<i>N</i>‐Substituted pyrimidinethione and acetophenone derivatives as a new therapeutic approach in diabetes

Taslimi, Parham; Sujayev, Afsun; Karaman, Muhammet; Maharramova, Gunel; Sadeghian, Nastaran; Osmanova, Sabiya; Sardarova, Sabira; Majdi, Nargiz; Özel, Handan Ucun; Gülçın, İlhami

doi:10.1002/ardp.202000075

Cited by 12 publications

(8 citation statements)

References 47 publications

(46 reference statements)

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“…The main descriptor of fermentation with FOS was 2-Butanone, 4-hydroxy (p < 0.01), while the principal of Eco0% was acetone (p < 0.05) (Figure S5C,D). Acetophenone deserves attention, since it acts as antimicrobial to different Gram-negative bacteria [51], and its N-substitute derivates have been proposed as a therapeutic approach in diabetes [52]. In our experimental condition, it probably derived from the bacterial deconjugation of polyphenols, where Eco4% is rich.…”

Section: Volatilome Analysis Through Spme Gc/msmentioning

confidence: 91%

Colonic In Vitro Model Assessment of the Prebiotic Potential of Bread Fortified with Polyphenols Rich Olive Fiber

et al. 2021

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The use of olive pomace could represent an innovative and low-cost strategy to formulate healthier and value-added foods, and bakery products are good candidates for enrichment. In this work, we explored the prebiotic potential of bread enriched with Polyphenol Rich Fiber (PRF), a defatted olive pomace byproduct previously studied in the European Project H2020 EcoProlive. To this aim, after in vitro digestion, the PRF-enriched bread, its standard control, and fructo-oligosaccharides (FOS) underwent distal colonic fermentation using the in vitro colon model MICODE (multi-unit colon gut model). Sampling was done prior, over and after 24 h of fermentation, then metabolomic analysis by Solid Phase Micro Extraction Gas Chromatography Mass Spectrometry (SPME GCMS), 16S-rDNA genomic sequencing of colonic microbiota by MiSeq, and absolute quantification of main bacterial species by qPCR were performed. The results indicated that PRF-enriched bread generated positive effects on the host gut model: (i) surge in eubiosis; (ii) increased abundance of beneficial bacterial groups, such as Bifidobacteriaceae and Lactobacillales; (iii) production of certain bioactive metabolites, such as low organic fatty acids; (iv) reduction in detrimental compounds, such as skatole. Our study not only evidenced the prebiotic role of PRF-enriched bread, thereby paving the road for further use of olive by-products, but also highlighted the potential of the in vitro gut model MICODE in the critical evaluation of functionality of food prototypes as modulators of the gut microbiota.

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Section: Volatilome Analysis Through Spme Gc/msmentioning

confidence: 91%

Colonic In Vitro Model Assessment of the Prebiotic Potential of Bread Fortified with Polyphenols Rich Olive Fiber

et al. 2021

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“…For determination of hCA inhibition assay, hCA I, and II isoenzymes were purified by Sepharose‐4B‐L‐Tyrosine‐sulfanilamide affinity column chromatography from human erythrocytes. [ 64 ] The inhibitory activities of the newly synthesized complexes (1a–e, 2a–e) were spectrophotometrically determined according to the method of Verpoorte et al [ 65 ] Both ChE inhibitory activities of the title complexes against AChE and BChE were determined by Ellman's method. [ 66 ] In this assay, AChE from electric eel ( Electrophorus electricus ) and BChE from equine serum were used.…”

Section: Methodsmentioning

confidence: 99%

Silver N‐heterocyclic carbene complexes bearing fluorinated benzyl group: Synthesis, characterization, crystal structure, computational studies, and inhibitory properties against some metabolic enzymes

Bal

Demirci

Şen

et al. 2021

Applied Organom Chemis

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A series of the silver N‐heterocyclic carbene (NHC) complexes have been synthesized from the reactions between benzimidazolium salts bearing fluorinated benzyl group and Ag2O via the deprotonation method. All Ag(I)NHC complexes were characterized by known spectroscopic techniques (1H nuclear magnetic resonance [NMR], 13C NMR, and Fourier transform infrared [FT‐IR]) and elemental analysis. The molecular structures of the two complexes were unambiguously elucidated through single‐crystal X‐ray diffraction analysis. Namely, X‐ray studies show that the coordination geometry around the Ag(I) atom in the case of complex 2c is revealed to be almost linear with C–Ag–Cl angle, whereas in complex 2e, it appears as a nonlinear structure. The inhibitory profiles of these new complexes are investigated on some metabolic enzymes. Representatively, the most potent complex against human carbonic anhydrase isoenzymes I and II (hCAs I and II), 2d, was 1.8 times more potent than standard inhibitor acetazolamide against hCAs I and II. On the other hand, complexes 2c and 2b as most potent compounds against both cholinesterase enzymes was around 5 and 1.6 times more potent than tacrine against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. The most active α‐glucosidase inhibitor 2d had similar activity to acarbose as a standard inhibitor. Furthermore, it confirms its in vitro studies as a result of molecular docking studies for each enzyme with (i) binding energy and inhibition constant values and (ii) the definition of the best conformation and nonbonding interactions of the related complexes (2b, 2c, and 2d) against the different target proteins.

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“…Considering their bioactivity, some are desirable, such as the ketones bodies [53]; others, such as acetone, are unwanted because they could be toxic for the host [54]. Acetophenone deserves attention since it acts as an antimicrobial to different Gram-negative bacteria [55], and its N-substitute derivates have been proposed as a therapeutic approach in diabetes [56]. In our experimental conditions, it probably derived from the bacterial deconjugation of polyphenols, where FLS is presumably rich.…”

Section: Volatilome Analysis Of Aldehydes Ketones Alcohols and Phenolicsmentioning

confidence: 96%

Multiunit In Vitro Colon Model for the Evaluation of Prebiotic Potential of a Fiber Plus D-Limonene Food Supplement

Nissen

Valerii

Spisni

et al. 2021

Foods

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The search for new fiber supplements that can claim to be “prebiotic” is expanding fast, as the role of prebiotics and intestinal microbiota in well-being has been well established. This work explored the prebiotic potential of a novel fiber plus D-Limonene supplement (FLS) in comparison to fructooligosaccharides (FOS) over distal colonic fermentation with the in vitro model MICODE (multi-unit in vitro colon gut model). During fermentation, volatilome characterization and core microbiota quantifications were performed, then correlations among volatiles and microbes were interpreted. The results indicated that FLS generated positive effects on the host gut model, determining: (i) eubiosis; (ii) increased abundance of beneficial bacteria, as Bifidobacteriaceae; (iii) production of beneficial compounds, as n-Decanoic acid; (iv) reduction in detrimental bacteria, as Enterobaceteriaceae; (v) reduction in detrimental compounds, as skatole. The approach that we followed permitted us to describe the prebiotic potential of FLS and its ability to steadily maintain the metabolism of colon microbiota over time. This aspect is two-faced and should be investigated further because if a fast microbial turnover and production of beneficial compounds is a hallmark of a prebiotic, the ability to reduce microbiota changes and to reduce imbalances in the productions of microbial metabolites could be an added value to FLS. In fact, it has been recently demonstrated that these aspects could serve as an adjuvant in metabolic disorders and cognitive decline.

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N‐Substituted pyrimidinethione and acetophenone derivatives as a new therapeutic approach in diabetes

Cited by 12 publications

References 47 publications

Colonic In Vitro Model Assessment of the Prebiotic Potential of Bread Fortified with Polyphenols Rich Olive Fiber

Colonic In Vitro Model Assessment of the Prebiotic Potential of Bread Fortified with Polyphenols Rich Olive Fiber

Silver N‐heterocyclic carbene complexes bearing fluorinated benzyl group: Synthesis, characterization, crystal structure, computational studies, and inhibitory properties against some metabolic enzymes

Multiunit In Vitro Colon Model for the Evaluation of Prebiotic Potential of a Fiber Plus D-Limonene Food Supplement

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