RESUMEN

Background: Hypertension is a global public health concern. A synbiotic preparation containing Bifidobacterium lactis and Lactobacillus acidophilus has been used as adjunct therapy for hypertension. We sought to elucidate the antihypertensive activity of this preparation and explore the underlying mechanisms. Methods and results: Blood pressure in rats was measured using the tail-cuff method. Colonization of the gastrointestinal tract by the two probiotics was determined by real-time quantitative polymerase chain reaction (qPCR). Mechanistic studies were performed by proteomic analyses based on liquid chromatography-mass spectrometry and STRING database and metabolomic analyses using the UHPLC-Q-TOF/MS platform and peroxisome proliferator-activated receptor (PPAR)ß/γ antagonists. Although biochemical analysis of blood samples showed that the synbiotic preparation did not alter the levels of angiotensin II, aldosterone, or cortisol, it significantly lowered the systolic blood pressure in the treatment group. Moreover, the synbiotic preparation contributed to the localization of the two probiotics in the ileum and colon of the treatment group. Proteomics, immunochemistry, and real-time qPCR analyses showed that administration of the synbiotic preparation activated the PPAR signaling pathway in the ileum and significantly upregulated PPARß and PPARγ. The antagonist studies further confirmed this finding. In addition, metabolomic analyses demonstrated that among the 27 metabolites that showed significant differences between the control and model groups, administration of the synbiotic preparation significantly upregulated lysophosphatidylethanolamine and phosphatidylcholine in the ileum of the treatment group. Conclusion: The results of the study suggest that the novel synbiotic preparation reduces blood pressure by altering the composition of the intestinal microbiota, regulating PPAR signaling pathway, and activating the PPARß and PPARγ cascade reactions in the ileum.

RESUMEN

The main objective of this work was to investigate the impact of ultrasonication assisted enzymatic treatment on the physicochemical and bioactive properties of broad bean (BBP), lentil bean (LBP), and mung bean (MBP) protein isolates. The protein was extracted using alkaline acid precipitation method, ultrasonicated at a frequency of 20 kHz, temperature 20-30 °C and then hydrolysed using alcalase enzyme (1 % w/w, pH 8.5, 30 min, 55 οC). The generated hydrolysates were characterized by degree of hydrolysis (DH), SDS, FTIR, surface hydrophobicity, amino acid composition, antioxidant and antihypertensive properties. Results showed that the degree of hydrolysis was found to increase in ultrasonicated protein hydrolysate (18.9 to 40.71 %) in comparison to non- ultrasonicated protein hydrolysate (11 to 16.3 %). SDS-PAGE results showed significant changes in protein molecular weight profiles (100-11kDa) in comparison to their natives. However, no substantial change was found in ultrasonicated and non-ultrasonicated protein hydrolysates. The FTIR spectrum showed structural alterations in ultrasonicated and non-ultrasonicated protein hydrolysates, suggesting modifications in secondary structure such as amide A, amide I and amide II regions. The essential amino acid content varied in the range of 60.09 mg/g to 73.77 mg/g and 28.73 to 50.26 mg/g in case of ultrasonicated and non-ultrasonicated protein hydrolysates, and non-essential content varied in the range of 49.42 to 65.93 mg/g and 43.12 to 47.12 mg/g. Both antioxidant and antihypertensive activities were found to increase significantly in ultrasonicated and non-ultrasonicated protein hydrolysates in comparison to their native counterparts, highlighting their potential as functional ingredients for management of hypertension. It was concluded that ultrasonication assisted enzymatic hydrolysis is an efficient approach for production of bioactive pulse protein hydrolysates with enhanced nutracutical properties, thus offering promising avenues for their utilization in the food industry and beyond.

Asunto(s)

Inhibidores de la Enzima Convertidora de Angiotensina , Antioxidantes , Hidrolisados de Proteína , Hidrolisados de Proteína/química , Inhibidores de la Enzima Convertidora de Angiotensina/química , Inhibidores de la Enzima Convertidora de Angiotensina/farmacología , Antioxidantes/química , Antioxidantes/metabolismo , Hidrólisis , Sonicación , Subtilisinas/metabolismo , Subtilisinas/química , Interacciones Hidrofóbicas e Hidrofílicas , Aminoácidos/química , Aminoácidos/metabolismo , Proteínas de Plantas/química , Proteínas de Plantas/metabolismo , Antihipertensivos/química , Antihipertensivos/farmacología , Espectroscopía Infrarroja por Transformada de Fourier , Peso Molecular

RESUMEN

The subcritical water extraction of Undaria pinnatifida (blade, sporophyll, and root) was evaluated to determine its chemical properties and biological activities. The extraction was conducted at 180 °C and 3 MPa. Root extracts exhibited the highest phenolic content (43.32 ± 0.19 mg phloroglucinol/g) and flavonoid content (31.54 ± 1.63 mg quercetin/g). Sporophyll extracts had the highest total sugar, reducing sugar, and protein content, with 97.35 ± 4.23 mg glucose/g, 56.44 ± 3.10 mg glucose/g, and 84.93 ± 2.82 mg bovine serum albumin (BSA)/g, respectively. The sporophyll contained the highest fucose (41.99%) and mannose (10.37%), whereas the blade had the highest galactose (48.57%) and glucose (17.27%) content. Sporophyll had the highest sulfate content (7.76%). Key compounds included sorbitol, glycerol, L-fucose, and palmitic acid. Root extracts contained the highest antioxidant activity, with IC50 values of 1.51 mg/mL (DPPH), 3.31 mg/mL (ABTS+), and 2.23 mg/mL (FRAP). The root extract exhibited significant α-glucosidase inhibitory activity with an IC50 of 5.07 mg/mL, indicating strong antidiabetic potential. The blade extract showed notable antihypertensive activity with an IC50 of 0.62 mg/mL. Hence, subcritical water extraction to obtain bioactive compounds from U. pinnatifida, supporting their use in functional foods, cosmetics, and pharmaceuticals is highlighted. This study uniquely demonstrates the variation in bioactive compound composition and bioactivities across different parts of U. pinnatifida, providing deeper insights. Significant correlations between chemical properties and biological activities emphasize the use of U. pinnatifida extracts for chronic conditions.

Asunto(s)

Antioxidantes , Extractos Vegetales , Undaria , Antioxidantes/farmacología , Antioxidantes/aislamiento & purificación , Antioxidantes/química , Undaria/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Agua/química , Raíces de Plantas/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Flavonoides/química , Antihipertensivos/farmacología , Antihipertensivos/aislamiento & purificación , Antihipertensivos/química , Fenoles/aislamiento & purificación , Fenoles/farmacología , Fenoles/química , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Inhibidores de Glicósido Hidrolasas/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Algas Comestibles

RESUMEN

Cardiovascular diseases (CVDs) affect the quality of life or are fatal in the worst cases, resulting in a significant economic and social burden. Therefore, there is an urgent need to invent functional products or drugs for improving patient health and alleviating and controlling these diseases. Marine bioactive peptides reduce and control CVDs. Many of the predisposing factors triggering CVDs can be alleviated by consuming functional foods containing marine biopeptides. Therefore, improving CVD incidence through the use of effective biopeptide foods from marine sources has attracted increasing interest and attention. This review reports information on bioactive peptides derived from various marine organisms, focusing on the process of the separation, purification, and identification of biological peptides, biological characteristics, and functional food for promoting cardiovascular health. Increasing evidence shows that the bioactivity and safety of marine peptides significantly impact their storage, purification, and processing. It is feasible to develop further strategies involving functional foods to treat CVDs through effective safety testing methods. Future work should focus on producing high-quality marine peptides and applying them in the food and drug industry.

RESUMEN

This study was conducted to compare and analyze the changes in the biochemical characteristics and biological activity of peptide extracts derived from Chickso, Hanwoo, and Wagyu beef during digestion. The results of the in vitro digestion analysis revealed that the digestion rate, total free amino acid content, and antioxidant and antihypertensive activities of Chickso loin and shank myofibrillar proteins were significantly higher (p<0.05) than those of Hanwoo and Wagyu loin and shank myofibrillar proteins. Particularly, the peptide extracts of Chickso loin and shank had a high angiotensin-converting enzyme inhibitory activity. In mice in vivo digestion experiment, the blood serum of mice fed with Chickso loin peptide extract (<10 kDa) showed the highest antioxidant enzyme activity. Thus, Chickso peptide extracts were deemed to be similar or more bioactive than Hanwoo and Wagyu peptide extracts, and can be used as bioactive materials.

RESUMEN

This study aims to seek angiotensin-I-converting enzyme inhibitory (ACEi) peptides from walnut using different enzymatic hydrolysis, and further to validate the potent ACEi peptides identified and screened via peptidomics and in silico analysis against hypertension in spontaneously hypertensive rats (SHRs). Results showed that walnut protein hydrolysate (WPH) prepared by combination of alcalase and simulated gastrointestinal digestion exhibited high ACEi activity. WPH was separated via Sephadex-G25, and four peptides were identified, screened and verified based on their PeptideRanker score, structural characteristic and ACE inhibition. Interestingly, FDWLR showed the highest ACEi activity with IC50 value of 8.02 µg/mL, which might be related to its close affinity with ACE observed in molecular docking. Subsequently, high absorption and non-toxicity of FDWLR was predicted via in silico absorption, distribution, metabolism, excretion and toxicity. Furthermore, FDWLR exhibited positively vasoregulation in Ang II-induced human umbilical vein endothelial cells, and great blood pressure lowering effect in SHRs.

Asunto(s)

Angiotensina II , Inhibidores de la Enzima Convertidora de Angiotensina , Células Endoteliales de la Vena Umbilical Humana , Hipertensión , Juglans , Simulación del Acoplamiento Molecular , Hidrolisados de Proteína , Ratas Endogámicas SHR , Juglans/química , Animales , Inhibidores de la Enzima Convertidora de Angiotensina/farmacología , Inhibidores de la Enzima Convertidora de Angiotensina/química , Humanos , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Hidrolisados de Proteína/farmacología , Hidrolisados de Proteína/química , Ratas , Hipertensión/tratamiento farmacológico , Hipertensión/metabolismo , Angiotensina II/metabolismo , Péptidos/química , Péptidos/farmacología , Masculino , Peptidil-Dipeptidasa A/metabolismo , Antihipertensivos/farmacología , Antihipertensivos/química , Presión Sanguínea/efectos de los fármacos , Proteínas de Plantas/farmacología , Proteínas de Plantas/química

RESUMEN

Fish by-catches, along with other fish side-streams, were previously used as raw material for the production of fishmeal and fish oil but appropriate handling allows their use in more valuable options. The aim of this research was to valorize undersized hake (Merluccius merluccius) as a model of using fish by-catch from the Bay of Biscay to produce protein hydrolysates with bioactivities. Six enzymes, with different proteolytic activities (endo- or exoproteases) and specificities, were tested to produce protein hydrolysates. Products obtained with an endoprotease of serine resulted in the most promising results in terms of protein extraction yield (68%), with an average molecular weight of 2.5 kDa, and bioactivity yield (antioxidant activity = 88.5 mg TE antioxidant capacity/g fish protein; antihypertensive activity = 47% inhibition at 1 mg/mL). Then, process conditions for the use of this enzyme to produce bioactive products were optimized using Box-Behnken design. The most favorable process conditions (time = 2 h, solids = 50% and enzyme/substrate = 2% with respect to protein) were scaled up (from 0.5 L to 150 L reactor) to confirm laboratory scale and model forecasts. The results obtained in the pilot-scale testing matched the outcomes predicted by the model, confirming the technical viability of the proposed process.

Asunto(s)

Gadiformes , Perciformes , Animales , Hidrólisis , Gadiformes/metabolismo , Hidrolisados de Proteína/química , Péptidos/química , Antihipertensivos/farmacología , Peces/metabolismo , Perciformes/metabolismo , Antioxidantes/farmacología , Antioxidantes/metabolismo

RESUMEN

Ethnopharmacological relevance: Canarium schweinfurthii, also called ''Elemierd'Afrique'', is used in Cameroonian folk medicine (bark decoction) to treat patients suffering from hypertension.Aim of the study: This study aimed at evaluating the antihypertensive activities of the stem bark of Canarium schweinfurthii and identifying potential compounds present in its extract that may support or oppose its ethnomedicinial use. Materials and methods: Stem bark extract of Canarium schweinfurthii was prepared by maceration using 70 % ethanol followed by redissolution in methanol and hyphenated. Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry (UPLC-MS/MS) analysis for the detection and characterisation of secondary metabolites. Antihypertensive effects were assessed in Wistar rats after induction of hypertension with sodium chloride (NaCl) 18 % at a dose of 0.01mL/gbody weight once a day for four weeks.Hemodynamic parameters were measured weekly by anon-invasive method using the CODA system. Results: The ethanolic bark extract of C. schweinfurthii significantly inhibited the increase of blood pressure with a maximum of 23.18 % (systolic pressure, p < 0.0001), 24.77 % (diastolic pressure, p < 0.001) and 22.95 % (mean pressure, p < 0.0001) at a dose of 200 mg/kgbody weight at the 4th week, compared to agroup of Wistar rats that received only NaCl (negative control). Similarly, the extract significantly inhibited the increase in heart rate by 18.84 % (p < 0.001) at 200 mg/kgbody weight at week four. Hematological parameters did not differ significantly between the extract-treated and control groups. The UPLC-MS/MS spectrometric analysis provided evidence for the presence of several C30 terpenoids containing three or five oxygen atoms and exhibiting pentacyclic triterpenoid structures, as well as C29 terpenoids and related compounds containing nitrogen in addition to oxygen, using spectral matching, and in silico molecular formula and structure prediction. Additionally, two features were annotated with high-confidence as lignans, structurally closely related to hinokinin and dehydrocubebin through MS/MS-based in silico structure prediction using CSI: Finger ID in SIRIUS5. The lignans have been previously reported from stem bark of plants belonging to the Burseraceae family. Conclusion: The ethanolic stem bark extract of C. schweinfurthii demonstrated antihypertensive properties on the tested Wistar rats. These results support the ethnopharmacological use of C. schweinfurthii concoctions for the treatment of hypertension and suggest a protective effect against salt damage, hypothetically by the up regulation of antioxidative enzymes and/or lipids, mitigatings membrane peroxidation.

RESUMEN

This study aimed to identify angiotensin I-converting enzyme (ACE) from in vitro digestion products of pork sausage with partial substitution of NaCl by KCl (PSRK). Peptides from in vitro digestion products of PSRK were identified through liquid chromatography with tandem mass spectrometry analysis coupled with de novo sequencing. Subsequently, the ACE inhibitory peptides LIVGFPAYGH and IVGFPAYGH were screened based on PeptideRanker, in silico absorption, molecular docking, and the determination of ACE inhibitory activity. In addition, the ACE inhibitory peptides LIVGFPAYGH and IVGFPAYGH were mixed-type inhibitors; these peptides' ACE inhibitory activities were expressed as the 50% inhibitory concentration (IC50) values in vitro, which were 196.16 and 150.88 µM, respectively. After 2 h of incubation, LIVGFPAYGH and IVGFPAYGH could be transported through Caco-2 cell monolayers with paracellular passive diffusion. Furthermore, LIVGFPAYGH and IVGFPAYGH significantly increased the levels of ACE2 and nitric oxide while decreasing the levels of ACE, angiotensin II, and endothelin-1 in Ang I-treated human umbilical vein endothelial cells, indicating the ACE inhibitory effect of LIVGFPAYGH and IVGFPAYGH. In summary, LIVGFPAYGH and IVGFPAYGH from PSRK can be used as functional foods with antihypertensive activity.

Asunto(s)

Carne de Cerdo , Carne Roja , Animales , Humanos , Porcinos , Inhibidores de la Enzima Convertidora de Angiotensina/farmacología , Inhibidores de la Enzima Convertidora de Angiotensina/química , Peptidil-Dipeptidasa A/química , Cloruro de Sodio , Simulación del Acoplamiento Molecular , Células CACO-2 , Células Endoteliales , Péptidos/farmacología , Péptidos/química , Digestión

RESUMEN

The use of halophyte plants appears as a potential solution for degraded soil, food safety, freshwater scarcity, and coastal area utilization. These plants have been considered an alternative crop soilless agriculture for sustainable use of natural resources. There are few studies carried out with cultivated halophytes using a soilless cultivation system (SCS) that report their nutraceutical value, as well as their benefits on human health. The objective of this study was to evaluate and correlate the nutritional composition, volatile profile, phytochemical content, and biological activities of seven halophyte species cultivated using a SCS (Disphyma crassifolium L., Crithmum maritimum L., Inula crithmoides L., Mesembryanthemum crystallinum L., Mesembryanthemum nodiflorum L., Salicornia ramosissima J. Woods, and Sarcocornia fruticosa (Mill.) A. J. Scott.). Among these species, results showed that S. fruticosa had a higher content in protein (4.44 g/100 g FW), ash (5.70 g/100 g FW), salt (2.80 g/100 g FW), chloride (4.84 g/100 g FW), minerals (Na, K, Fe, Mg, Mn, Zn, Cu), total phenolics (0.33 mg GAE/g FW), and antioxidant activity (8.17 µmol TEAC/g FW). Regarding the phenolic classes, S. fruticosa and M. nodiflorum were predominant in the flavonoids, while M. crystallinum, C. maritimum, and S. ramosissima were in the phenolic acids. Moreover, S. fruticosa, S. ramosissima, M. nodiflorum, M. crystallinum, and I. crithmoides showed ACE-inhibitory activity, an important target control for hypertension. Concerning the volatile profile, C. maritimum, I. crithmoides, and D. crassifolium were abundant in terpenes and esters, while M. nodiflorum, S. fruticosa, and M. crystallinum were richer in alcohols and aldehydes, and S. ramosissima was richer in aldehydes. Considering the environmental and sustainable roles of cultivated halophytes using a SCS, these results indicate that these species could be considered an alternative to conventional table salt, due to their added nutritional and phytochemical composition, with potential contribution for the antioxidant and anti-hypertensive effects.

RESUMEN

Ocimum basilicum Linn. (basil) is an aromatic culinary herb that has shown a great potential in therapeutic world. It has many promising pharmacological activities that make it centre for investigations for many researchers. Current study has been planned to determine chemical constituents of basil leaves extracts and their in-vitro and ex-vivo antioxidant and in-vivo antihypertensive potential. GC-MS studies of non-polar extracts showed presence of 75 compounds including monoterpenes, hydrocarbons, sesquiterpenes, triterpenes, phyto-sterols and phthalates. Higher percentages of fatty acids were also identified. The major compounds include linalool (7.65%), terpineol (1.42%), tau-cadinol (13.55%), methyl palmitate (14.24%), palmitic acid (14.31%), linolenic acid (1.30%) and methyl linolenate (17.72%). Electron spray ionization mass spectrometry ESI-HRMS/MS of the polar extracts revealed the presence of alkaloids, phenolic acid, amino acid, coumarin, lignin, flavanoid and terpene derivative. Total phenolic content and total flavonoid content were determined using spectrophotometric technique and calculated as gallic acid equivalents GAE/g dry weight and rutin equivalent RE/g of dry weight respectively. The highest phenolic content and flavonoid content were found in ethyl acetate extract 9.40 mg GAE/g and 15.9 mg RE/g of dry weight. All the extracts showed significant antioxidant activity in DPPH and ABTS cation decolorization assays. Dichloromethane extract possess the highest DPPH scavenging activity, i.e., 64.12% ± 0.23 at concentration of 4 mg/ml. Moreover in ex-vivo studies all the extracts showed prominent effect by inhibiting AAPS induce oxidation in Human erythrocytes being 69.24% ± 0.18 in dichloromethane extract, 64.44% ± 0.04 in ethyl acetate and 53.33% ± 0.09 in acetone extract. The methanol extract of O. basilicum exhibited significant decrease in systolic blood pressure in l-Name induced hypertensive rats at the dose of 50 mg/kg for 28 days. Total phenolic content had a higher linear correlation (r = 0.678) with antihypertensive activity, with a level of significance 95% showing that phenolic compounds in the leaves of the plant has important role in inhibiting l -NAME induced hypertension while flavonoid compounds may play a key role in the antioxidant activities of the plant, through synergism. Conclusively, O. basilicum leaves with bioactive metabolites are a potential source for the development of antihypertensive drugs.

RESUMEN

The aim of this study was to determine the effects of fermentation and food matrix on the ACE inhibitory activities of the peptides obtained after in vitro gastrointestinal digestion, protein profiles (SDS-PAGE) and ß-glucan amounts of oat products. Furthermore, the physicochemical and microbiological properties of fermented oat drinks and oat yogurt-like product obtained from oat fermentation were evaluated. Oat grains were mixed with a certain ratio of water 1:3 w/v (oat:water, yogurt consistency) and 1:5 w/v (oat:water, drink consistency), and this mixture was fermented with yogurt culture and probiotic Lactobacillus plantarum and fermented drinks and yogurt were produced. The results indicated that the fermented oat drink and the oat yogurt-like product had L. plantarum viability over 107 cfu/g. After the in vitro gastrointestinal digestion of the samples, the hydrolysis levels ranged from 57.70 % to 82.06 %.The hydrolysis level of the samples with fermented-drink consistency was significantly higher than the samples with yogurt consistency (p < 0.05).The SDS-PAGE profiles of the non-digested samples showed that the bands had molecular weights of 12-15 kDa and around 35 kDa. Bands whose molecular weights were around 35 kDA disappeared after gastric digestion. ACE inhibitory activities of the fractions composed of molecular weights of 2 kDa and 2-5 kDa obtained after in vitro gastrointestinal digestion of the oat samples were in the range of 46.93-65.91 %. The effect of fermentation on the ACE inhibitory activities of the peptide mixture with molecular weights between 2 and 5 kDa was not statistically significant, however, fermentation caused an increase in the ACE inhibitory activities of the peptide mixture with a molecular weight<2 kDa (p < 0.05). The ß-glucan amounts of fermented and non-fermented oat products were in the range of 0.57-1.28 %. The ß-glucan amounts detected after gastric digestion decreased considerably and ß-glucan could not be detected in the supernatant after gastrointestinal digestion. This indicated that ß-glucan did not solubilize in the supernatant (bioaccessible) and remained in the pellet. In conclusion, fermentation is a valuable process for releasing peptides with moderately high ACE inhibitory effects from the parent oat proteins.

Asunto(s)

Probióticos , beta-Glucanos , Avena , Fermentación , Agua , Angiotensinas , Digestión

RESUMEN

This study aimed to evaluate 2-(N-((2'-(2H-tetrazole-5-yl)-[1,1'-biphenyl]-4yl)-methyl)-pentanamido)-3-methyl butanoic acid-based ester derivatives as a new class of angiotensin-II receptor antagonists. For this purpose, a series of compounds were synthesized using a variety of phenols. Their chemical characterization was established by FTIR, 1HNMR, and 13CNMR techniques. The biological activities including antioxidant potentials using the DPPH assay, the antihypertensive assay, the urease enzyme inhibition assay, and the antibacterial assay using agar well diffusion methods were performed. All the new compounds showed significant free radical scavenging potentials more than the parent drug while retaining antihypertensive potentials along with urease inhibition properties. However, the AV2 test compound was found to be the most potent against hypertension. Most of the synthesized analogs showed urease inhibitory actions. Molecular docking studies were performed for all the active analogs to decode the binding detail of the ligands with receptors of the enzyme's active site.

Asunto(s)

Antihipertensivos , Ureasa , Ácido Butírico , Simulación del Acoplamiento Molecular , Tetrazoles , Relación Estructura-Actividad

RESUMEN

The high hydrostatic pressure (HHP) process has been studied for several applications in food technology and has been commercially implemented in several countries, mainly for non-thermal pasteurization and shelf-life extension of food products. HHP processing has been demonstrated to accelerate proteolytic hydrolysis at a specific combination of pressure and pressure-holding time for a given protein source and enzyme. The enzymatic hydrolysis of proteins is a well-known alternative to producing biologically active peptides, with antioxidant and antihypertensive capacity, from different food protein sources. However, some of these protein sources contain allergenic epitopes which are often not degraded by traditional hydrolysis. Moreover, the peptide profile and related biological activity of a hydrolysate depend on the protein source, the enzymes used, the parameters of the proteolysis process (pH, temperature, time of hydrolysis), and the use of other technologies such as HHP. The present review aims to provide an update on the use of HHP for improving enzymatic hydrolysis, with a particular focus on studies which evaluated hydrolysate antihypertensive and antioxidant capacity, as well as residual allergenicity. Overall, HHP has been shown to improve the biological properties of hydrolysates. While protein allergenicity can be reduced with traditional hydrolysis, HHP can further reduce the allergenicity. Compared with traditional hydrolysis methods, HHP-assisted protein hydrolysis offers a greater opportunity to add value to protein-rich products through conversion into high-end hydrolysate products with enhanced nutritional and functional properties.

RESUMEN

By reducing the 2-nitrophenylhydrazone of cyclohexanone with sodium dithionite, an unexpected yellow compound was obtained instead of the corresponding colorless amino derivative. Many years later, the structure of this compound, namely, cyclohexane-3-spiro-3,4-dihydro-1,2,4-benzotriazine, was demonstrated. From that time, the reduction of 2-nitrophenylhydrazones of different kinds of ketones, followed by air oxidation of the initially formed amino compounds, has represented a general way to synthesize a variety of 3,3-disubstituted 3,4-dihydro-1,2,4-benzotriazines. Many derivatives have been obtained so far by a single research group, and most of them have demonstrated interesting pharmacological activities, mainly antihypertensive, anti-inflammatory, and diuretic effects and other activities with lower diffusion. Moreover, 3,3-disubstituted 3,4-dihydro-1,2,4-benzotriazines represent a novel class of ligands for sigma receptors, with nanomolar affinity to the σ1 subtype. This property might promote the development of agents for cardiovascular, neurodegenerative, and proliferative pathologies. The present commentary, by collecting compounds and biological results obtained so far, intends to celebrate the centennial of the discovery of the first member of this class of compounds and to promote further investigation in the field.

Asunto(s)

Receptores sigma , Antihipertensivos , Difusión , Cetonas , Triazinas/farmacología

RESUMEN

Candidate peptides with novel angiotensin-I-converting enzyme (ACE) inhibitor activity were obtained from hydrolysates of Gracilariopsis lemaneiformis by virtual screening method. Our results showed that G. lemaneiformis peptides (GLP) could significantly lower blood pressure in spontaneously hypertensive rats (SHR). At least 101 peptide sequences of GLP were identified by LC-MS/MS analysis and subjected to virtual screening. A total of 20 peptides with the highest docking score were selected and chemically synthesized in order to verify their ACE-inhibitory activities. Among them, SFYYGK, RLVPVPY, and YIGNNPAKG showed good effects with IC50 values of 6.45 ± 0.22, 9.18 ± 0.42, and 11.23 ± 0.23 µmoL/L, respectively. Molecular docking studies revealed that three peptides interacted with the active center of ACE by hydrogen bonding, hydrophobic interactions, and electrostatic forces. These peptides could form stable complexes with ACE. Furthermore, SFYYGK, RLVPVPY, and YIGNNPAKG significantly reduced systolic blood pressure (SBP) in SHR. YIGNNPAKG exhibited the highest antihypertensive effect, with the largest decrease in SBP (approximately 23 mmHg). In conclusion, SFYYGK, RLVPVPY, and YIGNNPAKG can function as potent therapeutic candidates for hypertension treatment.

Asunto(s)

Hipertensión , Rhodophyta , Ratas , Animales , Hipertensión/tratamiento farmacológico , Simulación del Acoplamiento Molecular , Cromatografía Liquida , Peptidil-Dipeptidasa A/química , Espectrometría de Masas en Tándem , Antihipertensivos/uso terapéutico , Inhibidores de la Enzima Convertidora de Angiotensina/uso terapéutico , Ratas Endogámicas SHR , Péptidos/química , Hidrolisados de Proteína/química

RESUMEN

The aim of this study was to assess the potential hypertensive effects of the IGTGIPGIW peptide purified from Hippocampus abdominalis alcalase hydrolysate (HA) for application in the functional food industry. We investigated the antihypertensive effects of IGTGIPGIW in vitro by assessing nitric oxide production in EA.hy926 endothelial cells, which is a major factor affecting vasorelaxation. The potential vasorelaxation effect was evaluated using 4-amino-5-methylamino-2',7'-difluorofluorescein diacetate, a fluorescent stain. IGTGIPGIW significantly increased the expression of endothelial-derived relaxing factors, including endothelial nitric oxide synthase and protein kinase B, in EA.hy926 cells. Furthermore, oral administration of IGTGIPGIW significantly lowered the systolic blood pressure (183.60 ± 1.34 mmHg) and rapidly recovered the diastolic blood pressure (143.50 ± 5.55 mmHg) in the spontaneously hypertensive rat model in vivo. Our results demonstrate the antihypertensive activity of the IGTGIPGIW peptide purified from H. abdominalis and indicate its suitability for application in the functional food industry.

Asunto(s)

Antihipertensivos , Óxido Nítrico Sintasa de Tipo III , Smegmamorpha , Animales , Antihipertensivos/farmacología , Presión Sanguínea , Células Endoteliales , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo III/metabolismo , Péptidos/farmacología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Ratas , Ratas Endogámicas SHR

RESUMEN

Artina pectinata (Comb pen shell, CPS) is a high-protein source that contains a variety of essential amino acids. Subcritical water hydrolysis (SWH) was used to recover amino acids from the posterior adductor muscle (PAM), anterior adductor muscle (ADM), and mantle. The temperatures ranged from 120 °C to 200 °C, and the pressure and time of hydrolysis were 3 MPa and 30 min, respectively. Further characterization of the hydrolysates was performed to ascertain amino acid profiles and biofunctional properties. The hydrolysates contained more free amino acids than the untreated samples. Antioxidant activity of treated samples increased as SW temperatures increased. At 200 °C, those inhibiting ACE had a maximum antihypertensive activity of 200 °C in 1% PAM, ADM, and mantle with 85.85 ± 0.67, 84.55 ± 0.18, and 82.15 ± 0.85%, respectively, compared to 97.57 ± 0.67% in 1% standard captopril. Perhaps the most significant finding was the predominance of taurine in the three parts following SW treatment at 120 °C. The hydrolysates may be of considerable interest for use in food or energy drinks. SWH demonstrates efficacy in recovering amino acids, particularly taurine, from edible parts of A. pectinata.

Asunto(s)

Bivalvos , Agua , Aminoácidos , Animales , Hidrólisis , Taurina , Agua/química

RESUMEN

Seaweeds have a long history of use as both food and medicine, especially in Asian cultures. Moreover, there is growing interest in the use of seaweed ingredients and bioactive compounds in pharmaceutical and nutraceutical products. One ailment that seaweed bioactive compounds may impact is hypertension caused by the enzyme Angiotensin Converting Enzyme 1 (ACE-1; EC 3.4.15.1), found within the Renin-Angiotensin Aldosterone System (RAAS), which causes vasoconstriction of blood vessels, including veins and arteries. The aim of this paper is to generate bioactive peptide containing protein hydrolysates from the brown seaweed Laminaria digitata (Hudson) JV Lamouroux 1813. Proteins were extracted from this seaweed by disrupting the seaweed cell wall using a combination of carbohydrases and proteolytic enzymes. Bioactive peptide containing permeates were generated from L. digitata protein hydrolysates, and both hydrolysates and permeates were screened for their ability to inhibit the enzyme ACE-1. The protein content of the permeate fractions was found to be 23.87% compared to the untreated seaweed, which contained 15.08% protein using LECO analysis. Hydrolysis and filtration resulted in a "white" protein powder, and the protein content of this powder increased by 9% compared to the whole seaweed. The total amino acid (TAA) content of the L. digitata protein permeate was 53.65 g/100 g of the sample, and contains over 32% essential amino acids (EAA). Furthermore, the L. digitata permeate was found to inhibit the ACE-1 enzyme by 75% when compared to the commercial drug Captopril© when assayed at a concentration of 1 mg/mL. The inhibition of ACE-1 (the IC50 value) of 590 µg/mL for the L. digitata permeate compares well with Captopril©, which had 100% inhibition of ACE-1, with an IC50 value of 500 µg/mL. This study indicates that there is potential to develop protein powders with ACE-1 inhibitory bioactivities from the brown seaweed L. digitata using enzymatic hydrolysis as a cell disruption and protein extraction/hydrolysate generation procedure.

RESUMEN

Cardiovascular diseases are increasingly threating the global human health, hypertension is the most important risk factor for cardiovascular and cerebrovascular diseases. To improve the antihypertensive activity and cardiovascular protective effect of natural product (±)-7,8-dihydroxy-3-methyl-isochroman-4-one [(±)-XJP], a series of novel H2S-releasing isochroman-4-one derivatives were designed and synthesized by coupling hydrogen sulfide (H2S)-releasing donors with the analogs of (±)-XJP. Further, the H2S-releasing assay indicated that some target compounds showed excellent H2S generating ability. Moreover, these novel hybrids exhibited moderate to good in vitro vasodilation efficacy. Among them, the most potent compound exhibited potent in vivo antihypertensive activity with the maximum antihypertensive amplitude about 27%, which was more potent than that of the lead compound (±)-XJP. These results suggested that the hybridization of H2S-donors and (±)-XJP analogs may provide a promising approach for the discovery of novel antihypertensive agents.

Asunto(s)

Sulfuro de Hidrógeno , Hipertensión , Antihipertensivos , Humanos , Sulfuro de Hidrógeno/farmacología , Hipertensión/tratamiento farmacológico , Vasodilatación