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It is now believed that the inhibition of carbohydrate hydrolyzing enzymes (CHEs) in the digestive tract can significantly prolong the overall carbohydrate digestion time and decrease the postprandial hyperglycemia after a meal. Therefore, inhibitors of CHEs can be useful therapeutic approaches in the management of diabetes mellitus, especially in...
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... For thin-layer chromatography, a TLC aluminum sheet precoated with silica gel (silica gel 60 F254) was used and visualized under UV (λmax = 254 nm and/or 366 nm). The 1 H NMR and 13 C NMR spectra were recorded using a Bruker Advance spectrometer (500 MHz for 1 H NMR and 125 MHz for 13 C NMR, Bruker Bioscience, Billerica, MA, USA). Chemical shifts were referenced to TMS or the residual solvent (CDCl3 = 7.26 ppm for 1 H and 77.0 ppm for 13 C spectroscopy; Acetone-d6 = 2.05 ppm for 1 H and 29.9, 206.7 ppm for 13 C spectroscopy). ...
... The crude residue was purified by column chromatography (silica gel, n-hexane-EtOAc mixture) to afford the coupling products. 19 13 (E)-N- (2-(3,4,5-trimethoxystyryl) 13 ...
... The crude residue was purified by column chromatography (silica gel, n-hexane-EtOAc mixture) to afford the coupling products. 19 13 (E)-N- (2-(3,4,5-trimethoxystyryl) 13 ...
... It should be noted that a large number of Salvia species have been scarcely studied for their antidiabetic potential. A study by Nickavar and Abolhasani [67] reported that the ethanolic extract of Salvia virgata showed a dose-dependent α-amylase inhibition with an IC 50 of 19.08 mg/mL. Enzyme inhibition assays performed on the Salvia urmiensis Bunge methanolic extract showed the highest α-glucosidase and α-amylase inhibition with the lowest IC 50 values (IC 50 = 8.3 and 24 µg/mL) [68]. ...
Context: Salvia balansae de Noé (S. balansae) (Lamiaceae) is known to be an important plant used in folk medicine as an herbal remedy in Algeria. Objective: The purpose of the present study was to demonstrate the phytochemical composition, antioxidant activities, enzyme inhibitory activities, and antimicrobial activities of S. balansae extracts. Materials and methods: A methanolic extract and a petroleum ether extract from the aerial parts of the plant were assessed for their chemical composition. HPLC-MS and HPLC-DAD assessed the content of phenols, GC-MS the fatty acid composition, and ICP-MS the mineral profiles of the plant. Additionally, we evaluated the bioactivities of S. balansae extracts by the DPPH, ABTS, and CUPRAC assays, including the antioxidant potential against AChE, BChE, α-amylase, and α-glucosidase for enzyme inhibition. The antibacterial and antifungal activities of the methanolic extract were determined by the disc diffusion test against several strains of bacteria and yeasts. Results: Our findings revealed that the aerial parts of S. balansae were rich in phytochemical components and contained large amounts of minerals. Quantitative analysis of phenolic compounds by HPLC-DAD revealed the presence of 12 compounds in three major classes, flavonoids, hydroxycinnamic acid, and phenolic acid derivatives, with 0.61, 0.45, and 0.29 mg/g of extract, respectively. Nine phenolic constituents were quantified by HPLC-MS analysis; catechin (72.5%) was the main compound, followed by myricetin (21.7%). The fatty acid composition of the S. balansae petroleum ether extract by GC-MS analysis was quantified. Seventeen compounds, including palmitic acid, were identified as the major fatty acids. The antioxidant activity of the S. balansae extracts was measured by three different methods: the methanol extract provided better results than the petroleum ether extract, and interesting values were noted for the DPPH, ABTS, and CUPRAC assays of 242.7 ± 7.44, 124.1 ± 9.70, and 222.9 ± 6.05 µg/mL, respectively. The enzyme inhibition activity of the plant could not be determined. The antimicrobial results of the methanolic extract obtained from the disc diffusion method, followed by measurements of MIC, MBC, and MFC against several bacteria and yeasts, indicated that S. balansae exhibited noticeable antimicrobial and antifungal activities. Conclusions: These results provided new data about the main phenolic compounds and biological activities of extracts of the aerial parts of S. balansae, which might be an alternative source for synthetic bioactive compounds.
... Alpha-glucosidase and alpha-amylase are digestive enzymes accountable for interrupting carbohydrates for absorption [56,57]. Therefore, synthesized products having inhibitory effects on carbohydrate hydrolyzing enzymes may be a useful way to manage diabetes [57,58]. According to Balan et al. [59], α-glucosidase inhibition is useful for treating non-insulin diabetes. ...
Background:
The current study aimed to develop an economic plant-based therapeutic agent to improve the treatment strategies for diseases at the nano-scale because Cancer and Diabetes mellitus are major concerns in developing countries. Therefore, in vitro and in vivo anti-diabetic and anti-cancerous activities of Trillium govanianum conjugated silver nanoparticles were assessed.
Methods:
In the current study synthesis of silver nanoparticles using Trillium govanianum and characterization were done using a scanning electron microscope, UV-visible spectrophotometer, and FTIR analysis. The in vitro and in vivo anti-diabetic and anti-cancerous potential (200 mg/kg and 400 mg/kg) were carried out.
Results:
It was discovered that Balb/c mice did not show any major alterations during observation of acute oral toxicity when administered orally both TGaqu (1000 mg/kg) and TGAgNPs (1000 mg/kg), and results revealed that 1000 mg/kg is not lethal dose as did not find any abnormalities in epidermal and dermal layers when exposed to TGAgNPs. In vitro studies showed that TGAgNPs could not only inhibit alpha-glucosidase and protein kinases but were also potent against the brine shrimp. Though, a significant reduction in blood glucose levels and significant anti-cancerous effects was recorded when alloxan-treated and CCl4-induced mice were treated with TGAgNPs and TGaqu.
Conclusion:
Both in vivo and in vitro studies revealed that TGaqu and TGAgNPs are not toxic at 200 mg/kg, 400 mg/kg, and 1000 mg/kg doses and possess strong anti-diabetic and anti-cancerous effects due to the presence of phyto-constituents. Further, suggesting that green synthesized silver nanoparticles could be used in pharmaceutical industries to develop potent therapeutic agents.
... Chrysoeriol (31) and tricetin (32) are closely related to luteolin but lesser researched flavones. Interestingly, there was great consensus in the three studies confirming chrysoeriol's stronger activity on α-glucosidase than acarbose, 57,102,132 and one result reporting on its generally weak inhibition of α-amylase at 1,270 µM, 133 making chrysoeriol (31) an attractive ligand for further optimization. Meanwhile, tricetin (32) was the subject of only one paper and was found to weakly inhibit both enzymes. ...
... 32,44,57,58,81,172,195,201,206,209,224,234,235 Quercitrin (99), also known as quercetin-3-rhamnoside, appeared to potently inhibit α-glucosidase in a mixed manner, 218 noticeably better than acarbose in more than 12 studies. 38,55,58,78,83,102,133,140,188,217,237,238 However, only one research examined quercitrin as an α-amylase inhibitor, which showed quercitrin as roughly 30 times stronger than acarbose. 47 Following this, quercetin-3-rutinoside or rutin (100) had excellent α-glucosidase inhibitory activity while marginally inhibiting α-amylase, which could be a promising antidiabetic agent. ...
Diabetes mellitus remains a major global health burden and great attention is directed at natural therapeutics. This systematic review aimed to evaluate the potential of flavonoids as antidiabetic agents through their ability to inhibit α-amylase and α-glucosidase, two key starch digestive enzymes. Six scientific databases were queried up until August 21, 2022, for in vitro studies reporting the IC50 results of purified flavonoids on α-amylase or α-glucosidase, along with the respective data of acarbose control. A total of 339 articles were assessed as eligible and subjected to the data extraction process, resulting in 1643 retrieved flavonoid structures. Chemical structures were then rigorously standardized and curated to 974 unique compounds, in which 177 flavonoids showed both inhibitions against α-amylase and α-glucosidase. Quality assessment was conducted following a modified CONSORT checklist. The structure-activity relationships revealed that a double bond C2=C3 and a keto group C4=O is essential for simultaneous inhibition. The hydroxyl group at C3 is favourable for α-glucosidase inhibition but detrimental to the effect against α-amylase. Further notable features which affect α-glucosidase and α-amylase inhibition were also discussed. Several limitations were considered, including the inconsistency among included studies, language restriction, and the contemporaneity of the review. In conclusion, the systematic review has summarized some crucial findings in the investigation of flavonoids as dual-target inhibitors against α-glucosidase and α-amylase and proposed several orientations for future research.
... Chrysoeriol (31) and tricetin (32) are closely related to luteolin but lesser researched flavones. Interestingly, there was great consensus in the three studies confirming chrysoeriol's stronger activity on α-glucosidase than acarbose, 76,117,146 and one result reporting on its generally weak inhibition of α-amylase at 1,270 µM, 147 making chrysoeriol (31) an attractive ligand for further optimization. Meanwhile, tricetin (32) was the subject of only one paper and was found to weakly inhibit both enzymes. ...
Diabetes mellitus remains a major global health burden and great attention is directed at natural therapeutics. This systematic review aimed to evaluate the potential of flavonoids as antidiabetic agents through their ability to inhibit α-amylase and α-glucosidase, two key starch digestive enzymes. Six scientific databases were queried up until August 21, 2022, for in vitro studies reporting the IC50 results of purified flavonoids on α-amylase or α-glucosidase, along with the respective data of acarbose control. A total of 339 articles were assessed as eligible and subjected to the data extraction process, resulting in 1643 retrieved flavonoid structures. Chemical structures were then rigorously standardized and curated to 974 unique compounds, in which 177 flavonoids showed both inhibitions against α-amylase and α-glucosidase. Quality assessment was conducted following a modified CONSORT checklist. The structure-activity relationships revealed that a double bond C2=C3 and a keto group C4=O is essential for simultaneous inhibition. The hydroxyl group at C3 is favourable for α-glucosidase inhibition but detrimental to the effect against α-amylase. Further notable features which affect α-glucosidase and α-amylase inhibition were also discussed. Several limitations were considered, including the inconsistency among included studies, language restriction, and the contemporaneity of the review. In conclusion, the systematic review has summarized some crucial findings in the investigation of flavonoids as dual-target inhibitors against α-glucosidase and α-amylase and proposed several orientations for future research.
... Chrysoeriol (31) and tricetin (32) are closely related to luteolin but lesser researched flavones. Interestingly, there was great consensus in the three studies confirming chrysoeriol's stronger activity on α-glucosidase than acarbose, 78,119,148 and one result reporting on its generally weak inhibition of α-amylase at 1,270 µM, 149 making chrysoeriol (31) an attractive ligand for further optimization. Meanwhile, tricetin (32) was the subject of only one paper and was found to weakly inhibit both enzymes. ...
Diabetes mellitus remains a major global health burden and great attention is directed at natural therapeutics. This systematic review aimed to evaluate the potential of flavonoids as antidiabetic agents through their ability to inhibit α-amylase and α-glucosidase, two key starch digestive enzymes. Six scientific databases were queried up until August 21, 2022, for in vitro studies reporting the IC50 results of purified flavonoids on α-amylase or α-glucosidase, along with the respective data of acarbose control. A total of 339 articles were assessed as eligible and subjected to the data extraction process, resulting in 1643 retrieved structures, 177 compounds of which showed both inhibitions against α-amylase and α-glucosidase. Quality assessment was conducted following a modified CONSORT checklist. The structureactivity relationships revealed that a double bond C2=C3 and a keto group C4=O is essential for simultaneous inhibition. The hydroxyl group at C3 is favourable for α-glucosidase inhibition but detrimental to the effect against α-amylase. Further notable features which affect α-glucosidase and α-amylase inhibition were also discussed. Several limitations were considered, including the inconsistency among included studies, language restriction, and the contemporaneity of the review. In conclusion, the systematic review has summarized some crucial findings in the investigation of flavonoids as dual-target inhibitors against α-glucosidase and α-amylase and proposed several orientations for future research.
... Hence, patients suffering from diabetes should need to take every possible control measures to minimize their postprandial blood glucose level (Xiao-Ping et al., 2010). One of the effective therapeutic approaches for treating diabetes is to lower the postprandial hyperglycemia level by suppressing glucose absorption through inhibition of the carbohydrate-hydrolyzing enzymes, namely α-amylase and α-glucosidase (De Souza Schmidt Goncalves et al., 2010;Nickavar & Abolhasani, 2013). According to Western medical practice, acarbose can help in blunting the postprandial plasma glucose rise by prolonging the enzymatic hydrolysis of complex carbohydrates, thereby delaying glucose absorption (Shobana et al., 2009). ...
Fourier transform infrared spectroscopy (FTIR) is a simple, rapid analytical technique used for the identification of organic functional groups of biomolecules. This study aimed to investigate the use of FTIR spectroscopy method for rapid detection of the α-glucosidase inhibitory activity of crude extracts of edible leafy plants, characterization of functional groups of chemical components present in crude extracts, and identification of possible biomolecules responsible for α-glucosidase inhibitory activity. Powdered leaves of five different plants, namely Le-kola pala (LE) (Premna procumbens), Kora kaha (KK) (Memecylon umbellatum), Koppa (KO) (Polyscias scutellaria), Stevia (ST) (Stevia rebaudiana), and Yaki naran (YK) (Atlantia ceylanica) were sequentially extracted with hexane, ethyl acetate (EtOAc) and methanol (MeOH). The FTIR spectra of crude plant extracts were obtained following the KBr pellet method, within the range of 4000-500 cm-1. The plant extracts were subjected to assay the α-glucosidase inhibitory activity. Further, the multivariate predictive models for α-glucosidase inhibitory activity were developed using partial least square (PLS) regression analysis. The highest Rc 2 (0.96), Rcv 2 (0.87), Rp 2 (0.93), and the lowest RMSEC (24.10), RMSECV (41.70), and RMSEP (81.04) values were noticed for spectral region range from 1700 cm-1 to 1800 cm-1 , indicating the strongest correlation to the α-glucosidase inhibitory activity, while the spectral region range from 1500 cm-1 to 1700 cm-1 was found to have the lowest Rc 2 (0.71), Rcv 2 (0.52), Rp 2 (0.45) and the highest RMSEC (61.14) and RMSECV (80.21), indicating the lowest correlation to the α-glucosidase inhibitory activity. As the peak appearing in the range of 1700-1800 cm-1 is usually ascribed to C=O stretching vibration of ester groups, ketones, and carboxylic acids, there was a strong correlation between α-glucosidase inhibitory activity with those organic functional groups. The present study suggests that FTIR spectral analysis together with PLS regression analysis would be a convenient, rapid tool to determine α-glucosidase inhibitory activity of plant extracts.
... Diabetes mellitus could be a gathering of metabolic maladies in which there are tall blood sugar levels over a drawn-out period. A restorative approach to diminish hyperglycemia is to restrain the carbohydrate processing chemicals (α-glucosidase and α-amylase), in this manner avoiding the breakdown of carbohydrates into monosaccharides which may be a fundamental cause of expanding blood glucose levels [22,23]. In this manner, creating compounds having inhibitory exercises toward carbohydrate hydrolyzing proteins may be a valuable way to oversee diabetes. ...
Ecofriendly nanoparticle synthesis is an ongoing worldwide effort to treat many human diseases. In the present study, Punica granatum peel extract is a reducing agent for green synthesizing silver nanoparticles (AgNPs). Further partially characterized by preliminary phytochemical screening, UV–visible spectroscopy analysis, Fourier-transform infrared spectroscopy (FT-IR) and gas chromatography–mass spectroscopy analysis (GC–MS). AgNPs potential was confirmed by in vitro antidiabetic activity, and its ability to inhibit carbohydrate digesting enzymes. AgNPs showed the least inhibition of enzymes with the highest value of 84.0% at 20 mg/ml, 79.0% at 20 mg/ml concentration of α-amylase and α-glucosidase enzyme activity, respectively. The enzymatic assay results revealed the existence of AgNPs can exhibit the dose-dependent inhibition on α Amylase enzyme α-glucosidase potentials. Our results suggest that P. granatum peel extract contains (AgNPs) a good antidiabetic agent against the key enzymes involved in diabetes. Hence, moral activity can be used to make appropriate nanomedicines and pharmaceutical industries.
... In animal models, it has ameliorated acute skin inflammation [21] and exhibited reno-protection against acute kidney injury [22]. Additionally, chrysoeriol has proved to be a promising antidiabetic compound in vitro [23][24][25][26] and in animal models [27][28][29][30][31][32]. It has also exhibited anti-hyperlipidemic activity in diabetic rats [33]. ...
... Moreover, the results indicated that this extract was more effective on the α-glucosidase inhibitory experiment (IC50 = 2.55 mg/mL), this activity could be due to the synergistic actions of different bioactive metabolites quantified in this medicinal plant as well as the content of C-glycosyl flavones. These findings are consistent with the results of the research produced by Nickavar and Abolhasani [26], in which they found that chrysoeriol isolated from the aerial parts of Salvia virgata Jacq. Exhibited strong antihyperglycemic activity. ...
A flavone, chrysoeriol is synthetized in several plant species. It comes from several natural sources, especially medicinal plants. The identification and isolation of this compound has been carried out and verified by several research teams using different spectral methods. It seems that the concentration of this molecule is variable and fluctuating depending on the source, the part extracted, the region, and the methods of extraction and characterization. The aim of this paper is to highlight the in vitro and in vivo pharmacological properties of chrysoeriol and to provide insight into its pharmacokinetics. Anticancer, anti-inflammatory, antibacterial, antifungal, anti-osteoporosis, anti-insecticide, and neuroprotective actions have been shown in a number of studies on this chemical. Different mechanisms in theses pharmacological effects include subcellular, cellular, and molecular targets. In vivo pharmacokinetic analysis has proved the good stability of this molecule, showing its promising potential to prevent or treat diseases including cancer, diabetes, inflammation, osteoporosis, Parkinson’s disease, and cardiovascular diseases.
... Chrysoeriol also increased hepatic glycogen synthase activity and decreased hepatic glycogen phosphorylase activities to increase hepatic glycogen content, thereby preventing the liver damage and preventing the shrinkage of pancreatic islet β-cells with reduced fatty infiltration (Krishnan et al. 2020). Moreover, it was demonstrated that chrysoeriol concentration-dependently inhibited the pancreatic α-amylase activity in-vitro, thus suggesting that chrysoeriol reduces the breakdown of glycogen (Nickavar and Abolhasani 2013). These effects of chrysoeriol likely account for the protection of liver and kidney function in STZ-induced diabetic rats (Amélia, et al. 2010;Krishnan, Pugalendi, and Saravanan 2019). ...
Diabetes, being the most widespread illness, poses a serious threat to global public health. It seems that inflammation plays a critical role in the pathophysiology of diabetes. This review aims to demonstrate a probable link between type 2 diabetes mellitus (T2DM) and chronic inflammation during its development. Additionally, the current review examined the bioactivity of natural flavones and the possible molecular mechanisms by which they influence diabetes and inflammation. While natural flavones possess remarkable anti-diabetic and anti-inflammatory bioactivities, their therapeutic use is limited by the low oral bioavailability. Several factors contribute to the low bioavailability, including poor water solubility, food interaction, and unsatisfied metabolic behaviors, while the diseases (diabetes, inflammation, etc.) causing even less bioavailability. Throughout the years, different strategies have been developed to boost flavones' bioavailability, including structural alteration, biological transformation, and innovative drug delivery system design. This review addresses current advancements in improving the bioavailability of flavonoids in general, and flavones in particular. Clinical trials were also analyzed to provide insight into the potential application of flavonoids in diabetes and inflammatory therapies.
