Anthraquinone-type inhibitor of α-glucosidase enhances glucose uptake by activating an insulin-like signaling pathway in C2C12 myotubes

Alam, Badrul; Bajpai, Vivek K.; Ra, Jeong-Sic; Lim, Jin Hee; An, Hongyan; Shukla̽, Shruti; Quan, Khong Trong; Khan, Imran; Huh, Yun Suk; Han, Young‐Kyu; Na, MinKyun; Lee, Sang‐Han

doi:10.1016/j.fct.2019.05.005

Cited by 7 publications

(7 citation statements)

References 27 publications

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“…Values of Vmax and Km were calculated by fitting the slope of linear regression in the Michaelis-Menten formula and are listed in Table 3 . As (1) the inhibitor concentration is increased and the Km value is also increased without affecting the value Vmax, (2) the Lineweaver–Burk plot shows the intersection of straight lines with different slopes on the Y axis, which were characteristic of the reversible competitive inhibitor [ 25 ]. Consequently, the kinetic analyzed data demonstrated that the inhibition of the KGDHC by parapyruvate was typically a concentration-dependent reversible competitive type rather than an irreversible inhibitor.…”

Section: Resultsmentioning

confidence: 99%

Using Taguchi Method to Determine the Optimum Conditions for Synthesizing Parapyruvate

Lee

Yang

2022

Molecules

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The synthesis of parapyruvate is important for the analysis of the content in the pyruvate supplements and the study of aging-related neurodegenerative diseases. However, the pure parapyruvate crystal is not, as yet, commercially available. In this study, we applied the Taguchi’s L9 orthogonal array to investigate the optimal conditions for the preparation of the pure parapyruvate by the alkaline treatment of the pyruvic acid and then followed it with the solvent crystallization steps. We were also interested in revealing the major factors that affect the yield for the synthesized pure parapyruvate crystals. In addition, the parapyruvate-inhibited enzyme kinetic of α-ketoglutarate dehydrogenase complex (KGDHC) was also investigated. We found that the pure parapyruvate could be obtained in combination with an alkaline treatment and two solvent crystallization steps. The main factors affecting the yield of the pure parapyruvate were the concentration of the pyruvic acid (the reactant), the pH of the alkali treatment, the type of solvent used for the crystallization and the volume ratio of solvent used for crystallization. Finally, the optimal conditions could prepare parapyruvate crystals with a high purity of 99.8% and a high yield of 72.8%. In addition, the results demonstrate that parapyruvate is a reversibly competitive inhibitor for KGDHC.

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Section: Resultsmentioning

confidence: 99%

Using Taguchi Method to Determine the Optimum Conditions for Synthesizing Parapyruvate

Lee

Yang

2022

Molecules

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“…The antioxidant and enzyme inhibitory capability of various URADP extracts was evaluated using the procedures outlined in earlier publications [ 8 , 39 , 52 , 53 ]. Antioxidant experiments employed ascorbic acid as a positive control.…”

Section: Methodsmentioning

confidence: 99%

Antioxidant, Tyrosinase, α-Glucosidase, and Elastase Enzyme Inhibition Activities of Optimized Unripe Ajwa Date Pulp (Phoenix dactylifera) Extracts by Response Surface Methodology

Alshammari

Alam

Song

et al. 2023

IJMS

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The Ajwa date (Phoenix dactylifera L., Arecaceae family) is a popular edible fruit consumed all over the world. The profiling of the polyphenolic compounds of optimized unripe Ajwa date pulp (URADP) extracts is scarce. The aim of this study was to extract polyphenols from URADP as effectively as possible by using response surface methodology (RSM). A central composite design (CCD) was used to optimize the extraction conditions with respect to ethanol concentration, extraction time, and temperature and to achieve the maximum amount of polyphenolic compounds. High-resolution mass spectrometry was used to identify the URADP’s polyphenolic compounds. The DPPH-, ABTS-radical scavenging, α-glucosidase, elastase and tyrosinase enzyme inhibition of optimized extracts of URADP was also evaluated. According to RSM, the highest amounts of TPC (24.25 ± 1.02 mgGAE/g) and TFC (23.98 ± 0.65 mgCAE/g) were obtained at 52% ethanol, 81 min time, and 63 °C. Seventy (70) secondary metabolites, including phenolic, flavonoids, fatty acids, and sugar, were discovered using high-resolution mass spectrometry. In addition, twelve (12) new phytoconstituents were identified for the first time in this plant. Optimized URADP extract showed inhibition of DPPH-radical (IC50 = 87.56 mg/mL), ABTS-radical (IC50 = 172.36 mg/mL), α-glucosidase (IC50 = 221.59 mg/mL), elastase (IC50 = 372.25 mg/mL) and tyrosinase (IC50 = 59.53 mg/mL) enzymes. The results revealed a significant amount of phytoconstituents, making it an excellent contender for the pharmaceutical and food industries.

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“…The capability of ZLE to restrain α-glucosidase activity was determined in accordance with the reported method [79]. With 0.2 U/mL of α-glucosidase in 0.1 M sodium phosphate buffer (pH 7.0), the sample solutions of 2 µL of different concentrations (1,3,10,30, and 100 µg/mL) were mixed, and incubated for 10 min at 37 • C. Then, pNPG (substrate) was mixed into the prepared solution to terminate enzyme-substrate activity at 37 • C for 1 h. The enzyme-substrate reaction was carried out at 37 • C for 30 min.…”

Section: Inhibitory Assay Of α-Glucosidasementioning

confidence: 99%

Metabolite Profiling of Manilkara zapota L. Leaves by High-Resolution Mass Spectrometry Coupled with ESI and APCI and In Vitro Antioxidant Activity, α-Glucosidase, and Elastase Inhibition Assays

Islam

Alam

Ann

et al. 2020

IJMS

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High-resolution mass spectrometry equipped with electrospray ionization (ESI) and atmospheric pressure chemical ionization (APCI) sources was used to enhance the characterization of phytochemicals of ethanol extracts of Manilkara zapota L. leaves (ZLE). Sugar compounds, dicarboxylic acids, compounds of phenolic acids and flavonoids groups, and other phytochemicals were detected from the leaves. Antioxidant activity and inhibition potentiality of ZLE against α-glucosidase enzyme, and elastase enzyme activities were evaluated in in vitro analysis. ZLE significantly inhibited activities of α-glucosidase enzyme at a lower concentration (IC50 2.51 ± 0.15 µg/mL). Glucose uptake in C2C12 cells was significantly enhanced by 42.13 ± 0.15% following the treatment with ZLE at 30 µg/mL. It also exhibited potential antioxidant activities and elastase enzyme inhibition activity (IC50 27.51 ± 1.70 µg/mL). Atmospheric pressure chemical ionization mass spectrometry (APCI–MS) detected more m/z peaks than electrospray ionization mass spectrometry (ESI–MS), and both ionization techniques illustrated the biological activities of the detected compounds more thoroughly compared to single-mode analysis. Our findings suggest that APCI along with ESI is a potential ionization technique for metabolite profiling, and ZLE has the potential in managing diabetes by inhibiting α-glucosidase activity and enhancing glucose uptake.

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Anthraquinone-type inhibitor of α-glucosidase enhances glucose uptake by activating an insulin-like signaling pathway in C2C12 myotubes

Cited by 7 publications

References 27 publications

Using Taguchi Method to Determine the Optimum Conditions for Synthesizing Parapyruvate

Using Taguchi Method to Determine the Optimum Conditions for Synthesizing Parapyruvate

Antioxidant, Tyrosinase, α-Glucosidase, and Elastase Enzyme Inhibition Activities of Optimized Unripe Ajwa Date Pulp (Phoenix dactylifera) Extracts by Response Surface Methodology

Metabolite Profiling of Manilkara zapota L. Leaves by High-Resolution Mass Spectrometry Coupled with ESI and APCI and In Vitro Antioxidant Activity, α-Glucosidase, and Elastase Inhibition Assays

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