Α-glucosidase Inhibitory Effects Research Articles

Effects of different adzuki bean flour additions on structural and functional characteristics of extruded buckwheat noodles.

Understanding the effects of different additions of adzuki bean flour (ABF) on structural and functional characteristics of extruded buckwheat noodles is important in developing high-quality starchy foods with desirable glycemic indexes. This study explored how varying amounts of ABF in extruded buckwheat noodles influenced their structural and functional characteristics. The findings indicated that adding ABF substantially boosted the levels of protein and flavonoids, while decreasing the content of fat and starch. Adding ABF to the noodles extended the optimum cooking time and led to a reduction in both the stickiness of the cooked noodles and the pore size of the starch gel structure, compared with pure buckwheat noodles. Fourier transform infrared spectroscopy indicated that R1047/1022 increased with the content of ABF increased, while R1022/995 decreased. X-ray diffraction showed that the relative crystallinity of buckwheat noodles was enhanced with increasing ABF amount. Adding ABF notably significantly decreased the estimated glycemic index. The buckwheat noodles extruded with 20% ABF addition demonstrated notably stronger α-glucosidase inhibitory effects than those extruded with no ABF addition. The present study demonstrates that the additions of ABF improved the structure and hypoglycemic activity of extruded buckwheat noodles while decreasing starch digestibility, and the optimal value was reached at an ABF addition of 20%. The study might fill gaps in starch noodle research and provide a new strategy for the development of functional food in the food industry. © 2024 Society of Chemical Industry.

Black and Red Currant Pomaces as Raw Materials to Create Smoothies with In Vitro Health-Promoting Potential.

Pomace is a by-product resulting from the pressing of fruits and vegetables into juices, and it is typically treated as waste. Interestingly, pomace contains minimal amounts of protein and fat but is characterized by its high polyphenol and dietary fiber contents, which may have health benefits for human physiology. Therefore, they are a potentially attractive raw material for the food industry, but to our knowledge, no smoothies with their addition have been prepared and described so far. Consequently, products derived from apple juice, incorporating different doses of fresh (6% and 12%) and dried (3% and 6%) black or red currant pomace, were formulated, and their physical properties, chemical composition, bioactive compound content, and health-promoting potential (in vitro antioxidant and antidiabetic activity) were evaluated. Additionally, the products underwent sensory assessment by consumers. The fortified beverages exhibited different physical characteristics and chemical compositions than apple juice. All smoothies were characterized by higher concentrations of anthocyanins, flavonols, and procyanidin polymers compared to the base product. Moreover, 75% of them exhibited a significantly elevated phenolic acid content as well as a higher concentration of flavan-3-ols. The majority of fresh smoothies exhibited significantly higher in vitro antioxidant capacities and increased in vitro α-amylase and α-glucosidase inhibitory effects compared to the base product. The highest ABTS activity was recorded in the variant with 6% dried black currant pomace. In turn, the smoothie with 3% dried red currant pomace had the most effective FRAP effect and, together with the product containing 12% fresh black currant pomace, ORAC antioxidant activity and α-glucosidase inhibition also. The introduction of 6% dried red currant pomace led to the creation of a beverage that most effectively inhibited α-glucosidase. The study showed that the application of various types of pomace, mainly that of black currant, into apple juice enables the development of new functional products with sensory attributes that are favorably evaluated by consumers.

Antidiabetic potentials of crude and purified sulphated polysaccharides isolated from Gracilaria gracilis, a seaweed from South Africa

Over 90 % of all cases of diabetes that have been diagnosed are type 2 diabetes (T2D), a disease exacerbated by an increase in sedentary behaviour, bad eating habits, and obesity. This study investigated the antidiabetic properties of Gracilaria gracilis, using in vitro and ex vivo experimental models. The sulphated polysaccharides (SPs) from crude extracts of the seaweed powder was prepared via hot (100°C) and cold (25°C) aqueous extraction procedures before purification via an anion exchange chromatographic technique. Both the crude and purified extracts were characterised by Fourier-transform infrared spectroscopy (FT-IR), LC-MS analysis, and Nuclear Magnetic Resonance (NMR) spectroscopy. The crude cold-aqueous and purified hot-aqueous SPs from G. gracilis had the strongest α-glucosidase inhibitory effect with IC50 value of 0.15 and 0.07 mg/ml, respectively. The purified cold-aqueous SP was the most potent inhibitor of α-glucosidase with an IC50 value of 0.17 mg/ml. The crude and purified SP-rich extracts inhibited pancreatic lipase (hot aqueous SP = 0.03 mg/ml) activity and effectively stimulated glucose uptake in yeast cells. Moreover, they showed significantly (p < 0.05) better intestinal glucose absorption inhibitory properties at the highest concentration (1 mg/ml) and displayed significantly (p < 0.05) better muscle glucose uptake compared to the commercial antidiabetic drug, metformin, at the same concentration. Overall, the current findings indicate that G. gracilis SPs may inhibit carbohydrate-hydrolysing enzymes, limit the release of simple sugars from the gut whilst effectively stimulating the use of glucose by peripheral tissue thus may be suitable to develop antidiabetic food supplements after further animal and clinical trials.

In vitro α-amylase and α-glucosidase inhibitory effects and antioxidant potential of new dihydrochalcones from Baphia massaiensis Taub

Two previously undescribed dihydrochalcones, 4,2′-dihydroxy- [2″, 2″-dimethylpyrano (3″, 4″: 4′, 5′]) dihydrochalcone (1) and 4, 2′, 4′, 2″-tetrahydroxy-5′-(3″-methylbut-3″-enyl) dihydrochalcone (2), along with six known compounds (3-8) were isolated from chloroform-methanol (1:1) extract of Baphia Massaiensis twigs. Their chemical structures were determined using NMR analysis, mass spectrometry, electronic circular dichroism (ECD), density functional theory (DFT) calculations, and a thorough comparison with reported data from the literature. All the isolated compounds (1−8) were assessed for their antioxidant activities, α-amylase and α-glucosidase inhibition effects. Dihydrochalcone 1 showed significant antioxidant activity with IC50 value of 118.8 ± 2.95 µM, and a more potent antioxidant activity was exhibited by compounds 3 and 6 with IC50 values of 84.3 ± 0.07 µM and 62.1 ± 1.59 µM, respectively, compared to the positive control, gallic acid with IC50 value of 92.9 µM. Dihydrochalcone 2 showed moderate inhibition against α-amylase and α-glucosidase with IC50 values of 44.0 ± 4.83 µM and 51.7 ± 9.72 µM compared to the standard acarbose with IC50 values of 22.9 ± 0.92 µM and 31.5 ± 0.63 µM, respectively. Molecular docking studies of the new dihydrochalcones 1 and 2, revealed the active binding sites which support the observed α-amylase and α-glucosidase inhibitory effects.

Essential oil of Hygrophila salicifolia (Vahl) Nees: Chemical composition, evaluation of antioxidant activity, anti-acetylcholinesterase and anti-α-glucosidase activities integrating molecular docking, and network pharmacology analysis

Hygrophila salicifolia (Vahl) Nees is a traditional Chinese herbal medicine widely circulated in the Chinese medicinal materials market. It has gained significant popularity for its therapeutic effects in clearing heat and reducing swelling. The present study evaluated the chemical composition, antioxidant capacity, acetylcholinesterase, and α-glucosidase inhibitory effect of this species' essential oil. The major compounds of H. salicifolia essential oil were 1-octen-3-ol (29.0 %), phytol (5.7 %), phytone (4.6 %), cubebol (3.7 %), estragole (3.5 %), 7-epi-silphiperfol-5-ene (3.3 %), and ylangenol (3.1 %). The essential oil of H. salicifolia revealed antioxidant activity against both 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals with half-maximal inhibitory concentration (IC50) values of 2.13 ± 0.17 and 0.22 ± 0.02 mg/mL. The ferric reducing antioxidant power (FRAP) value was 170.97 ± 3.68 μmol·g−1. The essential oil has moderate activity against acetylcholinesterase (IC50 = 360.4 ± 12.7 μg/mL) and weak activity against α-glucosidase (14.2 % inhibition at 500 μg/mL). Moreover, we conducted in silico network pharmacology analysis and molecular docking to evidence the results of in vitro tests, providing a theoretical foundation for future drug development. The presented results suggest that the essential oil of H. salicifolia possesses the potential to be used in cosmetics, food, and pharmacological industries, emphasizing the need for further investigation.

Alpha-glucosidase Inhibitory Effects of Flavonoids, Phenolic Acids and Iridoids Isolated From Vinca soneri: In vitro and in silico Perspectives.

Various Vinca species have been traditionally used for their antihypertensive, sedative, and hemostatic properties, as well as for treating diabetes. In this study, some flavonoids, phenolic acids and iridoids were isolated from an endemic Vinca species, Vinca soneri for the first time. α-Glucosidase inhibitory effects of the isolates were tested and kaempferol-3-O-α-rhamnopyranosyl (1→6) β-galactopyranoside (1) was found to be the most active one with an IC50 value of 285.73 ± 7.35 µM. Enzyme kinetic assay revealed that it inhibited α-glucosidase in competitive manner. Molecular geometry of 1 was predicted and Frontier molecular orbital analysis was performed using Density Functional Theory (DFT) calculations. Molecular docking and MM-GBSA calculations predicted good fit for 1 in the enzyme active site and key interactions with the catalytic residues. As a result, current study identifies 1 as a promising competitive α-glucosidase inhibitor to be developed as a potential antidiabetic drug candidate.

Human α-glucosidase inhibition and phytochemical profile of natural and shinzuke treated olives: implications from the processing method

Olive (Olea europaea) phytochemicals are associated with a reduced risk of type 2 diabetes. Table olives typically have higher phytochemical concentrations than olive oil, but their impact on human intestinal α-glucosidase is largely unknown. Shinzuke, the most common trade preparation in Japan, are alkali-treated non-fermented green olives. In contrast, natural olives are debittered by brining, which may enhance phytochemical retention. We evaluated the α-glucosidase inhibitory effect of Shinzuke and natural green olives produced in-house and compared them with commercial table olives. Eight types of table olives were tested against human intestinal α-glucosidase. Shinzuke Mission was the least effective (IC50 0.710 ± 0.058 mg/mL), while Natural green olives showed double to triple activity, with a non-competitive mechanism. Natural table olives retained more phytochemicals than shinzuke and other treated olives, and are good inhibitors of human α-glucosidase in vitro, exhibiting potential as a functional food for the management of postprandial glycaemia.Graphical

In vitro cholinesterases, tyrosinase, α-glucosidase inhibitory and anticancer effects of novel silicon phthalocyanines containing geraniol/phytol

The axially silicon phthalocyanines, consisting of different acyclic hydrocarbons, were generated by SiPcCl2 reacting with either geraniol or phytol in toluene in the presence of NaH. FT-IR, UV–Vis, MALDI TOF, and NMR spectroscopy all provided information about the structures of silicon phthalocyanines. The cholinesterase, tyrosinase, and α-glucosidase inhibitory effects of G-SiPc and P-SiPc were tested using spectrophotometric assays. The IC50 values of G-SiPc and P-SiPc were 7.22 ± 0.53 and 11.28 ± 2.73 µM for AChE; 70.05 ± 3.00 and 60.55 ± 3.80 µM for BuChE. In addition, G-SiPc and P-SiPc inhibited the tyrosinase enzyme with IC50 values of 280.36 ± 7.92 µM and 40.51 ± 3.88 µM, respectively. P-SiPc had about seven times stronger inhibitory properties than G-SiPc. The substances exhibited less inhibition than acarbose in the α-glucosidase inhibitory assay. Finally, the cytotoxic effects of G-SiPc and P-SiPc were investigated using the MTT assay on L-929 mouse fibroblast cells as normal cells. G-SiPc and P-SiPc did not reach IC50 values up to 100 μM.

In Vitro Alpha-Glucosidase Inhibitory Effect of Etlingera Elatior Ethanol Extract Growing in Gayo Highland, Aceh Province, Indonesia

Background The prevalence of diabetes mellitus (DM) is increasing overtime, potentially leading to various severe health complications and mortality. Despite therapeutic agents have currently been developed, unexpected adverse effects are inevitable. Hence, safe and effective medications such as those of plant origin are critical to prevent unexpected complication in DM sufferers. Etlingera elatior has been widely used as spice and traditional medicine to treat diabetes in Aceh Province, Indonesia. However, study regarding α-glucosidase inhibitory effect of E. elatior growing in Gayo highlands, Aceh, Indonesia, is completely lacking. The aim of this study was to evaluate in vitro α-glucosidase inhibitory effect of E. elatior ethanol extracts (EEEE) growing in Gayo highlands, Aceh Province, Indonesia. Methods Antioxidant activity was determined using DPPH procedure, whereas α-glucosidase inhibition assay was carried out using spectrophotometric method. Data analysis was performed using One-Way Analysis of Variance (ANOVA), followed by Duncan’s multiple range test at α=0.05. Results Phytochemical analysis revealed the presence of total phenolic (TPC), total flavonoid (TFC), and total tannin (TTC) content in all E. elatior plant parts, in which the highest TPC was found in the stem (158.38 GAE/g), whereas the highest TFC and TTC was obtained in the rhizome extracts. The extract of fruit showed the strongest antioxidant activities, followed by the stem and leaf, with IC50 of 2.381 μg/mL, 6.966 μg/mL, and 19.365 μg/mL, respectively. All E. elatior extracts revealed a significant inhibitory activity against α-glucosidase at the concentration of 500 μg/mL, in which the stem extract showed the most effective α-glucosidase inhibitory effect with IC50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. Conclusions This study highlights E. elatior potency as a novel source of antioxidant and natural antidiabetic compounds that are useful for the prevention and treatment of diabetes.

Labdanum Resin from Cistus ladanifer L. as a Source of Compounds with Anti-Diabetic, Neuroprotective and Anti-Proliferative Activity.

Labdanum resin or "gum" can be obtained from Cistus ladanifer L. by two different extraction methods: the Zamorean and the Andalusian processes. Although its main use is in the fragrance and perfumery sectors, ethnobotanical reports describe its use for medicinal purposes in managing hyperglycemia and mental illnesses. However, data concerning the bioactivities and pharmacological applications are scarce. In this work, it was found that the yield of labdanum resin extracted by the Andalusian process was 25-fold higher than the Zamorean one. Both resins were purified as absolutes, and the Andalusian absolute was purified into diterpenoid and flavonoid fractions. GC-EI-MS analysis confirmed the presence of phenylpropanoids, labdane-type diterpenoids, and methylated flavonoids, which are already described in the literature, but revealed other compounds, and showed that the different extracts presented distinct chemical profile. The potential antidiabetic activity, by inhibition of α-amylase and α-glucosidase, and the potential neuroprotective activity, by inhibition of acetylcholinesterase, were investigated. Diterpenoid fraction produced the higher α-amylase inhibitory effect (~30% and ~40% at 0.5 and 1 mg/mL, respectively). Zamorean absolute showed the highest α-glucosidase inhibitory effect (~14% and ~24%, at 0.5 and 1 mg/mL, respectively). Andalusian absolute showed the highest acetylcholinesterase inhibitory effect (~70% and ~75%, at 0.5 and 1 mg/mL, respectively). Using Caco-2 and HepG2 cell lines, Andalusian absolute and its purified fractions showed moderate cytotoxic/anti-proliferative activity at 24 h exposure (IC50 = 45-70 µg/mL, for Caco-2; IC50 = 60-80 µg/mL, for HepG2), whereas Zamorean absolute did not produce cytotoxicity (IC50 ≥ 200.00 µg/mL). Here we show, for the first time, that labdanum resin obtained by the Andalusian process, and its fractions, are composed of phytochemicals with anti-diabetic, neuroprotective and anti-proliferative potential, which are worth investigating for the pharmaceutical industry. However, toxic side-effects must also be addressed when using these products by ingestion, as done traditionally.

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.

Identification of Novel Peptides in Distillers' Grains as Antioxidants, α-Glucosidase Inhibitors, and Insulin Sensitizers: In Silico and In Vitro Evaluation.

Distillers' grains are rich in protein and constitute a high-quality source of various bioactive peptides. The purpose of this study is to identify novel bioactive peptides with α-glucosidase inhibitory, antioxidant, and insulin resistance-ameliorating effects from distiller's grains protein hydrolysate. Three novel peptides (YPLPR, AFEPLR, and NDPF) showed good potential bioactivities, and the YPLPR peptide had the strongest bioactivities, whose IC50 values towards α-glucosidase inhibition, radical scavenging rates of 2,2'-azino-bis (3-ethylbenzothiazoline-6- sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) were about 5.31 mmol/L, 6.05 mmol/L, and 7.94 mmol/L, respectively. The glucose consumption of HepG2 cells treated with YPLPR increased significantly under insulin resistance condition. Moreover, the YPLPR peptide also had a good scavenging effect on intracellular reactive oxygen species (ROS) induced by H2O2 (the relative contents: 102.35% vs. 100%). Molecular docking results showed that these peptides could stably combine with α-glucosidase, ABTS, and DPPH free radicals, as well as related targets of the insulin signaling pathway through hydrogen bonding and van der Waals forces. This research presents a potentially valuable natural resource for reducing oxidative stress damage and regulating blood glucose in diabetes, thereby increasing the usage of distillers' grains peptides and boosting their economic worth.

Screening of α-Glucosidase Inhibitors in Cichorium glandulosum Boiss. et Huet Extracts and Study of Interaction Mechanisms.

Cichorium glandulosum Boiss. et Huet (CGB) extract has an α-glucosidase inhibitory effect (IC50 = 59.34 ± 0.07 μg/mL, positive control drug acarbose IC50 = 126.1 ± 0.02 μg/mL), but the precise enzyme inhibitors implicated in this process are not known. The screening of α-glucosidase inhibitors in CGB extracts was conducted by bioaffinity ultrafiltration, and six potential inhibitors (quercetin, lactucin, 3-O-methylquercetin, hyperoside, lactucopicrin, and isochlorogenic acid B) were screened as the precise inhibitors. The binding rate calculations and evaluation of enzyme inhibitory effects showed that lactucin and lactucopicrin exhibited the greatest inhibitory activities. Next, the inhibiting effects of the active components of CGB, lactucin and lactucopicrin, on α-glucosidase and their mechanisms were investigated through α-glucosidase activity assay, enzyme kinetics, multispectral analysis, and molecular docking simulation. The findings demonstrated that lactucin (IC50 = 52.76 ± 0.21 μM) and lactucopicrin (IC50 = 17.71 ± 0.64 μM) exhibited more inhibitory effects on α-glucosidase in comparison to acarbose (positive drug, IC50 = 195.2 ± 0.30 μM). Enzyme kinetic research revealed that lactucin inhibits α-glucosidase through a noncompetitive inhibition mechanism, while lactucopicrin inhibits it through a competitive inhibition mechanism. The fluorescence results suggested that lactucin and lactucopicrin effectively reduce the fluorescence of α-glucosidase by creating lactucin-α-glucosidase and lactucopicrin-α-glucosidase complexes through static quenching. Furthermore, the circular dichroism (CD) and Fourier transform infrared spectroscopy (FT-IR) analyses revealed that the interaction between lactucin or lactucopicrin and α-glucosidase resulted in a modification of the α-glucosidase's conformation. The findings from molecular docking and molecular dynamics simulations offer further confirmation that lactucopicrin has a robust binding affinity for certain residues located within the active cavity of α-glucosidase. Furthermore, it has a greater affinity for α-glucosidase compared to lactucin. The results validate the suppressive impact of lactucin and lactucopicrin on α-glucosidase and elucidate their underlying processes. Additionally, they serve as a foundation for the structural alteration of sesquiterpene derived from CGB, with the intention of using it for the management of diabetic mellitus.

Industrial upcycling of almond skin through production of novel brioches

The global sustainability policy emphasizes reusing of agri-food waste and by-products to enhance food bioactive properties. Thus, brioches were processed incorporating almond skin powder (ASP): control (CTR), without ASP addition; 5-ASP, with 5% (w/w) ASP; and 10-ASP, with 10% (w/w) ASP. Seven different brioches shapes were obtained for each recipe. Flavonoids were mainly detected in Tuono almond skin by Ultra-High Performance Liquid Chromatography coupled to High-Resolution Mass Spectrometry (UHPLC-HRMSMS), in particular, flavan-3-ol monomers. The ethanolic extract of Tuono almond skins contained polar lipids (oxylipins and phospholipids). Gas Chromatography–Mass Spectrometry (GC-MS) identified six major fatty acids, mainly oleic acid (48.01%). Photothermal degradation impact on bioactive compounds was evaluated using a first-order kinetic model. Antioxidant activity was studied using 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), 2,2-diphenyl-1-picrylhydrazyl and β-carotene bleaching test. α-amylase, α-glucosidase, and lipase inhibitory effect were also tested. The acidification of the doughs was consistent across all trials. Lactic acid bacteria and yeast levels increased. Importantly, the final products were free from undesirable microorganisms. The addition of ASP led to reduced weight loss and specific volume for all seven brioche types. Furthermore, the firmness, crumb structure, and sensory profile of the final products were noticeably influenced. Tasters clearly favoured the Treccina brioches. The production of sweet leavened baked goods was carried out in triplicate in two independent experiments. The statistical model applied to the data considered the effects of brioche shape and the addition of ASP. Kinetic data revealed that the half-life extension for both total phenol and flavonoid content was observed in the 10-ASP sample (18.00382). 10-ASP sample exhibited promising ABTS radical scavenging activity, with inhibitory concentration 50% (IC50) values of 18.64 mg/mL after 9 days of photothermal degradation. Moreover, when testing 10-ASP Treccina against α-amylase and α-glucosidase, the IC50 values were 198.16 and 190.23 μg/mL, respectively, even after 9 days.

Inhibitory Activities of Thai Culinary Vegetables against Key Enzymes Relevant to Diabetes Mellitus and the Kinetics of Enzyme Inhibitions

Diabetes mellitus (DM) is one of the most challenging noncommunicable diseases, as it causes significant costs for medical treatment as well as high morbidity and mortality rates. Dietary plants with antidiabetic properties have been explored as an alternative to synthetic medicines to treat DM because of their safety and nutrition. Hence, the objective of the present study was to determine the inhibitory activities of twenty commonly consumed Thai culinary vegetables against α-glucosidase and α-amylase. All vegetables were extracted using deionized water, ethanol, and hexane at 150 rpm and 30°C for 24 hours. The enzyme inhibitory activities were performed using a colorimetric assay. Diverse results for α-glucosidase and α-amylase inhibitory activities were found for all vegetable extracts. The most potent anti-α-glucosidase activity was obtained from the ethanolic extract of Leucaena leucocephala (Lamk.) de Wit with the half maximal inhibitory concentration (IC50) of 13.39 ± 0.14 μg/mL, followed by the aqueous and ethanolic extracts of Polygonum odoratum Lour with IC50 of 25.60 ± 0.42 and 49.03 ± 0.72 μg/mL, respectively. All the samples exhibited mixed, noncompetitive, and uncompetitive inhibition. It can be concluded that the α-glucosidase and α-amylose inhibitory effects of the investigated extracts may be an indicator of antidiabetic potency, and these extracts might potentially be beneficial as functional components for postprandial hyperglycemia treatment.

Chromatographic Fingerprinting of Cacao Pod Husk Extracts (Theobroma cacao L.): Exploring Antibacterial, Antioxidant, and Antidiabetic Properties with In Silico Molecular Docking Analysis.

Naturaldrugs derived from plants are becoming more popular because of their apparent biologicalefficacy, affordability, and safety. A byproduct of cocoa farms, cocoa pod husk (CPH), is often disregarded yet contains an abundance of phenolic chemicalsthat 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. Theantibacterial and antioxidant properties of such extracts and their impact on cytotoxicity and α-glucosidasewere explored. According to our results, the 80% ethanol and dichloromethane extracts contained 19 and 12 phytochemical components, respectively. Interestingly, at 250µg/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 35.26µg/mL than the dichloromethane extract, which had an IC50 value of 23.88µg/mL. Furthermore, the α-glucosidase inhibitory effect of the dichloromethane extract was found to be better, as shown by its IC50 value of 126.5µg/mL, which was lower than that of the ethanol extract at 151.3µg/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 extractswere confirmed by molecular docking investigations aimed at interacting with α-glucosidase proteins. Our thorough analysis makes CPH extracts seem like theexcellent candidates for biomedical uses. These results provide new insights into the therapeutic potential of CPH extractsand pave the way for the development of innovative medications and natural remedies.

Cassia angustifolia Vahl. Leaves: Determination of Total Phenolic and Sennoside Contents of Different Fractions in Comparison with Their α- Glucosidase and Tyrosinase Inhibitory Effects.

Cassia angustifolia Vahl. (Senna) is a medicinal plant containing anthraquinone compounds such as sennoside. Senna is primarily valued for its laxative properties. In Persian medicine, this plant has been also used to treat various disorders such as diabetes and skin hyperpigmentation. Previous studies have shown that different species of senna, such as C. articulata, C. alata, C. Siamea, C. Surattensis inhibit alpha-amylase and α-glucosidase enzymes. To the best of our knowledge, no previous evidence is available on tyrosinase and α-glucosidase inhibitory effects of the extract and different fractions of C. angustifolia leaves. The purpose of this study was to investigate the inhibitory effect of the methanol-water extract and different fractions (hexane, chloroform, ethyl acetate, and remaining crude extract) of senna against tyrosinase and α-glucosidase and to investigate their total phenolic and sennoside B contents. Our findings depicted that the methanol-water extract and fractions had no significant anti-tyrosinase activity; however, some fractions were active toward α-glucosidase. The hexane fraction and the remaining crude extract demonstrated the highest inhibition on α-glucosidase compared to acarbose (positive control). In addition, the ethyl acetate fraction contains high phenolic and hydroxy anthraquinone derivatives based on the amount of sennoside B contents equivalent to 382.25 μg/mL of gallic acid and 1.525% of sennoside B, respectively. Moreover, no correlation was observed between the phenolic and sennoside contents of different fractions and their α-glucosidase inhibitory effect. Considering the α-glucosidase inhibition results, the hexane fraction of C. angustifolia can be a valuable fraction for in vitro and in vivo antidiabetic studies as well as further phytochemical studies. Further studies to identify the active substances and the exact mechanism of the bioactive ingredients on the inhibitory effects of α-glucosidase can provide promising results in the future.

Identification of in vitro α-glucosidase and urease inhibitory effect, and in silico studies of Naproxen-derived 1,3,4-oxadiazole-based Schiff-base derivatives

In search of new α-glucosidase and urease inhibitors, a series of naproxen-derived 1,3,4-oxadiazole-containing ketones 6a-e and their Schiff-base derivatives 7a-o were synthesized. The isolated compounds were identified by HRMS (EI), 1H NMR and 13C NMR spectroscopic techniques. Among the series, compounds 7j, 7i, 7e, 7d and 7o were found to be significantly active against α-glucosidase with IC50 values of 6.14 ± 1.23, 9.90 ± 1.23, 25.90 ± 1.31, 38.07 ± 1.51 and 34.23 ± 1.08 µM, respectively. These values indicate a significantly higher potency compared to the standard acarbose (IC50 = 375.82 ± 1.76 µM). In the case of urease, compounds 7d, 7e, 6a, 7i and 6c showed potent inhibitory activity with IC50 values of 6.68 ± 0.97, 11.39 ± 0.10, 14.18 ± 0.38, 14.39 ± 1.05 and 18.68 ± 0.25 µM, respectively, as compared to the reference standard thiourea (IC50 = 21.37 ± 1.76 µM). The molecular docking gave an insight into the binding interactions established by the selected most active analogues with the catalytic sites of α-glucosidase and urease. The results obtained can be correlated with several key intermolecular interactions including π-cation, π-anion, π-sulphur, π-alkyl, π-π T shaped, π-π stacked, π-lone pair, hydrogen bonding and Van der Waals attraction with the active sites of α-glucosidase and urease.

Essential Oils of Two Species of Zingiberaceae Family from Vietnam: Chemical Compositions and α-Glucosidase, α-Amylase Inhibitory Effects

The ginger family (Zingiberaceae) is one of the most diverse and abundant families in the plant kingdom in terms of number of species. In terms of chemistry, this is a family of plants containing much essential oil with mainly monoterpene and sesquiterpene derivatives, which has been widely used in medicine, food, and flavor industries. In our series of studies on ginger family plants, the two new species including Wurfbainia schmidtii (K. Schum.) Škorničk. &amp; A.D. Poulsen and Zingiber atroporphyreus Škorničk. &amp; Q.B. Nguyen has been investigated for the first time. This study aimed to identify the chemical compositions of essential oils extracted from the rhizomes and leaves of these two species using gas chromatography-mass spectrometry (GC/MS) analysis and evaluate their hypoglycemic effects through the α-glucosidase and α-amylase inhibitory assays. In terms of chemical composition, in general, the main compounds appearing in the essential oils of both leaves and rhizomes of each species are similar but they are differences in the percentage of the main components, for example, 1,8-cineole is a main component in leaves whereas fenchyl acetate is the main one in rhizomes of W. schmidtii. Several distinctive compounds, in comparison with other members in the genus Zingiber, namely β-pinene, α-pinene, β-elemene, and sabinene, were found in the essential oil of Z. atroporphyreus. Regarding hypoglycemic effects, the essential oils from the two species tested possessed weak α-glucosidase and α-amylase inhibitory effects. For the first time, this study was designed to investigate the chemical composition as well as the hypoglycemic effect of essential oils distilled from the rhizomes and leaves of two species W. schmidtii and Z. atroporphyreus have been reported, serving as a premise for further systematic research on their phytochemistry and pharmacological effects being conducted.

Metabolites profiling of Sapota fruit pulp via a multiplex approach of gas and ultra performance liquid chromatography/mass spectroscopy in relation to its lipase inhibition effect.

Sapota, Manilkara zapota L., are tasty, juicy, and nutrient-rich fruits, and likewise used for several medicinal uses. The current study represents an integrated metabolites profiling of sapota fruits pulp via GC/MS and UPLC/MS, alongside assessment of antioxidant capacity, pancreatic lipase (PL), and α-glucosidase enzymes inhibitory effects. GC/MS analysis of silylated primary polar metabolites led to the identification of 68 compounds belonging to sugars (74%), sugar acids (18.27%), and sugar alcohols (7%) mediating the fruit sweetness. Headspace SPME-GC/MS analysis led to the detection of 17 volatile compounds belonging to nitrogenous compounds (72%), ethers (7.8%), terpenes (7.6%), and aldehydes (5.8%). Non-polar metabolites profiling by HR-UPLC/MS/MS-based Global Natural Products Social (GNPS) molecular networking led to the assignment of 31 peaks, with several novel sphingolipids and fatty acyl amides reported for the first time. Total phenolic content was estimated at 6.79 ±0.12 mg gallic acid equivalent/gram extract (GAE/g extract), but no flavonoids were detected. The antioxidant capacities of fruit were at 1.62 ±0.2, 1.49 ±0.11, and 3.58 ±0.14 mg Trolox equivalent/gram extract (TE/g extract) via DPPH, ABTS, and FRAP assays, respectively. In vitro enzyme inhibition assays revealed a considerable pancreatic lipase inhibition effect (IC50 = 2.2 ±0.25 mg/mL), whereas no inhibitory effect towards α-glucosidase enzyme was detected. This study provides better insight into sapota fruit's flavor, nutritional, and secondary metabolites composition mediating for its sensory and health attributes.