Antiglycation Activity Research Articles

Cannflavins A and B with Anti-Ferroptosis, Anti-Glycation, and Antioxidant Activities Protect Human Keratinocytes in a Cell Death Model with Erastin and Reactive Carbonyl Species.

Precursors of advanced glycation endproducts, namely, reactive carbonyl species (RCSs), are aging biomarkers that contribute to cell death. However, the impact of RCSs on ferroptosis-an iron-dependent form of cell death-in skin cells remains unknown. Herein, we constructed a cellular model (with human keratinocyte; HaCaT cells) to evaluate the cytotoxicity of the combinations of RCSs (including glyoxal; GO and methyglyoxal; MGO) and erastin (a ferroptosis inducer) using bioassays (measuring cellular lipid peroxidation and iron content) and proteomics with sequential window acquisition of all theoretical mass spectra. Additionally, a data-independent acquisition approach was used to characterize RCSs' and erastin's molecular network including genes, canonical pathways, and upstream regulators. Using this model, we evaluated the cytoprotective effects of two dietary flavonoids including cannflavins A and B against RCSs and erastin-induced cytotoxicity in HaCaT cells. Cannflavins A and B (at 0.625 to 20 µM) inhibited ferroptosis by restoring the cell viability (by 56.6-78.6% and 63.8-81.1%) and suppressing cellular lipid peroxidation (by 42.3-70.2% and 28.8-63.6%), respectively. They also alleviated GO + erastin- or MGO + erastin-induced cytotoxicity by 62.2-67.6% and 56.1-69.3%, and 35.6-54.5% and 33.8-62.0%, respectively. Mechanistic studies supported that the cytoprotective effects of cannflavins A and B are associated with their antioxidant activities including free radical scavenging capacity and an inhibitory effect on glycation. This is the first study showing that cannflavins A and B protect human keratinocytes from RCSs + erastin-induced cytotoxicity, which supports their potential applications as dietary interventions for aging-related skin conditions.

Effect of <i>Syzygium guineense</i> and <i>Borassus aethiopum</i> leaves on protein glycation and oxidative stress suppression

The quest for discovery of a new antiglycation and antioxidant drug still remains a major priority in medicine and related clinical sectors. Against this backdrop, the antioxidant and antiglycation activities of ethylacetate, chloroform, methanol and aqueous extracts of Syzygium guineense (SG) and Borassus aethiopum (BA) leaves including their phytochemical compositions were evaluated in an in vitro trial. DPPH free radical scavenging capacity, antiglycation activity and qualitative phytochemical screening in vitro assay were employed respectively. Our result revealed that triterpenes, cardiac glycosides, tannins and flavonoids were detected in the plants leaves extracts. The extracts demonstrated a significantly (p < 0.05) low antioxidant and antiglycation activities except the aqueous extract of BA leaves, which displayed a significantly (p < 0.05) high antiglycation ability. Overall, data from the current study showed that ethylacetate, chloroform, methanol and aqueous extracts of the plants leaves have potential effect towards lowering oxidative stress and protein glycation and thus should be exploited for further research in the area of drug discovery.

Innovative Wound Dressing Coated with Drug-Loaded Adipose Mesenchymal Stem Cells to Promote Wound Healing in Diabetes

Impaired wound healing is associated with hyperglycaemia in patients with diabetes. Hyperglycaemia induces protein glycation and the formation of Advanced Glycation End-Products (AGEs). The accumulation of AGEs in the body results in the structural and functional modification of tissue proteins. This study was conducted to evaluate compounds with antiglycation activities (S-Ally1 Cysteine (SAC), N-Acetylcysteine (NAC) and the mimic compound A). The extent of glycation in the presence and absence of several inhibitors was assessed via several methods including fluorescence, Sodium Dodecyl Sulphate-Polyacrylamide Gel Electrophoresis (SDS-PAGE)- silver stain, Western blotting, and Enzyme-Linked Immunosorbent Assays (ELISA). Additionally, this research aimed to evaluate and quantify the potential of Human Adipose Mesenchymal Stem Cells (hADMSCs) to uptake and release these drugs as potential therapeutics. To achieve this, hADMSCs were primed with a combination of SAC/NAC and mimic compound A and their concentrations were analysed using High-Performance Liquid Chromatography (HPLC). The SAC/NAC and mimic compound A prohibit the formation of AGEs while the Conditioned Medium (CM) from SAC/NACand compound A-loaded hADMSCs induced cell migration and tube formation in BAECs. hADMSCs provide a unique opportunity for the development of an innovative targeting and drug-delivery system which could effectively deliver therapeutics to specific regions of wounds or other damaged tissues. The data provided demonstrate the potential of hADMSCs as a drug delivery method with the potential to improve wound healing, and it may offer potential therapeutic targeting for the development of diabetic complications.

Phytochemical Profile, Antilipase, Hemoglobin Antiglycation, Antihyperglycemic, and Anti-Inflammatory Activities of Solanum elaeagnifolium Cav.

In the present investigation, the phenolic compounds of Solanum elaeagnifolium were identified, and the plant’s anti-lipase and anti-glycation effects on hemoglobin were discovered through in vitro experiments, as well as its short-term antihyperglycemic and anti-inflammatory effects. The chemical compound composition was detected using HPLC-DAD, the anti-lipase activity was tested in vitro using 4-nitrophenyl butyrate as a substrate, and the antiglycation activity of the plant extracts was also tested in vitro using a haemoglobin model. The antihyperglycemic effect was determined by inhibiting pancreatic α-amylase and α-glycosidase activity and performing an in vivo glucose tolerance test on normal rats, and the anti-inflammatory activity was determined by inducing paw inflammation with carrageenan. In both the SEFR (fruit) and SEFE (leaf) extracts, chromatographic analysis revealed the presence of quercetin 3-O-β-D-glucoside, rutin, and quercetin. SEFR inhibited the pancreatic lipase enzyme more effectively, with an IC50 of 0.106 ± 0.00 mg/mL. S. elaeagnifolium extracts demonstrated significant antiglycation activity, with 3.990 ± 0.23 mg/mL of SEFE and 3.997 ± 0.14 mg/mL of SEFR. When compared to positive and negative controls, plant extracts had very significant anti-diabetic and anti-inflammatory effects. The findings in this study and previous research on this plant encourage us to investigate other pharmacological activities of this plant besides its duiretic, cictrisant, and anti-ulcer activity.

Evaluation of Crocin Content and In Vitro Antioxidant and Anti-Glycation Activity of Different Saffron Extracts.

Crocin, a glycoside carotenoid that exhibits several health benefits, is mainly obtained from saffron (Crocus sativus L.), whose quality and content of phytochemicals can be strongly affected by environmental conditions. Therefore, in this work, the crocin content and in vitro antioxidant activity of saffron extracts obtained from three different varieties (Greek, Sicilian, and Iranian saffron) were assessed. Crocin content in saffron extracts was quantified via ultra-performance liquid chromatography coupled with mass spectrometry. The antioxidant activity of saffron extracts was evaluated using the oxygen radical absorbance capacity (ORAC) assay and nitric oxide (NO) radical scavenging test. The Maillard reaction was used to assess anti-glycation activity. Although the Sicilian and Iranian saffron extracts contained higher amounts of crocin (128 ± 6 ng/mL and 126 ± 4 ng/mL, respectively) compared to the Greek extracts (111 ± 2 ng/mL), ORAC values (50.9 ± 0.5) and % NO inhibition (35.2 ± 0.2) were higher for the Greek variety, which displayed a total phenolic content about two-fold greater than that of the other two extracts. Sicilian and Greek saffron had similar anti-glycation activities, while Iranian saffron was less effective. These results suggest that the antioxidant activity of saffron extracts could be ascribed to their naturally occurring complex mixture of phytochemicals, deserving further investigation as supplements to prevent pathological conditions induced by radical species.

Condensed tannins from the leave of Dimocarpus longan Lour. exhibit anti-tyrosinase, anti-melanogenesis, anti-browning, anti-α-glucosidase, and anti-glycation activities

Dimocarpus longan Lour. is a valuable industrial crop for its broad applications in food, traditional Chinese medicine, and other fields. In this paper, condensed tannins were isolated from the leave of D. longan Lour., and their structure, anti-tyrosinase, anti-melanogenesis, anti-browning, anti-α-glucosidase, and anti-glycation properties were methodically clarified. The joint application of matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS), electrospray ionization time-of-flight mass spectrometer (ESI+ TOF MS), and high-performance liquid chromatography-electrospray ionization-mass spectrometry (HPLC-ESI-MS) confirmed that the longan leave condensed tannins (LLCTs) were polymers of procyanidins (majority) and prodelphinidins. The polymers powerfully inhibit tyrosinase (TY) with a competitive mechanism. These compounds altered the microenvironment of the binding site through hydrophobic interaction and hydrogen bond, and caused conformational modification of the enzyme by changing the polypeptide framework and secondary structure, leading to a decrease in TY activity. Cell assays further suggested that LLCTs exhibited a strong inhibition against intracellular TY activity and melanin production, and caused apoptosis in B16F10 cells. Anti-browning studies demonstrated that LLCTs suppress the browning of fresh-cut apples. Furthermore, the LLCTs exhibited an impressive inhibition on both α-glucosidase and nonenzymatic glycation. Therefore, this study confirms the potential of LLCTs as new inhibitors of tyrosinase, melanogenesis, browning, α-glucosidase, and nonenzymatic glycation, which provided a theoretical basis for the potential utilization of these polymers in the cosmetics, pharmaceutical, and food industries.

Trapa Bispinosa Roxb. Inhibits the Insulin-Dependent AKT/WNK1 Pathway to Induce Autophagy in Mice with Type 2 Diabetes.

To elucidate the antiglycation activity of Trapa bispinosa Roxb. extract (TBE) and the related mechanism using a mouse model with type 2 diabetes. We prepared control mice by giving them a normal diet, leptin-deficient ob/ob mouse (ob/ob mice) with a normal diet (normal ob/ob mice), and ob/ob mice with a diet containing TBE (TBE ob/ob mice). The effect of TBE on diabetic retina was evaluated by immunohistochemical staining and quantitative real-time polymerase chain reaction (qPCR) analysis. In both groups with ob/ob mice, body weight and hyperglycemia levels increased over time. Immunohistochemical staining analysis revealed that glial fibrillary acidic protein (GFAP) and advanced glycation end products (AGEs) expression levels were higher in normal ob/ob mice than in control mice, and lower in the TBE ob/ob mice than in normal ob/ob mice. Light chain-3 (LC-3) expression levels reduced in normal ob/ob mice compared to the control mice, but increased in TBE ob/ob mice compared to normal ob/ob mice. In the qPCR analysis, LC-3 expression levels were significantly lower in normal ob/ob mice compared to control mice, and significantly higher in TBE ob/ob mice compared to normal ob/ob mice. Conversely, AKT1 and with-no-lysine kinases 1 (WNK1) expression levels were significantly higher in normal ob/ob mice compared to control mice, and significantly lower in TBE ob/ob mice than in normal ob/ob mice. In type 2 diabetes, it was suggested that TBE inhibits the insulin-dependent AKT/WNK1 pathway to induce autophagy, and thereby might promote anti-glycation and reduce retinal damage.

Preparation of Ribes nigrum L. polysaccharides-stabilized selenium nanoparticles for enhancement of the anti-glycation and α-glucosidase inhibitory activities

Seven kinds of selenium nanoparticles (RP-SeNPs) were prepared by using the polysaccharides extracted from Ribes nigrum L. (RP) as the stabilizer and dispersant. Among them, RP-SeNPs-1 (94.2 nm), RP-SeNPs-2 (101.2 nm) and RP-SeNPs-3 (107.6 nm) with relatively smaller mean particle size exhibited stronger α-glucosidase inhibitory activity than other RP-SeNPs (115.3–164.2 nm) and SeNPs (288.9 nm). Ultraviolet-visible spectrophotometry, Fourier transform-infrared, X-ray diffraction, energy dispersive X-ray and X-ray photoelectron spectroscopy analyses confirmed that SeNPs were ligated with RP to form nanocomposites and displayed amorphous form. Electron microscopy images revealed that RP-SeNPs-1 − RP-SeNPs-3 were regular shape spherical nanocomposites with much better dispersion than SeNPs. Compared with SeNPs, RP-SeNPs displayed relatively high thermal, storage, pH and salt ion stability. Moreover, RP-SeNPs-1–RP-SeNPs-3 showed significantly better anti-glycation and α-glucosidase inhibitory activity than SeNPs, especially RP-SeNPs-1 with the smallest particle size. Inhibitory kinetics analysis indicated that SeNPs and RP-SeNPs inhibited α-glucosidase with competitive type and reversible mechanism. In addition, the conformation of the α-glucosidase was changed after binding with the SeNPs and RP-SeNPs-1. Fluorescence quenching and isothermal titration calorimetry assays revealed that these two nanoparticles could interact with α-glucosidase to form non-fluorescent complexes through hydrogen bonding, and the formation was spontaneously driven by enthalpy.

Light-emitting diode-induced ellagic acid production in Drosera tokaiensis inhibits advanced glycation end-product formation

Drosera tokaiensis (DT) is an insectivorous plant that effectively inhibits advanced glycation end products (AGEs) generated from non-enzymatic reactions between reducing sugars and protein amino groups using phenolic compounds, including ellagic acid, myricitrin, and quercitrin. The accumulation of AGEs increases during the pathogenesis of non-communicable diseases, such as diabetes and nephropathy. Therefore, the extracts of Drosera species could have preventive effects against such diseases. The development of light-emitting diodes (LEDs) and their use in plant cultivation and tissue culture can enhance secondary metabolite production by controlling the wavelength of light in which plants are cultivated. We evaluated how LEDs affected the production of AGE-inhibitory compounds in extracts isolated from DT tissue cultures. DT was cultured for two months in different light wavelengths under unified photosynthetic photon flex density and the resulting extracts were used to examine changes in phenolic compound content and the inhibition of AGE formation. Cultivation in monochromatic light from LEDs had no significant effect on plant weight compared to conventional fluorescent cultivation, except for red LED light. Ellagic acid content increased regardless of LED coloration and the production and accumulation of myricitrin and quercitrin were inhibited. The extracts isolated from plantlets cultured under LEDs showed the same level of AGE inhibition as those cultured under fluorescent light. Therefore, for anti-glycation activity, DT can be grown stably and at a low cost using LED lights when compared to conventional culture methods.

Anti-aging and Antimicrobial Effects of the Stems and Roots of Sedum kamtschaticum in Cosmetic Production

Purpose: Sedum kamtschaticum Fisch. (SK), a plant native to Korea, was studied as a natural preservative and antiaging cosmetic ingredient.Methods: The stems and roots of SK were separated; extracted through reflux with 70% ethanol; and fractionated with n-hexane, chloroform, ethyl acetate, n-butyl alcohol, and water. The ethyl acetate fractions were evaluated for their antiaging effects, including antiglycation activity and elastase and collagenase inhibitory activity. Their antimicrobial activity on seven microorganisms was evaluated using the paper disk diffusion method and challenge test. In addition, the stability of lotion formulations and skin penetration were assessed using the Franz diffusion cell method.Results: The ethyl acetate fractions of SK with the best antioxidant effects exhibited better antiglycation and collagenase-inhibitory activity than the positive control as well as excellent antibacterial effects against Escherichia coli and Staphylococcus aureus. Emulsion formulations containing 0.05% and 0.1% SK stem extract exhibited synergistic preservative effects. The SK stem extract displayed the ability to penetrate into an artificial membrane and human cadaver skin.Conclusion: SK extracts can be used as antiaging and antimicrobial cosmetic materials.

Comparison of Policosanols via Incorporation into Reconstituted High-Density Lipoproteins: Cuban Policosanol (Raydel®) Exerts the Highest Antioxidant, Anti-Glycation, and Anti-Inflammatory Activity.

Reconstituted high-density lipoproteins (rHDL) containing each policosanol from Cuba (Raydel®), China (Shaanxi Pioneer), and the United States (Lesstanol®) were synthesized to compare the physiological properties of policosanol depending on sources and origin countries. After synthesis with apolipoproteinA-I (apoA-I) into rHDL, all policosanols bound well with phospholipid and apoA-I to form discoidal rHDL. An rHDL containing Cuban policosanol (rHDL-1) showed the largest rHDL particle size of around 83 ± 3 nm, while rHDL containing Chinese policosanol (rHDL-2) or American policosanol (rHDL-3) showed smaller particles around 63 ± 3 nm and 60 ± 2 nm in diameter, respectively. The rHDL-1 showed the strongest anti-glycation activity to protect the apoA-I degradation of HDL from fructose-mediated glycation: approximately 2.7-times higher ability to suppress glycation and 1.4-times higher protection ability of apoA-I than that of rHDL-2 and rHDL-3. The rHDL-1 showed the highest antioxidant ability to inhibit cupric ion-mediated LDL oxidation in electromobility and the quantification of oxidized species. A microinjection of each rHDL into a zebrafish embryo in the presence of carboxymethyllysine (CML) showed that rHDL-1 displayed the strongest anti-oxidant activity with the highest embryo survivability, whereas rHDL-2 and rHDL-3 showed much weaker protection ability, similar to rHDL alone (rHDL-0). An intraperitoneal injection of CML (250 μg) into adult zebrafish caused acute death and hyperinflammation with an elevation of infiltration of neutrophils and IL-6 production in the liver. On the other hand, a co-injection of rHDL-1 resulted in the highest survivability and the strongest anti-inflammatory ability to suppress IL-6 production with an improvement of the blood lipid profile, such as elevation of HDL-C and lowering of the total cholesterol, LDL-cholesterol, and triglyceride. In conclusion, Cuban policosanol exhibited the most desirable properties for the in vitro synthesis of rHDL with the stabilization of apoA-I, the largest particle size, anti-glycation against fructation, and antioxidant activities to prevent LDL oxidation. Cuban policosanol in rHDL also exhibited the strongest in vivo antioxidant and anti-inflammatory activities with the highest survivability in zebrafish embryos and adults via the prevention of hyperinflammation in the presence of CML.

In vitro Antiglycation Activity of Isorhamnetin on Bovine Serum Albumin with different sugars using Sodium Dodecyl Sulphate Polyacrylamide Gel Electrophoresis

Advanced glycation end products (AGEs) resulting from glycation of proteins, lipids and nucleic acids has several pathophysiological manifestations by altering the structure and functions of molecular proteins. Isorhamnetin is a flavonoid with anti-inflammatory, anti-oxidant, anti-obesity, anticancer, antidiabetic and anti-atherosclerosis activity. Based on the structure activity relationship and our insilico antiglycation study of isorhamnetin, we hypothised that isorhamnetin may have antiglycation activity by inhibiting protein glycation on sugar molecules due to its antioxidant and free radical scavenging activity. Hence our aim of the study was to determine the glycation level of bovine serum albumin (BSA) with varying sugar concentration of glucose, fructose and ribose on 14th and 21st day of incubation. Our second objective of the study was to determine the antiglycation activity of isorhamnetin on BSA using all the sugars at 14th and 21st day of incubation using SDS - PAGE. Our study showed that increase in concentration of glucose, fructose and ribose (0 – 50mM) showed a dose dependent decrease in migration of protein implying increased glycation of BSA. Isorhamnetin (100µM) exhibited antiglycation activity for fructose (30mM) at 14th day onwards and for glucose (30mM) was at 21st day onwards. But isorhamnetin did not exert antiglycation activity for ribose (30mM) on both 14th and 21st day of incubation. Our study establishes the antiglycation activity of isorhamnetin however further invivo studies are necessary to warrant this activity.

In vitro antioxidant, antiglycation, α-glucosidase and α-amylase inhibitory activities of extracts and solvent fractions of Elaeocarpus serratus L.

Plants are an essential source of unique pharmacologically active natural products beneficial to human and animal health. In this research, crude extracts and solvent fractions from the leaves, bark, stem, seeds and fruit pulp of Elaeocarpus serratus (Cylon olive) were assessed for their antioxidant potential, antiglycation and enzymatic inhibitory activity. Phytochemical contents were analyzed by the colorimetric method. Antioxidant activities were estimated by DPPH radical scavenging, superoxide anion radical and ferrous ion chelating assays. Antiglycation properties were determined through the bovine serum albumin-methylglyoxal (BSA-MG) test and enzyme inhibitory activities were tested in vitro on α-glucosidase and α-amylase. The ethyl acetate fraction of the leaves exhibited high phenolic content (71.63 ± 0.01 mg GAE/g DW). The n-butanol fraction of the bark had high flavonoid content (37.37 ± 0.07 mg QE/g DW). The n-butanol fraction of the bark also significantly inhibited both α-glucosidase and α-amylase with IC50 values of 2.32 ± 0.62, and 2.81 ± 0.37 μg/mL, respectively, compared with quercetin (43.27 ± 3.24 μg/mL) and acarbose (17.72 ± 2.35 μg/mL). These findings indicate that E. serratus can be a source of plant-based pharmaceuticals and natural products, which may be considered for the treatment of diabetes and the formulation of healthy food supplements. However, further studies are required on the isolation, identification and toxicity of components from E. serratus.

Optimization of aqueous extraction of antioxidants from Chrysanthemum (C. morifolium Ramat and C. indicum L.) flowers and evaluation of their protection from glycoxidation damage on human αA-crystallin

Chrysanthemum tea is commonly consumed by Chinese consumers mainly due to the Chrysanthemum flower being a potential source of antioxidants. The current study investigates the effects of extraction time and temperature on Chrysanthemum flower aqueous extract (CFAE) antioxidant capacity, including Trolox equivalent antioxidant capacity (TEAC), ferrous iron-chelating activity, and superoxide radical scavenging capacity (SRSC) using a two-factor, three-level factorial design of the response surface method (RSM). The TEAC and SRSC of CFAE are higher at higher temperatures and longer times up to a certain point, and the highest TEAC and SRSC are achieved at a 100 °C extraction temperature for 45 min. The fructose induced-αA-crystallin (Cry) glycation model system was used to evaluate the effects of the CFAE on anti-glycoxidation activities. The antioxidant ingredients obtained from CFAE significantly impede the production of advanced glycation end products from protein glycoxidation products (dityrosine, kynurenine, and N′-methylkynurenine) in the glycation process of αA-Cry and exhibit strong anti-glycating activity. The glycation inhibitory effects of CFAE are concentration-dependent. C. indicum L. exhibits greater potential for preventing cataracts compared to C. morifolium Ramat CFAE's antioxidant and anti-glycation properties suggest its potential application as a natural ingredient in the development of agents to combat glycation.

Glycation derived AuNPs bioconjugated novel herbal drug isoferulic acid: As a potential anti-glycation, anti-diabetic and antineoplastic agent

Based on the significance and impact of serum protein glycation and the possibility that AGEs play a role in diabetes-related complications and cancer, this study examined the anti-glycation, anti-cancer, and α-amylase inhibition activities of isoferulic acid (IFA) and its gold nanoparticle (IFA-AuNPs) bioconjugated formulations. In comparison to the control (glycated) samples, IFA and IFA-AuNPs were found to show a significant reduction in the KM moieties, carbonyl content, and HMF content that were produced during the glycation, demonstrating that the glycation reaction generated less superoxide radicals, had fewer intermediates, and did not cause as many structural perturbations to BSA. The IFA and IFA-AuNPs treated samples had a higher proportion of unreacted lysine and arginine deposits than the control (glycated) samples, suggesting that the inhibitors prevented the association of negatively charged arginine deposits with 2′-Deoxyribose. Purified IFA (IC50 = 4.3 mM) decreased α-amylase activity insignificantly compared to acarbose (IC50 = 0.118 mM). Therefore, IFA may not be suited for targeting α-amylase. However, IFA and its analogs have been reported to inhibit several malignancies, including leukemia, breast, colon, and lung cancer. Therefore, the cytotoxicity study was conducted using human keratinocytes (HaCat cells), and the IC50 values for IFA and IFA-AuNPs were determined to be 6062.4 µM and 151.6 µM, respectively. Their cytotoxic effects on human lung cancer epithelial cells (A549), however, were estimated to be 5593 µM and 117.5 µM. Our study confirmed that IFA-treated A549 cells at a greater concentration (5593 µM) caused less disruption of mitochondrial membrane potential (ΔΨm) and production of ROS burst than IFA-AuNPs at a significantly lower concentration (117,5 µM). When ΔΨm was disrupted, Cyt-c-mediated apoptosis was elicited, which then allowed IFA and AuNPs to work synergistically to degrade DNA. It was discovered that IFA-AuNPs target cancer cells through different pathways, with AuNPs potentiating the effect of IFA.

In Vitro Bioactivities of Commonly Consumed Cereal, Vegetable, and Legume Seeds as Related to Their Bioactive Components: An Untargeted Metabolomics Approach Using UHPLC-QTOF-MS2.

We conducted a comprehensive evaluation of the antioxidant, anti-obesity, anti-diabetic, and anti-glycation activities associated with the consumption of broccoli, red cabbage, alfalfa, and buckwheat seeds. Additionally, we explored the relationship between these biological activities and the profiles of amino acids, polyphenols, and organic acids identified in the seeds. Our findings demonstrated that red cabbage, broccoli, and buckwheat extracts exhibited significantly higher antioxidant potential compared to the alfalfa extract. Moreover, buckwheat displayed the most significant capacity for inhibiting alpha-glucosidase. Remarkably, broccoli and red cabbage demonstrated substantial anti-glycation and lipase inhibitory potentials. We identified the presence of amino acids, polyphenols, and organic acids in the extracts through untargeted metabolomics analysis. Correlation analysis revealed that pyroglutamic acid positively correlated with all the investigated functional properties. Most polyphenols made positive contributions to the functional properties, with the exception of ferulic acid, which displayed a negative correlation with all tested biological activities. Furthermore, gluconic acid and arabinonic acid among the organic acids identified displayed a positive correlation with all the functional properties. These results strongly support the anti-diabetic, anti-obesity, and anti-glycation potential of red cabbage, broccoli, and buckwheat seeds.

Antiglycation and antioxidant activity of herbal medicines used in the treatment of climacteric symptoms

ObjectivesThis work had the objective to evaluate the antiglycation and antioxidant potential of Cimicifuga racemosa L., Trifolium pratense L., Humulus lupulus L. and Morus nigra L., commonly used in traditional medicine for the treatment of climacteric symptoms. MethodsAntioxidant activity was evaluated by 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, ferric reducing antioxidant power, inhibition of lipid peroxidation thiobarbituric acid reactive substances (TBARS), nitric oxide (NO) radical scavenging and inhibition of oxidative haemolysis test. The evaluation of antiglycation activity was performed by the determination of relative electrophoretic mobility of bovine serum albumin (BSA) with ribose and BSA with methylglyoxa in the presence and absence of Cu2+ ion. Total polyphenol and flavonoid contents were determined by spectrophotometric methods. ResultsThe highest antioxidant activity for DPPH and ferric reducing antioxidant power test was detected in Humulus lupulus (83.56% and 46.95 µM TE/g dry extract, respectively). For the inhibition of lipid peroxidation, the lowest percentages of TBARS were found in M. nigra (4.82%) and H. lupulus (18.26%). C. racemosa presented the lowest nitrite formation (34.57 µmol/mL nitrite formed) in nitric oxide test. T. pratense presented the highest polyphenol (24.61 mg GAE/g dry extract) and flavonoid (22.79 mg RE/g dry extract) contents. For the oxidative haemolysis assay, the extracts showed concentration-dependent inhibitory capacity, while for the antiglycation activity all extracts showed antiglycation potential against glycation of BSA promoted by Ribose evaluated by the electrophoretic profile. ConclusionsIn view of the results obtained in this study, it was possible to verify that the dry extracts of herbal medicines used for climacteric symptoms present antioxidant and antiglycation activities, mainly due to the presence of phenols compounds in their composition.

Trapa bispinosa Roxb. Pericarp Extract Exerts 5α-Reductase Inhibitory Activity in Castrated Benign Prostatic Hyperplasia Model Mice.

Trapa bispinosa Roxb. pericarp extract (TBE) has a polyphenol-rich composition and exhibits potent antioxidant and anti-glycation activities in vitro. In the present study, we investigated the inhibitory effects of TBE on 5α-reductase in vitro using LNCaP cells and in vivo using a mouse model of castrated benign prostatic hyperplasia. TBE showed concentration-dependent inhibitory effects in the 5α-reductase (5αR) activity assay. In a reporter assay using AR-Luc/LNCaP cells, TBE inhibited the activity induced by testosterone, but not that induced by dihydrotestosterone. TBE also suppressed prostate cell proliferation, prostate-specific antigens, and transmembrane protease serine 2 expression in a castrated benign prostatic hyperplasia mouse model. In addition, ellagic acid, but not gallic acid, decreased 5αR and AR-Luc activities. Together, these results suggest a potential role for TBE in benign prostatic hyperplasia through inhibition of 5αR.

Antioxidant, Anti-Tyrosinase, Antiglycation and Safety of Longan Leaf Extract for Cosmeceutical Application

Abstract Many potential bioactive phytoconstituents in longan (Dimocarpus longan Lour.) leaf have been reported. Most chemical compounds belong to either phenolics or flavonoids, known as potent antioxidants. This research explores the multifunctional potential as a bioactive cosmetic ingredient used in skin care for adding value to longan leaves. The dried powder of longan leaves was extracted with 50%(v/v) ethanol in de-ionized water, then quantified for total phenolic and flavonoid contents. The hydroethanolic extract was investigated for various antioxidant methods including DPPH, nitric oxide (NO) scavenging and lipid peroxidation inhibition assays. The anti-tyrosinase activity was also evaluated for skin-whitening properties. Furthermore, Anti-aging activity in term of antiglycation was also conducted. The high number of polyphenols within the extract possessed a high antioxidant potential with IC50 0.023 ± 0.002, 0.478 ± 0.033 and 1.495 ± 0.153 mg/ml for DPPH scavenging, NO scavenging and lipid peroxidation inhibition, respectively. The extract could inhibit the tyrosinase enzyme with IC50 4.90 ± 0.50 and 6.60 ± 0.18 mg/ml for L-tyrosine and L-DOPA as substrates. The extract also exhibited a potent antiglycation activity with IC50 0.023 ± 0.003 mg/ml. Moreover, it showed no irritation effect on the chorioallantoic membranes (CAMs) within 5 min using the Hen’s Egg Test-Chorioallantoic Membranes (HET-CAMs). In conclusion, the polyphenolic-rich longan leaf extract displayed a good antioxidant, anti-tyrosinase and excellent antiglycation potential with safety that could constitute a promising multifunctional bioactive ingredient for skin care cosmeceutical products. Keywords: Longan leaf extract, Antioxidants, Anti-tyrosinase, Antiglycation, Irritation, HET-CAMs, Cosmeceutical

Prospects of silver nanoparticles (AgNPs) synthesized by Justicia secunda aqueous extracts on diabetes and its related complications

The wide range of secondary metabolites in medicinal plant extracts are used to treat and manage various diseases worldwide but more recently plant-mediated bio-nanotechnology is rapidly generating great research interest. Herein, the in-vitro study of the antidiabetic, anti-inflammatory, antiglycation, and antioxidant potentials of silver nanoparticles (AgNPs) synthesized by Justicia secunda aqueous extracts was evaluated. The synthesized AgNPs was characterized by UV-visible spectrophotometer, Fourier transform infrared spectroscopy (FT-IR) and Scanning electron microscopy (SEM). The antioxidant activity was evaluated via reducing power, 2,2-diphenyl-1-picrylhydrazyl (DPPH), total antioxidant capacity (TAC) and nitric oxide scavenging assays; antidiabetic activity was evaluated with α-glucosidase and α-amylase inhibitory assays; antiglycation activity was evaluated using fructosamine inhibitory assay, and anti-inflammatory activity was performed using trypsin inhibitory and albumin denaturation assays. The AgNPs from all the plant parts showed good biological potentials investigated compared to the plant extracts however, the synthesized AgNPs using the leaf aqueous extract (AgNPs-JsL) showed a better antioxidant, antidiabetic, antiglycation, and anti-inflammatory potentials with an essential quality absorption band in the ultraviolet region of 410 nm and average size distribution of 50.47nm. In conclusion, all the parts of J. secunda showed substantial antidiabetic, antioxidant, antiglycation and anti-inflammatory potentials with high yield of various bioactive metabolites, however, the AgNPs-JsL was more potent followed by the flower, stem and roots extracts, respectively.