ArticleNature metabolism2023
Inactivation of the antidiabetic drug acarbose by human intestinal microbial-mediated degradation.
Article in Nature metabolism, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 45 citations in OpenAlex.
- Article
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- Mapping the reciprocal interactions between antidepressants and the gut microbiome: novel targets for the personalisation and optimization of drug response.Molecular psychiatry · 2026Review
- Pharmacomicrobiomics in metabolic syndrome and type 2 diabetes: the microbiome-drug-host triad.Frontiers in pharmacology · 2026Review
- Dual antidiabetic potential of arjunglucoside I and arjunetin fromAnimal cells and systems · 2026Article
- Focus on gut microbiota regulation: exploring the potential of fermented traditional Chinese medicines in the prevention and treatment of type 2 diabetes mellitus.Frontiers in microbiology · 2026Review
- MetaMDA: explainable prediction of microbe-drug association utilizing random walks on a microbe-metabolite-drug heterogeneous network.Bioinformatics (Oxford, England) · 2025Article
- Aqueous Extracts and Flavonoids Obtained fromPharmaceuticals (Basel, Switzerland) · 2025Article
- Discovery of α-glucosidase inhibitors from Paenibacillus sp. JNUCC 31 via genome mining, fatty acid profiling, and in silico analysis.Scientific reports · 2025Article
- The microbiome in cancer.iMeta · 2025Review
- Molecular insights of acarbose metabolization catalyzed by acarbose-preferred glucosidase.Nature communications · 2025Article
- Emerging gut microbial glycoside hydrolase inhibitors.RSC chemical biology · 2025Review
- Harnessing Pharmacomultiomics for Precision Medicine in Diabetes: A Comprehensive Review.Biomedicines · 2025Review
- Machine learning prediction of intestinal α-glucosidase inhibitors using a diverse set of ligands: a drug repurposing effort with drugBank database screening.In silico pharmacology · 2025Article
- Acarbose impairs gutmBio · 2024Article
- Enzymolysis Modes Trigger Diversity in Inhibitor-α-Amylase Aggregating Behaviors and Activity Inhibition: A New Insight Into Enzyme Inhibition.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Acarbose enhances the efficacy of immunotherapy against solid tumours by modulating the gut microbiota.Nature metabolism · 2024Article
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16 authors at 6 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Drugs can be modified or degraded by the gut microbiota, which needs to be considered in personalized therapy. The clinical efficacy of the antidiabetic drug acarbose, an inhibitor of α-glucosidase, varies greatly among individuals for reasons that are largely unknown. Here we identify in the human gut acarbose-degrading bacteria, termed Klebsiella grimontii TD1, whose presence is associated with acarbose resistance in patients. Metagenomic analyses reveal that the abundance of K. grimontii TD1 is higher in patients with a weak response to acarbose and increases over time with acarbose treatment. In male diabetic mice, co-administration of K. grimontii TD1 reduces the hypoglycaemic effect of acarbose. Using induced transcriptome and protein profiling, we further identify an acarbose preferred glucosidase, Apg, in K. grimontii TD1, which can degrade acarbose into small molecules with loss of inhibitor function and is widely distributed in human intestinal microorganisms, especially in Klebsiella. Our results suggest that a comparatively large group of individuals could be at risk of acarbose resistance due to its degradation by intestinal bacteria, which may represent a clinically relevant example of non-antibiotic drug resistance.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.