A natural ursolic compound, 2β, 3β, 23-trihydroxy-urs-12-ene-28-olic acid (TUA) was isolated from the root of Actinidia chinensis Planch (A. chinensis Radix). Since a large number of triterpenoid compound has marked anticancer effects toward various types of cancer cell lines in vitro, this study was carried out to investigate the anticancer effect of TUA in non-small cell lung cancer cells (NSCLCCs) and the underlying apoptotic mechanism of TUA was examined in NCI-H460 cell lines. Cell proliferation, apoptosis and cell cycle were measured using a cell counting kit-8 (CCK-8) assay and flow cytometry, respectively. The activity of transcription factor NF-κB was determined by EMSA method. The expression of apoptosis- and proliferation-related proteins was determined by western blotting. The effect of TUA on NF-κB mRNA expression in NCI-H460 cells was detected by RT-PCR. TUA significantly suppressed the viability of NCI-H460 cells. Also, TUA significantly increased the sub G1 population by cell cycle analysis and in a concentration dependent manner in NCI-H460 cells. Such an effect was accompanied by p65 (NF-κB subunit) inactivation by an inhibition of IκBα phosphorylation, and by inhibition of p65 mRNA expressions. Consistently Overall, our findings suggest that TUA induces apoptosis via inhibition of NF-κB (p65) expression level and activation of IκBα in NCI-H460 cells as a potent anticancer candidate for lung cancer treatment.
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http://dx.doi.org/10.1016/j.cbi.2015.06.038 | DOI Listing |
Phytochemistry
January 2025
Research Center for Marine Drugs, Clinical Pharmacy College, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China. Electronic address:
Four previously undescribed cyclic peptides, reniochpeptins A-D (1-4), were isolated from the marine sponge Reniochalina sp. Their structures were elucidated through comprehensive spectroscopic analyses and a modified advanced Marfey's method. This method utilized ultra-high-performance liquid chromatography coupled with tandem multiple reaction monitoring mass spectrometry, employing a CORTECS T column to achieve simultaneous separation of derivatized -Leu, -Ile, -allo-Ile, -Leu, -Ile, and -allo-Ile within 25 minutes in a single analytical run.
View Article and Find Full Text PDFEur J Pharmacol
February 2025
i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, 4200-135, Porto, Portugal; Cancer Drug Resistance Group, IPATIMUP - Institute of Molecular Pathology and Immunology, University of Porto, 4200-135, Porto, Portugal; FFUP - Faculty of Pharmacy of the University of Porto, 4050-313, Porto, Portugal. Electronic address:
Multidrug resistance (MDR) is a major challenge in cancer research. Collateral sensitizers, compounds that exploit the enhanced defense mechanisms of MDR cells as weaknesses, are a proposed strategy to overcome MDR. Our previous work reported the synthesis of two novel Isoquinolinequinone (IQQ) N-oxides that induce collateral sensitivity in MDR ABCB1-overexpressing non-small cell lung cancer (NSCLC) and colorectal cancer cells.
View Article and Find Full Text PDFPlants (Basel)
December 2024
Research Centre for Pharmaco-Toxicological Evaluation, Victor Babes University of Medicine and Pharmacy, Eftimie Murgu Square, No. 2, 300041 Timisoara, Romania.
The current study proposes the in vitro and in silico anticancer evaluation of clove ( L.) essential oil (CEO). The steam hydrodistillation method used yielded 10.
View Article and Find Full Text PDFDalton Trans
January 2025
School of Chemical Sciences, The University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
[M(arene)(HQ)Cl] complexes (M = Ru/Os/Rh/Ir; HQ = 8-hydroxyquinoline) have shown promise as anticancer agents. To assess the effect of conjugating biotin (vitamin B7) to such compounds and improve their tumor-targeting ability through interaction with the sodium-dependent multivitamin transporter (SMVT), the chlorido co-ligand was exchanged with biotinylated 6-aminoindazole. The complexes were characterized by NMR spectroscopy and mass spectrometry, and purity was determined by elemental analysis.
View Article and Find Full Text PDFJ Transl Med
December 2024
Department of Pharmacy, Honghui Hospital, Xi'an Jiaotong University, Xi'an, 710054, China.
Despite the proven inhibitory effects of drugs targeting vascular endothelial growth factor receptor 2 (VEGFR2) on solid tumors, including non-small cell lung cancer (NSCLC), the development of anti-NSCLC drugs solely targeting VEGFR2 still faces risks such as off-target effects and limited efficacy. This study aims to develop a novel fingerprint-enhanced graph attention convolutional network (FnGATGCN) model for predicting the activity of anti-NSCLC drugs. Employing a multimodal fusion strategy, the model integrates a feature extraction layer that comprises molecular graph feature extraction and molecular fingerprint feature extraction.
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