B-ring unsubstituted flavones (of which the most widely known are chrysin, baicalein, wogonin, and oroxylin A) are 2-phenylchromen-4-one molecules of which the B-ring is devoid of any hydroxy, methoxy, or other substituent. They may be found naturally in a number of herbal products used for therapeutic purposes, and several have been designed by researchers and obtained in the laboratory. They have generated interest in the scientific community for their potential use in a variety of pathologies, and understanding their pharmacokinetics is important for a grasp of their optimal use. Based on a comprehensive survey of the relevant literature, this paper examines their absorption (with deglycosylation as a preliminary step) and their fate in the body, from metabolism to excretion. Differences among species (inter-individual) and within the same species (intra-individual) variability have been examined based on the available data, and finally, knowledge gaps and directions of future research are discussed.
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http://dx.doi.org/10.3390/pharmaceutics11080370 | DOI Listing |
Biology (Basel)
December 2024
Department of Pharmaceutical Biology and Biotechnology, Division Pharmaceutical Biology and Botany, Wroclaw Medical University, Borowska 211A, 50-556 Wroclaw, Poland.
Georgi is a valuable medicinal plant of the family. Its roots have been used in Traditional Chinese Medicine (under the name Huang-qin) since antiquity and are nowadays included in Chinese and European Pharmacopoeias. It is abundant in bioactive compounds which constitute up to 20% of dried root mass.
View Article and Find Full Text PDFEur J Med Chem
October 2024
School of Pharmacy and Pharmaceutical Sciences, Panoz Institute and Trinity Biomedical Sciences Institute, Trinity College Dublin, 152 - 160 Pearse St, Dublin 2, D02 R590, Ireland. Electronic address:
Biocatalysis is a valuable industrial approach in active pharmaceutical ingredient (API) manufacturing for asymmetric induction and synthesis of chiral APIs. Herein, we investigated synthesis of a panel of microtubule-destabilising antiproliferative β-lactam enantiomers employing a commercially available immobilised Candida antarctica lipase B enzyme together with methanol and MTBE. The β-lactam ring remained intact during chiral kinetic resolution reactions, plausibly due to a bulky N-1 phenyl substituent on the β-lactam ring substrate.
View Article and Find Full Text PDFFront Plant Sci
March 2023
Department of Pharmaceutical Biology and Biotechnology, Division of Pharmaceutical Biology and Botany, Wroclaw Medical University, Wroclaw, Poland.
Unlabelled: Georgi is a valuable medicinal plant of the family. The roots, , are valued in the traditional medicine of East Asia and are also listed in several pharmacopeias, such as the Chinese and European versions. The roots contain a high amount of flavones, such as baicalein, wogonin and their glucuronides, baicalin and wogonoside, respectively, with rare structures of unsubstituted B-ring.
View Article and Find Full Text PDFInt J Mol Sci
March 2022
School of Ecosystem and Forest Sciences, The University of Melbourne, Parkville, VIC 3010, Australia.
Flavonoids are ubiquitous polyphenolic compounds in plants, long recognised for their health-promoting properties in humans. Methylated flavonoids have received increasing attention due to the potential of methylation to enhance medicinal efficacy. Recently, species with high levels of the -methylated flavanone pinostrobin have been identified.
View Article and Find Full Text PDFMolecules
October 2021
Department of Pharmacology and Toxicology, Wrocław University of Environmental and Life Sciences, C.K. Norwida 31, 50-375 Wrocław, Poland.
Background: The study investigated four flavanone-derived γ-oxa-ε-lactones: a parent unsubstituted compound and its three derivatives with the methoxy group in positions 2', 4' and 8. Our objective was to find out if the introduction of the methoxy group into the aromatic ring affects in vitro anti-tumor potency of the investigated lactones.
Methods: Cytotoxic and pro-apoptotic effects were assessed with cytometric tests with propidium iodide, annexin V, and Western blot techniques.
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