HMGCR and rosuvastatin regulates GLP-1 secretion and expression - a translational study
(2025) In The Journal of clinical endocrinology and metabolism- Abstract
CONTEXT: Statin use is associated with increased risk of type 2 diabetes and mild hyperglycemia. The underlying mechanisms are not well studied and the effect of statin treatment on GLP-1 secretion or production are unknown.
OBJECTIVE: To assess the effects of rosuvastatin on GLP-1 secretion and production.
METHODS: We performed association studies in the Malmö Diet and Cancer study cardiovascular cohort (MDCS-CC) re-examination cohort, in vitro investigations using GLUTag cells and acute and chronic studies in female, normoglycemic C57Bl/6j mice.
RESULTS: Studies in the MDCS-CC reexamination cohort(n=3734) revealed that in individuals without type 2 diabetes, statin usage was associated with higher fasting GIP,... (More)
CONTEXT: Statin use is associated with increased risk of type 2 diabetes and mild hyperglycemia. The underlying mechanisms are not well studied and the effect of statin treatment on GLP-1 secretion or production are unknown.
OBJECTIVE: To assess the effects of rosuvastatin on GLP-1 secretion and production.
METHODS: We performed association studies in the Malmö Diet and Cancer study cardiovascular cohort (MDCS-CC) re-examination cohort, in vitro investigations using GLUTag cells and acute and chronic studies in female, normoglycemic C57Bl/6j mice.
RESULTS: Studies in the MDCS-CC reexamination cohort(n=3734) revealed that in individuals without type 2 diabetes, statin usage was associated with higher fasting GIP, insulin, glucose, glucagon and HOMA-IR, but not GLP-1. However, in patients with type 2 diabetes, statin usage was associated with higher fasting GLP-1 levels.Rosuvastatin treatment or Hmgcr knockdown reduced GLP-1 secretion and increased Gcg mRNA in GLUTag cells. Rosuvastatin acutely reduced postprandial GLP-1 secretion, whereas chronic rosuvastatin treatment in mice caused hyperglycemia and increased postprandial GLP-1 levels. The acute effect of Hmgcr KD on GLP-1 secretion could be mimicked by targeting intracellular cholesterol using a PCSK9 inhibitor. Finally, transcriptomic alterations induced by rosuvastatin were limited to genes involved in cholesterol biosynthesis.
CONCLUSIONS: We have established HMGCR as a regulator of GLP-1 secretion and provide a plausible explanation for the clinically observed mild hyperglycemia associated with statin use. Given the negative acute effect on GLP-1 secretion, monitoring of blood glucose levels is recommended after prescribing rosuvastatin."
(Less)
- author
- organization
-
- Neuroendocrine Cell Biology (research group)
- EXODIAB: Excellence of Diabetes Research in Sweden
- Diabetes - Islet Cell Exocytosis (research group)
- Diabetic Complications (research group)
- Department Office of Experimental Medical Science
- EXODIAB VAAG ALLAN
- Internal Medicine - Epidemiology (research group)
- eSSENCE: The e-Science Collaboration
- Diabetes - Molecular Metabolism (research group)
- Cardiovascular Research - Hypertension (research group)
- EpiHealth: Epidemiology for Health
- publishing date
- 2025-11-05
- type
- Contribution to journal
- publication status
- epub
- subject
- in
- The Journal of clinical endocrinology and metabolism
- publisher
- Oxford University Press
- external identifiers
-
- pmid:41206007
- ISSN
- 1945-7197
- DOI
- 10.1210/clinem/dgaf608
- language
- English
- LU publication?
- yes
- additional info
- © The Author(s) 2025. Published by Oxford University Press on behalf of the Endocrine Society.
- id
- b1dfb0a3-5cde-4cb9-afb4-348cf7f1e5c1
- date added to LUP
- 2025-11-10 08:58:02
- date last changed
- 2025-12-08 11:59:37
@article{b1dfb0a3-5cde-4cb9-afb4-348cf7f1e5c1,
abstract = {{<p>CONTEXT: Statin use is associated with increased risk of type 2 diabetes and mild hyperglycemia. The underlying mechanisms are not well studied and the effect of statin treatment on GLP-1 secretion or production are unknown.</p><p>OBJECTIVE: To assess the effects of rosuvastatin on GLP-1 secretion and production.</p><p>METHODS: We performed association studies in the Malmö Diet and Cancer study cardiovascular cohort (MDCS-CC) re-examination cohort, in vitro investigations using GLUTag cells and acute and chronic studies in female, normoglycemic C57Bl/6j mice.</p><p>RESULTS: Studies in the MDCS-CC reexamination cohort(n=3734) revealed that in individuals without type 2 diabetes, statin usage was associated with higher fasting GIP, insulin, glucose, glucagon and HOMA-IR, but not GLP-1. However, in patients with type 2 diabetes, statin usage was associated with higher fasting GLP-1 levels.Rosuvastatin treatment or Hmgcr knockdown reduced GLP-1 secretion and increased Gcg mRNA in GLUTag cells. Rosuvastatin acutely reduced postprandial GLP-1 secretion, whereas chronic rosuvastatin treatment in mice caused hyperglycemia and increased postprandial GLP-1 levels. The acute effect of Hmgcr KD on GLP-1 secretion could be mimicked by targeting intracellular cholesterol using a PCSK9 inhibitor. Finally, transcriptomic alterations induced by rosuvastatin were limited to genes involved in cholesterol biosynthesis.</p><p>CONCLUSIONS: We have established HMGCR as a regulator of GLP-1 secretion and provide a plausible explanation for the clinically observed mild hyperglycemia associated with statin use. Given the negative acute effect on GLP-1 secretion, monitoring of blood glucose levels is recommended after prescribing rosuvastatin."</p>}},
author = {{Miskelly, Michael G and Lindqvist, Andreas and Jujić, Amra and Hamilton, Alexander and Cowan, Elaine and Raikundalia, Sweta and Dutius Andersson, Anna-Maria and Nergård, Bent J and Del Giudice, Rita and Kryvokhyzha, Dmytro and Nilsson, Peter M and Juul-Holst, Jens and Torekov, Signe Sørensen and Lagerstedt, Jens O and Gomez, Maria F and Eliasson, Lena and Mulder, Hindrik and Hedenbro, Jan and Magnusson, Martin and Wierup, Nils}},
issn = {{1945-7197}},
language = {{eng}},
month = {{11}},
publisher = {{Oxford University Press}},
series = {{The Journal of clinical endocrinology and metabolism}},
title = {{HMGCR and rosuvastatin regulates GLP-1 secretion and expression - a translational study}},
url = {{http://dx.doi.org/10.1210/clinem/dgaf608}},
doi = {{10.1210/clinem/dgaf608}},
year = {{2025}},
}
