ArticlePharmaceutical research2006
Mechanisms responsible for poor oral bioavailability of paeoniflorin: Role of intestinal disposition and interactions with sinomenine.
Article in Pharmaceutical research, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 114 citations in OpenAlex.
- Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats.Acta pharmacologica Sinica · 2016Trial
- Paeoniflorin: a natural candidate for the treatment of metabolic diseases.Nutrition & metabolism · 2026Review
- Paeoniflorin as a candidate disease-modifying therapy for diabetic peripheral neuropathy: mechanisms, exposure challenges, and translational priorities.Frontiers in pharmacology · 2026Review
- Formation of self-assembly aggregates in traditional Chinese medicine decoctions and their application in cancer treatments.RSC advances · 2025Review
- Article
- Advances of paeoniflorin in depression: the molecular mechanism and formula application.Frontiers in pharmacology · 2025Review
- Traditional Chinese medicine compounds modulate signaling pathways to improve cardiac-related pathology.Frontiers in pharmacology · 2025Review
- Natural terpenoids with therapeutic potential against pulmonary arterial hypertension.Frontiers in pharmacology · 2025Review
- Comparative Evaluation of Nano-Assemblies From Shaoyao Gancao Decoction on Paeoniflorin Bioavailability.International journal of nanomedicine · 2025Article
- Therapeutic potential of natural products in ischemic stroke: targeting angiogenesis.Frontiers in pharmacology · 2025Review
- Paeoniflorin: a review of its pharmacology, pharmacokinetics and toxicity in diabetes.Frontiers in pharmacology · 2025Review
- Article
- Phytochemical Analysis, Biological Activities, and Molecular Docking Studies of Root Extracts fromPharmaceuticals (Basel, Switzerland) · 2024Article
- Role of P-glycoprotein in Regulating the Efficacy, Toxicity and Pharmacokinetics of Yunaconitine.Current drug metabolism · 2024Article
- New Monoterpene Glycoside Paeoniflorin Derivatives as NO and IL-1Molecules (Basel, Switzerland) · 2023Article
- Protective effects of paeoniflorin on cardiovascular diseases: A pharmacological and mechanistic overview.Frontiers in pharmacology · 2023Review
- Integrating pharmacokinetics and network analysis to investigate the mechanism of Moutan Cortex in blood-heat and blood stasis syndrome.Chinese medicine · 2022Article
- Network pharmacology-based analysis and experimental in vitro validation on the mechanism of Paeonia lactiflora Pall. in the treatment for type I allergy.BMC complementary medicine and therapies · 2022Article
- Effects of Tumor-Derived DNA on CXCL12-CXCR4 and CCL21-CCR7 Axes of Hepatocellular Carcinoma Cells and the Regulation of Sinomenine Hydrochloride.Frontiers in oncology · 2022Article
- Therapeutic potential of paeoniflorin in atherosclerosis: A cellular action and mechanism-based perspective.Frontiers in immunology · 2022Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
purposeTo determine the intestinal disposition mechanisms of paeoniflorin, a bioactive glucoside, and to investigate the mechanisms by which sinomenine increases paeoniflorin bioavailability. MATERIALS AND
methodsA single-pass "four-site" rat intestinal perfusion model and a cultured Caco-2 cell model were employed.
resultsIn both model systems, paeoniflorin permeability was poor. In the perfusion model, maximal absorption and metabolism of paeoniflorin occurred in duodenum and jejunum, which were significantly decreased by a glucosidase inhibitor gluconolactone (20 mM). On the other hand, paeoniflorin absorption in terminal ileum increased significantly but its metabolism did not in the presence of sinomenine and cyclosporine A. In the Caco-2 cell model, paeoniflorin was transported 48-fold slower than its aglycone (paeoniflorigenin). Absorptive transport of paeoniflorin was significantly (p < 0.05) increased by sinomenine (38%), verapamil (27%), and cyclosporine A (41%), whereas its secretory transport was significantly (p < 0.01) decreased by sinomenine (50%), verapamil (35%) and cyclosporine A (37%). In contrast, MRP inhibitors MK-571 and leukotriene C4 did not affect transport of paeoniflorin. Lastly, sinomenine was also shown to significantly increase the absorptive transport of digoxin (a prototypical p-glycoprotein substrate) and to significantly decrease its secretory transport.
conclusionsPoor permeation, p-gp-mediated efflux, and hydrolysis via a glucosidase contributed to the poor bioavailability of paeoniflorin. Sinomenine (an inhibitor of the p-gp-mediated digoxin efflux) increased paeoniflorin's bioavailability via the inhibition of p-gp-mediated paeoniflorin efflux in the intestine.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.