Selection, purification, and evaluation of acarbose−an α-glucosidase inhibitor from Actinoplanes sp.

Tuyến, Đỗ Thị; Yew, Guo Yong; Cuong, Nguyen Tien; Hoang, Le Thanh; Yen, Hoang; Thao, Phan Thi Hong; Thảo, Nguyễn Thị; Thanh, Nguyen Sy Le; Trang, Nguyen Thi; Trung, Nguyen Thi; Anh, Dao Thi Mai; Show, Pau Loke

doi:10.1016/j.chemosphere.2020.129167

Cited by 17 publications

(19 citation statements)

References 14 publications

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“…The lower the IC 50 , the stronger the inhibitory activity. Of the 42 cultivars investigated, 27 cultivars exhibited stronger alpha-glucosidase inhibitory activity with IC 50 values significantly lower than that of acarbose (1.07 mg/mL), which is a widely used drug for the treatment of type-2 diabetes [ 38 ]. Eleven of the cultivars (Berg X Mexican, Blue Motto, Cross X, Ficus Indice, Messina, Nepgen, Ofer, Polypoly, Postmasburg, Roedtan and Sharsheret) demonstrated alpha-glucosidase inhibitory activity (IC 50 < 0.1 mg/mL) that was 10-fold stronger) when compared to acarbose.…”

Section: Resultsmentioning

confidence: 99%

Phytochemical Content, Antioxidant, Alpha-Glucosidase Inhibitory and Antibacterial Activities of Spineless Cactus Pear Cultivars

Mabotja

Venter

Plooy

et al. 2021

Plants

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Variation in cultivars can influence plant biological activities. This study aimed to identify superior cultivars while determining the variability in the phytochemical content, antioxidant, alpha-glucosidase inhibitory and antibacterial activities of cladode extracts from selected spineless Burbank cactus pear (Opuntia ficus-indica and Opuntia robusta) cultivars. Total phenolic and flavonoid contents were determined using the Folin-Ciocalteu and aluminum chloride spectrophotometric methods, respectively. Antioxidant activity was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and β-carotene linoleic acid assays. Alpha-glucosidase inhibition was determined using a spectrophotometric method and antibacterial activity using a non-polar (petroleum ether) and polar (50% methanol) extracts against two Gram-positive and two Gram-negative bacteria. Significant variation in phytochemical content, antioxidant, antidiabetic and antibacterial activities was observed amongst the cultivars. Alpha-glucosidase inhibitory activity varied widely with IC50 values ranging from 0.06 to 1.85 mg/mL. Radical scavenging activity of Polypoly cultivar was about seven fold higher than that recorded in other cultivars with low activity. Turpin and Berg x Mexican cultivars had the highest total phenolic and flavonoid contents, whilst the non-polar extract of Turpin also exhibited higher antibacterial activity against Bacillus subtilis and Escherichia coli. Sicilian Indian Fig was amongst the cultivars with a higher antioxidant activity, whilst also showing a strong inhibition against B. subtilis and E. coli. Polypoly cultivar demonstrated strong antioxidant and antidiabetic activities while its polar extract showed the highest total antibacterial activity against B. subtilis. The cultivar Malta was superior in terms of its antibacterial potency and efficacy against B. subtilis, Staphylococcus aureus and E. coli. The potential of using spineless cactus pear cladodes as a functional food with antioxidant, antidiabetic and antibacterial properties against pathogenic food spoilage bacteria in place of synthetic compounds was established. The significance of cultivar selection to increase this potential was highlighted.

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Section: Resultsmentioning

confidence: 99%

Phytochemical Content, Antioxidant, Alpha-Glucosidase Inhibitory and Antibacterial Activities of Spineless Cactus Pear Cultivars

Mabotja

Venter

Plooy

et al. 2021

Plants

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“…These therapeutic drugs have been widely used in clinical trials because of their own characteristics in hypoglycemic control. For example, α-glucosidase inhibitors have been used to control postprandial glucose levels caused by type 2 diabetes since 1990 (Ríos et al, 2015;Flores-Bocanegra et al, 2017;Santos et al, 2018;Dhameja and Gupta, 2019;Usman et al, 2019;Mi et al, 2021;Tuyen et al, 2021). Acarbose (Chiasson et al, 2002) and miglitol (Satoru et al, 2015), which were clinically used for treating type 2 diabetes, may control blood glucose levels by targeting α-amylases and α-glucosidases (Lyann et al, 2010;Ren et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Targeting N-Terminal Human Maltase-Glucoamylase to Unravel Possible Inhibitors Using Molecular Docking, Molecular Dynamics Simulations, and Adaptive Steered Molecular Dynamics Simulations

et al. 2021

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There are multiple drugs for the treatment of type 2 diabetes, including traditional sulfonylureas biguanides, glinides, thiazolidinediones, α-glucosidase inhibitors, glucagon-like peptide-1 (GLP-1) receptor agonists, dipeptidyl peptidase IV (DPP-4) inhibitors, and sodium-glucose cotransporter 2 (SGLT2) inhibitors. α-Glucosidase inhibitors have been used to control postprandial glucose levels caused by type 2 diabetes since 1990. α-Glucosidases are rather crucial in the human metabolic system and are principally found in families 13 and 31. Maltase-glucoamylase (MGAM) belongs to glycoside hydrolase family 31. The main function of MGAM is to digest terminal starch products left after the enzymatic action of α-amylase; hence, MGAM becomes an efficient drug target for insulin resistance. In order to explore the conformational changes in the active pocket and unbinding pathway for NtMGAM, molecular dynamics (MD) simulations and adaptive steered molecular dynamics (ASMD) simulations were performed for two NtMGAM-inhibitor [de-O-sulfonated kotalanol (DSK) and acarbose] complexes. MD simulations indicated that DSK bound to NtMGAM may influence two domains (inserted loop 1 and inserted loop 2) by interfering with the spiralization of residue 497–499. The flexibility of inserted loop 1 and inserted loop 2 can influence the volume of the active pocket of NtMGAM, which can affect the binding progress for DSK to NtMGAM. ASMD simulations showed that compared to acarbose, DSK escaped from NtMGAM easily with lower energy. Asp542 is an important residue on the bottleneck of the active pocket of NtMGAM and could generate hydrogen bonds with DSK continuously. Our theoretical results may provide some useful clues for designing new α-glucosidase inhibitors to treat type 2 diabetes.

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“…Acarbose is an AGI, specifically a pseudo-tetrasaccharide that has a nitrogen between the first and second glucose molecules, possessing a particular high affinity for the α-glucosidase enzyme (Tuyen et al, 2021 ). Both enzymes are inhibited in a competitive way, reducing their affinity to the oligosaccharides from dietary starch as well as decreasing the monosaccharide formation rate (Rosak & Mertes, 2012 ).…”

Section: Diabetesmentioning

confidence: 99%

The α-Amylase and α-Glucosidase Inhibition Capacity of Grape Pomace: A Review

Cisneros‐Yupanqui

Lante

Mihaylova

et al. 2022

Food Bioprocess Technol

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The concept of functional foods is gaining more importance due to its role in maintaining a healthy status and preventing some metabolic diseases. The control of diabetes, in particular type-2 (T2DM), could be considered a big challenge since it involves other factors such as eating habits. From the pharmacological point of view, inhibiting digestive enzymes, such as α-amylase and α-glucosidase, is one of the mechanisms mainly used by synthetic drugs to control this disease; however, several side effects are described. For that reason, using bioactive compounds may appear as an alternative without presenting the complications synthetic drugs available on the market have. The winemaking industry generates tons of waste annually, and grape pomace (GP) is the most important. GP is recognized for its nutritional value and as a source of bioactive compounds that are helpful for human health. This review highlights the importance of GP as a possible source of α-amylase and α-glucosidase inhibitors. Also, it is emphasized the components involved in this bioactivity and the possible interactions among them. Especially, some phenolic compounds and fiber of GP are the main ones responsible for interfering with the human digestive enzymes. Preliminary studies in vitro confirmed this bioactivity; however, further information is required to allow the specific use of GP as a functional ingredient inside the market of products recommended for people with diabetes. Graphical abstract

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Selection, purification, and evaluation of acarbose−an α-glucosidase inhibitor from Actinoplanes sp.

Cited by 17 publications

References 14 publications

Phytochemical Content, Antioxidant, Alpha-Glucosidase Inhibitory and Antibacterial Activities of Spineless Cactus Pear Cultivars

Phytochemical Content, Antioxidant, Alpha-Glucosidase Inhibitory and Antibacterial Activities of Spineless Cactus Pear Cultivars

Targeting N-Terminal Human Maltase-Glucoamylase to Unravel Possible Inhibitors Using Molecular Docking, Molecular Dynamics Simulations, and Adaptive Steered Molecular Dynamics Simulations

The α-Amylase and α-Glucosidase Inhibition Capacity of Grape Pomace: A Review

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