Design, synthesis, characterization, enzymatic inhibition evaluations, and docking study of novel quinazolinone derivatives

Pedrood, Keyvan; Sherafati, Maedeh; Mohammadi‐Khanaposhtani, Maryam; Asgari, Mohammad; Hosseini, Samanesadat; Rastegar, Hossein; Larijani, Bagher; Mahdavi, Mohammad; Taslimi, Parham; Erden, Yavuz; Günay, Sevilay; Gülçın, İlhami

doi:10.1016/j.ijbiomac.2020.12.121

Cited by 44 publications

(51 citation statements)

References 82 publications

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“…Until recently, diabetes has remained one of the fastest growing, serious and costly health problems in the world. Its complete cure and effective drugs for treatment are still not available [75]. Recently, herbal extracts and their compounds have received great attention as antioxidants and potential inhibitors of key and metabolic enzymes, used in clinical conditions.…”

Section: Resultsmentioning

confidence: 99%

“…A recent research has been conducted directly towards the discovery of amylase inhibitors of naturally effective ingredients and extracts with potential use as therapeutic agents for the treatment of diabetes and prevention of diseases. Human saliva α-amylase is the most plentiful digestive enzyme in human saliva that hydrolyzes polysaccharides such as starch to oligosaccharides [75]. EEFO had IC50 value of 0.68 μg/mL (r 2 : 0.9706) toward α-glycosidase and 0.82 μg/mL against α-amylase enzyme (r 2 : 0.9525) (Table 3).…”

Section: Resultsmentioning

confidence: 99%

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Anticholinergic, Antidiabetic and Antioxidant Activities of Ferula orientalis L. Determination of Its Polyphenol Contents by LC-HRMS

Kızıltaş¹,

Gören²,

Bingöl³

et al. 2021

Rec.Nat.Prod.

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To evaluate the antioxidant activity of evaporated ethanolic extract of Ferula orientalis L. (EEFO) and lyophilized water extract of Ferula orientalis L. (WEFO) several in vitro antioxidant methods such as ABTS•+ scavenging activity, DPPH· scavenging activity, Fe3+reduction method, cupric ions (Cu2+) reduction capacity, and metal ion (Fe2+)-binding activities using ferrozine reagent were separately performed. Also, BHT, α-tocopherol and ascorbic acid were used as the standard antioxidant molecules. Moreover, some phenolic compounds that are responsible for antioxidant abilities of EEFO and WEFO were determined by LC-HRMS. EEFO and WEFO demonstrated effective antioxidant abilities when compared with the standards. EEFO demonstrated IC50 values of 1.946 µg/mL against acetylcholinesterase (AChE), 0.815 µg/mL against α-glycosidase, and 0.675 µg/mL against α-amylase.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Anticholinergic, Antidiabetic and Antioxidant Activities of Ferula orientalis L. Determination of Its Polyphenol Contents by LC-HRMS

Kızıltaş¹,

Gören²,

Bingöl³

et al. 2021

Rec.Nat.Prod.

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“…α-glycosidase inhibition efficacy of ethanol and water extracts of kınkor ( Ferulago stell ata ) was performed according to Tao et al [ 91 ] using p-nitrophenyl- d -glycopyranoside (p-NPG) substrate as described previously in details. The absorbances of samples were spectrophotometrically recorded at 405 nm [ 92 ]. First, 75 μL of phosphate buffer was mixed with 20 μL of the α-glycosidase solution (0.15 U/mL) in phosphate buffer (0.15 U/mL) pH 7.4) and 5 μL of different concentration ethanol and water extracts of kınkor ( Ferulago stell ata ) sample dissolved in ethanol and deionized water, respectively.…”

Section: Methodsmentioning

confidence: 99%

LC-HRMS Profiling and Antidiabetic, Anticholinergic, and Antioxidant Activities of Aerial Parts of Kınkor (Ferulago stellata)

et al. 2021

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Kınkor (Ferulago stellata) is Turkish medicinal plant species and used in folk medicine against some diseases. As far as we know, the data are not available on the biological activities and chemical composition of this medicinal plant. In this study, the phytochemical composition; some metabolic enzyme inhibition; and antidiabetic, anticholinergic, and antioxidant activities of this plant were assessed. In order to evaluate the antioxidant activity of evaporated ethanolic extract (EEFS) and lyophilized water extract (WEFS) of kınkor (Ferulago stellata), some putative antioxidant methods such as DPPH· scavenging activity, ABTS•+ scavenging activity, ferric ions (Fe3+) reduction method, cupric ions (Cu2+) reducing capacity, and ferrous ions (Fe2+)-binding activities were separately performed. Furthermore, ascorbic acid, BHT, and α-tocopherol were used as the standard compounds. Additionally, the main phenolic compounds that are responsible for antioxidant abilities of ethanol and water extracts of kınkor (Ferulago stellata) were determined by liquid chromatography-high-resolution mass spectrometry (LC-HRMS). Ethanol and water extracts of kınkor (Ferulago stellata) demonstrated effective antioxidant abilities when compared to standards. Moreover, ethanol extract of kınkor (Ferulago stellata) demonstrated IC50 values of 1.772 μg/mL against acetylcholinesterase (AChE), 33.56 ± 2.96 μg/mL against α-glycosidase, and 0.639 μg/mL against α-amylase enzyme respectively.

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“…The IC 50 was obtained from enzyme activity (%) versus and plant concentration plots [55]. Determination of IC 50 values were described previously [56].…”

Section: Determination Of Inhibition Parametersmentioning

confidence: 99%

Antidiabetic, anticholinergic and antioxidant activities of aerial parts of shaggy bindweed (Convulvulus betonicifolia Miller subsp.) – profiling of phenolic compounds by LC-HRMS

Bingöl

Kızıltaş

Gören

et al. 2021

Heliyon

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In order to evaluate the antioxidant activity of evaporated ethanolic extract (EESB) and lyophilized water extract (WESB) of Shaggy bindweed (Convulvulus betonicifolia Mill. Subs), some putative antioxidant methods such as DPPH⋅ scavenging activity, ABTS þ scavenging effect, ferric ions (Fe 3þ ) reduction method, cupric ions (Cu 2þ ) reducing capacity, and ferrous ions (Fe 2þ ) binding activities were separately performed. Also, ascorbic acid, α-tocopherol and BHT were used as the standard compounds. Additionally, some phenolic compounds that responsible for antioxidant abilities of EESB and WESB were screened by liquid chromatography-high resolution mass spectrometry (LC-HRMS). At the same concentration, EESB and WESB demonstrated effective antioxidant abilities when compared to standards. In addition, EESB demonstrated IC 50 values of 1.946 μg/mL against acetylcholinesterase (AChE), 0.815 μg/mL against α-glycosidase and 0.675 μg/mL against α-amylase enzymes.

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Design, synthesis, characterization, enzymatic inhibition evaluations, and docking study of novel quinazolinone derivatives

Cited by 44 publications

References 82 publications

Anticholinergic, Antidiabetic and Antioxidant Activities of Ferula orientalis L. Determination of Its Polyphenol Contents by LC-HRMS

Anticholinergic, Antidiabetic and Antioxidant Activities of Ferula orientalis L. Determination of Its Polyphenol Contents by LC-HRMS

LC-HRMS Profiling and Antidiabetic, Anticholinergic, and Antioxidant Activities of Aerial Parts of Kınkor (Ferulago stellata)

Antidiabetic, anticholinergic and antioxidant activities of aerial parts of shaggy bindweed (Convulvulus betonicifolia Miller subsp.) – profiling of phenolic compounds by LC-HRMS

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