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Dihydroberberine normalizes insulin secretion by regulating glucokinase.

Chenyang Zhang1, Xuelian Zhang2, Qianrui Zhang1

  • 1Department of Endocrinology, Beijing Diabetes Institute, Beijing Key Laboratory of Diabetes Research and Care, Beijing Tongren Hospital, Capital Medical University, Beijing, China.

Diabetes, Obesity & Metabolism
|October 13, 2025
PubMed
Summary

Dihydroberberine (DHB), a berberine analog, enhances glucose-stimulated insulin secretion by targeting glucokinase (GCK). This compound shows improved bioavailability and efficacy in preclinical models for diabetes treatment.

Keywords:
berberine analoguesdiabetesdihydroberberineglucokinaseglucoseinsulin secretion

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Area of Science:

  • Pharmacology
  • Endocrinology
  • Biochemistry

Background:

  • Berberine (BBR) is known for its glucose-lowering effects but suffers from poor bioavailability.
  • The precise molecular target of BBR in glucose regulation remains unclear.
  • Developing BBR analogs with improved pharmacokinetic properties and defined targets is crucial for diabetes therapy.

Purpose of the Study:

  • To investigate the efficacy and mechanism of dihydroberberine (DHB), a BBR analog, in regulating glucose metabolism and insulin secretion.
  • To identify the molecular target of DHB responsible for its anti-diabetic effects.
  • To evaluate DHB as a potential therapeutic agent for diabetes.

Main Methods:

  • In vitro studies using MIN6 and INS-1 pancreatic beta-cells to assess cell viability and glucose-stimulated insulin secretion (GSIS).
  • In vivo studies in mice including oral glucose tolerance tests (GTT) and insulin release tests (IRT).
  • Molecular docking, cellular thermal shift assays (CETSA), and siRNA knockdown experiments to identify and validate the drug target.

Main Results:

  • DHB significantly promoted GSIS in pancreatic beta-cells.
  • DHB demonstrated improved oral glucose tolerance and insulin release in mice compared to BBR.
  • Molecular docking and CETSA identified glucokinase (GCK) as a direct binding target of DHB.
  • GCK knockdown abrogated the insulinotropic and cytoprotective effects of DHB in beta-cells.

Conclusions:

  • Dihydroberberine (DHB) is a potent analog of berberine with enhanced bioavailability and efficacy.
  • DHB exerts its glucose-lowering and insulin-sensitizing effects by directly targeting and modulating glucokinase (GCK) activity.
  • DHB represents a promising therapeutic candidate for managing diabetes by targeting GCK in pancreatic beta-cells.