ArticleBioscience reports2019
Mitochondrial membrane potential played crucial roles in the accumulation of berberine in HepG2 cells.
Article in Bioscience reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 21 citations in OpenAlex.
- A novel photosensitizer berberine derivative B12 induces apoptosis and suppresses HIF-1α expression in colorectal cancer cells via mitochondria-to-nucleus sequential-targeting.Acta pharmacologica Sinica · 2026Article
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- Berberine dissociates mitochondrial complex I by SIRT3-dependent deacetylation of NDUFS1 to improve hepatocellular glucose and lipid metabolism.Science China. Life sciences · 2025Article
- Targeted co-delivery nanosystem based on methotrexate, curcumin, and PAMAM dendrimer for improvement of the therapeutic efficacy in cervical cancer.Scientific reports · 2025Article
- Enhancing of Rabbit Sperm Cryopreservation with Antioxidants Mito-Tempo and Berberine.Antioxidants (Basel, Switzerland) · 2024Article
- Dual Role of Vitamin C-Encapsulated Liposomal Berberine in Effective Colon Anticancer Immunotherapy.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Tissue distribution and integrated pharmacokinetic properties of major effective constituents of oralFrontiers in pharmacology · 2022Article
- Silibinin Promotes Cell Proliferation Through Facilitating G1/S Transitions by Activating Drp1-Mediated Mitochondrial Fission in Cells.Cell transplantationArticle
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Berberine is a natural alkaloid that has antineoplastic effects. However, in hepatoma cells like HepG2, the expressions of uptake transporters are minimal but efflux transporters are relatively high. Hence, how berberine enters and reaches a cytocidal concentration remains to be elucidated. In the present study, we revealed the accumulation mechanism of berberine in HepG2 cells. Cell organelles were isolated based on differential centrifugation; berberine concentration was measured using a liquid chromatography-tandem mass chromatography method or flow cytometry. Subcellular distribution of berberine was observed using a laser scanning confocal microscopy. The results showed that berberine was concentration-, temperature-, and time-dependently taken up and accumulated in HepG2 cells. Membrane drug transporters and cell membrane potential had limited effects in berberine uptake. However, qualitative and quantitative studies showed that berberine was enriched in the mitochondria; inhibition of mitochondrial membrane potential (MMP) by carbonyl cyanide 3-chlorophenylhydrazone (CCCP) significantly decreased the intracellular berberine by up to 70%. More importantly, MMP not only significantly enhanced berberine uptake driven by cell membrane potential (
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