Curcumin-based Antioxidant and Glycohydrolase Inhibitor Compounds : Synthesis and In Vitro Appraisal of the Dual Activity Against Diabetes
Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net..
BACKGROUND: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as an enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors.
OBJECTIVE: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia.
METHODS: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2- picrylhydrazyl (DPPH•) radical scavenging activity were done to appraise the antioxidant potential of these compounds in vitro.
RESULTS: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio).
CONCLUSION: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:17 |
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| Enthalten in: |
Medicinal chemistry (Shariqah (United Arab Emirates)) - 17(2021), 7 vom: 29., Seite 677-698 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Esmaeili, Sajjad [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 03.09.2021 Date Revised 03.09.2021 published: Print Citation Status MEDLINE |
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| doi: |
10.2174/1573406416666200506083718 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 500 | |a Date Revised 03.09.2021 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net. | ||
| 520 | |a BACKGROUND: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as an enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors | ||
| 520 | |a OBJECTIVE: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia | ||
| 520 | |a METHODS: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2- picrylhydrazyl (DPPH•) radical scavenging activity were done to appraise the antioxidant potential of these compounds in vitro | ||
| 520 | |a RESULTS: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio) | ||
| 520 | |a CONCLUSION: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Curcumin derivatives | |
| 650 | 4 | |a antioxidant activity | |
| 650 | 4 | |a diabetes | |
| 650 | 4 | |a enzyme inhibition | |
| 650 | 4 | |a α-amylase | |
| 650 | 4 | |a α-glucosidase. | |
| 650 | 7 | |a Antioxidants |2 NLM | |
| 650 | 7 | |a Glycoside Hydrolase Inhibitors |2 NLM | |
| 650 | 7 | |a Hypoglycemic Agents |2 NLM | |
| 650 | 7 | |a Glycoside Hydrolases |2 NLM | |
| 650 | 7 | |a EC 3.2.1.- |2 NLM | |
| 650 | 7 | |a Curcumin |2 NLM | |
| 650 | 7 | |a IT942ZTH98 |2 NLM | |
| 700 | 1 | |a Ghobadi, Nazanin |e verfasserin |4 aut | |
| 700 | 1 | |a Nazari, Donya |e verfasserin |4 aut | |
| 700 | 1 | |a Pourhossein, Alireza |e verfasserin |4 aut | |
| 700 | 1 | |a Rasouli, Hassan |e verfasserin |4 aut | |
| 700 | 1 | |a Adibi, Hadi |e verfasserin |4 aut | |
| 700 | 1 | |a Khodarahmi, Reza |e verfasserin |4 aut | |
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