Berberine and magnolol exert cooperative effects on ulcerative colitis in mice by self-assembling into carrier-free nanostructures.

Publisher: BioMed Central Country of Publication: England NLM ID: 101152208 Publication Model: Electronic Cited Medium: Internet ISSN: 1477-3155 (Electronic) Linking ISSN: 14773155 NLM ISO Abbreviation: J Nanobiotechnology Subsets: MEDLINE

Original Publication: London : BioMed Central, 2003-

Colitis, Ulcerative*/drug therapy ; Berberine*/chemistry ; Berberine*/pharmacology ; Berberine*/therapeutic use ; Lignans*/chemistry ; Lignans*/pharmacology ; Lignans*/therapeutic use ; Biphenyl Compounds*/chemistry ; Nanostructures*/chemistry; Animals ; Mice ; Male ; Dextran Sulfate/chemistry ; Colon/drug effects ; Colon/pathology ; Disease Models, Animal ; Tissue Distribution ; Mice, Inbred C57BL ; Gastrointestinal Microbiome/drug effects ; Biological Availability

The risk of ulcerative colitis (UC) is increasing worldwide with limited success using classical drugs, which has underscored the development of novel agents. Recently, carrier-free molecular assembly has been proven to be an effective drug delivery system, but it has yet to be examined for UC drug development using phytochemicals. Based on traditional Chinese medicine compatibility and potential medicinal uses, a pair of natural compounds, berberine (BBR) and magnolol (MAG), were found to self-assemble into nanostructures in aqueous solutions. Spectral analysis revealed that the assembly mechanisms of BBR and MAG were mediated through charge interactions and π-π stacking. Pharmacokinetic studies and animal imaging showed that BBR-MAG self-assembly (BM) effectively promoted the oral bioavailability and biodistribution of BBR in the colon. BM exhibited superior effects in regulating inflammatory factors, maintaining colon barrier integrity, and regulating gut microbiota in a dextran sulfate sodium salt-induced colitis mouse model. Additionally, no apparent signs of toxicity were observed, suggesting that BM has a favorable safety profile. This study presents a new strategy for UC management and highlights the cooperative effects of combined phytochemicals.
(© 2024. The Author(s).)

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2023M732316 China Postdoctoral Science Foundation; ITC RC/IHK/4/7 Health@InnoHK Initiative Fund of the Hong Kong Special Administrative Region Government; 00151/2020/A3 & 001/2023/ALC and the Science and Technology Development Fund, Macao SAR

Keywords: Berberine; Gut microbiota; Magnolol; Self-assembly; Ulcerative colitis

001E35HGVF (magnolol)
0I8Y3P32UF (Berberine)
0 (Lignans)
0 (Biphenyl Compounds)
9042-14-2 (Dextran Sulfate)

Date Created: 20240903 Date Completed: 20240904 Latest Revision: 20240906

20240906

PMC11373475

10.1186/s12951-024-02804-x

39227962