Breast Cancer Resistance Protein (BCRP/ABCG2) belongs to the superfamily of ATP binding cassette (ABC) transporters. Characteristic of some of these transporter proteins is the transport of a variety of structurally unrelated substances against a concentration gradient by using the energy of ATP hydrolysis. ABCG2 has been found to confer multidrug resistance (MDR) in cancer cells. Several anticancer drugs have been identified as ABCG2 substrates including mitoxantrone, etoposide and topotecan. As inhibition of the transporter is one of the strategies to overcome MDR, we have synthesized and tested several 3-methoxy flavones and investigated them for their ABCG2 inhibition. Among these, pentamethyl quercetin (compound 4) and pentamethyl morin (compound 5) were found to be fluorescent and hence screened for their possible transport by ABCG2 using confocal microscopy. This study showed that pentamethyl quercetin was far less accumulated in ABCG2 overexpressing MDCK BCRP cells as compared to MDCK sensitive cells, suggesting possible efflux of this compound by ABCG2. Pentamethyl morin showed no visible difference in both cell lines. Based on this observation, we studied several other fluorescent 3-methoxy flavones for their accumulation in ABCG2 overexpressing cells. To confirm the substrate or inhibitor nature of the tested compounds, these compounds were further investigated by ATPase assay. If stimulation of the transporter ATPase activity is detected, one can conclude that the compound is probably a transported substrate. All compounds except pentamethyl morin (compound 5) and tetramethyl quercetin (compound 6) were found to stimulate ATPase activity pointing to possible substrates despite being potent inhibitors of ABCG2.
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http://dx.doi.org/10.1016/j.bbamem.2014.08.003 | DOI Listing |
Molecules
May 2024
Tyrosine Peptide Multiuse Research Group, Department of Anatomy and Convergence Medical Sciences, Institute of Medical Sciences, College of Medicine, Antiaging Bio Cell Factory Regional Leading Research Center, Gyeongsang National University, 15 Jinju-daero 816 Beongil, Jinju 52727, Republic of Korea.
Spinach () is one of the most famous vegetables worldwide, rich in essential metabolites for various health benefits. It is a valuable plant source that has the potential to be a nutraceutical. This study aimed to evaluate the single characteristic marker compound to establish the validation of HPLC-DAD methods applied to the development of a nutraceutical using spinach samples.
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April 2024
Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), Hanoi, Vietnam.
Phytochemical study on the aerial parts of resulted in the isolation of 11 secondary metabolites, including a new caffeoyl quinic acid derivative, 3---caffeoyl-4--acetylquinic acid methyl ester (), a new dihydrobenzofuran neolignan, 3,5-dimethoxy-4-(1″,3″-dihydroxy-2″-propyloxyl)-4',7-epoxy-8,5'-neolignan-4,9,9'-triol () and nine known compounds, methyl 4--coumaroylquinate (), (7*,8*)-3-methoxy-3',7-epoxy-8,4'-oxyneolignan-4,9,9'-triol (), kompasinol A (), lyoniresinol (), schizandriside (), (-)-isolariciresinol 3a---D-xylopyranoside (), lyoniside (), vitexin () and luteolin 4'---glucopyranoside (). Their structures were elucidated using comprehensive spectroscopic methods, including 1D and 2D NMR and HRESI mass spectra. The absolute configurations of and were deduced by electronic circular dichroism spectroscopy.
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January 2024
Natural Products Research Unit, Department of Chemistry, Faculty of Science, Center of Excellence for Innovation in Chemistry, Ministry of Higher Education, Science, Research, and Innovation (Implementation Unit-IU, Khon Kaen University), Khon Kaen University, Khon Kaen, 40002, Thailand.
Chrysin (5,7-dihydroxyflavone, 6) and galangin 3-methyl ether (5,7-dihydroxy-3-methoxy flavone, 7) were obtained from the leaves of Oroxylum indicum (L.) Kurz in 4% and 6% yields, respectively. Both compounds could act as pan-histone deacetylase (HDAC) inhibitors.
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March 2023
Zhuzhou Qianjin Pharmaceutical Co., Ltd., Zhuzhou 412003, China.
Molecules
March 2022
Pharmaceutical Biology Department, School of Pharmacy, Institut Teknologi Bandung, Ganesha 10, Bandung 40132, Indonesia.
Diabetes mellitus is a major health issue that has posed a significant challenge over the years. is a well-known plant that can be potentially used to treat this disease. Therefore, this study aimed to evaluate the inhibitory effect of its root, stem bark, leaves, and flower extracts on alpha-glucosidase using an in vitro inhibition assay to isolate the bioactive compounds and determine their levels in the samples.
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