A facile approach synthesis of benzoylaryl benzimidazole as potential α-amylase and α-glucosidase inhibitor with antioxidant activity

2021 ◽  
pp. 105073
Author(s):  
Lotfi M. Aroua ◽  
Hind R. Almuhaylan ◽  
Fahad M. Alminderej ◽  
Sabri Messaoudi ◽  
Sridevi Chigurupati ◽  
...  
2017 ◽  
Vol 17 (1) ◽  
pp. 39 ◽  
Author(s):  
Jainur Rochman ◽  
Tri Agus Siswoyo ◽  
A.A. Istri Ratnadewi

Study activities phenolic extract of bungur leaf as an antioxidant and inhibitor for the enzyme α-glucosidase was performed by spectrophotometric method. The extraction was carried out by three solvents with different polarity level in order to get three types of extracts namely hexane extract Bungur (HB), ethyl acetate extract Bungur (EAB), and the methanol extract Bungur (MB). The units, used in the analysis, is the total phenolic that standardized in gallic acid. The antioxidant activity of phenolic extracts Bungur leaf can be seen from its ability to reduce free radicals through the damping test DPPH radical, superoxide anion, and hydroxyl. Potential extract phenolic leaf Bungur as an inhibitor of α-glucosidase were analyzed by inhibition of α-glucosidase, but in this study also tested the inhibition of the enzyme α-amylase because both of these enzymes worked on the digestive system and hydrolyze carbohydrates. The results generally showed that the methanol extract of leaves Bungur potential as antioxidants that compared with standard vitamin C. In addition, it had as well as potential for inhibitors of α-glucosidase and α-amylase that compared akarbosa standard, which is expected to be a natural antidiabetic agent.Keywords: phenolic, bungur, antioxidant, inhibitor, α-amilase, α-glukosidase 


2020 ◽  
Vol 17 (10) ◽  
pp. 806-814
Author(s):  
Emre Menteşe ◽  
Fatih Yılmaz ◽  
Nimet Baltaş

In this work, some new 2-[(3,4-dichlorophenyl)methyl]-1H-benzimidazole derivatives containing different five-membered heterocycles like 1,3,4-oxadiazole, 1,3,4-triazole, and 1,3,4- thiadiazole moieties were designed and efficiently synthesized starting from 2-[(3,4-dichlorophenyl) methyl]-1H-benzimidazole. The products were screened for their in vitro antioxidant and α-glucosidase inhibitory activities. Among the synthesized compounds, some of them showed efficient α-glucosidase inhibition with IC50 values ranging between 16.05 ± 0.94 and 77.02 ± 1.12 μg/mL when they were compared with the standard α-glucosidase inhibitor acarbose having IC50 value 12.04 ± 0.68 μg/mL. The antioxidant activity of all products was screened by using various in vitro antioxidant assays, including CUPric Reducing Antioxidant Capacity (CUPRAC) and Ferric Reducing Antioxidant Power (FRAP) assays. Also, the radical scavenging activities of the products were assayed by using the ABTS method. method.


INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (12) ◽  
pp. 41-50
Author(s):  
Priyanka Rathod ◽  
Chandana Kulkarni ◽  
Raman P. Yadav

In recent years, pancreatic lipase inhibitor and α- glucosidase inhibitor have been highlighted as potential anti-diabesity principles. In the present study, seeds of Phyllanthus emblica L. (Family: Phyllanthaceae) was studied for anti-diabesity potential in terms of pancreatic lipase inhibitory activity, α-glucosidase inhibitory activity and antioxidant activity. At 100μg/ml concentration, pancreatic lipase inhibition of the methanolic extract using synthetic substrate obtained was 73.2±0.1% (IC50 59.1μg/ml), whereas pancreatic lipase inhibition using natural substrate was 87.9 ± 2.62%. α- glucosidase inhibition of the extract at 50μg/ml was measured as 94.4±0.37% (IC50 34.4μg/ml). The superoxide scavenging activity of the extract was found to be 81.5±0.41%. Interestingly, upon TLC fingerprinting, only one band with Rf 0.70 showed multifunctional activity. The phytochemical found to be present was an alkaloid. The results evidenced the presence of multifunctional smart molecule in methanolic extract of P. emblica L and showed an alkaloid as the component responsible for anti-diabesity potential.


2020 ◽  
Vol 15 (1) ◽  
pp. 47
Author(s):  
Syahira Addina ◽  
Subaryono Subaryono ◽  
Sukarno Sukarno

Oligosakarida alginat (OSA) adalah produk hasil depolimerisasi polimer alginat yang biasanya terdiri dari 2-25 monomer. Produksi OSA dapat dilakukan melalui proses enzimatis, fisik maupun kimiawi. Tujuan penelitian ini adalah mengetahui karakteristik dan bioaktivitas OSA sebagai antioksidan dan inhibitor α-glukosidase. Proses produksi OSA dilakukan secara enzimatis dengan 3 cara penambahan alginat liase yaitu ditambahkan satu kali di awal reaksi (E1), ditambahkan 4 kali dengan interval  2 jam (E2) dan 2 kali interval 4 jam (E3) dengan total volume sama, yaitu 0,15 mL dan aktivitas enzim (1 unit/mL). Total waktu inkubasi adalah 8 jam. Karakterisasi OSA yang dilakukan adalah perhitungan rendemen, analisis profil TLC dan FTIR serta kadar gula pereduksi. Metode DPPH (1,1-diphenyl-2-picrylhydrazyl) digunakan untuk menguji aktivitas antioksidan OSA, sedangkan pengamatan terhadap aktivitas inhibitor α-glukosidase dilakukan dengan melihat aktivitas α-glukosidase dalam mengubah substrat yang diberikan. Hasil penelitian menunjukkan bahwa rendemen OSA dan kadar gula pereduksi tidak berbeda nyata antar perlakuan dengan rendemen OSA berkisar antara 77,29±1,97% hingga 85,46±9,15% dan kadar gula pereduksi OSA berkisar antara 290,32±20,42 µg/mL hingga 312,76±4,74 µg/mL. Aktivitas antioksidan tertinggi diperlihatkan oleh OSA E1 dengan penghambatan terhadap DPPH sebagai radikal bebas sebesar 41,22±2,03% pada konsentrasi 1,2 mg/mL. Aktivitas inhibitor α-glukosidase OSA E1 lebih kecil dibandingkan dengan alginat dengan nilai IC50 masing-masing sebesar 11,23±4,17 ppm dan 5,27±0,29 ppm. Proses depolimerisasi alginat meningkatkan aktivitas alginat sebagai antioksidan namun tidak meningkatkan aktivitasnya sebagai inhibitor α-glukosidase. AbstractAlginate oligosaccharides (AOS) is depolymerization of alginate polymer product that consist of 2-25 monomers. Alginate oligosaccharides can be produced by enzymatic, physical and chemical processes. This research was conducted to find out the characteristics and bioactivity of AOS as an antioxidant and α-glucosidase inhibitor. AOS was produced by enzymatic process with 3 procedures of the addition of the alginate lyase that was added once at the beginning reaction (E1), 4 times every 2 hours (E2) and 2 times every 4 hours (E3) with the same addition of enzyme volume (0.15 mL) and enzyme activity (1 unit/mL). Total incubation times was 8 hours. Alginate oligosaccharides was then characterized their  yield, TLC, FTIR profiles and reducing sugar content.  DPPH (1,1-diphenyl-2-picrylhydrazyl) method was used to determine antioxidant activity of AOS while observation of α-glucosidase  activity in changing the substrate was used to determine inhibitor α-glucosidase activity of AOS. The results showed that yields and reducing sugar level of AOS were not significantly different between treatments. The AOS yields ranged from 77.29±1.97% to 85.46±9.15% and the reducing sugar levels ranged from 290.32±20.42 µg/mL to 312.76±4.74 µg/mL. The highest antioxidant activity was shown by AOS E1 with free radical (DPPH) inhibition of 41.22±2.03%. AOS E1 α-glucosidase inhibitor activity was lower than that of alginate, with the IC50 values of 5.27±0.29 ppm for alginate and 11.23±4.17 ppm for AOS. Depolymerization process of alginates increased antioxidant activity but did not enhance its activity as α-glucosidase inhibitor.  


2014 ◽  
Vol 24 (2) ◽  
pp. 737-743 ◽  
Author(s):  
Rizna Triana Dewi ◽  
Sanro Tachibana ◽  
Sofa Fajriah ◽  
Muhammad Hanafi

2017 ◽  
Vol 87 (3-4) ◽  
pp. 191-200 ◽  
Author(s):  
Nidhal Soualeh ◽  
Aliçia Stiévenard ◽  
Elie Baudelaire ◽  
Rachid Soulimani ◽  
Jaouad Bouayed

Abstract. In this study, cytoprotective and antioxidant activities of Rosa canina (RC) and Salix alba (SA), medicinal plants, were studied on mouse primary splenocytes by comparing Controlled Differential Sieving process (CDSp), which is a novel green solvent-free process, versus a conventional technique, employing hydroethanolic extraction (HEE). Thus, preventive antioxidant activity of three plant powders of homogeneous particle sizes, 50–100 µm, 100–180 µm and 180–315 µm, dissolved directly in the cellular buffer, were compared to those of hydroethanolic (HE) extract, at 2 concentrations (250 and 500 µg/mL) in H2O2-treated spleen cells. Overall, compared to HE extract, the superfine powders, i. e., fractions < 180 µm, at the lowest concentration, resulted in greater reactive oxygen species (ROS) elimination, increased glutathione peroxidase (GPx) activity and lower malondialdehyde (MDA) production. Better antioxidant and preventive effects in pre-treated cells were found with the superfine powders for SA (i. e., 50–100 µm and 100–180 µm, both p < 0.001), and with the intermediate powder for RC (i. e., 100–180 µm, p < 0.05) versus HE extract. The activity levels of catalase (CAT) and superoxide dismutase (SOD) in pretreated splenocytes exposed to H2O2, albeit reduced, were near to those in unexposed cells, suggesting that pretreatment with the fine powders has relatively restored the normal levels of antioxidant-related enzymes. These findings supported that CDSp improved the biological activities of plants, avoiding the use of organic solvents and thus it could be a good alternative to conventional extraction techniques.


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