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Bufalin is a cardiotonic steroid and a key active ingredient of the Chinese medicine . It has significant anti-tumor activity against many malignancies, including hepatocellular carcinoma (HCC). Previous studies have shown that human bodies contain an endogenous bufalin-like substance. This study aimed to confirm whether the endogenous bufalin-like substances is bufalin and further detect the differences between HCC and control groups of endogenous bufalin concentration by the high-performance liquid chromatography coupled tandem mass spectrometry (HPLC-MS/MS). The results confirmed the endogenous bufalin-like substance is bufalin. Totally, 227 serum samples were collected: 54 from HCC patients and 173 from healthy volunteers constituting a control group. Both the test group and the control group contained bufalin in serum, revealing that bufalin is indeed an endogenous substance. The bufalin concentration was 1.3 nM in HCC patients and 5.7 nM in normal people ( < 0.0001). These results indicate that human bodies contain endogenous bufalin, and it may be negatively correlated with the incidence of HCC.
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http://dx.doi.org/10.3389/fonc.2019.01572 | DOI Listing |
Headache
June 2025
College of Osteopathic Medicine, Lake Erie College of Osteopathic Medicine, Bradenton, Florida, USA.
Background: The sodium theory for migraine proposes that excessive sodium pumping into the cerebrospinal fluid (CSF) leads to sodium infiltration into the neural tissue, which can lead to activation and central sensitization of trigeminovascular neurons, predisposing individuals to migraine. Dysregulation of the Na, K-ATPase pump in the choroid plexus is likely to be the primary cause of elevated sodium in the CSF. The identity of intrinsic regulatory molecules that are inhibitors for this pump and their involvement in migraine have been the subject of numerous studies; however, data detailing the involvement of only a few of these regulatory molecules in migraine pathology are published.
View Article and Find Full Text PDFJ Control Release
July 2025
Department of Musculoskeletal Oncology, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China.. Electronic address:
Poor bioavailability and dose-limiting cardiotoxicity persistently hinder the clinical application of bufalin (BF). Conventional BF-based nanoagents have shown promise in tackling these challenges, yet advanced nanostrategies with further improved performance and clinical accessibility still await development. Herein, we introduce a novel cooperative nanoparadigm based on disulfide-linked BF homodimeric prodrugs (SBF) and metal-phenolic networks (MPNs).
View Article and Find Full Text PDFMol Pharmacol
October 2024
Laboratório de Farmacologia Bioquímica e Molecular, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil (P.A.-N., F.N., L.E.M.Q.); Laboratório de Síntese Orgânica e Nanoestruturas, Universidade Federal de São João del-Rei Campus Centro-Oeste Dona
The antitumor effect of cardiotonic steroids (CTS) has stimulated the search for new methods to evaluate both kinetic and thermodynamic aspects of their binding to Na/K-ATPase (IUBMB Enzyme Nomenclature). We propose a real-time assay based on a chromogenic substrate for phosphatase activity (pNPPase activity), using only two concentrations with an inhibitory progression curve, to obtain the association rate ( ), dissociation rate ( ), and equilibrium ( ) constants of CTS for the structure-kinetics relationship in drug screening. We show that changing conditions (from ATPase to pNPPase activity) resulted in an increase of of the cardenolides digitoxigenin, essentially due to a reduction of In contrast, the of the structurally related bufadienolide bufalin increased much less due to the reduction of its partially compensating the decrease of its When evaluating the kinetics of 15 natural and semisynthetic CTS, we observed that both and correlated with (Spearman test), suggesting that differences in potency depend on variations of both and A rhamnose in C3 of the steroidal nucleus enhanced the inhibitory potency by a reduction of rather than an increase of Raising the temperature did not alter the of digitoxin, generating a ΔH ( ) of -10.
View Article and Find Full Text PDFArch Biochem Biophys
September 2024
Laboratory of Epigenetics, Institute of Medical Biology, Polish Academy of Sciences, 93-232, Lodz, Poland. Electronic address:
Cardiac glycosides, derived from plants and animals, have been recognized since ancient times. These substances hinder the function of the sodium-potassium pump within eukaryotic cells. Many reports have shown that these compounds influence the activity of nuclear receptors.
View Article and Find Full Text PDFComput Biol Med
May 2023
Clinical Medical Laboratory Center, Jining First People's Hospital, Jining, 272000, China. Electronic address:
Background: This study aims to evaluate the efficacy and therapeutic mechanism of bufalin on lung adenocarcinoma (LUAD) through a comprehensive strategy integrating network pharmacology, metabolomics and molecular biology verification.
Methods: The putative targets of bufalin were discerned from PharmMapper and Swiss Target Prediction database. LUAD-related targets were obtained by target filtering of GeneCard database and data mining of GEO database.