α-Glucosidase inhibitory effects of polyphenols from Geranium asphodeloides: Inhibition kinetics and mechanistic insights through in vitro and in silico studies

Renda, Gülin; Sarı, Suat; Barut, Burak; Šoral, Michal; Liptaj, Tibor; Korkmaz, Büşra; Özel, Arzu; Erik, İshak; Şöhretoğlu, Didem

doi:10.1016/j.bioorg.2018.09.009

Cited by 30 publications

(23 citation statements)

References 36 publications

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“…The results showed that both quercetin and isoquercitrin can significantly reduce the glucose production in hepatocytes, accompanied by a significant decrease in the expressions of PEPCK and G6Pase, suggesting that these flavonoids can reduce hepatic gluconeogenesis by inhibiting the transcription of key enzyme genes. At present, it has been found that quercetin and isoquercitrin have hypoglycemic effects, and possible mechanisms include antagonizing oxidative stress and insulin resistance (13,14), inhibiting intestinal α-glucosidase (15,16), increasing endogenous glucagon-like peptide-1 (GLP-1) level (17), etc., suggesting that quercetin and isoquercitrin have independent roles in regulating glucose metabolism and improving insulin secretion. Our results are consistent with those of other scholars on the hypoglycemic effects of quercetin and isoquercetin.…”

Section: Discussionmentioning

confidence: 99%

Quercetin And Isoquercitrin Inhibiting Hepatic Gluconeogenesis Through Lkb1-Ampka Pathway

et al. 2020

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Objective. To observe the impact of quercetin and isoquercitrin on gluconeogenesis in hepatocytes. Methods. Mouse primary hepatocytes were cultured with lactic acid and pyruvic acid. After treatment with quercetin and isoquercitrin for 24 hours, the glucose concentration in the culture supernatant was determined. RT-PCR was used to detect the mRNAs of PEPCK, G6Pase, LKB1, and AMPKα. Protein levels of LKB1, AMPKα, and Thr172 phosphorylation were evaluated by Western blot. Results. The glucose concentration in the gluconeogenesis group (GN) was significantly higher than in the control group (C), but the glucose concentrations in the high level quercetin(group 80Q) and high level isoquercitrin (group 80I) were significantly lower than in the group GN, P<0.01. In the group 80Q, and group 80I, the mRNA levels of PEPCK and LKB1were significantly lower than in the group GN (P<0.01), and the G6Pase mRNA were significantly lower than in the group GN (P<0.05). The protein levels of LKB1 and the phosphorylation of AMPKα Thr172 in the group 80Q, group 40I, and group 80I were higher than in the group GN. The effects of quercetin and isoquercitrin on LKB1 and AMPKα were similar to those of metformin. Conclusions. Quercetin and isoquercitrin inhibit gluconeogenesis in hepatocytes, which may be related to the LKB1 upregulation and phosphorylation of AMPKα.

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Section: Discussionmentioning

confidence: 99%

Quercetin And Isoquercitrin Inhibiting Hepatic Gluconeogenesis Through Lkb1-Ampka Pathway

et al. 2020

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“…Figure 3b shows the double reciprocal lines of initial velocity against TF‐3‐G substrate, revealing that the values of maximum reaction velocity ( V max , reciprocal of y ‐axis intercept) remained constant and Michaelis constant ( K m , reciprocal of x ‐axis intercept) increased with increasing TF‐3‐G concentration, which confirmed a competitive inhibitory mode (Li et al., 2009; Renda et al., 2018; Zheng et al., 2020). Therefore, TF‐3‐G competed with the p NPG substrate for the α‐GC active site, resulting in the inhibition of α‐GC activity.…”

Section: Resultsmentioning

confidence: 83%

“…To elucidate the α-GC inhibitory mechanism of TF-3-G, enzymatic kinetic analysis was performed using different concentrations of α-GC and TF-3-G. with increasing TF-3-G concentration, which confirmed a competitive inhibitory mode (Li et al, 2009;Renda et al, 2018;Zheng et al, 2020). Therefore, TF-3-G competed with the pNPG substrate for the α-GC active site, resulting in the inhibition of α-GC activity.…”

Section: Analysis Of α-Gc Inhibitory Mechanism Of Tf-3-gmentioning

confidence: 90%

Insight into interaction mechanism between theaflavin‐3‐gallate and α‐glucosidase using spectroscopy and molecular docking analysis

Liu

Yin

et al. 2020

J. Food Biochem.

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Diabetes is a metabolic disease characterized by hyperglycemia and includes type 1 and type 2 diabetes (Zhang et al., 2016; Zhu et al., 2016). Type 2 diabetes is the most common form of diabetes, accounting for more than 90% of all cases, and is caused by insulin resistance, insufficient insulin secretion, or both (Wang et al., 2019). α-Glucosidase (α-GC), an important glycoside hydrolase in the digestive system, can hydrolyze the glycosidic bonds of starch and oligosaccharides in food and release glucose. Therefore, inhibiting

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“…At 30% AE, the high levels of polyphenols present could act as inhibitors of some enzymes involved in the metabolization of disaccharides and oligosaccharides, thus precluding their utilization. Many natural polyphenols like flavonoids and phenolic alcohols can act as enzymes inhibitors with IC50 starting from 0.6 mg/L (Rasouli et al 2017;Renda et al 2018;Bhatia et al 2019;Lim et al 2019). Most of them are present in alperujo and since they are water soluble, they are expected to be present in the AE (Araújo et al 2015;Rubio-Senent et al 2013).…”

Section: Characterization Of Alperujo Water and Aqueous Extract Of Almentioning

confidence: 99%

Evaluation of olive mill waste as substrate for carotenoid production by Rhodotorula mucilaginosa

Ghilardi

Negrete

Carelli

et al. 2020

Bioresour. Bioprocess.

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The “alperujo” is a waste from the olive oil industry with great potential for valorization. It has a high organic load, with the presence of valuable compounds such as biophenols and sugars. The use of this waste can be thought of as a biorefinery from which different compounds of high added value can be obtained, whether they are present in the “alperujo” such as biophenols or can be generated from the “alperujo”. Therefore, the production of carotenoids by Rhodotorula mucilaginosa was evaluated using the liquid fraction of ‘alperujo’ (Alperujo Water, AW) or an aqueous extract (AE) of “alperujo” at different concentrations (5, 10, 20 and 30% w/V) as substrates. The AEs had an acidic pH, a total sugar concentration ranging from 1.6 to 7.6 g/L, a polyphenols content from 0.4 to 2.9 g/L and a significant amount of proteins (0.5–3 g/L). AW is similar in composition as 30% AE, but with a higher amount of total sugars. Rh. mucilaginosa was able to grow at the different mediums with consumption of glucose and fructose, a reduction in protein content and alkalinization of the medium. Maximum total carotenoid production (7.3 ± 0.6 mg/L) was achieved at AW, while the specific production was higher when the yeast grew at AW or at 30% AE (0.78 ± 0.06 and 0.73 ± 0.10 mg/g of biomass, respectively). Torulene and torularhodin were the main carotenoids produced. Polyphenol content did not change; thus, it is still possible to recover these compounds after producing carotenoids. These results demonstrate the feasibility of using alperujo-based mediums as cheap substrates to produce torularhodin and torulene and to include this bioprocess as a step in an integral approach for alperujo valorization.

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α-Glucosidase inhibitory effects of polyphenols from Geranium asphodeloides: Inhibition kinetics and mechanistic insights through in vitro and in silico studies

Cited by 30 publications

References 36 publications

Quercetin And Isoquercitrin Inhibiting Hepatic Gluconeogenesis Through Lkb1-Ampka Pathway

Quercetin And Isoquercitrin Inhibiting Hepatic Gluconeogenesis Through Lkb1-Ampka Pathway

Insight into interaction mechanism between theaflavin‐3‐gallate and α‐glucosidase using spectroscopy and molecular docking analysis

Evaluation of olive mill waste as substrate for carotenoid production by Rhodotorula mucilaginosa

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