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Scopolin (SC-1), scopoletin (SC-2) and isofraxidin (IS-1) are the main active constituents in Chimonanthi Radix. However, the in vivo metabolism of SC-1, SC-2 and IS-1 have not been comprehensively clarified. In this study, the in vivo metabolic profiles of these three coumarins in the rat plasma, urine and feces were analyzed. Ultra-high performance liquid chromatography-quadrupole time of flight mass spectrometry (UHPLC-QTOF-MS/MS) method was applied to characterize the prototypes and metabolites of SC-1, SC-2 and IS-1 in rat feces, urine, and plasma after intravenous administration. A total of 11 metabolites of the three parent compounds were tentatively identified. The main metabolic pathways were analyzed by identification of metabolites, and it was found that these three coumarins underwent multiple in vivo metabolic reactions including glucuronidation, sulfonation, isomerism and reduction. In this study, the analysis of metabolites of three coumarins basically demonstrated their in vivo metabolic process, providing basis for the further pharmacokinetics and pharmacological evaluations of SC-1, SC-2 and IS-1.
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http://dx.doi.org/10.19540/j.cnki.cjcmm.20180815.005 | DOI Listing |
RSC Adv
September 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University Zagazig 44511 Egypt
A novel isatin-thiazole-coumarin hybrid and three isatin-hydantoin hybrids were synthesized and assessed for their α-glucosidase and anticholinesterase inhibitory activities. Moreover, their anticancer properties have been observed against the breast cancer cell lines MCF-7 and MDA-MB-231. The coumarin-containing hybrid exhibited the most potent biological activity across all assays.
View Article and Find Full Text PDFChem Commun (Camb)
September 2025
Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang, Hubei 443002, China.
An unexpected additive-controlled chemodivergent multi-component domino reaction of salicylaldehydes with MBH carbonates has been skillfully developed. Interestingly, acid additives regulate the reaction to form functionalized cyclohexenes or natural coumarin derivatives. Notably, the coumarins were produced a novel phosphine-mediated α-umpolung/Wittig olefination/cycloaddition/lactonization/elimination cascade.
View Article and Find Full Text PDFMini Rev Med Chem
August 2025
Department of Pharmaceutical Chemistry, University Institute of Pharma Sciences and Research, Chandigarh University, Mohali, Punjab, India.
Breast cancer remains the most prevalent cancer among women worldwide, with increasing toxicity and resistance to current therapies posing a serious challenge to healthcare systems. The urgent demand for more effective and safer treatments has highlighted coumarin, a naturally occurring compound with a unique ring structure, due to its promising potential in combating breast cancer. Over the past three decades, numerous synthetic coumarin derivatives have been developed to enhance therapeutic efficacy.
View Article and Find Full Text PDFBiomed Pharmacother
September 2025
Department of Embryology, Reproductive Biomedicine Research Center, Royan Institute for Reproductive Biomedicine, ACECR, Tehran, Iran. Electronic address:
Cyclophosphamide (CTX) is a chemotherapy alkylating agent that causes many side effects, including the occurrence of Premature ovarian failure (POF). The present study aims to investigate the effects of coumarin (COU), as an antioxidant, on apoptosis and oxidative stress in the CTX-induced POF mouse model. NMRI female mice were randomly divided into four groups: 1- The control group received 200 mg/kg normal saline every two days for 6 days.
View Article and Find Full Text PDFCNS Neurosci Ther
September 2025
Center for Stem Cell & Gene Therapies Research & Practice, Kocaeli University, Kocaeli, Turkey.
Aims: Nanoparticle-mediated drug delivery systems are being investigated for the controlled release of drugs to treat neurodegenerative diseases (ND). We aimed to investigate the effects of poly(lactic-co-glycolic acid) nanoparticles (PLGA-NPs) containing different growth factors (GFs) on rat brain-derived neural stem cells (NSCs) in vitro differentiation, providing insights that may contribute to future approaches for treating Parkinson's disease.
Methods: Three different PLGA-NPs loaded with Brain-Derived Neurotrophic Factor (BDNF), Glial-Derived Neurotrophic Factor (GDNF), and Transforming Growth Factor beta 3 (TGF-β3) were developed and characterized in terms of size, zeta potential, encapsulation efficiency, and release profile.