Synthesis and biological evaluation of bromophenol derivatives with cyclopropyl moiety: Ring opening of cyclopropane with monoester

Boztaş, Murat; Taslimi, Parham; Yavari, Mirali Akbar; Gülçın, İlhami; Şahin, Ertan; Menzek, Abdullah

doi:10.1016/j.bioorg.2019.103017

Cited by 81 publications

(38 citation statements)

References 88 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Comparing current results with previous results, it was found that novel bromophenols (Ki: 159.6-924.2 nM) [4] , oxazolidinone (Ki: 16.5-35.6 nM) [48] , pyrazolines (Ki: 48.2-84.1 nM) [76] , hydrazones (Ki: 66-128 nM) [77] , tacrine derivatives (Ki: 68-8480 nM) [78] , sulfamides (Ki: 0.027-0.076 nM) [79] , olivetol (Ki: 3.40 nM) [73] , and benzenesulfonamides (Ki: 22.7-109.1 nM) [80] effectively inhibited AChE enzyme. As seen in Figure 4, α-glycosidase enzyme, which released from intestine cells, hydrolyzes the oligosaccharides and polysaccharide to monosaccharide units, such as glucose and fructose in small intestine.…”

Section: Resultssupporting

confidence: 82%

“…Enzymes are catalyst molecules that are specific to reactions, which accelerate chemical reactions and return to their original state even if they have been physically altered during these reactions. [1][2][3][4] Reduce or destroy the enzymes in the event of activity both in vivo and in vitro by certain compounds called enzyme inhibition. Inhibitor is a molecule or ions that binds to an enzyme and decreases its activity.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

The inhibition profile of sesamol against α-glycosidase and acetylcholinesterase enzymes

Topal

2019

International Journal of Food Properties

View full text Add to dashboard Cite

Sesamol (1,3-benzodioxol-5-ol) is found in the oilseed product, sesame. In our study, the inhibitory effects of sesamol compound on acetylcholinesterase and α-glycosidase enzymes were evaluated. Another aim of this study was to compare the inhibitory effects of sesamol to acarbose for α-glycosidase enzyme and tacrine for acetylcholinesterase (AChE). Sesamol exhibited noncompetitive inhibition for both metabolic enzymes. IC 50 values for AChE and αglycosidase enzymes were calculated as 86.63 nM and 99.00 nM, respectively. On the other hand, K i values were calculated as 46.68 nM and 75.33 nM for AChE and α-glycosidase enzymes, respectively. According to the obtained results showed effective inhibition at low concentrations. ARTICLE HISTORY

show abstract

Section: Resultssupporting

confidence: 82%

Section: Introductionmentioning

confidence: 99%

The inhibition profile of sesamol against α-glycosidase and acetylcholinesterase enzymes

Topal

2019

International Journal of Food Properties

View full text Add to dashboard Cite

show abstract

“…Thus, digestive enzyme inhibition had a crucial therapeutic route for the treatment of DM. [59,60] α-Amylase and α-glycosidase enzymes were released from small intestine cells. Both digestive enzymes hydrolyze oligosaccharide and polysaccharide molecules to monosaccharides such as glucose.…”

Section: Introductionmentioning

confidence: 99%

Anticholinergic, antidiabetic and antioxidant activities of cinnamon ( cinnamomum verum ) bark extracts: polyphenol contents analysis by LC-MS/MS

Gülçın

Kaya

Gören

et al. 2019

International Journal of Food Properties

Self Cite

131

View full text Add to dashboard Cite

Ethanolic (EEC) and aqueous (WEC) extracts of cinnamon (Cinnamomum verum)were evaluated for their antioxidant profiles by eight distinguished bioanalytical antioxidant methods. Their inhibitory effects were tested against some enzymes including acetylcholinesterase, butyrylcholinesterase, α-glycosidase and αamylase, which linked to different diseases. Additionally, the antioxidant properties were determined and polyphenolic compositions of the both extracts were evaluated by LC-MS/MS analysis. According to the LC-MS/MS experiments, thirteen compounds were found in WEC and EEC. Also, p-hydroxybenzoic acid (321.1 mg/kg extract), p-coumaric acid (291.4 mg/kg extract), and pyrogallol (142.4 mg/kg extract) were found to be the most abundant ingredients in the WEC. On the other hand, pyrogallol (264.3 mg/kg extract), ferulic acid (224.7 mg/ kg extract) and p-coumaric acid (170.2 mg/kg extract) were found as the most plentiful chemicals in the EEC. For the estimation of the antioxidant capacities of the both extracts (WEC and EEC), DPPH· and ABTS •+ scavenging activities, as well as Fe 3+ -Fe 2+ , and Cu 2+ -Cu + reducing assays were studied. The IC 50 values of the WEC and EEC indicated that they were potent effective DPPH· (21. 25 and 15.71 μg/mL) and ABTS •+ (6.52 and 5.79 μg/mL) scavengers, as well as AChE (221.33 and 110.26 μg/mL), BChE (461.69 and 94.93 μg/mL), α-glycosidase (206.86 and 220.00 μg/mL) and α-amylase (189.86 and 200.86 μg/mL) inhibitors. As a conclusion, both EEC and WEC had rich phenolic contents and demonstrated effective anticholinergic, antidiabetic and antioxidant effects. ARTICLE HISTORY

show abstract

“…The pathophysiology of Alzheimer's disease (AD) is related to the depletion of neurotransmitter acetylcholine (ACh) due to acetylcholinesterase (AChE) activity. One of the curative strategies (possible) is to increase the concentration of ACh in brain cells using AChE inhibitors.BChE enzyme is an enzyme used in cholinergic mechanism and is actively used in this system [23,24]. Cholinesterase inhibitors (ChEIs) are extensively used in medicine pharmacological correction of cholinergic neurotransmission pathology.…”

Section: Introductionmentioning

confidence: 99%

Formulation a modern chemotherapeutic drug of Ziziphora clinopodides Lam leaf aqueous extract conjugated cadmium nanoparticles and analysis of their anti-acute myeloid leukemia potentials in comparison to Daunorubicin in leukemic mouse and cellular models: Antidiabetic and Anticholinergics Potentials

Mahdavi

Zangeneh

Paydarfar

et al. 2020

Preprint

Self Cite

View full text Add to dashboard Cite

In this study, the anti-acute myeloid leukemia (AML) effects of Ziziphora clinopodioides Lam leaf aqueous extract conjugated cadmium nanoparticles (CdNPs) were compared with daunorubicin as a common chemotherapeutic drug. To synthesize CdNPs, Z. clinopodioides aqueous extract was combined with Cd(NO 3 ) 2 .4H 2 O. For analyzing CdNPs, SEM, UV-Vis. spectroscopy, X-ray powder diffraction and Energy dispersing X-ray spectroscopy, Fourier Transform Infrared techniques were used. In FE-SEM images of CdNPs, the diameter of particle dimension was on means of 26.78 nm. To survey the cytotoxicity and anti-AML effects of Cd(NO 3 ) 2 , Z. clinopodioides, Daunorubicin, CdNPs and MTT assay was used on the human AML cell lines. The IC50 of the cadmium nanoparticles was 168, 205 and 210 µg/mL against Murine C1498, 32D/FLT3-ITD and Human HL-60/vcr cell lines, respectively. In vivo study, CdNPs like daunorubicin ameliorated importantly (P≤0.01) the biochemical, WBC, RBC, inflammatory, platelet, stereological, histopathological and cellular-molecular parameters compared to the other groups. As mentioned, the cadmium nanoparticles had significant anti-AML effects. After approving the above eventuate in the clinical trial studies, these cadmium nanoparticles could be used in humans as a chemotherapeutic medicament for the treatment of AML. Additionally, the novel nanoparticles (Cd(NO 3 ) 2 and CdNPs) were good inhibitors of the α-glycosidase, and cholinesterase enzymes.

show abstract

Synthesis and biological evaluation of bromophenol derivatives with cyclopropyl moiety: Ring opening of cyclopropane with monoester

Cited by 81 publications

References 88 publications

The inhibition profile of sesamol against α-glycosidase and acetylcholinesterase enzymes

The inhibition profile of sesamol against α-glycosidase and acetylcholinesterase enzymes

Anticholinergic, antidiabetic and antioxidant activities of cinnamon ( cinnamomum verum ) bark extracts: polyphenol contents analysis by LC-MS/MS

Contact Info

Product

Resources

About