Search

This study investigates the multifunctional potential of horse oil fermented with barley nuruk, a traditional fermentation starter, focusing on its α-glucosidase inhibitory activity and bioactive applicability. Gas chromatography–tandem mass spectrometry (GC-MS/MS) revealed significant changes in fatty acid composition during fermentation, with oleic acid amide and palmitic acid amide remaining stable and stearic acid amide forming prominently by day 10. Molecular docking demonstrated that the amide structures play a key role in α-glucosidase inhibition through essential hydrogen bonding interactions. Next-generation sequencing (NGS) analysis showed a notable reduction in pathogenic bacteria, such as Salmonella enterica, and a dominance of Lactobacillus acidophilus (95.2%) by day 10. The α-glucosidase inhibitory activity increased progressively with fermentation, with the day 10 extract surpassing the synthetic inhibitor acarbose, highlighting its potential for diabetes management. A human skin primary irritation test confirmed the hypoallergenic nature of both hexane-extracted and fermented horse oil products, ensuring their safety for topical applications. In conclusion, fermented horse oil demonstrates significant α-glucosidase inhibitory activity and proven safety, positioning it as a promising natural resource for therapeutic and functional product development. Further studies are needed for clinical validation and commercialization in diabetes management and related applications. [ABSTRACT FROM AUTHOR]

Two rarely occurring diphenylheptanoid-phenylheptanoid hybrid dimers (1 and 2) and one new oxygenated fatty acid (3), as well as two known fatty acid analogues (4 and 5), were isolated from the 70% EtOH extract of the pollen of Typha angustifolia. Their planar structures were established by interpretation of MS and NMR spectroscopic data, and the absolute configurations of 1 and 2 were determined by Mosher's method and quantum chemical TD-DFT calculations of ECD spectra. An in vitro anti-diabetic evaluation of these isolates revealed that compounds 1 and 2 exhibited promising inhibitory activity against α-glucosidase with IC50 values of 11.85 ± 0.69 and 17.06 ± 3.08 μM, respectively. It is the first report on both diphenylheptanoid constituents and α-glucosidase inhibitors from the title plant, which represents a significant phytochemical progress of this herbal species and may serve as a reference for its future medicinal applications. [ABSTRACT FROM AUTHOR]

Diabetes is a prevalent and serious metabolic disorder affecting millions globally, and it poses extensive health risks due to elevated blood glucose levels. One promising approach for managing diabetes is the inhibition of α-glucosidase, an enzyme that plays a crucial role in carbohydrate metabolism. Targeting α-glucosidase can help delay glucose absorption, thus controlling postprandial blood sugar spikes. Dihydropyrimidones, a core structural class present in various biologically active natural compounds, have been recognized for their diverse therapeutic potential, including anti-diabetic properties. In this study, we evaluated a library of previously synthesized 37 Dihydropyrimidone derivatives to assess their potential as α-glucosidase inhibitors. We identified 34 derivatives with significant inhibitory activity, exhibiting IC50 values in the range of 5.30–56.72 µM. Among these, compounds 2, 4–7, 9–11, 13–16, 31, 32, and 33 demonstrated high potency, with IC50 values below 20 µM; the most active compound, 5, achieved an IC50 of 5.30 µM. A detailed kinetic study on compound 5 revealed a competitive inhibition mode with a Ki value of 16.10 ± 0.0075 µM. Additionally, cytotoxicity assays confirmed that compound 5 is non-toxic to BJ cell lines, underscoring its safety for therapeutic use. The computational studies further supported the inhibitory potential by illustrating key interactions and binding affinities between the Dihydropyrimidone derivatives and the α-glucosidase, highlighting these compounds as promising candidates for diabetes management. [ABSTRACT FROM AUTHOR]

Purpose: To determine the phytochemical compounds, in leaves, branches and roots of two mulberry cultivars, Monnoi and Buriram 60 (Br.60). Methods: Both cultivars were grown under organic conditions. Extraction of plant parts was done using either distilled water (autoclave), 50 % ethanol or 95 % ethanol and the proximate chemical analysis including 1-Deoxynojirimycin (DNJ) content, total flavonoid (TFC) and total phenolic contents (TPC), antioxidant and α-glucosidase inhibitory properties of the plant extracts were analyzed. Results: The proximate analysis showed that both cultivars had high protein content in leaves (21 – 25 %) compared to branches and roots. The carbohydrate content was high in all parts of both cultivars (32 – 50 %) and the DNJ content of all parts using 50 % ethanol extraction was higher compared to the other two methods, ranging from 10 – 17 mg/g Ext. Total phenolic content (TPC) in Monnoi branches extracted with distilled water (autoclave) was 13.45 ± 0.26 mg GE/g Ext while Br.60 roots with distilled water extraction (autoclave) showed the highest total flavonoid content (TFC) at 1.55 ± 0.02 mg QE/g Ext. Antioxidant activities of the extract on FRAP, DPPH radical and ABTS were high for both cultivars but the IC50 value was higher and significantly different (p < 0.05) compared to two standards used as controls (Trolox and Ascorbic acid). The α-glucosidase assay showed that the leaves and branches of Monnoi had IC50 values of 2.21 ± 0.09 and 2.45 ± 0.1, respectively, with the potential to reduce enzymatic activity but less than the standard substance Acarbose with an IC50 of 0.31 ± 0.01. Conclusion: Two mulberry cultivars, Monnoi and Br.60, show high potential for diabetes treatment owing to their bioactive compounds. Extraction with 50 % ethanol gives the highest yield. Further isolation and characterization and possible mechanism of action of phytoactive constituents such as 1- deoxynojirimycin (DNJ) would be necessary. [ABSTRACT FROM AUTHOR]

Black elderberry (Sambucus nigra L.) flowers are rich in polyphenolic compounds, including chlorogenic acid and quercetin derivatives, which are known for their health benefits, particularly their antioxidant and antidiabetic properties. This study aimed to optimize the extraction conditions using the Box–Behnken model to maximize polyphenol yields from different elderberry flower cultivars and to evaluate their potential for antidiabetic action. The extracts were analyzed for their phytochemical content and assessed for enzyme inhibition, specifically targeting enzymes critical in carbohydrate digestion and glucose regulation. The anti-inflammatory activity was also assessed. Results indicated that the Black Beauty, Obelisk, and Haschberg cultivars demonstrated significant inhibition of α-glucosidase, with a high inhibitory potential against α-amylase enzymes for the Obelisk cultivar. Additionally, high chlorogenic acid content was strongly correlated with enzyme inhibition and antioxidant activity, suggesting its substantial role in glucose regulation. This study underscores the potential of elderberry flower extracts, particularly those rich in chlorogenic acid, as natural agents for managing blood glucose levels, warranting further exploration of their use in antidiabetic applications. [ABSTRACT FROM AUTHOR]

BACKGROUND: In recent years, the demand for high‐quality natural extracts to be included in nutraceutical formulations has increased sharply. Hazelnut (Corylus avellana L.) shells (HZS) are underrated agricultural by‐products that could be exploited as a source of active ingredients with pro‐healthy properties. In the present study, a fully green microwave‐assisted extraction (MAE) method was established for the first time aiming to recover bioactive constituents from HZS with significant nutraceutical value. Key MAE parameters, including ethanol in water concentration, microwave power, irradiation time and solvent‐to‐powder ratio, were optimized through response surface methodology utilizing a Box–Behnken design to achieve the highest total phenolic content and antioxidant/antiradical activities in the final extract. RESULTS: The optimal MAE conditions (28% v/v ethanol/water, 270 s, 670 W, and 37 mL g−1) yielded an extract with significant scavenging capacity against reactive oxygen species and remarkable inhibitory activity towards both α‐amylase (IC50 = 7.73 μg mL−1) and α‐glucosidase (IC50 = 49.44 μg mL−1), demonstrating stronger hypoglycaemic properties than the anti‐diabetic drug acarbose. Additionally, fluorescence spectroscopy results highlighted the ability of the optimized extract from HZS (OHS‐E) to counteract advanced glycation end‐product formation throughout the glycation cascade in a dose‐dependent manner. Liquid chromatography/electrospray ionization‐tandem mass spectrometry profiling unveiled the presence of fatty acids and phenolic compounds, including lignans, flavonoids, gallic acid derivatives and diarylheptanoids. Lastly, the biocompatibility of OHS‐E was attested on HT29‐MTX and Caco‐2 intestinal cells. CONCLUSION: Altogether, these findings encourage the potential application of OHS‐E as an effective nutraceutical component against type 2 diabetes mellitus and oxidative stress. © 2024 The Author(s). Journal of the Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Guarumo leaves (Cecropia sp.) have been traditionally used in Latin America to manage diabetes mellitus. This work aimed to evaluate the potential α -glucosidase inhibitory activity of leaf extracts from six Cecropia species collected in Panama. Additionally, the chemical compounds associated with this activity were characterized. We identified the most likely bioactive candidates by using UPLC-MS untargeted metabolomics. Among the evaluated Cecropia species, C. obtusifolia, C. hispidissima, C. longipes, and C. peltata (CA) showed significant α -glucosidase inhibitory activity with IC 50 values ranging from 9.0 to 29.8 μg/mL, as compared to acarbose (5069.72 μg/mL), used as a positive control. In contrast, C. insignis , C. heterochroma , and C. peltata (SC) did not show a significant effect in this assay. The OPLS-DA model exhibited strong predictive performance, clearly distinguishing between active and inactive extracts. Through this analysis, we identified three putative bioactive compounds, namely Procyanidin B, ourateacatechin, and kaji-ichigoside F1, that were found in higher concentrations in the active extracts and demonstrated strong α -glucosidase inhibition. Additionally, the metabolites identified showed VIP scores > 1.5, indicating their significant contribution to the observed activity. This research identifies four Cecropia species as promising natural sources of α -glucosidase inhibitors, which could lead to new treatments for type 2 diabetes by helping to manage blood sugar levels. [Display omitted] • Four Cecropia species were identified with significant α -glucosidase inhibitory activity. • A untargeted metabolomics helped to identify key metabolites via OPLS-DA. • Procyanidin B, ourateacatechin, kaji-ichigoside F1 are predicted to be the most active compouds. [ABSTRACT FROM AUTHOR]

Copyright of Modern Food Science & Technology is the property of Editorial Office of Modern Food Science & Technology and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The by-product of extracting oil from sesame has good functional properties for use in the development of new food products. In this study, the effect of simulated gastrointestinal digestion on the bioaccessibility of phenolic compounds, as well as the antioxidant, antidiabetic, and hypoglycemic properties of a beverage from sesame by-products was analyzed. Oral digestion significantly decreased the total phenolic content of the beverage, while the total flavonoid content increased. Both phytochemicals increased after gastric and intestinal digestion. Twenty-five phenolic compounds were characterized in the sesame by-product beverage, including feruloylquinic acid, which was present in all the digestive fractions analyzed. The most abundant free phenolic was quercetin, which was also present in all the digested fractions. On the other hand, the most abundant phenolic in the digested fractions was isorhamnetin. During gastrointestinal digestion, the antioxidant activity and inhibitory effects on the α-glucosidase and DPP-IV of the beverage significantly improved, while the ability to inhibit the α-amylase significantly increased during oral digestion, remaining constant throughout digestion. Correlation analysis indicated that flavonoids, including quercetin, may be the compounds with the greatest effect on the evaluated activities. The results of this study not only improve the understanding of the impact of gastrointestinal digestion on the bioaccessibility of phenolic compounds but also suggest potential applications in formulating functional foods with enhanced antioxidant, hypoglycemic, and antidiabetic properties, contributing to the development of health-promoting food products. [ABSTRACT FROM AUTHOR]

Chili (Capsicum annuum) consumption is often suggested, and using functional food cultivars is the most effective strategy post COVID-19 pandemic. Controlling chili breeding activity is one of the most effective methods to produce new hybrid varieties. However, the general combining ability (GCA), specific combining ability (SCA), and heterotic effect of functional biochemicals (polyphenol content, antioxidant activities, and α-glucosidase inhibitory compounds) remain poorly known in C. annuum. This study aimed to estimate these parameters in C. annuum by using five different genotypes and their hybrid combinations based on growth characteristics, yield, yield components, and fruit functional biochemicals. The F1 and F1R progenies were obtained from crosses in a greenhouse with a full diallel mating design. Each parent used in this study had a GCA advantage for each characteristic. The hybrid combination of IPB074 × IPB005 and IPB435 × IPB367 displayed the best yield results. However, the results indicated the opposite regarding α-glucosidase inhibitory compounds. The heterotic effect of functional biochemicals was observed for traits related to genotypes, polyphenol content, antioxidant activity, α-glucosidase inhibitory compounds, and similar properties related to yield and yield components, indicating their use in hybrid chili production.

One new prenyl flavanone (1), (2S)-8-prenyl-5,6-dihydroxy-7-methoxyflavanone, and one new diarylbutanol (2), (7′S)-3′-hydroxy-linderagatin-A, were isolated from the stem bark of Uvaria siamensis (Annonaceae), along with five known compounds, eriodictyol (3), quercetin (4), paprazine (5), N-trans-caffeoyltyramine (6), and N-trans-feruloyltyramine (7). Their structures were determined through extensive spectroscopic analyses and comparison with the literature. The α-glucosidase inhibitory potential of 1-7 was evaluated. Compound 6 showed the highest inhibitory activity against α-glucosidase and exhibited superior potency compared to the positive control, with an IC50 value of 0.12 μM. [ABSTRACT FROM AUTHOR]

• Strychnos henningsii extracts showed high antioxidant and low cytotoxicity. • Methanolic extract inhibited α-glucosidase; alkaloid extract inhibited α-amylase. • Alkaloids were the highest phytochemical content, followed by flavonoids, phenols, and terpenes. • Five bioactive triterpenes showed low to moderate cytotoxicity and enzyme inhibition. The pervasiveness of diabetes mellitus, particularly type II diabetes, is escalating in South Africa, where complications from this condition rank as the second leading cause of natural mortality. Locally, the bark of Strychnos henningsii Gilg. has been traditionally employed to manage type II diabetes, a chronic ailment necessitating continuous attention. This study aims to assess the cytotoxic, antioxidant, and antidiabetic enzyme inhibitory potentials of S. henningsii , based on its perceived antidiabetic properties. The investigation involved HPTLC, UV–vis spectrophotometry, and LC-MS analyses to ascertain the phytochemical composition. In vitro MTT cytotoxicity, DPPH radical scavenging, ORAC, α-glucosidase and α-amylase inhibition were evaluated on the methanolic (MSHB) and total tertiary alkaloid crude extracts (TTA SHB) of S. henningsii. Furthermore, five bioactive pentacyclic triterpenes isolated from S. henningsii were evaluated for their cytotoxicity and antidiabetic enzymatic potential. The phytochemical examination showed a notable occurrence of alkaloids, then came flavonoids, phenols, and terpenes. MSHB and TTA SHB extracts exhibited minimal MTT cytotoxicity, with the lowest percentage inhibition recorded at 79.83 ± 7.66 % for MSHB at 500 µg/mL. Strong antioxidant activity was evident in both extracts, with IC 50 values less than those of ascorbic acid in DPPH radical scavenging assays. α-Glucosidase inhibition was demonstrated in the MSHB extract, while α-amylase inhibition was observed in the TTA SHB extract. The isolated pentacyclic triterpenes displayed low to moderate cytotoxicity, with IC 50 values ranging between 60.69 and 300.5 µg/mL. Moreover, all isolated triterpenes exhibited α-amylase and α-glucosidase inhibition, with alpha-amyrin acetate (SH-4) demonstrating notably higher α-glucosidase inhibition compared to the positive control, reaching 93.34 ± 0.52 % at 500 µM. The findings suggest that S. henningsii and its bioactive pentacyclic triterpenes possess promising attributes, including low cytotoxicity, potent antioxidant properties, and enzymatic inhibition, thereby potentially serving as valuable candidates for developing novel therapeutic interventions targeting type II diabetes. [ABSTRACT FROM AUTHOR]

Summary: Alpinia mutica Roxb. possesses diverse phytochemicals with potential as treatment modalities in managing diabetes and obesity. Employing a nuclear magnetic resonance (NMR)‐based metabolomics, we conducted discriminative analysis to investigate the metabolite profiles across different extraction solvents (ethanol:water −100:0, 80:20, 60:40, 40:60, 20:80 and 0:100) and correlated these profiles with bioactivities. Metabolites were identified using NMR supplemented with liquid chromatography tandem mass spectrometry (LC–MS/MS) analysis. The 40:60 extract showed high phenolic content, strong ferric ion reduction capability and low IC50 value in scavenging free radicals, pancreatic lipase and α‐glucosidase inhibitory assays. Partial Least Square (PLS) biplot indicated that isorhamnetin, catechin, zerumin B, curcumanggoside, curcuzederone, demethoxycurcumin, ascorbic acid, apigenin, and phenylalanine in the 40:60 extract exhibited good correlations with the measured bioactivities. Additionally, LC–MS/MS tentatively identified proanthocyanidins and multiple flavonoid glucuronides in this extract. This study provides preliminary insight into its chemistry and highlight the potential of A. mutica extract as natural antioxidant and antiobesity agent. [ABSTRACT FROM AUTHOR]

Copyright of Current Research in Health Sciences is the property of Ataturk University Coordinatorship of Scientific Journals and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Natural drugs derived from plants are becoming more popular because of their apparent biological efficacy, affordability, and safety. A byproduct of cocoa farms, cocoa pod husk (CPH), is often disregarded yet contains an abundance of phenolic chemicals that have antimicrobial and antioxidant features, which has led to intensive investigation into possible biomedical applications. In order to identify crucial functional groups and phytochemical components, we carefully examined the 80% ethanol and dichloromethane extracts of CPH using gas chromatography–mass spectrometry (GC-MS) and HPLC. The antibacterial and antioxidant properties of such extracts and their impact on cytotoxicity and α-glucosidase were explored. According to our results, the 80% ethanol and dichloromethane extracts contained 19 and 12 phytochemical components, respectively. Interestingly, at 250 µg/mL, all CPH extracts showed strong antibacterial properties that totally prevented the bacterial growth. At 66.6% and 82.7%, respectively, the ethanol and dichloromethane extracts showed impressive antioxidant and DPPH scavenging capabilities where the ethanol extract showed a substantially lower IC50 value of 35.26 µg/mL than the dichloromethane extract, which had an IC50 value of 23.88 µg/mL. Furthermore, the α-glucosidase inhibitory effect of the dichloromethane extract was found to be better, as shown by its IC50 value of 126.5 µg/mL, which was lower than that of the ethanol extract at 151.3 µg/mL. The extracts' compatibility was verified by cytotoxicity tests, which revealed no appreciable alterations in the cell lines. Additionally, novel in silico molecular docking experiments were performed on 25 discovered compounds, providing insight into their possible bioactivity. Broad-spectrum activities of extracts were confirmed by molecular docking investigations aimed at interacting with α-glucosidase proteins. Our thorough analysis makes CPH extracts seem like the excellent candidates for biomedical uses. These results provide new insights into the therapeutic potential of CPH extracts and pave the way for the development of innovative medications and natural remedies. [ABSTRACT FROM AUTHOR]

In connection with our interest in the phytochemical investigation of Elaeocarpus hainanensis Oliv. (Elaeocarpaceae) growing in Vietnam, two new sulphated oleanane triterpenes were obtained herein and structurally identified. Based on the combination of the extensive 1D-, 2D NMR and HR ESI MS spectroscopic data analysis, their chemical structures have been elucidated as 1α,3β-dihydroxy-olean-18-ene 1-sulphate (1) and 1α,3β-dihydroxy-olean-12-ene 1-sulphate (2). Notably, compounds 1 and 2 are corroborating the proposition that triterpenoid sulphates serve as chemosystematic markers of the Elaeocarpus genus. Additionally, all these two new compounds 1 and 2 strongly inhibited α-glucosidase in vitro with the respective IC50 values of 3.81 ± 0.33 µM and 21.27 ± 0.48 µM, which were significantly better than that obtained from positive control, acarbose (IC50 247.73 ± 11.85 µM). [ABSTRACT FROM AUTHOR]

This study evaluated the antioxidant and anti-glycemic properties of black lemon Chenpi (BLC) (Citrus limon (L.) Burm. f. cv. Eureka), processed using three thermal browning models—hot-air drying (HAL), high temperature and humidity, and steam-drying cycle (SCL)—and compared them to fresh lemon peel and commercial Chenpi. The moisture-assisted aging technology (MAAT) is an environmentally friendly process for inducing browning reactions in the lemon peel, enhancing its functional properties. Our results demonstrated significant increases in sucrose, total flavonoid content, and antioxidant capacities (2,2-diphenylpicrylhydrazyl: 12.86 Trolox/g dry weight; ferric reducing antioxidant power: 14.92 mg Trolox/g dry weight) with the MAAT-HAL model. The MAAT-SCL model significantly improved the browning degree, fructose, total polyphenol content, narirutin, and 5-hydroxymethylfurfural synthesis (p < 0.05). Additionally, aged lemon peel exhibited potential α-glucosidase inhibitory activity (28.28%), suggesting its role in blood sugar regulation after meals. The multivariate analysis (principal component and heatmap analyses) indicated that BLC processed using the MAAT-SCL model exhibited similarities to commercial Chenpi, indicating its potential for functional food development. Our results indicate that MAAT-SCL can enhance the economic value of lemon by-products, offering a sustainable and functional alternative to traditional Chenpi. [ABSTRACT FROM AUTHOR]

Phytochemical investigation of the stems of Bridelia stipularis led to the isolation of a new triterpene, 3β-O-trans-feruloylfriedelinol (1), together with five known compounds, friedelin (2), 3β-friedelinol (3), lupeol (4), stigmasterol (5), and 4-(1,5-dimethyl-3-oxo-4-hexenyl)benzoic acid (6). Their structures were identified by intensive spectroscopic analysis including 1D and 2D nuclear magnetic resonance, infrared, and mass spectrometry. Compound 1 showed significant α-glucosidase inhibitory activity (IC50 = 337.49 ± 0.59 µM) close to the standard, acarbose. Furthermore, the structure activity relationship of 1 was analyzed by molecular docking studies. In addition, the molecular docking results showed that the interaction between 1 and the active site occurred through hydrophobic forces and hydrogen bonds. [ABSTRACT FROM AUTHOR]

A new lanostane-type triterpene, uvariaol (1), was isolated from the branches of Thai Uvaria siamensis, along with three known compounds, polycarpol (2), fisetinidol (3), and stigmast-4-en-3-one (4). Their structures were elucidated through extensive spectroscopic analyses and comparison with existing literature. The α-glucosidase inhibitory potential of compounds 1–4 was evaluated. Compound 1 exhibited significant inhibitory activity against α-glucosidase, surpassing the potency of the positive control, with an IC50 value of 30.8 ± 1.5 μM. [ABSTRACT FROM AUTHOR]

Cassia mimosoides L. (CM), a member of the family Leguminosae, represents an underexplored component within the Katakakhadiradi Kashayam, an Ayurvedic preparation primarily utilized for the management and treatment of diabetes mellitus. For the first time, the potential of CM to address diabetic complications was scientifically validated using in vitro methods. The significant alpha-glucosidase activity of ethanol-water extract (IC 50 of 1.02 ± 0.12 μg/mL) as against the standard acarbose (IC 50 19.28 ± 1.42 μg/mL) has prompted further column separation to identify the active components. Using bioassay-guided fractionation based on Dipeptidyl Peptidase-IV (DPP-IV) inhibitory activity, four compounds were isolated and identified through NMR and HRMS. All the four compounds, orientin, isoorientin, diosmetin and luteolin exhibited marked inhibition over the DPP-IV enzyme. Among them disometin showed significantly higher activity with an IC 50 of 2.80 ± 0.38 μM. At non-cytotoxic concentrations these compounds effectively stimulated 2-NBDG [2-(7-nitrobenz-2-oxa-1,3-diazol- 4-yl) amino-2-deoxy-d-glucose] uptake in L6 myotubes. Notably, this investigation represents the first report elucidating the glucose uptake-enhancing potential of the flavonoid isoorientin in L6 myoblast cell lines. Moreover, isoorientin also exhibited significant antiglycation activity in assay using bovine serum albumin and methylglyoxal. IC 50 values for isoorientin and positive control aminoguanidine were found to be 51.45 ± 0.03 µg/mL and 45.18 ± 0.03 µg/mL, respectively. In addition, virtual docking studies of the four compounds against α-glucosidase, α-amylase, and DPP-IV demonstrated strong affinity, thus providing further evidence to substantiate the observed activity. Consequently, this study revealed the hypoglycemic efficacy of the plant CM and proposed the exploration of its compounds in ameliorating type 2 diabetes mellitus. [Display omitted] • Cassia mimosoides L. (CM) exhibits promising multi-modal anti-diabetic efficacy. • The proanthocyanidin-rich fraction demonstrated superior inhibition of α-glucosidase and α-amylase. • Isoorientin exhibits enhanced glucose uptake potential for the first time in L6 cell lines. • All the compounds showed significant potential against DPP-IV. [ABSTRACT FROM AUTHOR]

The study focused on the characterization of an Ethiopian traditional beverage, borde, produced by lactic acid bacteria (LAB) and yeast through natural fermentation. Samples were collected from three distinct locations in Ethiopia and subjected to analyses encompassing microbiological, antioxidant, enzyme inhibition, rheological and physicochemical aspects. The early stages of fermentation exhibited prevalence of Enterobacteriaceae and aerobic mesophilic bacteria. Towards the end of fermentation, yeast (6.07–6.72) and LAB (6.52–7.12) (log CFU mL−1) dominated the microbiological profile of all borde samples. Significant difference (P

Marine associated-bacteria is an excellent source for novel enzymes. The quest to find new agarases with unique properties for industrial application is continually growing. Agarase hydrolyzed agar to oligoagar for broader applications. Herein, we report the production of β-agarase from Alteromonas macleodii BC7.1, a marine sediment bacteria collected in Barra Cadi Island, South Sulawesi, Indonesia. The enzyme production was optimal using a medium containing 0.4 % of agar after 48 h incubation. The enzyme has an optimum activity at 45 °C, pH 7–8 and was stable for 12 h incubation. Agarase BC7.1 (Aga-BC7.1) was resistant to most ions (except Zn and Mn), denaturing agents and chemicals. The Km and Vmax values were 18 mg/mL and 100 U/mg, respectively. The molecular size of agarase in its native condition was 220 kDa. Based on α-glucosidase inhibition activity indicated that oligosaccharides can be produced within 8–24 hours using 0.3–0.5 % (w/v) substrate, at 30–37 °C, with 50 mM Tris-HCl buffer at pH 7.0 and various types of agar. The HPLC analyses of the hydrolysis products confirmed the presence of neoagarooligosaccharides (NAOS), neoagaro-biose (NA2), -tetraose (NA4), and -hexose (NA6). A mixture of oligosaccharides with a major content of NA2 exhibits the highest α-glucosidase inhibition activity compared to crude oligosaccharides and other fractions. This study thus highlights the potency of β-agarase from A. macleodii for industrial application.

A new spiroterpenoid, namely tinctorin (1), along with one known compound, norreticulatin (2), were isolated from the lichen Parmotrema tinctorum (Despr. ex Nyl.) Hale. Their structures were elucidated by extensive spectroscopic analyses and electronic circular dichroism (ECD) calculations. The absolute configuration of 2 was established for the first time. Compound 1 was evaluated for its inhibitory activity against α-glucosidase and found to be inactive. [ABSTRACT FROM AUTHOR]

Ultrasonication is a potential and highly efficient green technique to extract bioactive elements from plants. In this study, ultrasonication technology is used to extract reducing sugar and polyphenolic compounds from burdock root waste (Arctium lappa L.) using the response surface approach. For this, the ultrasonic extraction parameters, solid-to-water ratio (20–40 g/mL), sonication time (60–100 min), and sonication temperature (40–60 °C) were optimized through response surface methodology (RSM), where the reducing sugar and total phenolic content were selected as the responses. The results indicated that all the parameters considered had a significant impact (p<0.05) on reducing sugar (ranging from 4.38 to 6.12%) and total phenolic content (ranging between 4.94 and 6.98 mg GAE/g). The optimized condition was solid to liquid ratio of 38.52 g/mL, sonication time of 90.06 min, and sonication temperature of 59.86 °C, which predicted reducing sugar of 6.12% (6.48% after validation) and total phenolic content of 7.04 mg GAE/g dw (7.44 mg GAE/g dw after validation). Furthermore, in vitro biological activities of burdock root extracts exhibited excellency in retaining the reducing sugar (6.48–6.97%), total flavonoid content (40.66—42.36 mg RE/g), DPPH (33.70—43.45 μmol TE/g), and ABTS+ (28.10—29.83 μmol TE/g) radical scavenging activity, ferric-reducing antioxidant power (54.53—58.70 μmol TE/g), and α-glucosidase inhibitory activity (>20%) both in ultrasonic and conventionally extracted samples with ultrasonication showed the higher activity. The results suggest that ultrasonication is an effective green technology and that burdock root waste has significant antioxidant and antidiabetic potential and could be used as a promising source of functional components. [ABSTRACT FROM AUTHOR]

Viburnum luzonicum Rolfe is widely used in China as folk medicine. The bioactivity evaluation indicated that the n-BuOH fraction of V. luzonicum leaves (VLLB) could significantly inhibit α‑amylase and α-glucosidase. In order to clarify its active constituents, the phytochemical analysis on VLLB was first performed using HPLC-QTOF-MS/MS, and three new phenolic compounds, viburosides A–C (1–3), along with seven known analogues (4–10) were isolated through preparative HPLC. The undescribed compounds were determined by extensive spectroscopic analyses (1H and 13C NMR, HSQC, HMBC, HRESIMS, and ORD) and enzymatic hydrolysis. In the in vitro enzyme assays, compounds 1–8 showed potent α‑amylase and α-glucosidase inhibitory activities. The enzymatic kinetics and molecular docking of the strongest inhibitors 2 and 3 against the corresponding target enzyme were also performed. [ABSTRACT FROM AUTHOR]

This study aimed to evaluate and compare the inhibitory effects of extracts from Bombyx batryticatus (BBE) and Bombyx mori (BME) on α-glucosidase, DPP-4, and LDL oxidation activities, focusing on their potential applications in managing postprandial hyperglycemia and metabolic syndrome. The results demonstrated that both BBE and BME effectively inhibited α-glucosidase and LDL oxidation, with BBE exhibiting higher inhibitory activity than BME. HPLC analysis identified linolenic acid, linoleic acid, linolenic acid ethyl ester, pheophorbide a, and pyropheophorbide a as key compounds contributing to these effects. Notably, the identified unsaturated fatty acids and pheophorbides showed strong α-glucosidase inhibitory activity, surpassing that of acarbose, a standard diabetic drug. These results suggest that, in addition to the previously reported 1-DNJ and fibroin proteins, unsaturated fatty acids and chlorophyll-derived pheophorbides may play significant roles in glycemic control. Compounds, particularly those from BBE, present promising opportunities for the development of natural therapeutic agents for diabetes management. The study concludes that BBE and BME have strong potential as functional ingredients in future diabetes treatment strategies, possibly offering enhanced efficacy over conventional inhibitors. [ABSTRACT FROM AUTHOR]

In this article, peripheral and non‐peripheral cobalt phthalocyanines (2 and 3) were synthesized and characterized by applying the spectroscopic methods (FT‐IR, 1H NMR, 13C NMR, Maldi‐Toff mass, and UV–vis). The synthesized compounds were used for the surficial modification of gold nanoparticles (AuNP). The novel conjugates (2‐AuNP and 3‐AuNP) were characterized using transmission electron microscopy. The antioxidant activities of bioagents (2, 3, 2‐AuNP, 3‐AuNP, and AuNP) were examined by performing three different methods, and the results were compared. When their antioxidant properties were examined, it was shown that the capacities of phthalocyanines were higher compared with the modified gold nanoparticles. In addition, antibacterial analysis of the compounds was carried out by applying two different methods. As a result of the analysis, it was determined that both cobalt phthalocyanines and nanoconjugates showed antibacterial activities against Escherichia coli. Phthalocyanine compounds showed lower IC50 results than phthalocyanine‐modified gold nanoparticles, while unmodified gold nanoparticles showed no α‐glucosidase inhibitory activity. [ABSTRACT FROM AUTHOR]

Panama boasts an expansive mangrove area and stands as one of the most biodiverse countries in America. While mangrove plants have long been utilized in traditional medicine, there are still unstudied species whose potential medicinal applications remain unknown. This study aimed to extract bioactive compounds from Mora oleifera (Triana ex Hemsl.) Ducke, an understudied mangrove species. Through bioassay-guided fractionation of the crude extract, we isolated seven active compounds identified as lupenone (1), lupeol (2), α-amyrin (3), β-amyrin (4), palmitic acid (5), sitosterol (6), and stigmasterol (7). Compound structures were determined using spectroscopic analyses, including APCI-HR-MS and NMR. Compounds 1–7 displayed concentration-dependent inhibition of the alpha-glucosidase enzyme, with IC50 values of 0.72, 1.05, 2.13, 1.22, 240.20, 18.70, and 163.10 µM, respectively. Their inhibitory activity surpassed acarbose, the positive control (IC50 241.6 µM). Kinetic analysis revealed that all compounds acted as competitive inhibitors. Docking analysis predicted that all triterpenes bonded to the same site as acarbose in human intestinal alpha-glucosidase (PDB: 3TOP). A complementary metabolomic analysis of M. oleifera active fractions revealed the presence of 64 compounds, shedding new light on the plant's chemical composition. These findings suggest that M. oleifera holds promise as a valuable botanical source for developing compounds for managing blood sugar levels in individuals with diabetes. [ABSTRACT FROM AUTHOR]

Agapanthus africanus L. (Amaryllidaceae) is a traditional herbal remedy widely used in South African traditional medicine. The phytochemical and biological profiles of this medicinal species have been rarely reported. Therefore, the current study evaluates the chemical composition of the total extract and different fractions of the subterranean organs of A. africanus along with their anti-diabetic, antioxidant, and anti-proliferative activities for the first time. As a result, a group of eight metabolites belonging to different chemical classes, including flavonoids, fatty acids, phenolic acid derivatives, and steroids were isolated and identified for the first time using different chromatographic and spectroscopic techniques. Among the tested fractions, the ethyl acetate fraction exhibited the highest phenolic and flavonoid contents (82.00 ± 1.85 mg gallic acid equivalent/g dried sample and 110.6 ± 2.2 mg rutin equivalent/g dried sample, respectively), as well as the highest DPPH scavenging properties (IC 50 =151.59 ± 1.36 μg/mL). The same fraction showed promising α -glucosidase inhibitory potential and anti-proliferative activity against HCT-116 (human colon cancer) (IC 50 = 53.75 ± 0.36 and 8.51 ± 0.5 μg/mL, respectively). Ultimately, molecular docking analysis of the isolated metabolites revealed their moderate to promising binding affinities to α-glucosidase, α-amylase, catalase, and CDK2 enzymes, highlighting their potential contribution to the observed effects of A. africanus. These results provide new insight into the potential of A. africanus as a natural source of medicinally relevant metabolites. [Display omitted] • The chemical composition, antioxidant, anti-proliferative and antidiabetic activities of A. africanus were explored. • A group of steroids, fatty acids, flavonoids, and phenolic acid derivatives were isolated from A. africanus for the first time. • The ethyl acetate fraction exhibited remarkable phenolic and flavonoid contents. • The ethyl acetate fraction exhibited the highest antioxidant, cytotoxic and α-glucosidase inhibitory potentials. • Molecular docking of the isolated metabolites showed their interesting binding ability to a group of targeted enzymes. [ABSTRACT FROM AUTHOR]

Rehmannia glutinosa was extensively used to control blood sugar in diabetes treatment in tradition Chinese medicine. In the present study, three new compounds, including an iridoid rehmannia A (1) and two ionone rehmannias B-C (7-8), together with fourteen known compounds (2-6 and 9-17), were isolated from the roots of R. glutinosa. The structures of these compounds were determined by physicochemical constants and spectral analysis (1D, 2D-NMR and MS). The effect of 1-17 on α-glucosidase activity was tested in vitro. Compounds 9, 10, and 11 (IC50: 5.0, 3.1, and 6.3 mM) showed moderate activity to suppress α-glucosidase relative to acarbose (IC50 = 3.0 mM). The findings provided some new insights to understand the hypoglycemic effect of R. glutinosa and the development towards the α-glucosidase inhibitor drugs. [ABSTRACT FROM AUTHOR]

Psidium guajava is a plant of the Myrtaceae with various pharmacological activity. In this study, the water extract and the isolated compounds from guava leaves were evaluated for in vitro α-glucosidase inhibition using spectrophotometric method. Ellagic acid, quercetin, quercetin-3-O-glucuronide, avicularin, isoquercitrin, and quercetin-3-galactoside showed α-glucosidase inhibitory activity, and their IC50 value were 25.0, 41.0, 53.5, 46.9, 60.0 and 72.1 μg/mL, respectively compared with the positive control acarbose (IC50 49.2 μg/mL). This study could provide a theoretical basis for the application of Psidium guajava in the treatment of hyperglycemia. [ABSTRACT FROM AUTHOR]

Alzheimer's disease (AD) and diabetes are non-communicable diseases with global impacts. Inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are suitable therapies for AD, while α-amylase and α-glucosidase inhibitors are employed as antidiabetic agents. Compounds were isolated from the medicinal plant Terminalia macroptera and evaluated for their AChE, BChE, α-amylase, and α-glucosidase inhibitions. From 1H and 13C NMR data, the compounds were identified as 3,3′-di-O-methyl ellagic acid (1), 3,3′,4′-tri-O-methyl ellagic acid-4-O-β-D-xylopyranoside (2), 3,3′,4′-tri-O-methyl ellagic acid-4-O-β-D-glucopyranoside (3), 3,3′-di-O-methyl ellagic acid-4-O-β-D-glucopyranoside (4), myricetin-3-O-rhamnoside (5), shikimic acid (6), arjungenin (7), terminolic acid (8), 24-deoxysericoside (9), arjunglucoside I (10), and chebuloside II (11). The derivatives of ellagic acid (1–4) showed moderate to good inhibition of cholinesterases, with the most potent being 3,3′-di-O-methyl ellagic acid, with IC50 values of 46.77 ± 0.90 µg/mL and 50.48 ± 1.10 µg/mL against AChE and BChE, respectively. The compounds exhibited potential inhibition of α-amylase and α-glucosidase, especially the phenolic compounds (1–5). Myricetin-3-O-rhamnoside had the highest α-amylase inhibition with an IC50 value of 65.17 ± 0.43 µg/mL compared to acarbose with an IC50 value of 32.25 ± 0.36 µg/mL. Two compounds, 3,3′-di-O-methyl ellagic acid (IC50 = 74.18 ± 0.29 µg/mL) and myricetin-3-O-rhamnoside (IC50 = 69.02 ± 0.65 µg/mL), were more active than the standard acarbose (IC50 = 87.70 ± 0.68 µg/mL) in the α-glucosidase assay. For α-glucosidase and α-amylase, the molecular docking results for 1–11 reveal that these compounds may fit well into the binding sites of the target enzymes, establishing stable complexes with negative binding energies in the range of −4.03 to −10.20 kcalmol−1. Though not all the compounds showed binding affinities with cholinesterases, some had negative binding energies, indicating that the inhibition was thermodynamically favorable. [ABSTRACT FROM AUTHOR]

Three new quinic acids derivatives, 3- O - trans- caffeoyl-5- O -galloylquinic acid (1), 3- O - trans -caffeoly-5- O -galloylquinic acid methyl ester (2), 3- O - trans -caffeoyl-4- O -galloylquinic acid methyl ester (3), and a new shikimic acid derivative as orthacanthain A (4), along with three known compounds, 3- O -caffeoylquinic acid (5), methyl-3- O -galloylquinic acid (6), and emblifatmin (7), were isolated from the 70% methanol extract of the leaves of Castanopsis orthacantha France. The structures of all compounds were identified by optical rotation, MS, UV, IR, 1D and 2D NMR spectral data and comparison with literature. The IC 50 value of compound 3 was (0.024±0.009) mmol/L, which had strong inhibitory activity on α-glucosidase. [Display omitted] ● Three new quinic acids derivatives and a new shikimic acid derivative were isolated from leaves of Castanopsis orthacantha France. ● Compound 3 showed strong inhibitory activity on α-glucosidase with an IC 50 value of (0.024±0.009) mmol/L. ● Castanopsis orthacantha France was rich in shikimic acid derivative. [ABSTRACT FROM AUTHOR]

The preliminary α-glucosidase inhibitory activity of the methanol extract of the leaves of Sandoricum koetjape Merr. exhibited promising results. The leaves was extracted with methanol to obtain the methanol extract that was continuedly partitioned with hexane and ethyl acetate. Those fractions were further purified by various chromatographic techniques. The isolation of the potent fractions furnished two new cycloartane-type triterpenoids (1 and 2) along with ten known compounds (3–12). Their chemical structures were unambiguously established by interpretation of NMR (1 D & 2 D) and high-resolution electrospray ionization mass spectrometry (HRESIMS) data. Furthermore, the configurations of two new compounds were determined by using NOESY spectrum as well as comparing their NMR data to the reference. These compounds were evaluated against α-glucosidase. All tested compounds revealed potent activity with IC50 value in the range of 2.17–49.2 µM compared to that of acarbose (IC50 100.6 µM). Compound 10 showed the lowest IC50 value. This compound was reported as a mixed-type inhibitor. Compound 3 possessed the second strong activity with an IC50 value of 14.0 μM and was further investigated on kinetic analysis which revealed as a mixed-type inhibitor with Ki and Ki′ values of 59.1 and 155.2 μM, respectively. [ABSTRACT FROM AUTHOR]

Recent research has demonstrated the positive impact of herbal tea consumption on postprandial blood glucose regulation. This study conducts a comparative analysis of aqueous and ethanol extractions on four herbal teas (Mallotus, Cyclocarya, Rubus, and Vine) to assess their phytochemical profiles and functional attributes. Phytochemical contents, antioxidant activities, α-glucosidase inhibitory activities, and chemical compositions are investigated via colorimetric analyses and UPLC-Q-Orbitrap HRMS/MS, respectively. Results indicate that Vine, among the teas studied, exhibits the most pronounced glucose-regulating effects under both extraction methods. While ethanol extractions yield higher phytochemical content overall, the compositions vary. Conversely, aqueous extracts demonstrate unexpectedly potent antioxidant activities and comparable α-glucosidase inhibitory activities to ethanol extracts. Phytochemical contents correlate positively with antioxidant activities and α-glucosidase inhibitory activities. However, antioxidant activities exhibit a weak positive correlation with α-glucosidase inhibitory activities. These findings provide evidence that aqueous extracts from herbal teas contain valuable phytochemical compositions beneficial for antioxidants and individuals with hyperglycemia, suggesting their potential as functional ingredients to enhance the nutritional value of herbal food products. [ABSTRACT FROM AUTHOR]