allylic alcohols, oxasilacyclopentenes, and silicon-stereogenic oxasilacyclopentenes) in a single chemical operation.
View Article and Find Full Text PDFPlant Physiol Biochem
January 2025
Centre for Nanobiotechnology, Vellore Institute of Technology, Vellore, Tamil Nadu, India. Electronic address:
The accumulation of disposable face masks (DFMs) has become a significant threat to the environment due to extensive use during the COVID-19 pandemic. In this research, we investigated the degradation of DFMs after their disposal in landfills. We replicated the potential degradation process of DFMs, including exposure to sunlight before subjecting them to synthetic landfill leachate (LL).
View Article and Find Full Text PDFJ Am Soc Mass Spectrom
January 2025
Suntory Institute for Bioorganic Research, Suntory Foundation for Life Sciences, 8-1-1 Seikadai, Seika-Cho, Soraku-Gun, Kyoto 619-0284 Japan.
In this study, we analyzed purine derivatives using multimatrix variation matrix-assisted laser desorption ionization mass spectrometry (MALDI MS) with α-cyano-4-hydroxycinnamic acid (CHCA), 1,5-diaminonaphtalene (DAN), 5-formylsalicylic acid (FSA), and 5-nitrosalicylic acid (NSA) as matrices. Further, we focused on the abstraction/attachment of hydrogen from/to analytes and detected [M - H], [M + 2H] and/or [M + 3H] in MALDI MS spectra of compounds containing nitrogen and/or carbonyl oxygen. Although [M - H] generation of purine compounds in MALDI MS with conventional matrices was challenging, NSA-MALDI MS effectively yielded the [M - H]species of purine derivatives compared with CHCA, FSA, and DAN, and the [M - H]/[M + H] ratios reflected their structures, such as the substituting groups and positions.
View Article and Find Full Text PDFArch Toxicol
January 2025
School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi, 530004, People's Republic of China.
Over the past decade, fentanyl-type new psychoactive substances (F-NPS) have emerged as the most representative synthetic opioids in third-generation drugs. These substances are characterized by their "low" fatal dose and parent drug levels in biological matrices, "fast" rates of derivatization and metabolism, and "many" derivatization sites and analogs. The low levels of parent fentanyl NPS in biological matrices complicate their detection, necessitating the use of characteristic metabolites as biomarkers for forensic analysis.
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