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In this study, a bioguided fractionation of extract was performed by chromatographic methods. It yielded one new -abietane diterpene, mutabilol (), and three known abietanes, coleon-U-quinone (), 8α,9α-epoxycoleon-U-quinone (), and coleon U (). The abietane diterpenoid was also tentatively identified using HPLC-MS/MS. Moreover, the extract profile and quantification of each isolated compound were determined by HPLC-DAD. Compound was the major compound in the extract. Compounds - were found to be selective toward cancer cell lines and were able to inhibit P-glycoprotein (P-gp) activity in NCI-H460/R cells at longer exposure of 72 h and consequently revert doxorubicin (DOX) resistance in subsequent combined treatment. None of the compounds influenced the P-gp expression in NCI-H460/R cells, while the extract significantly increased it.
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http://dx.doi.org/10.1021/acsmedchemlett.1c00711 | DOI Listing |
Eur 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,
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 PDFCancer Drug Resist
May 2024
i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, Porto 4200-135, Portugal.
Plants (Basel)
December 2023
University of Belgrade-Faculty of Chemistry, Studentski trg 12-16, 11000 Belgrade, Serbia.
ssp. Necker (ES) and (EC) with a habitat in the Deliblato Sands were the subject of this examination. The latexes of these so far insufficiently investigated species of the genus are used in traditional medicine for the treatment of wounds and warts on the skin.
View Article and Find Full Text PDFDiagnostics (Basel)
December 2023
Department of Neurobiology, Institute for Biological Research "Siniša Stanković"-National Institute of the Republic of Serbia, University of Belgrade, Bulevar Despota Stefana 142, 11108 Belgrade, Serbia.
Lung cancer remains the leading cause of cancer death globally, with non-small cell lung cancer (NSCLC) accounting for the majority of cases. Multidrug resistance (MDR), often caused by ATP-binding cassette (ABC) transporters, represents a significant obstacle in the treatment of NSCLC. While genetic profiling has an important role in personalized therapy, functional assays that measure cellular responses to drugs are gaining in importance.
View Article and Find Full Text PDFEur J Med Chem
December 2023
Centro de Química Estrutural, Institute of Molecular Sciences, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016, Lisboa, Portugal. Electronic address:
A family of ten novel ruthenium(II)-cyclopentadienyl organometallics of general formula [Ru(η-CH)(N,N)(PPh(CHCOOR)][CFSO] (1-10) in which (N,N) = 4,4'-R'-2,2'-bipyridyl (R = -H or -CHCHOH; R' = -H, -CH, -OCH, -CHOH, and -CH-biotin) was prepared from [Ru(η-CH)(PPh(CHCOOH))Cl]. All compounds were fully characterized by means of several spectroscopic and analytical techniques, and the molecular structures of [Ru(η-CH)(PPh(CHCOOH))Cl], 1, 3 and 4 have been additionally studied by single-crystal X-ray diffraction. The anticancer activity of all compounds was evaluated in sensitive and multidrug-resistant counterpart cell lines from human colorectal cancer (Colo 205 and Colo 320) and non-small cell lung cancer NSCLC (A549, NCI-H460 versus NCI-H460/R) as well.
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