| Description: |
1,3-Diphenyl-2-propen-1-one has anti-inflammatory, antifungal, antibacterial, antimalarial, antituberculosis, antitumor, antimicrobial and antiviral effects. It could be used to design effective inhibitors of alpha-amylase. |
| In vitro: |
| Mini Reviews in Medicinal Chemistry, 2013,13(1):87-94. | | Anti-Inflammatory Trends of 1, 3-Diphenyl-2-propen-1-one Derivatives.[Reference: WebLink] | Chalcones (1,3-Diphenyl-2-propen-1-one) are constituted by a three carbon α, β-unsaturated carbonyl system. The biosynthesis of flavonoids and isoflavonoids is initiated by chalcones. Notable pharmacological activities of chalcones and its derivatives include anti-inflammatory, antifungal, antibacterial, antimalarial, antituberculosis, antitumor, antimicrobial and antiviral effects respectively. Owing to simplicity of the chemical structures and a huge variety of pharmacological actions exhibited, the entities derived from chalcones are subjected to extensive consideration.
METHODS AND RESULTS:
This review article is an effort to sum up the anti-inflammatory activities of chalcone derived chemical entities. Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise. | | Molecular Biology Reports, 2011,38(3):1617-1620. | | Trans-chalcone: a novel small molecule inhibitor of mammalian alpha-amylase.[Reference: WebLink] |
METHODS AND RESULTS:
Trans-chalcone (1,3-diphenyl-2-propen-1-one), a biphenolic core structure of flavonoids precursor was tested for inhibitory activity toward alpha-amylase. Porcine pancreatic alpha-amylase was observed to be effectively inhibited by this compound, which showed competitive behavior with a K i of 48 μM. Soluble starch (the natural substrate of the enzyme) was used in this study in order to obtain more realistic results. The possible binding mode of the compound was assessed in silico, and the two residues Trp59, and Tyr62 were proposed as main interacting residues with trans-chalcone.
CONCLUSIONS:
In conclusion, this compound could be used to design effective inhibitors of alpha-amylase. |
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