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Article Abstract
Introduction: Postmenopausal osteoporosis, a skeletal disorder induced by estrogen deficiency, is commonly addressed in clinical practice through the use of Cuscutae semen and its compound formulations, owing to their significant therapeutic efficacy.
Objective: This study sought to systematically identify bioactive compounds present in Cuscutae semen that interact with estrogen receptor β (ESR2) using Affinity Ultrafiltration combined with Ultra-Performance Liquid Chromatography-Quadrupole-Orbitrap Mass Spectrometry (UPLC-QE-Orbitrap-MS) to find possible therapy options for PMOP.
Methods: The Cuscutae semen extract was fractionated using a C18 column to obtain fractions based on distinct polarity. Preliminary evaluation of anti-osteoporotic activity was conducted in MC3T3-E1 cells by assessing osteoprotegerin (OPG) expression. Affinity Ultrafiltration integrated with UPLC-QE-Orbitrap-MS was utilized to screen for ligands binding to ESR2, followed by molecular docking to validate the interaction mechanisms. The osteogenic effects of the identified compounds were further confirmed through CCK-8 proliferation assays, OPG quantification, and alkaline phosphatase (ALP) activity analysis.
Results: The fraction of Cuscutae semen extract eluted with 100% methanol exhibited significant anti-osteoporotic activity. Three flavonoids-Astragalin, Isorhamnetin, and Quercitrin-that interact with ESR2 were successfully identified. In vitro validation demonstrated the efficacy of these compounds.
Conclusion: This study presents a comprehensive strategy that integrates Affinity Ultrafiltration, UPLC-QE-Orbitrap-MS, and bioactivity validation to efficiently identify ESR2-targeted postmenopausal osteoporosis compounds in Cuscutae Semen. The findings offer both theoretical and empirical foundations for the development of innovative therapeutics for postmenopausal osteoporosis.
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| http://dx.doi.org/10.1002/pca.70018 | DOI Listing |
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