The putative active metabolite of aeruginascin, a naturally occurring tryptamine of "magic mushrooms," has been synthesized and structurally characterized. Competitive radioligand binding assays demonstrate that it has a high affinity at human serotonin receptors 5-HT, 5-HT, and 5-HT, though it does not bind at the 5-HT receptor, where activity was previously predicted.
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http://dx.doi.org/10.1021/acsomega.0c02208 | DOI Listing |
Clin Pharmacokinet
January 2025
Facultés de Médecine et de Pharmacie de Lyon, Univ Lyon, Université Claude Bernard Lyon 1, Lyon, France.
Background And Objective: Limited information is available on the pharmacokinetics of rifampicin (RIF) along with that of its active metabolite, 25-deacetylrifampicin (25-dRIF). This study aimed to analyse the pharmacokinetic data of RIF and 25-dRIF collected in adult patients treated for tuberculosis.
Methods: In adult patients receiving 10 mg/kg of RIF as part of a standard regimen for drug-susceptible pulmonary tuberculosis enrolled in the Opti-4TB study, plasma RIF and 25-dRIF concentrations were measured at various occasions.
Z Naturforsch C J Biosci
January 2025
Armauer Hansen Research Institute, P.O. Box 1005, Addis Ababa, Ethiopia.
, known as "Dhumuugaa" in Afan Oromo and "Sensel" or "Smiza" in Amharic, is traditionally used to treat ailments such as scabies, fever, asthma, diarrhea, malaria, and more. This study explored the chemical composition and biological activity of its extracts and isolated compounds. The essential oils were extracted using the hydrodistillation method, and their chemical composition was evaluated using GC-MS.
View Article and Find Full Text PDFCurr Top Dev Biol
January 2025
Department of Pharmaceutics, School of Pharmacy, University of Washington.
The active metabolite of vitamin A, all-trans-retinoic acid (atRA), is critical for maintenance of many cellular processes. Although the enzymes that can synthesize and clear atRA in mammals have been identified, their tissue and cell-type specific roles are still not fully established. Based on the plasma protein binding, tissue distribution and lipophilicity of atRA, atRA partitions extensively to lipid membranes and other neutral lipids in cells.
View Article and Find Full Text PDFJ Pharm Sci
January 2025
Clinical Pharmacology, Pharmacometrics & Bioanalysis, Bristol Myers Squibb, Princeton, NJ, USA.
Iberdomide, a novel potent cereblon E3 ligase modulator, is under investigation for multiple myeloma. This study assessed how renal impairment (RI) affects iberdomide pharmacokinetics (PK). Twenty-six subjects with varying renal function, including those with severe renal impairment and those requiring intermittent hemodialysis (IHD), received a single oral 1 mg dose of iberdomide.
View Article and Find Full Text PDFPlanta Med
January 2025
Instituto de Química, Departamento de Productos Naturales, Universidad Nacional Autónoma de México, Mexico City, Mexico.
An approach combining enzymatic inhibition and untargeted metabolomics through molecular networking was employed to search for human recombinant full-length protein tyrosine phosphatase 1B (PTP1 B) inhibitors from a collection of 66 mangrove-associated fungal taxa. This strategy prioritized two strains (IQ-1612, section , and IQ-1620, section ) for further studies. Chemical investigation of strain IQ-1612 resulted in the isolation of a new nonanolide derivative, roseoglobuloside A (1: ), along with two known metabolites (2: and 3: ), whereas strain IQ-1620 led to the isolation of four known naphtho-γ-pyrones and one known diketopiperazine (4: -8: ).
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