A review: extraction, phytochemicals, and biological activities of rambutan (Nephelium lappaceum L) peel extract.

Rambutan (Nephelium lappaceum L.) peels are produced during application process. Drying methods of rambutan peel, including open sun, oven, oven vacuum, and freeze-drying, have been describes in this study. The extraction technologies of dried rambutan peels were reviewed, such as maceration and hot extraction, microwave-assisted extraction, ultrasonic-assisted extraction, and supercritical fluid extraction. The phytochemicals of rambutan peel extracts were analyzed, and the purification and stability of geraniin was reviewed. Rambutan peel extracts exhibit wide bioactivities in vitro and in vivo, and these bioactivities depend chiefly on the phenolic contents and profiles in the different extracts. The safety of rambutan peel extracts was analyzed. In addition, rambutan peel extracts could be used as important components to make different products, which are potentially applied in food, medicine, and cosmetic. However, the extracts efficiency must be further increased using some emerging technologies. Furthermore, the bioactive mechanism and bioavailability of the extract in human system should be further evaluated.

Identification of in vitro angiotensin-converting enzyme and dipeptidyl peptidase IV inhibitory peptides from draft beer by virtual screening and molecular docking.

BACKGROUND: Hypertension and diabetes are two kinds of senile diseases which often occur simultaneously. The commonly used drugs in clinic may produce certain side effects. Food-derived polypeptide is a kind of polypeptide with great development potential, which has many functions of regulating human physiological function. Beer is rich in nutrition but there are few researches on bioactive peptides in beer. RESULTS: In this study, a rapid virtual screening method was established to obtain bioactive peptides from Tsingtao draft beer. The peptide sequence was analyzed by ultra-performance liquid chromatography-quadrupole-Orbitrap-tandem mass spectrometry (UPLC-Q-Orbitrap-MS2 ), and 50 peptides were identified. Eight peptides with potential biological activities were screened by using Peptide Ranker software and previous literature references. On the basis of absorption prediction, toxicity prediction, and molecular docking analysis, LNFDPNR and LPQQQAQFK were finally confirmed. The molecular docking results showed that two peptides could bind angiotensin-converting enzyme (ACE) and dipeptidyl peptidase IV (DPP-IV) tightly by hydrogen bonding and hydrophobic interaction. The in vitro activity evaluation results showed that two peptides had obvious ACE and DPP-IV inhibitory activity. CONCLUSION: This study established a method for rapidly screening bioactive peptides from Tsingtao draft beer, screened two ACE and DPP-IV inhibitory peptides in beer and analyzed their active action mechanism. This article may have great theoretical significance and practical value to further explore the health function of beer. © 2021 Society of Chemical Industry.

Novel umami peptides from tilapia lower jaw and molecular docking to the taste receptor T1R1/T1R3.

This study aimed to isolate and identify peptides with intense umami taste from tilapia lower jaw. The aqueous extract was separated using ultrafiltration and Sephadex G-15 gel filtration chromatography. The peptide fraction with an intense umami taste was selected by sensory evaluation. The five novel peptides with strong umami taste were VADLMR, STELFK, FVGLQER, DALKKK, and VVLNPVARVE. Electronic tongue analysis and sensory evaluation showed that five peptides had obvious umami taste characteristics, and the recognition thresholds of umami peptides were in the range 0.125-0.250 mg/mL. Molecular docking was used to study the interaction of the peptides and umami taste receptor T1R1/T1R3. The five peptides could perfectly be inserted into the binding pocket of the Venus flytrap domain in the T1R3 subunit. Hydrogen bonding and hydrophobic interaction were the important interaction forces. The five peptides may bind with Asp219, Glu217, and Glu148 in T1R1/T1R3 receptor and produce the umami taste.

UPLC-Q-Orbitrap-MS2 analysis of Moringa oleifera leaf extract and its antioxidant, antibacterial and anti-inflammatory activities.

Moringa oleifera leaf acetone extract (MLE) was prepared. Phytochemicals of MLE and their antioxidant, antibacterial, and anti-inflammatory activities were evaluated. Results showed that MLE contained total phenolic content of 20.16 mg gallic acid equivalents/g dry weight. A total of 39 compounds were identified by mass spectrometry. The contents of acetyl-glucomoringin, caffeoylquinic acid, feruloylquinic acid, and coumarylquinic acid were high. MLE had high DPPH· and ABTS•+ scavenging activities and reducing powder. In addition, MLE could effectively inhibit S. aureus and B. subtilis, but little effect on E. coli was found. The anti-inflammatory effect of MLE was evaluated using a lipopolysaccharide (LPS) -induced RAW 264.7 cell model. MLE significantly inhibited nitric oxide (NO) production and inducible NO synthase (iNOS) mRNA levels in LPS-induced RAW 264.7 cells. The inhibitory activity increased in a dose-dependent manner. The bioactivities of MLE were related to its phenolic content and phenolic profiles.[Figure: see text].

Identification and characterization of the peptides with calcium-binding capacity from tilapia (Oreochromis niloticus) skin gelatin enzymatic hydrolysates.

The aim of this study was to isolate and identify the peptides with calcium-binding capacity from the different tilapia skin gelatin enzymatic hydrolysates. The complex protease was selected and its hydrolysates were further separated using gel filtration chromatography (Sephadex G-25) and reverse phase high-performance liquid chromatography. Two purified peptides with strong calcium-binding capacity were identified as Tyr-Gly-Thr-Gly-Leu (YGTGL, 509.25 Da) and Leu-Val-Phe-Leu (LVFL, 490.32 Da). The calcium-binding capacities of YGTGL and LVFL reached 76.03 and 79.50 µg/mg, respectively. The structures of the complex of purified peptides and calcium (YGTGL-Ca and LVFL-Ca) were characterized by ultraviolet-visible spectroscopy (UV-VIS), scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and mass spectrometry (LC-MS/MS). The results of UV-VIS, SEM, and XRD indicated that YGTGL-Ca and LVFL-Ca were formed as new compounds. The results of FTIR and LC-MS/MS indicated the nitrogen atom of the amino group and the oxygen atom of the carboxyl group in terminates of the peptides provided primary binding sites. Moreover, the hydrophobic amino acids in purified peptides could provide more chelating spaces. This study was of great significance for the development of calcium supplement foods. PRACTICAL APPLICATION: Compared with inorganic calcium and organic calcium, the bioactive gelatin peptide chelated calcium has the characteristics of high utilization rate, high solubility, and high absorption rate. The raw materials are extracted from the tilapia processed waste, which reduce the cost, make full use of resources, and improve the bioavailability. The tilapia skin gelatin peptide calcium chelate can be directly absorbed by the human body, and the absorption efficiency is high, further improving the resource utilization rate and having high economic benefits, which is a comprehensive supplement that can also be used as a functional food.

Preparation and identification of novel inhibitory angiotensin-I-converting enzyme peptides from tilapia skin gelatin hydrolysates: inhibition kinetics and molecular docking.

Tilapia skin gelatin was hydrolyzed by successive simulated gastrointestinal digestion, and the hydrolysates were further separated by transport across a Caco-2 cell monolayer. Angiotensin-I-converting enzyme inhibitory (ACEI) peptides were separated by successive chromatographic steps from the transport hydrolysates. We have identified two key ACEI peptides, namely VGLPNSR (741.4133 Da) and QAGLSPVR (826.4661 Da) with IC50 values of ACEI activity of 80.90 and 68.35 µM, respectively. Lineweaver-Burk plots indicated that the inhibitory ACE kinetics of the two peptides were noncompetitive. Molecular docking simulation showed that the two peptides could interact with the ACE site via hydrogen bonds with high binding power. However, the hydrogen bonds were not formed with the key amino acid residues in the active site of ACE. This finding was in accordance with the noncompetitive inhibition. This study established a novel approach to identify key ACEI peptides and suggested the use of tilapia peptides as functional food ingredients to prevent hypertension.

17ß-Estradiol inhibits testosterone-induced cell proliferation in HepG2 by modulating the relative ratios of 3 estrogen receptor isoforms to the androgen receptor.

Sex hormones, especially 17ß-estradiol (E2) and testosterone (TEST), play crucial roles in the oncogenesis and progression of liver cancer via hormone-related receptors. As women have a lower rate of hepatocellular carcinoma (HCC) than men, estrogens might attenuate the occurrence and development of HCC. This study aimed to investigate the inhibitory effects and mechanisms of E2 on TEST-induced HCC development; the HepG2 cell line was used as an in vitro model. Five endpoints, including cell viability, cell apoptosis, cell cycle, receptor protein expression, and messenger RNA transcription, were investigated. Different roles and the ratios of androgen receptor (AR) and 3 estrogen receptor (ER) subtypes were also estimated. Cell viability assay showed that co-treatment of E2 and TEST resulted in a significant inhibition of E2-induced or TEST-induced cell proliferation. Flow cytometry analysis revealed that combined treatment of E2 and TEST blocked the cell cycle in the G0/G1 phase as well as induced cell early apoptosis, characterized by decreased cyclin-dependent kinase transcription and the ratio of Bcl-2/Bax. Real-time quantitative polymerase chain reaction and Western blot analysis results further demonstrated that estrogen receptor estrogen receptor α66 (ERα66) and estrogen receptor ß (ERß) were upregulated, whereas AR and estrogen receptor α36 (ERα36) were downregulated, irrespective of whether E2 and TEST were considered separately or together, whereas the combined treatment of E2 and TEST resulted in a decrease in the ERα66/ERß ratio, the ERα66/ERα36 ratio, and the ERß/ERα36 ratio, but with an increase in the ERα66/AR ratio, the ERα36/AR ratio, and the ERß/AR ratio. To sum up, E2 could inhibit TEST-induced cell proliferation by modulating the ratio of different hormone-related receptors.

Purification and Characterization of Peptides Inhibiting MMP-1 Activity with C Terminate of Gly-Leu from Simulated Gastrointestinal Digestion Hydrolysates of Tilapia (Oreochromis niloticus) Skin Gelatin.

Tilapia skin gelatin hydrolysates (TSGHs) were prepared by simulated gastrointestinal digestion and separated by gel filtration and semi-preparative reversed-phase high-performance liquid chromatography. The anti-photoaging effects were evaluated using an ultraviolet radiation B (UVB)-induced mouse embryonic fibroblast (MEF) photoaging model in vitro. Three fractions from TSGHs with high inhibitory intercellular matrix metalloproteinase-1 (MMP-1) activities and reactive oxygen species (ROS) production were obtained. Three key peptides, GYTGL, LGATGL, and VLGL, were identified, and their C terminate was Gly-Leu. Three peptides were synthesized and exhibited a significant inhibition of intercellular MMP-1 activity and ROS production. Furthermore, three peptides inhibiting MMP-1 activities were evaluated through their docking of S1' and S3' active pockets of MMP-1. Hydrogen bonds and C terminate Gly-Leu played important roles. Finally, the protective effects of three peptides on intercellular collagen in UVB-induced MEFs were compared. Our results indicated that tilapia gelatin peptides exhibited potential activities to prevent and regulate photoaging.

Preparation, characterization and antiglycation activities of the novel polysaccharides from Boletus snicus.

Boletus snicus (BS) is one of the commercially important mushroom species. Two polysaccharides (BSP-1b and BSP-2b) were extracted and purified from the body of BS by DEAE-cellulose and Sephadex G-100 column chromatography. The average of molecular weight of BSP-1b and BSP-2b were 59.21kDa and 128.74kDa. BSP-1b is a heteropolysaccharide with a large number of glucose and a small amount of mannose, glucosamine hydrochloride and arabinose. The monosaccharide compositions of BSP-2b contain mannose, glucuronic acid, glucosamine hydrochloride, glucose, galactose, arabinose with the molar ratio of 10.70:6.95:12.05:12.57:1.83:1.00. The FTIR spectra and NMR analysis demonstrated that BSP-1b and BSP-2b existed pyranose ring structure and BSP-2b had high content of uronic acid. The antiglycation activities of BSP-1b and BSP-2b were investigated. The results showed BSP-1b and BSP-2b had high inhibitory effects on glycation and exhibited dose-dependent responses. BSP-2b showed stronger antiglycation activity than BSP-1b. This study indicated that the BSP-2b could effectively inhibit the formation of advanced glycation end-products.