Α-glucosidase Inhibitory Properties Research Articles

The screening of α-glucosidase inhibitory peptides from β-conglycinin and hypoglycemic mechanism in HepG2 cells and zebrafish larvae

Inhibition of carbohydrate digestive enzymes is a key focus across diverse fields, given the prominence of α-glucosidase inhibitors as preferred oral hypoglycaemic drugs for diabetes treatment. β-conglycinin is the most abundant functional protein in soy; however, it is unclear whether the peptides produced after its gastrointestinal digestion exhibit α-glucosidase inhibitory properties. Therefore, we examined the α-glucosidase inhibitory potential of soy peptides. Specifically, β-conglycinin was subjected to simulated gastrointestinal digestion by enzymatically cleaving it into 95 peptides with gastric, pancreatic and chymotrypsin enzymes. Eight soybean peptides were selected based on their predicted activity; absorption, distribution, metabolism, excretion and toxicity score; and molecular docking analysis. The results indicated that hydrogen bonding and electrostatic interactions play important roles in inhibiting α-glucosidase, with the tripeptide SGR exhibiting the greatest inhibitory effect (IC50 = 10.57 μg/mL). In vitro studies revealed that SGR markedly improved glucose metabolism disorders in insulin-resistant HepG2 cells without affecting cell viability. Animal experiments revealed that SGR significantly improved blood glucose and decreased maltase activity in type 2 diabetic zebrafish larvae, but it did not result in the death of zebrafish larvae. Transcriptomic analysis revealed that SGR exerts its anti-diabetic and hypoglycaemic effects by attenuating the expression of several genes, including Slc2a1, Hsp70, Cpt2, Serpinf1, Sfrp2 and Ggt1a. These results suggest that SGR is a potential food-borne bioactive peptide for managing diabetes.

Chiral (S)-BINOL-phosphates: Design, synthesis and their antibacterial and α-glucosidase inhibition studies

A new series of chiral (S)-BINOL-derived phosphoric acid derivatives (8a-k) with 3,3′-disubstitution were successfully synthesized under microwave irradiation, yielding high product quantities within a short reaction time. The antibacterial and α-glucosidase inhibitory properties of these compounds were evaluated. Notably, compound 8b exhibited remarkable antibacterial efficacy against B. subtilis, S. aureus, S. epidermidis, P. aeruginosa, and K. pneumoniae, with a MIC value of 1.17 g mL−1. Furthermore, the electron-withdrawing nitro group-containing derivative, 8d displayed potent antibacterial activity (MIC = 1.17 g mL−1) against B. subtilis, S. epidermidis, and E. coli. Among the synthesized compounds, compound 8b, containing chloro substitutions at the 3,5-positions of the phenyl groups in (S)-3,3′-disubstituted BINOL, demonstrated the most noteworthy α-glucosidase inhibitory activity with IC50 value of 2.067 ± 0.017 M.

Augmentation of α-amylase and α-glucosidase inhibitory properties of Callerya speciosa root extracts: An exploration through simulated human gastrointestinal digestion

The present work represents the first effort to evaluate the effect of an in vitro simulated human digestion model on the α-amylase and α-glucosidase inhibitory activities of Callerya speciosa root extracts. Through bioguided fractionation, a series of fractions were obtained from hexane (CSH) and ethyl acetate (CSE) extracts. Initial screening identified active fractions (CSH2, CSH3, CSE2, CSE3, and CSE4) for further in vitro digestion evaluation. The results showed a decrease in antioxidant activity across all samples after digestion, while a simultaneous increase in α-amylase and α-glucosidase inhibitory activities was observed during the small intestinal phase. Notably, compared with the undigested fraction, CSE3 demonstrated a 1.7-fold increase in α-amylase inhibition (IC50 = 0.86 mg/mL). Moreover, the α-glucosidase inhibitory activities of CSH3, CSE3, and CSE4 were significantly greater after digestion, with IC50 values of 0.18, 0.05, and 0.02 mg/mL, respectively. Impressively, during the small intestinal phase, the α-glucosidase inhibitory activities of CSH3, CSE3, and CSE4 were substantially greater than those of acarbose by 13.2-, 47.6-, and 119.0-fold, respectively, and greater than those of palmitic acid by 1.7-, 6.0-, and 15.0-fold, respectively. GC-MS and LC-ESI-MS/MS analyses identified isoflavonoids, fatty acids, and triterpenoids as key bioactive compounds in these fractions. The present work provided foundational insights for the future exploration of C. speciosa root extracts for diabetes management.

Characterization of microencapsulated powders rich in saponins from cocoa pod husk (Theobroma cacao L.) and medicinal plant an xoa (Helicteres hirsuta Lour.)

Cocoa pod husk (CPH) is a major residue of cocoa processing industry, while medicinal plant H. hirsuta is used for treatment of malaria and diabetes mellitus in folk medicine. This study aimed to produce microencapsulated powders from saponin-enriched CPH and H. hirsuta extracts and assess their physicochemical, phytochemical, antioxidant, and α-glucosidase inhibition properties. The findings show that the microencapsulated powders were achieved diserable physicochemical properties (moisture of 3.22–4.76 %, water activity of 0.43–0.46, water solubility index of 74.18–88.77 %, particle size of 254.2–719.7 nm, and zeta potential from −6.97 to −15.1 mV). The phytochemical content of microencapsulated CPH powders gained at high levels (total saponin content of 151.87–193.46 mg EE/g DS, total flavonoid content of 33.80–46.05 mg CE/g DS), total alkaloid content of 15.20–24.23 mg AA/g DS, and total phenolic content of 5.41–6.49 mg GAE/g DS). The antioxidant potential of microencapsulated CPH powders using ARSC and FRAP assays was 15.51–18.20 and 9.61–11.89 mg TE/g DS, respectively, while their α-glucosidase inhibition capacity at 100 μg/mL was found at 51.74–52.16 %. The phytochemical content (except total alkaloid content), antioxidant, and α-glucosidase inhibitory potential of microencapsulated CPH powders were smaller than those of microencapsulated H. hirsuta and combined powders. This study reveals that the microencapsulated CPH and H. hirsuta powders were prospective in reducing hyperglycemia activity. Therefore, this study provided an evidence for further application of CPH and H. hirsuta plant for functional food development.

Nanosupplements based on protein-polysaccharide coacervates loaded with essential oils: Evaluation of antioxidant and antidiabetic properties

Essential oils (EOs) have demonstrated potential in food products to prevent complications related to diabetes. Nevertheless, the physicochemical characteristics of pure EOs, including high volatility and low chemical stability, face significant challenges when considering their utilization as functional ingredients. Thus, this study aimed to develop nanosupplements based on protein-polysaccharide coacervates loaded with EOs, thyme (THY) and oregano (ORE), and to evaluate their colloidal, antioxidant, and α-glucosidase and α-amylase inhibitory properties following an in vitro gastrointestinal digestion process. First, heat-induced egg white protein nanoparticles (EWPn) were used to encapsulate both EOs as nanocomplexes. Second, the process to obtain nanosupplements involved the electrostatic deposition of high methoxyl pectin (HMP) onto the surface of pre-formed nanocomplexes, resulting in the production of EWPn-THY-HMP and EWPn-ORE-HMP powders through a freeze-drying process. The effects of in vitro digestion on particle size, zeta potential, stability, and bioaccessibility of systems were analyzed. HMP exhibited a slight ability to protect EWPn from gastric digestion, while encapsulation within the EWPn-HMP system prevented the chemical degradation of EOs during gastrointestinal digestion. Subsequently, the antioxidant properties and the inhibitory effects of digested systems on α-glucosidase and α-amylase activities were examined. After in vitro digestion, EWPn-THY-HMP and EWPn-ORE-HMP systems showed higher ABTS+ radical scavenging than pure EOs (around 70% vs. 30%, respectively). Additionally, reducing power activities (expressed as mg of ascorbic acid equivalents-AAE mL−1) of EWPn-THY-HMP and EWPn-ORE-HMP systems were higher (1.6 ± 0.0 mg and 1.8 ± 0.1 mg of AAE mL−1, respectively) compared to pure THY and ORE (approximately 1.5 mg of AAE mL−1 for both) after in vitro digestion. The α-glucosidase inhibitory activity of EOs decreased upon encapsulation within EWPn-HMP system from an IC50 value of 0.3–1.0 μg mL−1, approximately. However, the effect of encapsulation on α-amylase inhibitory activity was EOs-dependent, and it was higher for the EWPn-ORE-HMP system, with an IC50 value of 8.6 ± 0.2 μg mL−1. The results highlight the potential of EOs encapsulation within EWPn-HMP coacervate nanosupplements as a promising strategy to facilitate their incorporation into food matrices while preserving their antioxidant and α-glucosidase and α-amylase inhibitory properties.

Polydopamine Coating of Graphitic Carbon Nitride, g-C3N4, Improves Biomedical Application.

Graphitic carbon nitride (g-C3N4) is an intriguing nanomaterial that exhibits photoconductive fluorescence properties under UV-visible light. Dopamine (DA) coating of g-C3N4 prepared from melamine was accomplished via self-polymerization of DA as polydopamine (PDA). The g-C3N4 was coated with PDA 1, 3, and 5 times repeatedly as (PDA@g-C3N4) in tris buffer at pH 8.5. As the number of PDA coatings was increased on g-C3N4, the peak intensity at 1512 cm-1 for N-H bending increased. In addition, the increased weight loss values of PDA@g-C3N4 structures at 600 °C from TGA thermograms confirmed that the coating was accomplished. The band gap of g-C3N4, 2.72 eV, was reduced to 0.87 eV after five coatings with PDA. A pristine g-C3N4 was found to have an isoelectric point (IEP) of 4.0, whereas the isoelectric points of 1PDA@g-C3N4 and 3PDA@g-C3N4 are close to each other at 3.94 and 3.91, respectively. On the other hand, the IEP of 5PDA@g-C3N4 was determined at pH 5.75 assuming complete coating with g-C3N4. The biocompatibility of g-C3N4 and PDA@g-C3N4 against L929 fibroblast cell lines revealed that all PDA@g-C3N4 coatings were found to be biocompatible up to a 1000 mg/mL concentration, establishing that PDA coatings did not adversely affect the biocompatibility of the composite materials. In addition, PDA@g-C3N4 was screened for antioxidant potential via total phenol content (TPC) and total flavonoid content assays and it was found that PDA@g-C3N4 has recognizable TPC values and increased linearly with an increased number of PDA coatings. Furthermore, blood compatibility of pristine g-C3N4 is enhanced considerably upon PDA coating, affirmed by hemolysis and the blood clotting index%. Additionally, α-glucosidase inhibitory properties of PDA@g-C3N4 structures revealed that 67.6 + 9.8% of this enzyme was evenly inhibited by 3PDA@g-C3N4 structure.

In vitro α-glucosidase, docking and density functional theory studies on novel azide metal complexes.

Aim: The goal of this study is to synthesize new metal complexes containing N-methyl-1-(pyridin-2-yl)methanimine and azide ligands as α-glucosidase inhibitors for Type 2 diabetes. Materials & methods: The target complexes (12-16) were synthesized by reacting N-methyl-1-(pyridin-2-yl)methanimine (L1) with sodium azide in the presence of corresponding metal salts. The investigation of target protein interactions, vibrational, electronic and nonlinear optical properties for these complexes was performed by molecular docking and density functional theorystudies. Results: Among these complexes, complex 13 (IC50=0.2802±0.62μM) containing Hg ion showed the highest α-glucosidase inhibitory property. On the other hand, significant results were detected for complexes containing Cu and Ag ions. Conclusion: Complex 13 may be an alternate anti-diabetic inhibitor according to in vitro/docking results.

Non-aggregated and water soluble non-peripherally octa substituted Co(II) and Cu(II) phthalocyanines: Synthesis and α-glucosidase inhibitory effects

Type 2 diabetes (T2DM) is a progressive metabolic disease associated with high blood sugar levels that affects 537 million people worldwide. This study aim is to investigate the potential for use in the treatment of T2DM by examining the in vitro glucosidase inhibitory effects of novel synthesized metallophthalocyanines. For this reason, we have synthesized cobalt(II), copper(II) phthalocyanines (3PY-ON-CoQ, 3PY-ON-CuQ) that are both water-soluble and do not aggregate in water. These compounds were characterized by using various spectroscopic methods. The α-glucosidase inhibitory properties of 3PY-ON-CoQ and 3PY-ON-CuQ were carried out using the spectrophotometric method. Then, Lineweaver-Burk and Dixon plots were examined to determine the inhibitory type and constant (Ki). The IC50 values of 3PY-ON-CoQ and 3PY-ON-CuQ were 6.85 ± 1.25 μM and 55.09 ± 2.64 μM, respectively. Both compounds displayed mixed inhibitory effects on α-glucosidase according to Lineweaver-Burk plots. The Ki values of 3PY-ON-CoQ and 3PY-ON-CuQ were calculated as 6.30 ± 1.55 μM and 54.25 ± 1.20 μM, respectively. The results of this work may lead to the discovery of new compounds for the treatment of T2DM.

First report on glucocerebrosides from unripe banana peel: Its anti-inflammatory and α-glucosidase inhibition properties

Banana peel represents a significant waste product of banana processing industries that can yield high-value products. Banana peel contains flavonols, tannins, alkaloids, terpenoids, and various phenolic compounds such as catechin, epicatechin, and catecholamines. Recent studies have demonstrated the immunomodulatory, anti-inflammatory, and antidiabetic potential of these compounds. The current work serves as the first report on the glucocerebroside (GC) consortium from the unripe banana peel Musa (AAB) cv. Nendran. Through high resolution mass spectrometry analysis, we have identified eighteen molecular species of GC, containing α- and ω‑hydroxy fatty acids. The in vitro anti-inflammation potential of GC consortium was assessed in RAW 264.7 murine macrophage cell line. The GC consortium at a dose of 50 μg/mL, showed a significant reduction in lipopolysaccharide (LPS)-induced nitric oxide (NO) production. The enzyme-linked immunosorbent assay (ELISA) analysis demonstrated GC's immunomodulation potential by showing a reduction in pro-inflammatory cytokines and increase in anti-inflammatory cytokine production. Furthermore, GC exhibited potent α-glucosidase inhibition with an IC50 value of 5.12 ± 0.51 μg/mL, significantly lower than standard acarbose (IC50 = 87.32 ± 1.99 μg/mL). This research highlights the potential of GC as a promising candidate for therapeutic application due to its anti-inflammatory and α-glucosidase inhibition properties.

Chemical Profile and Bioactivity of Rubus idaeus L. Fruits Grown in Conventional and Aeroponic Systems.

Raspberry (Rubus idaeus L.) is a fruit of great interest due to its aroma, nutritional properties, and the presence of many bioactive compounds. However, differences among cultivation systems can affect its composition and, consequently, its potential bioactivity. Herein, for the first time, raspberries grown in an aeroponic system were investigated for their chemical profile and antioxidant and anti-inflammatory activity, as well as their enzyme (α-glucosidase and pancreatic lipase) inhibitory properties in comparison to wild and conventionally cultivated fruits. High-performance liquid chromatography coupled with diode array detection (HPLC-DAD) analyses revealed the presence of gallic acid, caffeic acid, chlorogenic acid, p-coumaric acid, ferulic acid, rutin, and catechin in all the samples. The extracts exhibited in vitro anti-inflammatory activity (inhibition of nitric oxide production) regardless of the cultivation method. Of particular interest is the ability of raspberries to inhibit pancreatic lipase. With the exception of the β-carotene bleaching test, the raspberries grown in conventional and aeroponic systems were more active in terms of antioxidants than wild fruits, as evidenced by the ABTS (IC50 in the range 1.6-3.4 μg/mL), DPPH (IC50 in the range 8.9-28.3 μg/mL), and FRAP tests (24.6-44.9 μM Fe(II)/g). The raspberries from aeroponic cultivation were generally able to exert the same bioactivity as those obtained from both conventionally cultivated and wild fruits, supporting the consideration that in the future, this technology could reshape agriculture by mitigating resource constraints, fostering sustainable practices and increasing yields.

Understanding Antidiabetic Potential of Oligosaccharides from Red Alga Dulse Devaleraea inkyuleei Xylan by Investigating α-Amylase and α-Glucosidase Inhibition.

In this study, the α-glucosidase (maltase-glucoamylase: MGAM) and α-amylase inhibitory properties elicited by xylooligosaccharides (XOSs) prepared from dulse xylan were analysed as a potential mechanism to control postprandial hyperglycaemia for type-2 diabetes prevention and treatment. Xylan was purified from red alga dulse powder and used for enzymatic hydrolysis using Sucrase X to produce XOSs. Fractionation of XOSs produced xylobiose (X2), β-(1→3)-xylosyl xylobiose (DX3), xylotriose (X3), β-(1→3)-xylosyl-xylotriose (DX4), and a dulse XOS mixture with n ≥ 4 xylose units (DXM). The different fractions exhibited moderate MGAM (IC50 = 11.41-23.44 mg/mL) and α-amylase (IC50 = 18.07-53.04 mg/mL) inhibitory activity, which was lower than that of acarbose. Kinetics studies revealed that XOSs bound to the active site of carbohydrate digestive enzymes, limiting access to the substrate by competitive inhibition. A molecular docking analysis of XOSs with MGAM and α-amylase clearly showed moderate strength of interactions, both hydrogen bonds and non-bonded contacts, at the active site of the enzymes. Overall, XOSs from dulse could prevent postprandial hyperglycaemia as functional food by a usual and continuous consumption.

Synthesis,Antidiabetic and Antitubercular Evaluation of Quinoline-pyrazolopyrimidine hybrids and Quinoline-4-Arylamines.

Two libraries of quinoline-based hybrids 1-(7-chloroquinolin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine and 7-chloro-N-phenylquinolin-4-amine were synthesized and evaluated for their α-glucosidase inhibitory and antioxidant properties. Compounds with 4-methylpiperidine and para-trifluoromethoxy groups, respectively, showed the most promising α-glucosidase inhibition activity with IC50 =46.70 and 40.84 μM, compared to the reference inhibitor, acarbose (IC50 =51.73 μM). Structure-activity relationship analysis suggested that the cyclic secondary amine pendants and para-phenyl substituents account for the variable enzyme inhibition. Antioxidant profiling further revealed that compounds with an N-methylpiperazine and N-ethylpiperazine ring, respectively, have good DPPH scavenging abilities with IC50 =0.18, 0.58 and 0.93 mM, as compared to ascorbic acid (IC50 =0.05 mM), while the best DPPH scavenger is NO2 -substituted compound (IC50 =0.08 mM). Also, compound with N-(2-hydroxyethyl)piperazine moiety emerged as the best NO radical scavenger with IC50 =0.28 mM. Molecular docking studies showed that the present compounds are orthosteric inhibitors with their quinoline, pyrimidine, and 4-amino units as crucial pharmacophores furnishing α-glucosidase binding at the catalytic site. Taken together, these compounds exhibit dual potentials; i. e., potent α-glucosidase inhibitors and excellent free radical scavengers. Hence, they may serve as structural templates in the search for agents to manage Type 2 diabetes mellitus. Finally, in preliminary assays investigating the anti-tubercular potential of these compounds, two pyrazolopyrimidine series compounds and a 7-chloro-N-phenylquinolin-4-amine hybrid showed sub-10 μM whole-cell activities against Mycobacterium tuberculosis.

Comparative Study on the Impact of Different Extraction Technologies on Structural Characteristics, Physicochemical Properties, and Biological Activities of Polysaccharides from Seedless Chestnut Rose (Rosa sterilis) Fruit.

Seedless chestnut rose (Rosa sterilis S. D. Shi, RS) is a fresh type of R. roxburghii Tratt with copious functional components in its fruit. Polysaccharides are recognized as one of the vital bioactive compounds in RS fruits, but their antioxidant and hypoglycemic properties have not been extensively explored. Hence, in this study, accelerated solvent extraction (RSP-W), citric acid (RSP-C), 5% sodium hydroxide/0.05% sodium borohydride (RSP-A), and 0.9% sodium chloride (RSP-S) solution extraction were individually utilized to obtain RS fruit polysaccharides. The physicochemical properties, structural characteristics, and biological activities were then compared. Results indicated that extraction methods had significant influences on the extraction yield, uronic acid content, monosaccharide composition, molecular weight, particle size, thermal stability, triple-helical structure, and surface morphology of RSPs apart from the major linkage bands and crystalline characteristics. The bioactivity tests showed that the RSP-S, which had the greatest amount of uronic acid and a comparatively lower molecular weight, exhibited more potent antioxidant and α-glucosidase inhibitory property. Furthermore, all RSPs inhibited α-glucosidase through a mixed-type manner and quenched their fluorescence predominantly via a static quenching mechanism, with RSP-S showing the highest binding efficiency. Our findings provide a theoretical basis for utilizing RSPs as functional ingredients in food industries.

Quercetin analogs as α-glucosidase inhibitors with antidiabetic activity

This study investigated the inhibitory effects of synthesized quercetin analogs (Q1–Q23) on α-glucosidase, particularly Q7. Q7, a synthetic analog of quercetin, exhibits superior α-glucosidase inhibitory properties compared with quercetin and the standard drug acarbose. This effect is attributed to the unique –CF3 group on the benzene ring of Q7, which enhances its inhibitory effect. As a non-competitive inhibitor, Q7 shows strong binding and stability within the α-glucosidase-Q7 complex. In vivo experiments showed that Q7 significantly reduced fasting blood sugar levels in diabetic mice, surpassing the effects of metformin. In addition, it affects the gut microbiota, particularly the microbes associated with anti-inflammatory responses and short-chain fatty acid production, which are crucial for the treatment of type 2 diabetes. However, the current Q7 dosage led to carbohydrate accumulation in the colon of mice, impairing the function of the intestinal microbiota. This study highlights the potential of Q7 for treating type 2 diabetes and emphasizes the need to determine the optimal dosages that balance therapeutic effects and gut health.

Synthesis, Spectroscopy and Biological Activities of Some Trivalent Lanthanide Complexes of Octadecyl N-salicylaldimine (ONsal)

A series of Ln(III) complexes of octadecyl N-salicylaldimine (ONsal) were synthesized and characterized by CHN analysis, magnetic moment, conductivity, thermoanalytical and spectroscopic methods. Elemental and thermal analysis data confirmed the formation of heptacoordinated [Ln(ONsal)2Cl2(H2O)]Cl complexes where Ln = Ce3+, Nd3+, Sm3+, Eu3+, Gd3+, Tb3+, Dy3+, Ho3+, which is further supported by the respective mass spectra. The ligand acts as a neutral bidentate species coordinating through azomethine nitrogen and phenolic O-atom. The linkage of one H2O molecule in all the complexes has been inferred from the thermal analysis. All the Ln(III) complexes are paramagnetic in nature and act as 2:1 electrolyte in 0.002 M DMF at 25 ºC. The complexes of Sm(III), Eu(III) and Tb(III) display luminescent properties. The powder XRD patterns of Nd(III) and Dy(III) complexes could be successfully indexed for monoclinic crystal systems, while the diffraction lines of Eu(III) complex are indexed for a triclinic crystal system. Methanolic solutions of the ligand and complexes were checked for α-glucosidase and α-amylase inhibitory properties where some of the Ln(III) complexes show significant α-glucosidase inhibitory potency while only Tb(III) complex shows inhibition against α-amylase.

Phenolic Compounds, Free Radical Scavenging Activity and α-Glucosidase Inhibition Properties of Green, Oolong and Black Sacha Inchi Tea Extract

Sacha Inchi leaves may possess antioxidant function which is naturally rich in bioactive ingredients and has been widely processed into herbal teas that has many benefits to human health. According to the global data from the World Health Organization (WHO), there has been a rise in the frequency of diabetes mellitus (DM) among adults. Sacha Inchi tea was prepared using several methods, with green tea not fermented, oolong partially fermented, and black tea completely fermented. The phenolic compounds (total phenolic content (TPC), total flavonoid content (TFC), tannin), free radical scavenging activity (DPPH) and inhibition properties of α-Glucosidase on green, oolong and black Sacha Inchi tea extract were determined. The green Sacha Inchi tea extract displayed the highest TPC and TFC values among the oolong and black Sacha Inchi tea extracts at a concentration of 500µg/mL, with values of 2.10±0.01 µg GAE/mL and 3.23±0.20 µg QE/mL, respectively. Meanwhile, at a concentration of 500µg/mL, Sacha Inchi black tea extract demonstrated strong antioxidant activity by DPPH with radical scavenging activity (%) (89.4±0.45). Furthermore, at a concentration of 15.625 µg/mL, black, oolong, and green tea extracts exhibited stronger inhibitory effects on α-Glucosidase (95%, 95%, 92%, respectively) than acarbose (90%). Therefore, the processing steps involved in tea production impact the phenolic compounds, free radical scavenging activity, and the ability to inhibit α-Glucosidase in green, oolong, and black tea extracts.

Comparative Assessment of Nutritional Metabolites in Yellow Soybeans at Different Growth Years and Their Antioxidant and α-Glucosidase Inhibition Properties

With regard to obtaining valuable information on the development of new breeding lines and functional agents, the present study was the first to demonstrate variations in nutritional metabolites and biological properties in yellow soybeans at three growth years. Three metabolites (fatty acid, amino acid, isoflavone) exhibited significant differences between cultivars and growth years; specifically, linoleic acid, glutamic acid, and malonylgenistin displayed the highest average contents at 38.7 mg/g, 59.9 mg/100 g, and 992.6 μg/g, exhibiting predominant changes in the range of 21.6–61.2 mg/g, 34.3–113.3 mg/100 g, and 455.8–1778.9 μg/g, respectively. Moreover, the biofunctional effects differed remarkably in the order ABTS > α-glucosidase > DPPH at 500 μg/mL (50% methanol extracts). The TPC, TFC, DNA protection, and FRAP ratios also showed remarkable changes in cultivars across growth times. Interestingly, the Daepung cultivar may be considered an alternative source for the development of new soybeans and nutraceutical foods due to its high metabolites (average contents, fatty acid: 80.8 mg/g; amino acid: 353.8 mg/100 g; isoflavone: 4048.2 μg/g) and excellent beneficial activities (75.1% ABTS, 52.5% DPPH, 100% DNA protection, 73.1% α-glucosidase, 1.54 OD593 nm FRAP at 500 μg/mL). Our observations may contribute to providing valuable information on the relationship between metabolites and the biological properties of yellow soybeans.

Ferruginoside D: A Novel Phenylethanoid from Verbascum leiocarpum.

A novel phenylethanoid, ferruginoside D, together with fourteen known compounds were isolated from the Verbascum leiocarpum for the first time. Chemical structures of isolated compounds were determined by spectroscopic analysis including HR-ESI-MS and NMR spectra. The antioxidant, α-glucosidase inhibitory properties, and antiproliferative activities against multiple cell lines (A172, C6, HeLa, A2780, SW620, HT29, Beas2B, RPE, and HSF) of the isolated compounds were evaluated in vitro. According to the results, iridoids, flavonoids (luteolin and apigenin), and phenylethanoids (poliumoside and isoverbascoside) with strong antiproliferative potential were also found to have cytostatic effects. Furthermore, the investigation revealed that compounds luteolin, poliumoside, verbascoside, isoverbascoside, ferruginoside C, ferruginoside D, and ursolic acid show potent alpha-glucosidase inhibitory activity, while compounds luteolin, verbascoside, and isoverbascoside exhibit substantial antioxidant activity. The new compound (ferruginoside D) was found moderately active against cancer cell lines, with strong alpha-glucosidase inhibitory activity, and moderate antioxidant properties.

The ethanol extract of Muntingia calabura exhibits in vitro antidiabetic potentials by inhibiting carbohydrate digestive enzymes

Objective: The present research study was conducted to investigate in vitro anti-diabetic potentials of ethanol extract of leaves of Muntingia calabura for α-glucosidase and α-amylase inhibitory activities.
 Materials & Methods: The leaves of Muntingia calabura were collected and authenticated. dried and powdered. The powdered drug was defatted using petroleum ether and extracted with ethanol. The ethanol extract of Muntingia calabura was subjected to preliminary phytochemical investigation. The in vitro α-glucosidase inhibitory and α-amylase inhibitory properties were determined for the ethanol extract and concentrations of extract required to inhibit absorbance (IC50 values) EEMC were determined.
 Results: Significant IC50 values were found in both tests that assessed the inhibitory activity of α-glucosidase and α-amylase, demonstrating the capacity of the ethanol extract of Muntingia calabura to block carbohydrate digesting enzymes and prevent postprandial blood glucose.
 Conclusion: The results of the presents investigation recommends that ethanol extract of Muntingia calabura possess significant α-glucosidase and α-amylase inhibitory activity.
 Keywords: Antidiabetic activity, Muntingia calabura, α-glucosidase and α-amylase and IC50values.

α-Glucosidase inhibition properties of novel azaphthalocyanines containing vanillin

α-Glucosidase inhibition properties of novel azaphthalocyanines containing vanillin