Interaction of antidiabetic α‐glucosidase inhibitors and gut bacteria α‐glucosidase

Tan, Kemin; Tesar, C.; Wilton, Rosemarie; Jedrzejczak, R.; Joachimiak, A.

doi:10.1002/pro.3444

Cited by 45 publications

(29 citation statements)

References 46 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Blaubia ( Ruminococcus ) obeum shares the same class Clostridia with Ruminococcus 2 and expresses α-glucosidases (Ro-αG1). Recently, a theory proposed that α-glycosidase inhibitors (acarbose, voglibose, miglitol) could affect the bacterial Ro-αG1 in human gut and exerted antidiabetic effects or created adverse gastrointestinal symptoms 37. Furthermore, Rumenococcus , SCFA-producing bacteria, mainly produced acetate and propionate38 to improve metabolic abnormalities and intestinal inflammation 39.…”

Section: Discussionmentioning

confidence: 99%

Effects of metformin, acarbose, and sitagliptin monotherapy on gut microbiota in Zucker diabetic fatty rats

Zhang

Feng

Yang

et al. 2019

BMJ Open Diab Res Care

View full text Add to dashboard Cite

ObjectiveRecent studies have demonstrated that gut microbiota was closely related to metabolic disorders such as type 2 diabetes. Oral antidiabetic medications including metformin, acarbose and sitagliptin lowered blood glucose levels via acting on the gastrointestinal tract. The aim of the study was to observe the comparisons among those medications on gut microbiota composition.Research design and methodsZucker diabetic fatty rats (n=32) were randomly divided into four groups, and had respectively gastric administration of normal saline (control), metformin (215.15 mg/kg/day), acarbose (32.27 mg/kg/day), or sitagliptin (10.76 mg/kg/day) for 4 weeks. Blood glucose levels were measured during an intragastric starch tolerance test after the treatments. 16S rRNA gene sequencing was used to access the microbiota in the fecal samples.ResultsMetformin, acarbose, and sitagliptin monotherapy effectively decreased fasting and postprandial blood glucose levels (p<0.001). Acarbose group displayed specific cluster and enterotype mainly composed byRuminococcus 2whileLactobacilluswas the dominant bacterium in the enterotype of the other three groups. The relative abundance of generaRuminococcus 2andBifidobacteriumwas dramatically higher in acarbose group. Metformin and sitagliptin increased the relative abundance of genus Lactobacillus. Metagenomic prediction showed that the functional profiles of carbohydrate metabolism were enriched in acarbose group.ConclusionsMetformin, acarbose and sitagliptin exerted different effects on the composition of gut microbiota and selectively increased the beneficial bacteria. Supplementation with specific probiotics may further improve the hypoglycemic effects of the antidiabetic drugs.

show abstract

Section: Discussionmentioning

confidence: 99%

Effects of metformin, acarbose, and sitagliptin monotherapy on gut microbiota in Zucker diabetic fatty rats

Zhang

Feng

Yang

et al. 2019

BMJ Open Diab Res Care

View full text Add to dashboard Cite

show abstract

“…The most commonly prescribed alpha-glucosidase inhibitor is acarbose and it is a pseudo-carbohydrate isolated from actinomycetes (Luo et al 2001 ). Other available inhibitors include, voglibose (from microbial origin) and miglitol (derived synthetically from 1‐deoxynojirimycin) (Tan et al 2018 ). The structural resemblance of these drugs with carbohydrates promote their attachment to the binding site of alpha-glucosidase enzyme.…”

Section: Alpha-glucosidase: Biological Role and Available Inhibitorsmentioning

confidence: 99%

A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes

et al. 2021

View full text Add to dashboard Cite

Diabetes mellitus is a multifactorial global health disorder that is rising at an alarming rate. Cardiovascular diseases, kidney damage and neuropathy are the main cause of high mortality rates among individuals with diabetes. One effective therapeutic approach for controlling hyperglycemia associated with type-2 diabetes is to target alpha-amylase and alpha-glucosidase, enzymes that catalyzes starch hydrolysis in the intestine. At present, approved inhibitors for these enzymes are restricted to acarbose, miglitol and voglibose. Although these inhibitors retard glucose absorption, undesirable gastrointestinal side effects impede their application. Therefore, research efforts continue to seek novel inhibitors with improved efficacy and minimal side effects. Natural products of plant origin have been a valuable source of therapeutic agents with lesser toxicity and side effects. The anti-diabetic potential through alpha-glucosidase inhibition of plant-derived molecules are summarized in this review. Eight molecules (Taxumariene F, Akebonoic acid, Morusin, Rhaponticin, Procyanidin A2, Alaternin, Mulberrofuran K and Psoralidin) were selected as promising drug candidates and their pharmacokinetic properties and toxicity were discussed where available. Supplementary Information The online version contains supplementary material available at 10.1007/s11101-021-09773-1.

show abstract

“…Human gut bacterium Blaubia ( Ruminococcus ) obeum expresses enzymes, such as α-glucosidases (Ro-αG1), which have specific crystal structures with free active site(s) to bind and interact with volatile substrates. Therefore, the proposed theory is that α-GIs (acarbose, voglibose, miglitol) can affect the bacterial Ro-αG1 in human gut and exert positive effects or create adverse gastrointestinal symptoms[ 52 ]. The α-GIs bind to the active site of Ro-αG1 and change the enzyme’s activity.…”

Section: Gut Microbiota and Alpha-gismentioning

confidence: 99%

Crosstalk between gut microbiota and antidiabetic drug action

Kyriachenko

Falalyeyeva

Korotkyi

et al. 2019

WJD

View full text Add to dashboard Cite

Type 2 diabetes (T2D) is a disorder characterized by chronic inflated blood glucose levels (hyperglycemia), at first due to insulin resistance and unregulated insulin secretion but with tendency towards global spreading. The gut microbiota is recognized to have an influence on T2D, although surveys have not formed a clear overview to date. Because of the interactions between gut microbiota and host homeostasis, intestinal bacteria are believed to play a large role in various diseases, including metabolic syndrome, obesity and associated disease. In this review, we highlight the animal and human studies which have elucidated the roles of metformin, α-glucosidase inhibitors, glucagon-like peptide-1 agonists, peroxisome proliferator-activated receptors γ agonists, inhibitors of dipeptidyl peptidase-4, sodium/glucose cotransporter inhibitors, and other less studied medications on gut microbiota. This review is dedicated to one of the most widespread diseases, T2D, and the currently used antidiabetic drugs and most promising new findings. In general, the gut microbiota has been shown to have an influence on host metabolism, food consumption, satiety, glucose homoeostasis, and weight gain. Altered intestinal microbiota composition has been noticed in cardiovascular diseases, colon cancer, rheumatoid arthritis, T2D, and obesity. Therefore, the main effect of antidiabetic drugs is on the microbiome composition, basically increasing the short-chain fatty acids-producing bacteria, responsible for losing weight and suppressing inflammation.

show abstract

Interaction of antidiabetic α‐glucosidase inhibitors and gut bacteria α‐glucosidase

Cited by 45 publications

References 46 publications

Effects of metformin, acarbose, and sitagliptin monotherapy on gut microbiota in Zucker diabetic fatty rats

Effects of metformin, acarbose, and sitagliptin monotherapy on gut microbiota in Zucker diabetic fatty rats

A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes

Crosstalk between gut microbiota and antidiabetic drug action

Contact Info

Product

Resources

About