-
International Journal of Biological... Dec 2023A series of new 1,ω-bis-(5-alkyl-3-tosyl-1,3,4,2-triazaphospholino)alkanes 2 and 3 were obtained in excellent yields by the condensation of...
A series of new 1,ω-bis-(5-alkyl-3-tosyl-1,3,4,2-triazaphospholino)alkanes 2 and 3 were obtained in excellent yields by the condensation of 1,ω-bis-(1-tosylamidrazone)alkanes 1 with two equivalent molars of Lawesson's Reagent (LR) and trisdimethylaminophosphine, respectively. All synthesized compounds were characterized by various spectroscopic techniques including IR, H NMR, C NMR and P NMR and elemental analysis. The newly synthesized compounds were evaluated against key enzymes related to diabetes and obesity such as α-amylase and lipase. This study showed that the compounds 3a and 2b are an excellent inhibitor of α-amylase (with IC = 18.8 mM) and lipase (with IC = 19 mM) respectively, as compared with standard, orlistat (IC = 22 mM). Among this series, compounds 3a and 2b with the CH or CH group at position 6 were identified as the most potent inhibitors against α-amylase, and lipase enzymes. The remaining compounds were found to be moderately active. Further, molecular docking simulation studies were done to identify the interactions and binding mode of synthesized analogs at binding site of α-amylase and lipase enzymes.
Topics: Molecular Structure; Structure-Activity Relationship; Enzyme Inhibitors; Molecular Docking Simulation; alpha-Amylases; Alkanes; Lipase
PubMed: 37793521
DOI: 10.1016/j.ijbiomac.2023.127195 -
Chemistry & Biodiversity Apr 2024The phytochemical investigation of Viburnum chinshanense leaves led to the isolation and identification of four new phenolic glycosides, viburninsides A-D (1-4), and...
The phytochemical investigation of Viburnum chinshanense leaves led to the isolation and identification of four new phenolic glycosides, viburninsides A-D (1-4), and eight known analogues (5-12). The structures of the four undescribed compounds were determined by spectroscopic techniques, including 1D NMR, 2D NMR, and HRESIMS, and their containing sugar units were confirmed by acid hydrolysis and HPLC analysis of the monosaccharide's chiral derivatives. Additionally, the α-amylase and α-glucosidase inhibitory activities of the isolated compounds were assessed. Compounds 1, 2, 4, 9, and 10 exhibited potential inhibitory activities against α-amylase and α-glucosidase with IC values ranging from 35.07 μM to 47.42 μM and 18.27 μM to 43.65 μM, respectively. Molecular docking analysis of compound 4 with the strongest inhibition against the target enzymes was also conducted.
Topics: Glycosides; Glycoside Hydrolase Inhibitors; alpha-Glucosidases; alpha-Amylases; Viburnum; Molecular Docking Simulation; Phenols
PubMed: 38380697
DOI: 10.1002/cbdv.202400236 -
Critical Reviews in Food Science and... Nov 2023Type 2 diabetes is caused by persistently high blood sugar levels, which leads to metabolic dysregulation and an increase in the risk of chronic diseases such as... (Review)
Review
Type 2 diabetes is caused by persistently high blood sugar levels, which leads to metabolic dysregulation and an increase in the risk of chronic diseases such as diabetes and obesity. High levels of rapidly digestible starches within foods may contribute to high blood sugar levels. Amylase inhibitors can reduce amylase activity, thereby inhibiting starch hydrolysis, and reducing blood sugar levels. Currently, amylase inhibitors are usually chemically synthesized substances, which can have undesirable side effects on the human body. The development of amylase inhibitors from food-grade ingredients that can be incorporated into the human diet is therefore of great interest. Several classes of phytochemicals, including polyphenols and flavonoids, have been shown to inhibit amylase, including certain types of food-grade nanoparticles. In this review, we summarize the main functions and characteristics of amylases within the human body, as well as their interactions with amylase inhibitors. A strong focus is given to the utilization of nanoparticles as amylase inhibitors. The information covered in this article may be useful for the design of functional foods that can better control blood glucose levels, which may help reduce the risk of diabetes and other diet-related diseases.
Topics: Humans; alpha-Amylases; Blood Glucose; Diabetes Mellitus, Type 2; Amylases; Enzyme Inhibitors; Starch; Hyperglycemia
PubMed: 35822304
DOI: 10.1080/10408398.2022.2098687 -
Food & Function Feb 2024A promising and efficacious approach to manage diabetes is inhibiting α-glucosidase and α-amylase activity. Therefore, the inhibitory activities of five natural...
A promising and efficacious approach to manage diabetes is inhibiting α-glucosidase and α-amylase activity. Therefore, the inhibitory activities of five natural sweeteners (mogrosides (Mog), stevioside (Ste), glycyrrhizinic acid (GA), crude trilobatin (CT), and crude rubusoside (CR)) against α-glucosidase and α-amylase and their interactions were evaluated using enzyme kinetics, fluorescence spectroscopy, Fourier infrared spectroscopy, and molecular docking. The inhibitor sequence was CT > GA > Ste, as GA competitively inhibited α-glycosidase activity while CT and Ste exhibited mixed inhibitory effects. Compared to a positive control acarbose, the inhibitory activity of CT was higher. For α-amylase, the mixed inhibitors CT, CR, and Mog and the competitive inhibitor Ste effectively inhibited the enzyme, with the following order: CT > CR > Ste > Mog; nevertheless, the inhibitors were slightly inferior to acarbose. Three-dimensional fluorescence spectra depicted that GA, CT, and CR bound to the hydrophobic cavity of α-glucosidase or α-amylase and changed the polarity of the hydrophobic amino acid-based microenvironment and structure of the polypeptide chain backbone. Infrared spectroscopy revealed that GA, CT, and CR could disrupt the secondary structure of α-glucosidase or α-amylase, which decreased enzyme activity. GA, trilobatin and rubusoside bound to amino acid residues through hydrogen bonds and hydrophobic interactions, changing the conformation of enzyme molecules to decrease the enzymatic activity. Thus, CT, CR and GA exhibit promising inhibitory effects against α-glucosidase and α-amylase.
Topics: Acarbose; Glycoside Hydrolase Inhibitors; Molecular Docking Simulation; alpha-Glucosidases; alpha-Amylases; Protein Structure, Secondary; Amino Acids; Flavonoids; Glucosides; Diterpenes, Kaurane; Polyphenols
PubMed: 38318730
DOI: 10.1039/d3fo05234f -
Molecules (Basel, Switzerland) Dec 2023Cannabis is considered ( L.) a sacred herb in many countries and is vastly employed in traditional medicine to remedy numerous diseases, such as diabetes. This research...
Cannabis is considered ( L.) a sacred herb in many countries and is vastly employed in traditional medicine to remedy numerous diseases, such as diabetes. This research investigates the chemical composition of the aqueous extracts from L. seeds. Furthermore, the impact of these extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase enzymes is evaluated, as well as their antihyperglycemic effect. Analysis of the chemical composition of the aqueous extract was conducted using high-performance liquid chromatography with a photodiode array detector (HPLC-DAD). In contrast, the ethanol, hexanic, dichloromethane, and aqueous extract compositions have been established. Additionally, the inhibitory effects of ethanolic, dichloromethane, and aqueous extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase activities were evaluated in vitro and in vivo. The results of HPLC analysis indicate that the most abundant phenolic compound in the aqueous cannabis seed extract is 3-hydroxycinnamic acid, followed by 4-hydroxybenzoic acid and rutin acid. Moreover, administration of ethanolic and aqueous extracts at a dose of 150 mg/Kg significantly suppressed postprandial hyperglycemia compared to the control group; the ethanolic, dichloromethane, and aqueous extracts significantly inhibit pancreatic α-amylase and lipase, and intestinal α-glucosidase in vitro. The pancreatic α-amylase test exhibited an inhibition with values of 16.36 ± 1.24 µg/mL, 19.33 ± 1.40 µg/mL, 23.53 ± 1.70 µg/mL, and 17.06 ± 9.91 µg/mL for EAq, EDm, EET, and EHx, respectively. EET has the highest inhibitory capacity for intestinal α-glucosidase activity, with an of 32.23 ± 3.26 µg/mL. The extracts inhibit porcine pancreatic lipase activity, demonstrating their potential as lipase inhibitors. Specifically, at a concentration of 1 mg/mL, the highest inhibition rate (77%) was observed for EDm. To confirm these results, the inhibitory effect of these extracts on enzymes was tested in vivo. The oral intake of aqueous extract markedly reduced starch- and sucrose-induced hyperglycemia in healthy rats. Administration of the ethanolic extract at a specific dose of 150 mg/kg significantly reduced postprandial glycemia compared with the control group. It is, therefore, undeniable that cannabis extracts represent a promising option as a potentially effective treatment for type 2 diabetes.
Topics: Animals; Rats; Swine; Hypoglycemic Agents; Cannabis; Pancreatic alpha-Amylases; alpha-Glucosidases; Diabetes Mellitus, Type 2; Methylene Chloride; Lipase; Hallucinogens; Hyperglycemia; Cannabinoid Receptor Agonists; Ethanol; Plant Extracts
PubMed: 38202676
DOI: 10.3390/molecules29010093 -
Microbial Cell Factories Aug 2023The purpose of the current study is to isolate a heavily amylase-producing bacteria of the genus Bacillus from soil samples, optimize the production of the enzyme,...
BACKGROUND AND AIM
The purpose of the current study is to isolate a heavily amylase-producing bacteria of the genus Bacillus from soil samples, optimize the production of the enzyme, purify it, and evaluate its activity against biofilm-producing bacteria. A total of 12 soil samples were collected and screened for promising Bacillus species with good amylolytic activity. Isolation was done by serial dilution and plating technique and amylolytic activity was determined by starch agar plate method. Among the 12 Bacillus isolates recovered from soil samples, 7 showed positive α-amylase production. The best isolate that recorded the greatest amylolytic activity was selected for further studies. This isolate was identified by 16S rRNA sequencing as Bacillus cereus and registered under gene bank accession number OP811897. Furthermore, the α-amylase enzyme was produced by a submerged fermentation technique using best production media and partially purified by ammonium sulfate and chilled ethanol and molecular weight had been determined by SDS-PAGE gel electrophoresis. The production of α-amylase was optimized experimentally by one-factor at a time protocol and statistically by Plackett-Burman design as well as RSM CCD design. Data obtained from OFAT and CCD revealed that α-amylase activities were 1.5- and twofold respectively higher as compared to un-optimized conditions. The most significant factors had been identified and optimized by CCD design.
RESULTS
Among the eleven independent variables tested by PBD, glucose, peptone, (NH4)SO4, and Mg SO were the most significant parameters for α-amylase production with an actual yield of 250U/ml. The best physical parameters affecting the enzyme production were incubation time at 35 °C, and pH 5.5 for 48 h. The partially purified enzyme with 60% ammonium sulphate saturation with 1.38- fold purification showed good stability characteristics at a storage temperature of 4 °C and pH up to 8.5 for 21 days. Antibiofilm activity of purified α-amylase was determined against Pseudomonas aeruginosa (ATCC 35659) by spectrophotometric analysis and CLSM microscopic analysis. Results demonstrated biofilm inhibition by 84% of the formed Pseudomonas biofilm using a microtiter plate assay and thickness inhibition activity by 83% with live/Dead cells percentage of 17%/83% using CLSM protocol.
CONCLUSIONS
A highly stable purified α-amylase from B. cereus showed promising antibiofilm activity against one of the clinically important biofilm-forming MDR organisms that could be used as a cost-effective tool in pharmaceutical industries.
Topics: alpha-Amylases; Bacillus cereus; Pseudomonas aeruginosa; RNA, Ribosomal, 16S; Hydrogen-Ion Concentration; Bacillus; Temperature; Biofilms; Soil
PubMed: 37528448
DOI: 10.1186/s12934-023-02139-6 -
Food Research International (Ottawa,... Jul 2024(Poly)phenols inhibit α-amylase by directly binding to the enzyme and/or by forming starch-polyphenol complexes. Conventional methods using starch as the substrate...
(Poly)phenols inhibit α-amylase by directly binding to the enzyme and/or by forming starch-polyphenol complexes. Conventional methods using starch as the substrate measure inhibition from both mechanisms, whereas the use of shorter oligosaccharides as substrates exclusively measures the direct interaction of (poly)phenols with the enzyme. In this study, using a chromatography-based method and a short oligosaccharide as the substrate, we investigated the detailed structural prerequisites for the direct inhibition of human salivary and pancreatic α-amylases by over 50 (poly)phenols from the (poly)phenol groups: flavonols, flavones, flavanones, flavan-3-ols, polymethoxyflavones, isoflavones, anthocyanidins and phenolic acids. Despite being structurally very similar (97% sequence homology), human salivary and pancreatic α-amylases were inhibited to different extents by the tested (poly)phenols. The most potent human salivary α-amylase inhibitors were luteolin and pelargonidin, while the methoxylated anthocyanidins, peonidin and petunidin, significantly blocked pancreatic enzyme activity. B-ring methoxylation of anthocyanidins increased inhibition against both human α-amylases while hydroxyl groups at C3 and B3' acted antagonistically in human salivary inhibition. C4 carbonyl reduction, or the positive charge on the flavonoid structure, was the key structural feature for human pancreatic inhibition. B-ring glycosylation did not affect salivary enzyme inhibition, but increased pancreatic enzyme inhibition when compared to its corresponding aglycone. Overall, our findings indicate that the efficacy of interaction with human α-amylase is mainly influenced by the type and placement of functional groups rather than the number of hydroxyl groups and molecular weight.
Topics: Humans; Structure-Activity Relationship; Polyphenols; Salivary alpha-Amylases; Pancreatic alpha-Amylases; Anthocyanins; Enzyme Inhibitors; alpha-Amylases; Saliva
PubMed: 38823880
DOI: 10.1016/j.foodres.2024.114504 -
International Journal of Nanomedicine 2023Vegetable waste has numerous essential values and can be used for various purposes. Unfortunately, it is often discarded worldwide due to a lack of awareness regarding...
INTRODUCTION
Vegetable waste has numerous essential values and can be used for various purposes. Unfortunately, it is often discarded worldwide due to a lack of awareness regarding its nutritional and practical significance. Even the nutrient-rich peels of fruits and vegetables are commonly wasted, despite their numerous useful applications. Utilizing vegetable waste to produce silver nanoparticles through green synthesis is an advantageous, economical, and environmentally friendly method for producing valuable products while addressing waste management concerns. The main emphasis of this study was to synthesize silver nanoparticles (AgNPs) by using vegetable waste from (potato) and (coriander).
METHODS
The stems of and peels of were used as extracts for the synthesis of AgNPs. The characterization of the synthesized AgNPs involved UV-spectroscopy, scanning electron microscopy (SEM), and X-ray diffraction (XRD). The phytochemical analysis was performed to analyze antimicrobial, cytotoxic, antidiabetic, antitumor, antioxidant, alpha-amylase, and protein inhibition activities.
RESULTS
The change in the color of the reaction mixture from yellowish green to brown following the addition of extracts to the silver nitrate solution confirmed nanoparticle synthesis. UV analysis has shown peaks in the range of 300-400nm. SEM confirmed the spherical and agglomerated morphology and size of 64nm for potato peel and 70nm for coriander stem. XRD confirmed the crystalline structure of silver nanoparticles. The phytochemical assays confirmed that silver nanoparticles had higher total phenolic and flavonoid contents. The biosynthesized silver nanoparticles showed promising antimicrobial, cytotoxic, antidiabetic, antitumor, and antioxidant properties and significant alpha-amylase and protein inhibition activities in comparison with the crude extracts.
CONCLUSION
The bioactivity of the plant suggests that it could be a suitable option for therapeutic purposes. This study demonstrates a potential method for sustainable nanoparticle synthesis and the therapeutic applications of AgNPs derived from vegetable waste. By utilizing the potential of vegetable waste, we can contribute to both environmental sustainability and the development of innovative, valuable products in fields such as medicine, agriculture, and materials science. These findings encourage further research on agricultural byproducts, promoting environmentally friendly and economically advantageous research and development efforts.
Topics: Antioxidants; Vegetables; Metal Nanoparticles; Spectroscopy, Fourier Transform Infrared; Silver; Anti-Infective Agents; Hypoglycemic Agents; X-Ray Diffraction; Phytochemicals; alpha-Amylases; Plant Extracts; Anti-Bacterial Agents
PubMed: 37965280
DOI: 10.2147/IJN.S432252 -
Nutrients Feb 2024Athletes often take sport supplements to reduce fatigue and immune disturbances during or after training. This study evaluated the acute effects of concurrent ingestion... (Randomized Controlled Trial)
Randomized Controlled Trial
Athletes often take sport supplements to reduce fatigue and immune disturbances during or after training. This study evaluated the acute effects of concurrent ingestion of alkaline water and L-glutamine on the salivary immunity and hormone responses of boxers after training. Twelve male boxing athletes were recruited in this study. During regular training, the participants were randomly divided into three groups and asked to consume 400 mL of alkaline water (Group A), 0.15 g/kg body weight of L-glutamine with 400 mL of water (Group G), and 0.15 g/kg of L-glutamine with 400 mL of alkaline water (Group A+G) at the same time each day for three consecutive weeks. Before and immediately after the training, saliva, heart rates, and the rate of perceived exertion were investigated. The activity of α-amylase and concentrations of lactoferrin, immunoglobulin A (IgA), testosterone, and cortisol in saliva were measured. The results showed that the ratio of α-amylase activity/total protein (TP) significantly increased after training in Group A+G but not in Group A or G, whereas the ratios of lactoferrin/TP and IgA/TP were unaffected in all three groups. The concentrations of salivary testosterone after training increased significantly in Group A+G but not in Group A or G, whereas the salivary cortisol concentrations were unaltered in all groups. In conclusion, concurrent ingestion of 400 mL of alkaline water and 0.15 g/kg of L-glutamine before training enhanced the salivary α-amylase activity and testosterone concentration of boxers, which would be beneficial for post-exercise recovery.
Topics: Humans; Male; Salivary alpha-Amylases; Glutamine; Testosterone; Boxing; Hydrocortisone; Lactoferrin; Immunoglobulin A; Athletes; Eating; Saliva
PubMed: 38337738
DOI: 10.3390/nu16030454 -
Psychoneuroendocrinology Dec 2023Elevated callous-unemotional (CU) traits (e.g., lack of empathy, deficient guilt/remorse, and shallow affect) are associated with increased antisociality and distinct...
Elevated callous-unemotional (CU) traits (e.g., lack of empathy, deficient guilt/remorse, and shallow affect) are associated with increased antisociality and distinct patterns of cognitive and emotional functioning. Previous investigations have suggested that deficits in physiological stress responses may underlie these associations, yet few studies simultaneously examine the multiple physiological systems responsible for mounting a stress response. To clarify how individuals with and without elevated CU traits respond to acute stress, the current study examined the association between CU traits and hormones released by three systems: cortisol from the hypothalamic-pituitary-adrenal (HPA) axis, alpha-amylase from the sympathetic nervous system (SNS), and testosterone from hypothalamic-pituitary-gonadal (HPG) axis. Specifically, we used fixed effect regression modeling to examine within-individual changes in each biomarker across the administration of a standardized laboratory stressor (Trier Social Stress Test) in a sample of 55 justice-involved young men (M= 22.84). Results indicated significant within-individual changes in cortisol, alpha-amylase, and testosterone following the stressor among those with low or average CU traits. However, those with high levels of CU exhibited no significant changes in their cortisol and testosterone levels. Furthermore, individuals with high CU traits exhibit an asymmetric stress response, such that alpha-amylase and testosterone levels were not associated with changes in cortisol levels. In sum, elevated CU traits were associated with blunted cortisol and testosterone reactivity and asymmetric response to stress. Additional work is needed to determine the behavioral and treatment implications of this distinct stress response.
Topics: Male; Humans; Conduct Disorder; Testosterone; Hydrocortisone; alpha-Amylases; Emotions; Stress, Psychological; Saliva
PubMed: 37776731
DOI: 10.1016/j.psyneuen.2023.106391