Reappraisal and perspectives of clinical drug–drug interaction potential of α-glucosidase inhibitors such as acarbose, voglibose and miglitol in the treatment of type 2 diabetes mellitus

Rp, Dash; Rj, Babu; Nr, Srinivas

doi:10.1080/00498254.2016.1275063

Cited by 56 publications

(43 citation statements)

References 52 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Miglitol is a second generation of a-glucosidase inhibitor (Sels et al, 1999). While greater than 98% of orally dosed acarbose is not absorbed (Dash et al, 2018), miglitol is completely absorbed by the small intestine (Sels et al, 1999;Dash et al, 2018) and therefore, an appropriate control for gut activity of acarbose. Oral administration of acarbose significantly suppressed CIA when given prior to or at the time of arthritis induction and reduced incidence of CIA when given prior to induction of arthritis ( Figure 1).…”

Section: Acarbose Suppressed Ciamentioning

confidence: 99%

Alpha-Glucosidase Inhibitors Alter Gut Microbiota and Ameliorate Collagen-Induced Arthritis

et al. 2020

View full text Add to dashboard Cite

Acarose is an anti-diabetic drug and exhibits anti-arthritic effects. We hypothesized that acarbose influences the gut microbiota to affect the course of arthritis and tested this hypothesis in a collagen-induced arthritis (CIA) murine model. Acarbose in drinking water was administered via gastric gavage started prior to or at the time of CIA induction. Gut microbiota were evaluated with 16S rRNA gene sequencing from fecal pellets collected prior to arthritis induction, during onset of arthritis, and after treatment. Immune response was evaluated by measuring changes in T helper-17 (Th17) and T regulatory (Treg) cells in the spleen and intestine, as well as serum cytokine levels. Before induction of CIA, acarbose significantly reduced the incidence of arthritis and attenuated clinical severity of arthritis. The frequency of Th17 cells was significantly decreased in the intestinal lamina propria in acarbose treated mice. Mice that were treated with acarbose showed significantly increased CD4 + CD25 + Foxp3 + Treg cells with elevation of Helios and CCR6. A remarkable alteration in microbial community was observed in acarbose treated mice. Bacterial diversity and richness in mice with arthritis were significantly lower than those in acarbose treated groups. The frequency of Firmicutes was significantly reduced after arthritis onset but was restored after treatment with acarbose. The frequency of Lactobacillus, Anaeroplasma, Adlercreutzia, RF39 and Corynebacterium was significantly higher in control groups than in acarbose treated, while Oscillospira, Desulfovibrio and Ruminococcus enriched in acarbose treated group. Miglitol, another aglucosidase inhibitor showed a similar but less potent anti-arthritic effect to that of acarbose. These data demonstrate that acarbose alleviated CIA through regulation of Th17/Treg cells in the intestinal mucosal immunity, which may have resulted from the impact of acarbose on gut microbial community. Inexpensive antidiabetic drugs with an excellent safety profile are potentially useful for managing rheumatoid arthritis.

show abstract

Section: Acarbose Suppressed Ciamentioning

confidence: 99%

Alpha-Glucosidase Inhibitors Alter Gut Microbiota and Ameliorate Collagen-Induced Arthritis

et al. 2020

View full text Add to dashboard Cite

show abstract

“…The enzyme, α-glucosidase cleaves carbohydrates into glucose and elevates the blood glucose level. Therefore, α-glucosidase inhibitors are considered as antidiabetic agents for type-2 diabetes (Dash et al, 2018 ). The use of natural products as α-glucosidase inhibitors has gained interest because they do not induce toxicity or negative symptoms for the liver, kidney, and gastrointestinal system.…”

Section: Pharmacological Activities Of P Urinaria mentioning

confidence: 99%

A Review of the Phytochemistry and Pharmacology of Phyllanthus urinaria L.

Geethangili

Ding

2018

Front. Pharmacol.

View full text Add to dashboard Cite

The genus Phyllanthus (L.) is one of the most important groups of plants belonging to the Phyllantaceae family. Phyllanthus urinaria (L.) is an annual perennial herbal species found in tropical Asia, America, China, and the Indian Ocean islands. P. urinaria is used in folk medicine as a cure to treat jaundice, diabetes, malaria, and liver diseases. This review provides traditional knowledge, phytochemistry, and biological activities of P. urinaria. The literature reviewed for this article was obtained from the Web of Science, SciFinder, PubMed, ScienceDirect, and Google Scholar journal papers published prior to December 2017. Phytochemical investigations reveal that the plant is a rich source of lignans, tannins, flavonoids, phenolics, terpenoids, and other secondary metabolites. Pharmacological activities include anticancer, hepatoprotective, antidiabetic, antimicrobial, and cardioprotective effects. Thus, this present review summarizes the phytochemical constituents and their biological activities including biological studies on various crude extracts and fractions both in vitro and in vivo, and on clinical trial information about P. urinaria. This review compiles 93 naturally occurring compounds from P. urinaria along with their structures and pharmacological activities. The review is expected to stimulate further research on P. urinaria, and its pharmacological potential to yield novel therapeutic agents.

show abstract

“…It is a pseudotetrasaccharide, consisting of a maltose bridged to acarvosine, and has a high specificity for α-glucosidases. As an inhibitor, acarbose reduces PPHG in patients with diabetes mellitus [ 13 , 14 ].…”

Section: Introductionmentioning

confidence: 99%

Optimization and Validation of a Microscale In vitro Method to Assess α-Glucosidase Inhibition Activity

Granados-Guzmán

Castro‐Ríos

Torres

et al. 2018

CAC

View full text Add to dashboard Cite

Background: Microscale in vitro assays are fast, simple, and inexpensive, with reduced reagent quantities, waste, and experimental animal use. However, they have low reproducibility and low correlation with the results of in vivo models, possibly due to differences in precision and accuracy in methodologies between laboratories.Objective: The objective was the optimization and validation of an in vitro assay, carried out on microscale, to assess the inhibition of α-glucosidase activity, which is indicative of antihyperglycemic activity.Methods: The optimization was carried out using a fractional factorial design taking into account the best inhibition percentage and the absorbance of the controls. With the optimized experimental conditions in hand, we carried out method validation.Results: The optimized conditions were as follows: enzyme concentration, 0.55 U/mL; substrate concentration, 111.5 μM; and 17.5 min incubation at 37°C. A linear range between 100 and 310.2 μg/mL of acarbose (r2 0.994) was established. The RSD was <2% and the % error was <3%. The Z factor was >0.96. This method was applied to four plant extracts, one of which was found to be very active.Conclusion: The method was found to be accurate, precise, selective, linear, and reliable in evaluating the antihyperglycemic activity of natural extracts in vitro.

show abstract

Reappraisal and perspectives of clinical drug–drug interaction potential of α-glucosidase inhibitors such as acarbose, voglibose and miglitol in the treatment of type 2 diabetes mellitus

Cited by 56 publications

References 52 publications

Alpha-Glucosidase Inhibitors Alter Gut Microbiota and Ameliorate Collagen-Induced Arthritis

Alpha-Glucosidase Inhibitors Alter Gut Microbiota and Ameliorate Collagen-Induced Arthritis

A Review of the Phytochemistry and Pharmacology of Phyllanthus urinaria L.

Optimization and Validation of a Microscale In vitro Method to Assess α-Glucosidase Inhibition Activity

Contact Info

Product

Resources

About