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A new biological pr...
A new biological prospective for the 2-phenylbenzofurans as inhibitors of α-glucosidase and of the islet amyloid polypeptide formation
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- Delogu, Giovanna Lucia (författare)
- Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
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- Era, Benedetta (författare)
- Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
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- Floris, Sonia (författare)
- Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
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- Medda, Rosaria (författare)
- Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
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- Sogos, Valeria (författare)
- Univ Cagliari, Dept Biomed Sci, I-09042 Cagliari, Italy
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- Pintus, Francesca (författare)
- Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
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- Gatto, Gianluca (författare)
- Univ Cagliari, Dept Elect & Elect Engn, Via Marengo 2, I-09123 Cagliari, Italy
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- Kumar, Amit (författare)
- Univ Cagliari, Dept Elect & Elect Engn, Via Marengo 2, I-09123 Cagliari, Italy
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- Torstensdotter Westermark, Gunilla (författare)
- Uppsala universitet,Institutionen för medicinsk cellbiologi
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- Fais, Antonella (författare)
- Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
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(creator_code:org_t)
- Elsevier, 2021
- 2021
- Engelska.
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Ingår i: International Journal of Biological Macromolecules. - : Elsevier. - 0141-8130 .- 1879-0003. ; 169, s. 428-435
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- In this study, we have investigated a series of hydroxylated 2-phenylbenzofurans compounds for their inhibitory activity against α-amylase and α-glucosidase activity.Inhibitors of carbohydrate degrading enzymes seem to have an important role as antidiabetic drugs.Diabetes mellitus is a wide-spread metabolic disease characterized by elevated levels of blood glucose. The most common is type 2 diabetes, which can lead to severe complications. Since the aggregates of islet amyloid polypeptide (IAPP) are common in diabetic patients, the effect of compounds to inhibit amyloid fibril formation was also determined.All the compounds assayed showed to be more active against α-glucosidase. Compound 16 showed the lowest IC50 value of the series, and it is found to be 167 times more active than acarbose, the reference compound. The enzymatic activity assays showed that compound 16 acts as a mixed-type inhibitor of α-glucosidase. Furthermore, compound 16 displayed effective inhibition of IAPP aggregation and it manifested no significant cytotoxicity.To predict the binding of compound 16 to IAPP and α-glucosidase protein complexes, molecular docking studies were performed.Altogether, our results support that the 2-phenylbenzofuran derivatives could represent a promising candidate for developing molecules able to modulate multiple targets involved in diabetes mellitus disorder.
Ämnesord
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Endokrinologi och diabetes (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Endocrinology and Diabetes (hsv//eng)
Nyckelord
- alpha-Glucosidase
- Islet amyloid polypeptide
- 2-phenylbenzofuran
- molecular docking
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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