ArticlePharmaceutical research2008
Intestinal absorption mechanisms of prenylated flavonoids present in the heat-processed Epimedium koreanum Nakai (Yin Yanghuo).
Article in Pharmaceutical research, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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32 citing papers in PubMed, 95 citations in OpenAlex.
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- A Novel Prenylflavonoid Icariside I Ameliorates Estrogen Deficiency-Induced Osteoporosis via Simultaneous Regulation of Osteoblast and Osteoclast Differentiation.ACS pharmacology & translational science · 2023Article
- Icariin: A Promising Natural Product in Biomedicine and Tissue Engineering.Journal of functional biomaterials · 2023Review
- Icariin: A Potential Neuroprotective Agent in Alzheimer's Disease and Parkinson's Disease.Neurochemical research · 2022Review
- Deciphering the myth of icariin and synthetic derivatives in improving erectile function from a molecular biology perspective: a narrative review.Translational andrology and urology · 2022Review
- Icaritin Inhibits Skin Fibrosis through Regulating AMPK and Wnt/β-catenin Signaling.Cell biochemistry and biophysics · 2021Article
- Bioactive Icariin/β-CD-IC/Bacterial Cellulose with Enhanced Biomedical Potential.Nanomaterials (Basel, Switzerland) · 2021Article
- The extraordinary transformation of traditional Chinese medicine: processing with liquid excipients.Pharmaceutical biology · 2020Review
- A comparative study on theDrug delivery · 2020Article
- Improved Pharmacokinetics of Icariin (ICA) within Formulation of PEG-PLLA/PDLA-PNIPAM Polymeric Micelles.Pharmaceutics · 2019Article
- Icariin and Its Metabolites as Potential Protective Phytochemicals Against Alzheimer's Disease.Frontiers in pharmacology · 2019Review
- Comparative Study of Crude and Wine-ProcessingEvidence-based complementary and alternative medicine : eCAM · 2019Article
- Glucuronidation of icaritin by human liver microsomes, human intestine microsomes and expressed UDP-glucuronosyltransferase enzymes: identification of UGT1A3, 1A9 and 2B7 as the main contributing enzymes.Xenobiotica; the fate of foreign compounds in biological systems · 2018Article
- The effect of icariin on bone metabolism and its potential clinical application.Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA · 2018Review
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Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
purposeThe purpose is to determine absorption mechanism of five bioactive prenylated flavonoids (baohuoside I, icariin, epimedine A, B, and C) present in heat-processed Epimedium koreanum Nakai (Yin Yanghuo).
methodsTransport of five prenylated flavonoids present in heat-processed herbs were studied in the human intestinal Caco-2 model and the perfused rat intestinal model.
resultsIn the perfused rat intestinal model, prenylated flavonoids with a monoglucosidic bond (e.g., icariin) was rapidly hydrolyzed into corresponding metabolites (e.g., baohuoside I). In the Caco-2 model, apical to basolateral permeability of a monoglycoside baohuoside I (1.46 x 10(-6) cm/sec) was more than 2 folds greater than four prenylated flavonoids with 2 or more sugar moieties (<0.6 x 10(-6) cm/sec). The slow apical to basolateral transport of baohuoside I was the result of efflux. This efflux was carrier-mediated and active since its transport was vectorial, concentration- and temperature-dependent with activation energies greater than 15 kcal/mol. Efflux of baohuoside I was significantly suppressed by inhibitors of BCRP and MRP2, whereas efflux of icariin was significantly inhibited only by p-glycoprotein inhibitor verapamil. Because YHH is often heat-processed for better efficacy, we determined and found the optimal condition for increasing contents of more bioavailable flavonoids (i.e., baohuoside I) to be 160-170 degrees C for 5-7 min.
conclusionsPoor bioavailability of prenylated flavonoids results from their poor intrinsic permeation and transporter-mediated efflux. Heat processing parameters may be optimized to preserve the herb's bioavailable flavonoids, which help retain and improve its efficacy during processing.
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