Cited by 51Berberine and alkaloids researchNatural Antidiabetic Agents StudiesDrug Transport and Resistance Mechanisms

Pharmacokinetics and Pharmacological Activities of Berberine in Diabetes Mellitus Treatment

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Han, Yunfeng, Xiang, Yunan, Shi, Yi, Tang, Xi, Pan, Lin, Gao, Jie, Bi, Ruohong, Lai, Xianrong·2021·Evidence-Based Complementary and Alternative Medicine

Abstract

Traditional Chinese medicine (TCM) has good clinical application prospects in diabetes treatment. In addition, TCM is less toxic and/or has fewer side effects and provides various therapeutic effects. Berberine (BBR) is isolated as the main component in many TCM kinds (e.g., Rhizoma Coptidis and Berberidis Cortex). Furthermore, BBR can reduce blood sugar and blood fat, alleviate inflammation, and improve the state of patients. Based on the recent study results of BBR in diabetes treatment, the BBR pharmacokinetics and mechanism on diabetes are mainly studied, and the specific molecular mechanism of related experimental BBR is systematically summarized and analyzed. Clinical studies have proved that BBR has a good therapeutic effect on diabetes, suggesting that BBR may be a promising drug candidate for diabetes. More detailed BBR mechanisms and pathways of BBR need to be studied further in depth, which will help understand the BBR pharmacology in diabetes treatment.

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Crossref · 10.1155/2021/9987097

Cites

131 of 131 references verified0 citation errors · 0 not checkable

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  • A usual oral dose of 400-500 mg gives peak plasma concentrations of a few nanograms per milliliter, roughly 1-10 nM.

    “A usual oral dose of 400–500 mg gives peak plasma concentrations of a few nanograms per milliliter, which for a molecule of about 336 Da is roughly 1–10 nM [49,56].”

    From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [56]

    Section 2.2 (Distribution; page unavailable) says berberine has low plasma content after oral administration, supporting the general point. Neither that section nor Section 2.1 (Absorption; page unavailable) gives a 400–500 mg dose, a peak concentration in ng/mL, or a value in nM; searches for those terms found no such passage. (LLM, conf=0.82)

    Experimental — accuracy not yet measured
  • Peak plasma concentration of berberine after usual doses is on the order of nanograms per milliliter, frequently below the in vitro activity threshold.

    “The peak plasma concentration after usual doses is on the order of nanograms per milliliter, frequently below the activity threshold observed in vitro [49,56]”

    From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [56]

    Section 2.2 (Distribution; page unavailable) says berberine has low plasma content after oral administration, and Section 2.1 (Absorption; page unavailable) describes poor oral bioavailability. Neither section gives a peak concentration in ng/mL after usual doses or compares plasma concentrations with an in vitro activity threshold. (LLM, conf=0.84)

    Experimental — accuracy not yet measured

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Research works printed but not linked: 1

  1. [123]Waranya C. Thinnakorn L. Kanokwan J. Improvement of superoxide dismutase and catalase in streptozotocin-nicotinamide-induced type 2-diabetes in mice by berberine and glibenclamide Pharmaceutical Biology 2013 52 4 24188560

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Authors
Han, Y., Xiang, Y., Shi, Y., Tang, X., Pan, L., Gao, J., Bi, R., & Lai, X.
Affiliations
Chengdu University of Traditional Chinese Medicine (CN)
Corresponding author
Lai, Xianrong
Venue
Evidence-Based Complementary and Alternative Medicine
Publisher
Wiley
Published
2021-08-21
Volume
2021
Pages
1-15
ISSN
  • 1741-427X (ISSN-L)
  • 1741-4288
OpenAlex
W3194644078
Cited by
51
References
131
Citations by year
2026: 10 · 2025: 11 · 2024: 11 · 2023: 9 · 2022: 8 · 2021: 2
FWCI
0.95
Type
journal article
Language
en
Open access
Locations
  • Evidence-based Complementary and Alternative Medicine (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
  • National Natural Science Foundation of China (81774007, 81473427, 81173360, 81560806, 2017YFC1703904, 16ZA0120)
  • National Key R&D Projects (81774007, 81473427, 81173360, 81560806, 2017YFC1703904, 16ZA0120)
  • Education Department of Sichuan Province (81774007, 81473427, 81173360, 81560806, 2017YFC1703904, 16ZA0120)
Topics
  • Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
  • Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Keywords
berberine, diabetes mellitus, pharmacokinetics, traditional Chinese medicine, Coptidis Rhizoma, blood glucose reduction, lipid metabolism, anti-inflammatory activity, molecular mechanisms, drug candidates

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