جستجوی مقالات مرتبط با کلیدواژه "alpha amylase" در نشریات گروه "شیمی"

A set of newer generation imidazolo-pyrimidine derivatives was designed, synthesized, and evaluated for in-vitro alpha amylase activity. The design of the molecules was fully depend upon the structural features of previously developed molecules, and then all the molecules were docked with 1OSE porcine alpha amylase enzyme which showed good docking interaction scores between (-9.2 and -10.2) kcal/mol compared to standard acarbose (-6.9 kcal/mol). The interacting residues of (F1-F6) and 1OSE showed similar amino acid lining as present in the active site. The synthetic procedure of the molecules (F1-F6) was divided into three parts such as synthesis of chalcone derivative using aromatic aldehyde and acetophenone, synthesis of phenyl linked oxazolone derivatives using aromatic aldehyde and hippuric acid, then finally merged both the final products of step 1 and step 2 in presence of glacial acetic acid to obtain the final series of molecules. All the molecules showed characteristic peaks in FTIR, 1H-NMR, and Mass spectrometry with sharp melting point and single peak in TLC plate. Then in vitro alpha amylase inhibition activity was performed which showed that all the molecules observed with good IC50 values than standard acarbose. The presence of hydroxyl and methoxy group showed good impact on biological activity. Finally the results postulated that F3 was the best molecule as in vitro alpha amylase inhibitor.

A newer generation pyrimidine derivatives were designed, synthesized, and evaluated in vitro alpha amylase and bacterial growth inhibitor. The molecules' design fully depended upon the structural features of previously pyrimidine derivatives. Then all the designed molecules (SD1-SD100) were docked with 1OSE pig pancreatic alpha-amylase isoenzyme. S-[4-(2-hydroxyphenyl)-6-phenylpyrimidin-2-yl] benzenecarbothioate, S-(4,6-diphenylpyrimidin-2-yl) benzenecarbothioate, S-[4-(4-hydroxy-3-methoxyphenyl)-6-phenylpyrimidin-2-yl] benzenecarbothioate, and S-[4,6-bis(4-hydroxyphenyl)pyrimidin-2-yl] benzenecarbothioate showed good docking interaction scores, as compared to acarbose. The interacting residues of the synthesized molecules and 1OSE showed similar amino acid lining as present in the active site. The synthetic procedure of the molecules was divided into two steps such as synthesis of chalcone derivative using aromatic aldehyde and acetophenone, reaction between chalcone and thiourea to form substituted pyrimidine-2-thiol, then finally substituted pyrimidine-2-thiol and benzoyl chloride reacted in presence of glacial acetic acid to obtain the best docked molecules. All the molecules show characteristic peaks in FTIR, 1H-NMR and Mass spectrometric data. Among all the synthesized molecules S-[4-(2-hydroxyphenyl)-6-phenylpyrimidin-2-yl] benzenecarbothioate showed best in vitro alpha amylase inhibition activity. Also, all synthesized molecules showed moderate to good antibacterial activities.

Raphanus sativus L., which belongs to the Brassicaceae family and is commonly known as Radish, is a vegetable grown and consumed around the world as a part of the human diet. All parts, including the seeds, of this plant are intended for diabetes treatment. However, due to the presence of poor water-soluble phytoconstituents and the low bioavailability of seeds, their nanoparticles were prepared by nanoprecipitation followed by the probe sonication method. They were also characterized by FTIR, FESEM, and zeta sizer. In addition, the plant extract was subjected to quantitative estimation of total flavonoid and phenolic compounds. The particle size and polydispersity index of prepared nanoparticles were found to be 203.76±2.24 nm and 0.89, respectively. The Zeta potential of the prepared nanoparticles was -6.29 mV. The in vitro antidiabetic effect of the prepared plant extract and its nanoparticles were estimated using the alpha-amylase and alpha-glucosidase inhibition methods and compared with the standard drug Acarbose, which shows significant inhibition of both amylolytic enzymes in a dose-dependent manner.

The various parts of Citrus sinensis plant have been employed over the years for medicinal purposes. As part of the concept of waste to wealth, the medicinal importance of the peels was exploited. This study aimed at determining the antioxidant and in vitro antidiabetic activities of fermented peel extracts of C. sinensis. Fermentation of the peels was carried out, and phytochemical tests were done. DPPH free radical scavenging activity, anti-lipid peroxidation and Antidiabetic assay method were performed in vitro using standard procedures. C. sinensis were rich in polyphenols and reducing sugars. Radical scavenging assay showed an IC50 of 0.57μg/ml and 1.60μg/ml for fresh peels and dried peels respectively for DPPH assay, and 0.67μg/ml (fresh) and 0.72μg/ml (dried) for anti-lipid peroxidation assay. The α-amylase inhibition assay showed that the fermented fresh peels and fermented dried peels had IC50 values of 2.23μg/ml and 2.73μg/ml respectively. The α-glucosidase assay showed better inhibition by the extracts. Fermented fresh and dried peels had IC50 values of 0.03μg/ml and 0.03μg/ml respectively. Fermented fresh peels of C. sinensis expressed relatively stronger protection in the antioxidant and antidiabetic assays than the fermented dried peels. This study revealed that extracts can be considered as an important addition to the therapeutic management for diabetes.