Cited by 1,391Berberine and alkaloids researchCholesterol and Lipid MetabolismLipoproteins and Cardiovascular Health

Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins

Kong, Weijia, Wei, Jing, Abidi, Parveen, Lin, Meihong, Inaba, Satoru, Li, Cong, Wang, Yanling, Wang, Zizheng +8 more·2004·Nature Medicine

Abstract

We identify berberine (BBR), a compound isolated from a Chinese herb, as a new cholesterol-lowering drug. Oral administration of BBR in 32 hypercholesterolemic patients for 3 months reduced serum cholesterol by 29%, triglycerides by 35% and LDL-cholesterol by 25%. Treatment of hyperlipidemic hamsters with BBR reduced serum cholesterol by 40% and LDL-cholesterol by 42%, with a 3.5-fold increase in hepatic LDLR mRNA and a 2.6-fold increase in hepatic LDLR protein. Using human hepatoma cells, we show that BBR upregulates LDLR expression independent of sterol regulatory element binding proteins, but dependent on ERK activation. BBR elevates LDLR expression through a post-transcriptional mechanism that stabilizes the mRNA. Using a heterologous system with luciferase as a reporter, we further identify the 5' proximal section of the LDLR mRNA 3' untranslated region responsible for the regulatory effect of BBR. These findings show BBR as a new hypolipidemic drug with a mechanism of action different from that of statin drugs.

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Crossref · 10.1038/nm1135

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2 of the 40 references couldn’t be matched to a known paper.

Research works printed but not linked: 4

  1. Cho, E. Berberini hydrochloride. in Pharmacopoeia of the People's Republic of China 2, 437–439 (1990).
  2. Luo, L.J. Experience of berberine in the treatment of diarrhea. Chin. J. Med. 41, 452–455 (1955).
  3. Liu . Berberine. Altern. Med. Rev. 5, 175–177 (2000).
  4. Zhao, S.P. Etiology and diagnosis of hyperlipidemia. Clinical Serum and Lipid 1, 72–94 (1997).

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Authors
Kong, W., Wei, J., Abidi, P., Lin, M., Inaba, S., Li, C., Wang, Y., Wang, Z., Si, S., Pan, H., Wang, S., Wu, J., Wang, Y., Li, Z., Liu, J., & Jiang, J.-D.
Affiliations
  • Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
  • Nanjing First Hospital (CN)
  • VA Palo Alto Health Care System (US)
  • Icahn School of Medicine at Mount Sinai (US)
Corresponding author
  • Liu, Jingwen
  • Jiang, Jian-Dong
Venue
Nature Medicine
Published
2004-11-07
Volume
10
Issue
12
Pages
1344-1351
ISSN
  • 1078-8956 (ISSN-L)
  • 1546-170X
OpenAlex
W2129582474
Cited by
1,391
References
40
Citations by year
2026: 48 · 2025: 67 · 2024: 57 · 2023: 72 · 2022: 84 · 2021: 99 · 2020: 98 · 2019: 79 · 2018: 88 · 2017: 84 · 2016: 72 · 2015: 71 · 2014: 65 · 2013: 62 · 2012: 60
FWCI
15.08
Type
journal article
Language
en
Open access
closed
Locations
  • Nature Medicine (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • National Institutes of Health (5r01ca083648-05)
  • National Cancer Institute (1R01CA83648-01)
Topics
  • Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
  • Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
  • Health Sciences › Medicine › Surgery › Lipoproteins and Cardiovascular Health
Keywords
berberine, hypercholesterolemia, LDL receptor upregulation, ERK signaling, mRNA stability, 3' untranslated region, post-transcriptional regulation, SREBP, lipid-lowering drugs, hyperlipidemia
MeSH terms
Animals, Anticholesteremic Agents, Berberine, China, Cholesterol, Flow Cytometry, Gene Expression Regulation, Cricetinae, Humans, Hypercholesterolemia, Cholesterol, LDL, Liver, Plasmids, Receptors, LDL, Regulatory Sequences, Nucleic Acid, Triglycerides, Tumor Cells, Cultured, Blotting, Northern, DNA Primers, Reverse Transcriptase Polymerase Chain Reaction

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