Antiglycation Activity Research Articles

Cuban Policosanol (Raydel®) Exerts Higher Antioxidant and Anti-Glycation Activities than Chinese Policosanol (BOC Sciences) in Reconstituted High-Density Lipoproteins: In Vivo Anti-Inflammatory Activities in Zebrafish and Its Embryos.

The present study compares sugarcane-wax purified policosanols sourced from Cuba (Raydel®) and China (BOC Sciences) and utilized following the synthesis of reconstituted high-density lipoproteins (rHDL). The two policosanols exhibited distinctly different ingredient ratios of long-chain aliphatic alcohols, particularly 1-octacosanol (C28) and 1-tetratriacotanol (C34). After synthesizing rHDL with apolipoprotein A-I (apoA-I), the two policosanols bound well with phospholipid and apoA-I to form the discoidal rHDL. Notably, rHDL-1, containing Cuban policosanol, displayed the largest particle diameter at approximately 78 ± 3 nm. In contrast, both control rHDL (rHDL-0) and rHDL containing Chinese policosanol (rHDL-2) exhibited smaller particles, with diameters of approximately 58 ± 3 nm and 61 ± 2 nm, respectively. Furthermore, rHDL-1 demonstrated enhanced anti-glycation activity, safeguarding apoA-I from degradation within HDL, and displayed the antioxidant ability to inhibit LDL oxidation. A microinjection of each rHDL into zebrafish embryos in the presence of carboxymethyllysine (CML) revealed rHDL-1 to have the strongest antioxidant activity with the highest embryo survivability and normal developmental morphology. Dermal application to recover the wound revealed rHDL-1 to have the highest wound-healing activity (75%) and survivability (92%) in the cutaneous wound area in the presence of CML. In adult zebrafish, injecting CML (250 μg) caused acute death and hyperinflammation, marked by heightened neutrophil infiltration and interleukin (IL)-6 production in liver. However, co-administering rHDL-1 notably increased survival (85%) and exhibited strong anti-inflammatory properties, reducing IL-6 production while improving the blood lipid profile. However, a co-injection of rHDL-2 resulted in the lowest survivability (47%) with more hepatic inflammation. In conclusion, Cuban policosanol (Raydel®) has more desirable properties for the in vitro synthesis of rHDL with stronger anti-glycation and antioxidant activities than those of Chinese policosanol (BOC Sciences). Moreover, Raydel-policosanol-integrated rHDL demonstrates a noteworthy effect on accelerated wound healing and robust anti-inflammatory properties, leading to increased survivability in zebrafish embryos and adults by effectively suppressing CML-induced hyperinflammation.

Extraction of Sesquiterpene Lactones from Inula helenium Roots by High-Pressure Homogenization and Effects on Antimicrobial, Antioxidant, and Antiglycation Activities

The sesquiterpene lactones (SL) of Inula helenium (I. helenium) roots were extracted using high-pressure homogenization (HPH) and compared against those derived from maceration. The effect of process conditions on the extraction efficiency of bioactive compounds (alantolactone, isoalantolactone, total phenols, and flavonoids); the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical-scavenging activity, ferric-reducing antioxidant power (FRAP), and antimicrobial activity of the extract; and the inhibition of advanced glycated end product (AGE) formation were assessed. The HPH of 90 MPa for 4 passes demonstrated the highest alantolactone (38.1 ± 0.7 mg/g) and isoalantolactone yields (34.4 ± 0.2 mg/g), respectively, which were significantly higher than the rates obtained using maceration (20.0 ± 0.2 mg/g and 18.9 ± 0.7 mg/g). Under optimal extraction conditions of 90 MPa for 4 passes, inhibition of AGE formation in the extract reached a rate of 97.16 ± 1.86%, with the highest DPPH and FRAP of 231.63 ± 2.96 µg/mL and 949.43 ± 1.86 µmol TE/100 mL, respectively. HPH exhibited lethal activity against all tested bacteria and fungi strains (Escherichia coli, Staphylococcus aureus, Listeria monocytogenes, Aspergillus niger, Fusarium oxysporum, and Penicillum expansum) at a concentration of 15 µL. SEM results proved that HPH severely damaged the cell structures of roots, increased solvent permeability, and improved the extraction rate of bioactive compounds. Additionally, this study also demonstrated that HPH yields high recovery with a specific energy consumption of 0.22 kWh/kg, which is close to the recommended minimum energy demand for an extraction procedure within industrial production processes. Therefore, these findings showed that HPH can be used as an efficient extraction technique for the production of SL in related industries.

Metabolomic Comparison of Guava (Psidium guajava L.) Leaf Extracts Fermented by Limosilactobacillus fermentum and Lactiplantibacillus plantarum and Their Antioxidant and Antiglycation Activities.

Probiotic fermentation of plant-based materials can lead to the generation of various bioactive substances via bacterial metabolites and the biotransformation of phenolic compounds. We compared the metabolic differences between fermentation by Limosilactobacillus fermentum KCTC15072BP (LFG) and fermentation by Lactiplantibacillus plantarum KGMB00831 (LPG) in guava leaf extract (0%, 0.5%, and 2% (w/v))-supplemented medium via non-targeted metabolite profiling. By performing multivariate statistical analysis and comparing the different guava leaf extract groups, 21 guava-derived and 30 bacterial metabolites were identified. The contents of guava-derived glucogallin, gallic acid, and sugar alcohols were significantly higher in LFG than they were in LPG. Similarly, significantly higher contents of guava-derived pyrogallol, vanillic acid, naringenin, phloretin, and aromatic amino acid catabolites were obtained with LPG than with LFG. LFG led to significantly higher antioxidant activities than LPG, while LPG led to significantly higher antiglycation activity than LFG. Interestingly, the fermentation-induced increase in the guava-leaf-extract-supplemented group was significantly higher than that in the control group. Thus, the increased bioactivity induced by guava fermentation with the Lactobacillaceae strain may be influenced by the synergistic effects between microbial metabolites and plant-derived compounds. Overall, examining the metabolic changes in plant-based food fermentation by differentiating the origin of metabolites provides a better understanding of food fermentation.

Antioxidant, Cytotoxic, Anti-Glycation, and Anti-Tyrosinase Compounds from the Leaves of Uvaria Siamensis.

A new oxidized heptene, 7-benzoyloxy-4-hydroxy-1-ethoxy-2E,4Z-heptadiene-1,6-dione, namely siamheptene A (1), together with eight known compounds (2-9), were isolated from the leaves of Uvaria siamensis. Their structures were elucidated by detailed analysis of spectroscopic (IR, 1D and 2D NMR) and mass spectrometric data. Compound 9 is reported for the first time from Uvaria genus. Siamheptene A was evaluated for cytotoxicity against HeLa (cervical cancer cells), A549 (lung cancer cells), and Vero cells using the MTT assay and screened for antibacterial activities. In addition, the isolated compounds (1-7, and 9) were investigated for their antioxidant (DPPH, FRAP and ABTS+ assays), anti-glycation, and anti-tyrosinase properties. Based on our results, compound 1 had mild cytotoxicity against Hela and A549 cancer cell lines, with IC50 ranging from 31.09 to 31.67 μg/mL. Compound 1 also showed antioxidant activities in all tasted assays. However, it showed no detectable activity (>128 μg/mL) against various bacterial strains, and it has no inhibitory effects on tyrosinase enzymes. Among of all tested compounds, chrysin (5), showcased highest anti-glycation and anti-tyrosinase activities. This comprehensive analysis provides highlighting the potential of 1 as a lead compound for further structural modification and development of cytotoxic or antioxidant agents.

A glutathione-independent DJ-1/Pfp1 domain containing glyoxalase III, OsDJ-1C, functions in abiotic stress adaptation in rice.

Overexpression of OsDJ-1C in rice improves root architecture, photosynthesis, yield and abiotic stress tolerance through modulating methylglyoxal levels, antioxidant defense, and redox homeostasis. Exposure to abiotic stresses leads to elevated methylglyoxal (MG) levels in plants, impacting seed germination and root growth. In response, the activation of NADPH-dependent aldo-keto reductase and glutathione (GSH)-dependent glyoxalase enzymes helps to regulate MG levels and reduce its toxic effects. However, detoxification may not be carried out effectively due to the limitation of GSH and NADPH in plants under stress. Recently, a novel enzyme called glyoxalase III (GLY III) has been discovered which can detoxify MG in a single step without needing GSH. To understand the physiological importance of this pathway in rice, we overexpressed the gene encoding GLYIII enzyme (OsDJ-1C) in rice. It was observed that OsDJ-1C overexpression in rice regulated MG levels under stress conditions thus, linked well with plants' abiotic stress tolerance potential. The OsDJ-1C overexpression lines displayed better root architecture, improved photosynthesis, and reduced yield penalty compared to the WT plants under salinity, and drought stress conditions. These plants demonstrated an improved GSH/GSSG ratio, reduced level of reactive oxygen species, increased antioxidant capacity, and higher anti-glycation activity thereby indicating that the GLYIII mediated MG detoxification plays a significant role in plants' ability to reduce the impact of abiotic stress. Furthermore, these findings imply the potential of OsDJ-1C in crop improvement programs.

Biotransformation of bitter gourd (Momordica charantia) by Lactobacillus plantarum and its bioactivities

Bitter gourd is renowned for its various bioactivities, including antioxidant, antiglycation, and antiplatelet aggregation. However, the bioactivity and bioavailability of plant extracts could be low. Biotransformation through Lactobacillus plantarum fermentation is capable of enhancing these beneficial properties. Therefore, the present work aimed to investigate the physical and pH profiles, total phytochemical contents, bioactive contents, and bioactivities of the juices of unfermented bitter gourd (UBG) and fermented bitter gourd at 48 (FBG-48) and 96 (FBG-96) h. Fermentation gradually altered the physical and pH profile of bitter gourd, while non-significant decrease was seen in the total flavonoid content (p > 0.05). The highest total phenolic content was observed in FBG-48, followed by UBG and FBG-96. UBG exhibited the highest total triterpenoid content, followed by FBG-48 and FBG-96. Interestingly, fermentation increased the antioxidant, antiglycation, and anti-aggregation activities of bitter gourd. FBG-48 demonstrated the highest antioxidant and antiglycation activities, with 10.77 and 8.68% higher activity, respectively, compared to UBG and FBG-96. Meanwhile, FBG-96 exhibited the highest antiglycation activity, with 60% increase. These could have been attributed to the biotransformation of tannic acid into syringic acid, and momordicoside Q into kuguacin P, along with the potential release of p-coumaric acid and caffeic acid from the cell walls. These findings demonstrated bitter gourd’s promising role in type-II diabetes complication treatment, particularly through its protein aggregation inhibition activity, and that fermentation could increase its bioactivities.

Comprehensive assessment of the extraction of Phyllanthus emblica L. based on the G1-Entropy Method and Response Surface Methodology

In this study, the G1-Entropy method was employed together with a response surface methodology (RSM) approach to establish a multi-index-based system for evaluating and optimizing the extraction of bioactive compounds from Phyllanthus emblica L. Seven chemical classes' contents were evaluated, including TPC (total phenolic content), TC (tannin content), DEY (dry extract yield), GA (gallic acid), CO (corilagin), CA (chebulagic acid), and EA (ellagic acid). The resultant extracts were also assessed for their antioxidant activity, as measured based on their DPPH radical, ABTS+, and hydroxyl radical scavenging activity levels and their capacity to reduce iron ions. The inhibition of fluorescent AGEs generation was also assessed in BSA-Fru and MGO-BSA model assays to gauge the anti-glycation activity of these extracts. In total, a comprehensive score was derived based on 13 indices and corresponding weight values, with these scores then being used to determine the extraction conditions that yielded the best outcome. Through this strategy, the ideal extraction processing parameters were found to include an ethanol concentration of 56%, a liquid-solid ratio of 8 mL/g, and an extraction duration of 100 min. Using these optimized conditions yielded a predicted comprehensive score (Y) of 94.91, while the response value based on three independent variables from the validation experiments performed using these conditions was 92.03. These results highlight the promise of leveraging Phyllanthus emblica as a resource for use in the cosmetic, food, biochemical, and pharmaceutical industries.

Protective effect of Inonotus obliquus polysaccharide on MGO-induced nonenzymatic glycation fibroblasts

BackgroundThe nonenzymatic glycation of fibroblasts causes functional downregulation and behavioral disorders in the skin. MethodsTo investigate the effect of Inonotus obliquus on the nonenzymatic glycation of skin, we examined the inhibition of advanced glycation end products (AGEs) using four extraction methods: n-butanol, ethyl acetate, n-hexane and aqueous alcohol precipitation. The physical properties and chemical structure of the most effective, purified, crude I. obliquus polysaccharide (IOP) were examined. The effects of IOP on carboxymethyl lysine (CML) accumulation, inflammatory factor release, reactive oxygen species (ROS) production, key extracellular matrix (ECM) protein (MMP 1, 2 and 9; FN-1, LM-5 and COL-1) mRNA expression, and cell survival, migration and adhesion were also examined via cellular assays. ResultsIOP is a polysaccharide with a molecular weight (Mw) of 2.396 × 104 (±6.626%) that is composed mainly of glucose, galactose, xylose, mannose and arabinose (29.094:21.705:14.857:9.375:7.709). In addition, a cellular antiglycation assay showed that IOP, which can promote ECM formation by inhibiting the accumulation of CML, inhibiting the release of inflammatory factors (IL-1β, IL-6, and TNF-α), inhibiting the production of reactive oxygen species (ROS), inhibiting the expression of matrix metalloproteinases (MMP-1\\-2\\-9), promoting the synthesis of ECMs (COL1, FN1, and LM5), and improving cellular dysfunction, had strong antiglycation activity at concentrations in the range of 6–24 μg/mL. ConclusionIOP effectively reduced the levels of inflammatory factors and reactive oxygen species produced by AGEs, further preventing the impairment of cell behavior (decreased migration and reduced cell adhesion) and preventing the downregulation of the expression of key extracellular matrix proteins induced by AGEs. The results indicate the potential application of IOP as an AGE inhibitor in skin care.

Eco-Friendly and Efficient Extraction of Polysaccharides from Acanthopanax senticosus by Ultrasound-Assisted Deep Eutectic Solvent.

A green extraction method was developed using deep eutectic solvent extraction for the polysaccharide from Acanthopanax senticosus (A. senticosus). Among the eight types of DES prepared, the DES with a ratio of 1:4 L-malic acid to L-proline was found to be a suitable extraction solvent based on the extraction efficiency. The extraction parameters were optimized by Plackett-Burman and response surface methodology (RSM). The best extraction conditions were found for L-malic acid. Under the conditions of an L-malic acid/L-proline ratio of 1:4, ultrasonic power of 240 W, material-liquid ratio of 31.068 g/mL, water content of 32.364%, extraction time of 129.119 min, and extraction temperature of 60 °C, the extraction rate of A. senticosus polysaccharides was 35.452 ± 0.388 mg-g-1. This rate was higher than that of polysaccharides obtained by hot water extraction (13.652 ± 0.09 mg-g-1). The experimental results were best fitted by the quasi-secondary kinetic model when compared to two other kinetic models. Electron microscopic observations showed that DESs were more destructive to plant cells. The polysaccharide extracted from DESs had more monosaccharide components, a lower molecular weight, a higher antioxidant capacity, and superior anti-glycation activity compared to polysaccharides extracted from water (ASPS-PW). This study demonstrates the effectiveness of DESs in obtaining polysaccharides from A. senticosus.

Pistachio green hull and pomegranate peel extracts as two natural antiglycation agents.

Advanced glycation end products (AGEs) are formed in the final step of the nonenzymatic Maillard reaction, which can contribute to various health problems such as diabetes mellitus, renal failure, and chronic inflammation. Bioactive compounds with antiglycation properties have the potential to inhibit AGE-related diseases. This study investigated the antiglycation potential of pistachio green hull (PGH) and pomegranate peel (PP) extracts, which are polyphenol-rich agro-residues, against fluorescent AGE formation and compared the results with pyridoxine (vitamin B6), metformin, and EDTA (as usual chemical antiglycation agents). The results showed that PGH and PP effectively inhibited the formation of AGEs in bovine serum albumin-glucose (BSA-Glu) and BSA-fructose (BSA-Fru) with antiglycation activities ranging from 92% to 97%. PP extract (with an IC50 of 94 mg ml-1) had a greater antiglycation ability than PGH extract (with an IC50 of 142 mg ml-1). Also, results indicated that the antiglycation activities of the extracts were comparable to that of pyridoxine, and higher than metformin and EDTA. These findings suggest that the two studied extracts can be used for sustainable production of high-added-value food products with a positive effect on consumers' health.

Green and efficient approach to extract bioactive flavonoids with antioxidant, antibacterial, antiglycation, and enzyme inhibitory activities from navel orange peel

Numerous previous studies have reported the extraction of flavonoids from orange peels, but a green and efficient approach suitable for the large-scale industrial production of flavonoids with versatile and excellent biological activities is still lacking. To tackle this issue, two easily accessible extraction methods, namely heat reflux (HR) and ultrasonication (US), coupled with four solvents (95% ethanol, 70% aqueous ethanol solution, methanol, and ethyl acetate), were used in the present study to extract flavonoids from navel orange peel, followed by chemical profile and biological activity (antioxidant, antibacterial, antiglycation, and enzyme inhibition) evaluation of all extracts obtained. The highest total phenolic content (TPC, 336.56 μmol GAE/g), total flavonoid content (TFC, 1194.31 μmol QE/g), flavonoid glycosides content (FGs, 461.82 mg/g), and the best antioxidant (IC50 = 21.35 mg/L for ABTS assay) and α-glucosidase inhibition (IC50 = 49.38 mg/L) activities, were found in the extract obtained by HR using ethyl acetate (EtOAc HR). However, the extract obtained by US with ethyl acetate (EtOAc US) contained the highest content of polymethoxyflavones (PMFs, 152.07 mg/g), and showed the most potent antiglycation (IC50 = 71.26 mg/L), antibacterial (MIC = 0.078 mg/mL against MRSA), and acetylcholinesterase inhibition (AChE, IC50 = 179.19 mg/L) activities compared to the other extracts. Furthermore, Pearson's correlation analysis was performed. This study provides simple and cost-effective methods for the preparation of orange peel extracts rich in flavonoids and versatile in biological activities, which will greatly contribute to the valorization of orange peel in food, pharmaceutical, and cosmetic industries.

Potent bioactive metabolites from Olea ferruginea

Seven known (1-7) and one new compound (8) were isolated and identified from the stem of Olea ferruginea. The species has been recognised as a new source for six of the known metabolites (1, 3, 4, 5, 6, and 7). Based on detailed spectroscopic analyses, these compounds were identified as scopoletin (1), 8-ketosetosterol (2), (+)-cycloolivil (3), (+)-africanal (4), isovanilic acid (5), hydroxytyrosol acetate (6), vanillic acid (7), and cycloolivil A (8). The crude extracts and purified compounds were analysed for their Leishmanicidal, anti-glycation, anti-cancer, and anti-inflammatory activities. n-Hexane fraction was found to be the most active (among all the fractions), against Leishmania parasites, exhibiting 97.85% inhibition at 15 μg/mL. However, none of the extracts showed any significant anti-glycation or anti-cancer potential, all the fractions, except the aqueous layer, displayed moderate to low anti-inflammatory activity. Compound 1 was found to have strong anti-inflammatory activity, exhibiting 96.7% stimulation at 25 μg/mL.

Molecular Docking Studies of Thiazolidinediones on Receptor for Advanced Glycation End Products (RAGE)

Background: Advanced glycation end products (AGE), are abnormal glycation of molecular proteins and nucleic acid, and its interaction with receptors for advanced glycation end products (RAGE) culminates in metabolic, neurodegenerative, and lifestyle disorders. Thiazolidinediones are insulin sensitizers with anti-glycation activity and are currently used clinically as anti-diabetic drugs. Research rationale: Studies show that thiazolidinediones also exhibit antioxidant and antiglycation activity; hence we proposed that this anti-glycation activity of thiazolidinedione may be due to its anti-RAGE action, thus preventing further RAGE-AGE interaction. Purpose of the study: Aim of the current study is to assess In-silico anti-RAGE activity of nine thiazolidinediones namely pioglitazone, rosiglitazone, ciglitazone, darglitazone, englitazone, netoglitazone, rivoglitazone, troglitazone and balaglitazone with RAGE. Materials and Methods: Nine thiazolidinediones namely, pioglitazone, rosiglitazone, ciglitazone, darglitazone, englitazone, netoglitazone, rivoglitazone, troglitazone and balaglitazone were downloaded from PubChem database. RAGE protein was downloaded from the PDB database. The nine thiazolidinediones were docked with RAGE protein using Auto Dock software and interaction parameters were studied. Result: All nine thiazolidinediones showed acceptable binding energy below (-8Kcal/mol) with 1-5 hydrogen bonds. Rosiglitazone exhibits the highest binding energy (-8.24Kcal/mol) with 2 hydrogen bonds for RAGE. Troglitazone exhibits the lowest binding energy (-9.95Kcal/mol) with 3 hydrogen bonds for RAGE. Conclusion: Thus our Insilco docking studies of thiazolidinedione derivatives with RAGE conclude that these nine thiazolidinedione derivatives exhibit anti-glycation activity by direct interaction with receptors of RAGE. Thus, this work warrants future preclinical studies to claim its RAGE receptor modulation activity.

Antioxidant and anti-glycation activity of eight Moroccan honeys from different botanical origins

Eight monofloral honey samples from different botanical and geographical origins in the central and eastern parts of Morocco were examined for their phenolic composition, capacity to scavenge free radicals, and ability to inhibit advanced glycation end–products. According to the melissopalynological analysis, the examined honey samples were considered to be natural honeys, and were classified as monofloral with very frequent pollen grains characteristic of each types of the selected Moroccan honey samples: Zantaz (Bupleurum sp.), fennel, thistle, eucalyptus, spurge, thyme, jujube, and carob. Our results showed that the average moisture content varied from 16.3 ± 0.1% to 19.9 ± 0.1%, and the mean color intensity ranged from 30.94 ± 7.42 to 166.9 ± 6.43 mm Pfund. The highest total phenolic content recorded was 163.83 ± 1.84 mg of gallic acid equivalent per kg, while the highest flavonoid content was 84.44 ± 1.20 mg of catechin equivalent per kg. Zantaz honey exhibited potent antioxidant capacity, as demonstrated by ABTS, DPPH, β-carotene bleaching, FRAP, and ORAC assays. The most significant results were obtained for the ORAC test, with the highest ORAC value of 4.65 mM Trolox equivalent per gram was recorded for Zantaz honey extract. HPLC–DAD analysis revealed different polyphenolic profiles, which can be attributed to differences in floral origin. Furthermore, our study revealed that the extracts of thistle honey, fennel honey, and Zantaz honey were the most effective glycation inhibitors, with the highest inhibition percentage of 96% obtained for the thistle honey extract.

Quantification of Rutin, an Anti-glycating Drug, in Selected Euphorbia Species by Florescence Spectroscopy and Partial Least Squares Regression Analysis

Background: Rutin is a natural flavonol that showed excellent antiglycation activity with an IC50 value of 294.5 ± 1.5 μM. In the current study, three selected plant species of Euphorbia, i.e., Euphorbia helioscopia, Euphorbia larica, and Euphorbia wallichii, were analyzed for the quantification of rutin. Methods: The quantification was done through a newly developed method of Emission spectroscopy coupled with Partial Least Square Regression (PLSR) and UV-visible spectroscopy as a parallel cross-validation method. Results: The spectroscopic results indicated the highest rutin concentration in the roots of E. helioscopia (11.25 mg/100 g) followed by roots of E. wallichii (9.93 mg/100 g), leaves of E. helioscopia and the whole plant of E. larica (9.41 mg/100 g). The leaves of E. wallichii (8.66 mg/100 g) were found to contain the lowest concentration of rutin among all the tested samples. Conclusion: The present method is one of the simple, robust, and non-destructive methods to carry out the quantitative estimation of rutin in plants.

Synergistic Anti-Inflammatory Activity of Apolipoprotein A-I and CIGB-258 in Reconstituted High-Density Lipoproteins (rHDL) against Acute Toxicity of Carboxymethyllysine in Zebrafish and Its Embryo.

CIGB-258 is a 3 kDa altered peptide ligand from heat shock protein (HSP) 60 that exhibits anti-inflammatory activity against the acute toxicity of carboxymethyllysine (CML) with antioxidant and anti-glycation activities via protection of high-density lipoprotein (HDL) and apolipoprotein A-I (apoA-I). It is necessary to test a synergistic interaction between apoA-I and CIGB-258 in reconstituted high-density lipoproteins (rHDL). Several rHDLs were synthesized containing palmitoyloleoyl phosphatidylcholine (POPC), cholesterol, apoA-I, and CIGB-258 at molar ratios of 95:5:1:0, 95:5:1:0.1, 95:5:1:0.5, and 95:5:1:1 for rHDL-(1:0), rHDL-(1:0.1), rHDL-(1:0.5), and rHDL-(1:1), respectively. As the CIGB-258 content in rHDL was increased, the particle size of rHDL was 1.4-times higher than rHDL-(1:0) to rHDL-(1:1), from 60 nm to 83 nm, respectively. As the CIGB-258 content was increased, the rHDL showed the most resistance to isothermal denaturation by a urea treatment, and rHDL-(1:1) exhibited the highest structural stability and the strongest antioxidant ability against LDL oxidation. Co-treatment of rHDL-(1:0), rHDL-(1:0.5), and rHDL-(1:1) resulted in up to 10%, 24%, and 34% inhibition of HDL glycation, inhibition of HDL glycation, which was caused by the CML, with protection of apoA-I. Microinjection of each rHDL into zebrafish embryos in the presence of CML showed that a higher CIGB-258 content in rHDL was associated with higher survivability with the least inflammation and apoptosis. Furthermore, an intraperitoneal injection of rHDL and CML showed that a higher CIGB-258 content in rHDL was also associated with higher survivability of zebrafish and faster recovery of swimming ability. The rHDL-(1:1) group showed the lowest triglyceride, AST, and ALT serum levels with the least production of interleukin-6, oxidized product, and neutrophil infiltration in hepatic tissue. In conclusion, CIGB-258 could bind well to phospholipids and cholesterol to stabilize apoA-I in the rHDL structure against denaturation stress and larger particle sizes. The rHDL containing CIGB-258 enhanced the in vitro antioxidant ability against LDL oxidation, the anti-glycation activity to protect HDL, and the in vivo anti-inflammatory activity against CML toxicity in zebrafish adults and embryos. Overall, incorporating apoA-I and CIGB-258 in rHDL resulted in a synergistic interaction to enhance the structural and functional correlations in a dose-dependent manner of CIGB-258.

Phytochemical composition of aerial parts and roots of Pfaffia glomerata (Spreng.) Pedersen and anticholinesterase, antioxidant, and antiglycation activities.

The Pfaffia glomerata, a plant popularly called Brazilian ginseng, is widely used in Brazil for the treatment of various pathologies, including those associated with the Central Nervous System. 20-hydroxyecdysone (20E), a phytosteroid present in this plant, can promote adaptogenic effects in the organism, providing greater body resistance to stressors. This study aimed to evaluate the phytochemical composition and the anticholinesterase, antioxidant, and antiglycation effects of extracts and fractions of aerial parts and roots of P. glomerata, also analyzing their possible cytotoxic effects. The fractions were obtained by partitioning methanol extracts from the aerial part and roots of P. glomerata with hexane, dichloromethane, ethyl acetate, n-butanol, and water. The samples were initially tested in anticholinesterase, antioxidant, and antiglycation assays, and the most promising samples were submitted for cytotoxicity and chromatographic analyses. Mass spectrometry and chromatography methods revealed that 20E was the main compound in the dichloromethane fractions, there being 35% more 20E in the aerial part (APD) than in the roots (RD). Added to the higher concentration of 20E, the APD fraction also presented more promising results than the RD fraction in anticholinesterase and antioxidant analyses, indicating that their effects may be related to the concentration of 20E. These same fractions showed no hemolytic effects but were cytotoxic in high concentrations. These new findings contribute to scientific information about P. glomerata and open more perspectives for the understanding of its therapeutic properties, allowing the association of biological activity with the presence of 20E.

NMR and multivariate methods: Identification of chemical markers in extracts of pedra-ume-caá and their antiglycation, antioxidant, and enzymatic inhibition activities.

In Brazil, the plant group popularly known as "pedra-ume-caá" is used in folk medicine for the treatment of diabetes, and its raw material is commonly sold. The aim of the study was to apply a method for chemical identification of extracts of dry pedra-ume-caá leaves using HPLC-high-resolution mass spectrometry (HRMS) and NMR and develop a multivariate model with NMR data to authenticate commercial samples. In addition, to evaluate the biological activities of the extracts. Dry extracts of Myrcia multiflora, Myrcia amazonica, Myrcia guianensis, Myrcia sylvatica, Eugenia punicifolia leaves, and 15 commercial samples (sold in Manaus and Belém, Brazil) were prepared by infusion. All the extracts were analysed using HPLC-high-resolution mass spectrometry (HRMS), NMR, principal component analysis (PCA), and hierarchical cluster analysis (HCA). The antidiabetic effect of extracts was evaluated according to enzymatic inhibition. Their content of total phenols, cell viability, and antioxidant and antiglycation activities were also determined. HPLC-HRMS and NMR analysis of these extracts permitted the identification of 17 compounds. 1H NMR data combined with multivariate analyses allowed us to conclude that catechin, myricitrin, quercitrin, and gallic and quinic acids are the main chemical markers of pedra-ume-caá species. These markers were identified in 15 commercial samples of pedra-ume-caá. Additionally, only the extracts of M. multiflora and E. punicifolia inhibited α-glucosidase. All the extracts inhibited the formation of advanced glycation end products (AGEs) and showed free-radical-scavenging activity. These extracts did not present cytotoxicity. This study revealed the chemical markers of matrices, and it was possible to differentiate the materials marketed as pedra-ume-caá. Moreover, this study corroborates the potential of these species for treating diabetes.

Antioxidant, Anti-Diabetic and Anti-Inflammatory Activities of Passifloara foetida grown in Sri Lanka

Passiflora foetida (Padagedi) is identified as an underutilized fruit in Sri Lanka, used in traditional medicine for several diseases. The objective of this study was to determine the antioxidant, anti-diabetic, and anti-inflammatory properties of the leaves and fruits of P. foetida. Methanol (100 %) was used to prepare the plant extracts. The antioxidant activity was determined using total phenolic content (TPC), total flavonoid content (TFC), total alkaloid content (TAC), 2,2-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) radical scavenging, ferric reducing antioxidant power (FRAP), and oxygen radical absorption capacity (ORAC) assays. The anti-diabetic effects of plant extracts were determined by using anti-glycation and anti-amylase inhibitory assays. Cell viability was analyzed by the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl-2H-tetrazolium bromide (MTT) assay. Based on the findings, the leaf extract of P. foetida showed a higher TPC (21.46±1.56 mg GAE/g of extract), TFC (4.25±0.23 mg QE/g of extract), TAC (4.37±6.50 mg/g of extract), DPPH (10.91±1.29 mg TE/g of extract), ABTS+ (105.80±18.62 mg TE/g of extract), FRAP (11.85±1.45 mg TE/g of extract), and ORAC (46.23±3.58 mg TE/g of extract) compared to its fruit extract. The anti-amylase and anti-glycation activities were high in the leaf extract of P. foetida (30.7% and 77.65 % respectively). The fruit extract of P. foetida had the highest cell viability and nitric oxide (NO) production-inhibition in RAW macrophage (264.7 cells) compared to the fruit extract. It can be concluded that P. foetida has good therapeutic properties, and could be a potential source for pharmaceuticals and nutraceuticals industries.

Myanmar traditional medicine formulations and their antioxidant, antiglycation and alpha-glucosidase inhibitory activities: Potentials for antidiabetes complications

Myanmar traditional medicine formulations and their antioxidant, antiglycation and alpha-glucosidase inhibitory activities: Potentials for antidiabetes complications