Synthesis, molecular modeling and biological evaluation of novel 2-allyl amino 4-methyl sulfanyl butyric acid as α-amylase and α-glucosidase inhibitor

Balan, Kannan; Perumal, Perumal; Narayanan, Shridhar; Palvannan, Thayumanavan

doi:10.1016/j.molstruc.2014.09.086

Cited by 6 publications

(4 citation statements)

References 34 publications

(31 reference statements)

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“…Our results are agreed with the previous studies [70,73]. According to various in vivo studies, for diabetes care, alpha-amylase inhibition is supposed to be one of the most operative methods [74,75].…”

Section: Antidiabetic Activitysupporting

confidence: 93%

In vitro bactericidal, antidiabetic, cytotoxic, anticoagulant, and hemolytic effect of green-synthesized silver nanoparticles using Allium sativum clove extract incubated at various temperatures

Andleeb

Tariq

Muneer

et al. 2020

Green Processing and Synthesis

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The current research aimed to evaluate in vitro biological activities of green-synthesized silver nanoparticles using the Allium sativum clove extract. The stability of green-synthesized silver nanoparticles was evaluated via storage at 4°C, room temperature (37°C), and calcined at 300°C, 500°C, and 700°C. The antibacterial effect was evaluated using agar well, spread plate, biofilm reduction, and cell proliferation inhibition assays. The cytotoxic and antidiabetic effects were determined via brine shrimp lethality, protein kinase inhibition, and α-amylase inhibition assays. DPPH scavenging, iron-chelating, anticoagulant, and hemolytic effects were evaluated. The highest inhibition of Klebsiella pneumoniae was observed when freshly prepared, calcined (300°C), and stored nanoparticles (4°C and 37°C) were applied (9.66, 9.55, 7.33, and 6.65 mm) against freshly prepared and calcined at 700°C which showed the highest inhibition of Pseudomonas aeruginosa (8.55 and 7.66 mm). Cell viability assay, biofilm reduction assay, and spread plate method showed a significant antibacterial effect of freshly prepared silver nanoparticles. Freshly prepared and calcined nanoparticles at 300°C and 500°C possessed strong antioxidant and iron-chelating activity. Among all the synthesized silver nanoparticles, freshly prepared and calcined nanoparticles (300°C and 500°C) increases the prothrombin time. Silver nanoparticles possessed significant anticoagulant properties and less toxic at least concentration toward human RBCs. In brine shrimp lethality assay, freshly prepared nanoparticles showed a stronger toxic effect and caused high mortality of larvae. Protein kinase inhibition assay revealed that freshly prepared nanoparticles had the highest zone of inhibition (18.0 mm) at 50 µg/disc. Green-synthesized nanoparticles would be used as potential therapeutic agents to overcome both infectious and noninfectious diseases.

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Section: Antidiabetic Activitysupporting

confidence: 93%

In vitro bactericidal, antidiabetic, cytotoxic, anticoagulant, and hemolytic effect of green-synthesized silver nanoparticles using Allium sativum clove extract incubated at various temperatures

Andleeb

Tariq

Muneer

et al. 2020

Green Processing and Synthesis

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“…2,32 According to numerous in vivo studies, the inhibition of a-amylase and a-glucosidase is believed to be one of the most effective approaches for diabetes care. [33][34][35][36]…”

Section: Inhibition Of A-amylase and A-glucosidase By Agnpsmentioning

confidence: 99%

Antidiabetic activity of silver nanoparticles from green synthesis using Lonicera japonica leaf extract

et al. 2016

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“…Among these three AGIs (acarbose, voglibose and miglitol), acarbose has promising effects on several intestinal enzymes; for example, it mainly inhibits α-amylases, including glucoamylase (90%), sucrose (65%), maltase (60%) and isomaltase (10%) [11]. α-Glucosidase is a membrane-bound enzyme found in intestinal cells that catalyses the production of glucose from a carbohydrate source [12] and α-Glucosidase cleaves α-glycosidic bonds. Glucosidase inhibitors can be used as first-line drugs for the treatment of T2DM, because they can lower the rate of carbohydrate absorption and suppress postprandial hyperglycaemia [13,14,15,16,17].…”

Section: Introductionmentioning

confidence: 99%

Novel C-2 Symmetric Molecules as α-Glucosidase and α-Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics

et al. 2019

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A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a–5h, have been synthesized, characterized by 1H-NMR and 13C-NMR, and evaluated for their in vitro α-glucosidase and α-amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both α-glucosidase and α-amylase. The IC50 of 5g against α-glucosidase was 0.35917 ± 0.0189 µM (standard acarbose IC50 = 6.109 ± 0.329 µM), and the IC50 value of 5g against α-amylase was 0.4379 ± 0.0423 µM (standard acarbose IC50 = 33.178 ± 2.392 µM). The Lineweaver-Burk plot indicated that compound 5g is a competitive inhibitor of α-glucosidase. The binding interactions of the most active analogues were confirmed through molecular docking studies. Docking studies showed that 5g interacts with the residues Trp690, Asp548, Arg425, and Glu426, which form hydrogen bonds to 5g with distances of 2.05, 2.20, 2.10 and 2.18 Å, respectively. All compounds showed high mutagenic and tumorigenic behaviors, and only 5e showed irritant properties. In addition, all the derivatives showed good antioxidant activities. The pharmacokinetic evaluation also revealed promising results

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Synthesis, molecular modeling and biological evaluation of novel 2-allyl amino 4-methyl sulfanyl butyric acid as α-amylase and α-glucosidase inhibitor

Cited by 6 publications

References 34 publications

In vitro bactericidal, antidiabetic, cytotoxic, anticoagulant, and hemolytic effect of green-synthesized silver nanoparticles using Allium sativum clove extract incubated at various temperatures

In vitro bactericidal, antidiabetic, cytotoxic, anticoagulant, and hemolytic effect of green-synthesized silver nanoparticles using Allium sativum clove extract incubated at various temperatures

Antidiabetic activity of silver nanoparticles from green synthesis using Lonicera japonica leaf extract

Novel C-2 Symmetric Molecules as α-Glucosidase and α-Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics

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