A review on α-glucosidase inhibitory activity of first row transition metal complexes: a futuristic strategy for treatment of type 2 diabetes

Sohrabi, Marzieh; Binaeizadeh, Mohammad Reza; Iraji, Aida; Larijani, Bagher; Khanavi, Mahnaz; Mahdavi, Mohammad

doi:10.1039/d2ra00067a

Cited by 35 publications

(28 citation statements)

References 115 publications

(277 reference statements)

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“…Type 2 diabetes mellitus (T2DM) with around 90% of all cases is categorized as a major sub-type of DM. It was considered that glycemic control could be effective prevention and treatment for T2DM 5 – 7 .…”

Section: Introductionmentioning

confidence: 99%

“…α-Glucosidase (EC 3.2.1.20) is a catalytic hydrolase enzyme present on the brush border of the small intestine which hydrolyzes oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides at their non-reducing ends 7 – 10 . The produced monosaccharides especially glucose enter the bloodstream, resulting in postprandial hyperglycemia thus causing diabetes 11 – 13 .…”

Section: Introductionmentioning

confidence: 99%

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Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

Noori

Davoodi

Iraji

et al. 2022

Sci Rep

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In this study, 18 novel quinoline-based-benzo[d]imidazole derivatives were synthesized and screened for their α-glucosidase inhibitory potential. All compounds in the series except 9q showed a significant α-glucosidase inhibition with IC50 values in the range of 3.2 ± 0.3–185.0 ± 0.3 µM, as compared to the standard drug acarbose (IC50 = 750.0 ± 5.0 µM). A kinetic study indicated that compound 9d as the most potent derivative against α-glucosidase was a competitive type inhibitor. Furthermore, the molecular docking study revealed the effective binding interactions of 9d with the active site of the α-glucosidase enzyme. The results indicate that the designed compounds have the potential to be further studied as new anti-diabetic agents.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

Noori

Davoodi

Iraji

et al. 2022

Sci Rep

Self Cite

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show abstract

“…In this regard, α-glucosidase is one of the most important enzyme found in the digestive system [ 11 , 12 ]. The α-glucosidase presented on the brush border of human intestinal mucosal cells participates in the body's carbohydrate metabolism to convert oligosaccharides and disaccharides into monosaccharides by hydrolyzing the α-1,4-glycosidic bond [ 13 – 15 ].…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and molecular docking studies of diphenylquinoxaline-6-carbohydrazide hybrids as potent α-glucosidase inhibitors

et al. 2022

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A novel series of diphenylquinoxaline-6-carbohydrazide hybrids 7a–o were rationally designed and synthesized as anti-diabetic agents. All synthesized compounds 7a–o were screened as possible α-glucosidase inhibitors and exhibited good inhibitory activity with IC50 values in the range of 110.6 ± 6.0 to 453.0 ± 4.7 µM in comparison with acarbose as the positive control (750.0 ± 10.5 µM). An exception in this trend came back to a compound 7k with IC50 value > 750 µM. Furthermore, the most potent derivative 7e bearing 3-fluorophenyl moiety was further explored by kinetic studies and showed the competitive type of inhibition. Additionally, the molecular docking of all derivatives was performed to get an insight into the binding mode of these derivatives within the active site of the enzyme. In silico assessments exhibited that 7e was well occupied in the binding pocket of the enzyme through favorable interactions with residues, correlating to the experimental results.

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“…In docking assessments databases of available molecules are docked into the region of interest of protein in silico and scored based on predicted interactions with the site. In these cases, compounds with a higher affinity toward the target can be discovered [ 32 ]. Molecular dynamic (MD) simulation is an effective technique to measure the behavior of fluids at the molecular level.…”

Section: Introductionmentioning

confidence: 99%

New solid phase methodology for the synthesis of biscoumarin derivatives: experimental and in silico approaches

et al. 2022

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The simple and greener one-pot approach for the synthesis of biscoumarin derivatives using catalytic amounts of nano-MoO3 catalyst under mortar-pestle grinding was described. The use of non-toxic and mild catalyst, cost-effectiveness, ordinary grinding, and good to the excellent yield of the final product makes this procedure a more attractive pathway for the synthesis of biologically remarkable pharmacophores. Accordingly, biscoumarin derivatives were successfully extended in the developed protocols. Next, a computational investigation was performed to identify the potential biological targets of this set of compounds. In this case, first, a similarity search on different virtual libraries was performed to find an ideal biological target for these derivatives. Results showed that the synthesized derivatives can be α-glucosidase inhibitors. In another step, molecular docking studies were carried out against human lysosomal acid-alpha-glucosidase (PDB ID: 5NN8) to determine the detailed binding modes and critical interactions with the proposed target. In silico assessments showed the gold score value in the range of 17.56 to 29.49. Additionally, molecular dynamic simulations and the MM-GBSA method of the most active derivative against α-glucosidase were conducted to study the behavior of selected compounds in the biological system. Ligand 1 stabilized after around 30 ns and participated in various interactions with Trp481, Asp518, Asp616, His674, Phe649, and Leu677 residues.

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A review on α-glucosidase inhibitory activity of first row transition metal complexes: a futuristic strategy for treatment of type 2 diabetes

Abstract: Type 2 diabetes mellitus (T2DM) is characterized by high blood glucose levels and has emerged as a controversial public health issue worldwide.

Cited by 35 publications

References 115 publications

Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

Design, synthesis, and molecular docking studies of diphenylquinoxaline-6-carbohydrazide hybrids as potent α-glucosidase inhibitors

New solid phase methodology for the synthesis of biscoumarin derivatives: experimental and in silico approaches

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