Journal of Food Biochemistry最新文献

The growing global burden of diabetes warrants search for natural, food-derived bioactive molecules, including peptides. In this paper, dipeptidyl peptidase 4 (DPP4), a type 2 diabetes drug target,inhibitory peptides from the seed protein hydrolysates of mung bean (Vigna radiata) were studied. The peptides were isolated using activity-guided purification and identified by LC-MS/MS. Two peptides: VSVPHKDAE (MPHPep1) and VAPPGKGEVR (MPHPep2) showed DPP4 inhibition via competitive and uncompetitive modes, respectively. The average K_i value of MPHPep1 and MPHPep2 was found to be 1.40 mm and 0.23 mm, respectively. Both peptides were stable towards gastric digestion conditions. While MPHPep1 is stable towards intestinal digestion, MPHPep2 exhibited 64% loss in its activity. Moreover, the peptides are stable with DPP4 and retain near-complete inhibition activity after incubation with DPP4 for 30 min. In vitro DPP4 inhibition observed in cell-based assays using the Caco-2 cell line further validated the inhibitory potential of these peptides. Finally, the possible interactions of MPHPep1 and MPHPep2 with DPP4 using molecular docking tool are discussed.

Hyperlipidemia is recognized as a major contributor to chronic noncommunicable diseases. The primary strategy regarding hyperlipidemia prevention is involved in the blockade of intestinal cholesterol absorption. Ezetimibe (Eze) is the sole prescribed drug that targets Niemann-Pick C1 Like 1 (NPC1L1), a key cholesterol transporter, resulting in reduced cholesterol levels. Nonetheless, several adverse effects have been reported, including headache, diarrhea, and cold-like symptoms. Thus, complementary and alternative intervention exerting antihyperlipidemia while ensuring safety is a challenging option. Previously, leaves of Ocimum sanctum L., commonly known as holy basil, have been shown to lower plasma lipid levels in both humans and animals with hypercholesterolemia. However, the beneficial effects of O. sanctum L. flowers and the mechanisms of action have not been investigated yet. Herein, we first investigated the biological activity of O. sanctum L. flower aqueous extract (OSLY). This study neatly established a fast and robust screening methodology for investigating cholesterol absorption using fluorescent-25-NBD-cholesterol incorporated by micelles (25-NBD-mc), followed by high-content imaging analysis detection in Caco-2 cells. Changes of physicochemical properties of cholesterol micelles by OSLY were addressed. The experimental findings demonstrated that 25-NBD-mc successfully mimicked NPC1L1-mediated dietary cholesterol absorption into Caco-2 cells. In addition, OSLY inhibited 25-NBD-mc uptake without cytotoxicity, similar to the positive drug Eze. Correspondingly, OSLY increased cholesterol micellar size and bile acid–binding capacity. Furthermore, like Eze, OSLY markedly reduced intestinal [³H]-cholesterol absorption compared to control in rat jejunal epithelial cells. Nonetheless, OSLY induced the gene expression of LXRα and PPARα, the regulator for downregulating NPC1L1, but not their activities, suggesting that OSLY inhibited the cholesterol absorption–mediated LXRα/PPARα-independent pathway. In summary, OSLY exhibits a lipid-lowering effect by reducing cholesterol absorption through interfering with the physicochemical properties of intestinal cholesterol micelles. As a result, OSLY is a promising alternative nutraceutical product aimed to prevent individuals with hyperlipidemia.

This study evaluated the hypoglycemic potential of a concentrated extract obtained from Clitoria ternatea extract (CTE), collected from Tay Ninh Province, Vietnam. The extract was obtained by aqueous extraction and characterized using LC–HRMS, revealing the presence of several bioactive compounds, including delphinidin derivatives, kaempferol 3-(6′-p-coumaroyl)-rutinoside, cyanidin-3-(p-coumaroyl) glucose, and kaempferol-rhamnosyl-malonyl-glucoside. Cyanidin-3-(p-coumaroyl) glucose was identified as the predominant anthocyanin and is considered a major candidate underlying the pharmacological activity of CTE. An in vivo study conducted on Mus musculus mice demonstrated that administration of CTE at a dose of 500 mg/kg body weight exhibited comparable antidiabetic efficacy to gliclazide administered at 10 mg/kg/day. CTE treatment significantly reduced blood glucose levels, with a final mean value of 158.00 mg/dL, indicating its potential antidiabetic activity. Given its established antioxidant and metabolic regulatory properties, cyanidin-3-(p-coumaroyl) glucose is likely to play a central role in the antidiabetic effect observed. Overall, the results emphasize the therapeutic relevance of CTE and warrant further investigation of cyanidin-3-(p-coumaroyl) glucose as a candidate for glycemic regulation.

Chronic hyperglycemia is one of the main causes of diabetes mellitus, a common metabolic disorder. α-Amylase inhibition, a key enzyme in carbohydrate digestion, is an appealing strategy for the regulation of postprandial blood glucose levels. The current research explored the α-amylase inhibitory activity of Pithecellobium dulce (Roxb.) leaf extracts by phytochemical analysis, GC–MS, in vitro enzyme assays, and in silico molecular modeling, including ADME, toxicity predictions, and molecular dynamics (MD) simulations. Among four solvent extracts, the ethyl acetate (EA) extract had the highest total phenolic (131.26 mg GAE/g) and flavonoid (244.78 mg CE/g) contents and exhibited 70.51% α-amylase inhibition at 400 μg/mL, approaching the activity of acarbose (82.72%). GC–MS analysis of the EA extract identified several bioactive constituents, with 3,7,11,15-tetramethyl-2-hexadecen-1-ol and 2-hexadecen-1-ol acetate exhibiting good docking scores (−5.9 and −5.7 kcal/mol, respectively). Among them, 1-cyclohexanol, 2-(2-ethylbutyl)- showed the best drug-likeness with good oral bioavailability (0.794) and zero predicted toxicity. MD simulations (100 ns) confirmed the stability of ligand–enzyme complexes with minimal RMSD fluctuations and stable hydrogen bonding. The findings suggest that P. dulce EA extract and phytocompounds are potential natural α-amylase inhibitors and putative antidiabetic drugs, meriting further in vivo validation.

Fritillaria thunbergii Miq. (FTM), a traditional medicinal and edible herb, has shown promise in alleviating metabolic disturbances, yet its mechanistic basis remains unclear. In this study, we investigated the therapeutic effects of FTM aqueous extract in a male KM mouse model of obesity induced by a high-sugar, high-fat diet (HSFD). A 7-week intervention with FTM significantly ameliorated obesity-related phenotypes, including weight gain, insulin resistance, hyperlipidemia, and histopathological damage in the liver and pancreas. Comprehensive RT-qPCR profiling of 38 hepatic genes revealed coordinated modulation of lipid metabolism (e.g., SREBP1 and FAS), insulin signaling (e.g., IRS1 and GLUT2), inflammation (e.g., NF-κB and IL-10), and mitochondrial function (e.g., PGC-1α), indicating transcriptional reprogramming as a core mechanism. UPLC-QTOF-MS identified eight cevanine-type alkaloids—including peimine, peiminine, and their glycosides—as major constituents, potentially contributing to the observed bioactivity via anti-inflammatory and metabolic regulatory pathways. Moreover, 16S rRNA sequencing demonstrated that FTM reshaped gut microbiota composition by enriching SCFA-producing taxa such as Lachnospiraceae and Faecalibaculum while suppressing Akkermansia overgrowth. Functional predictions further indicated normalization of microbial metabolic pathways disrupted by HSFD. These findings demonstrate that FTM exerts systemic benefits through the integrated modulation of hepatic gene networks, bioactive phytochemicals, and gut microbial communities, supporting its development as a multitarget functional food for the management of glycolipid metabolic disorders.

Numerous medical and food dual-purpose herbs have been used for thousands of years and are still gaining influence in our daily lives. However, there are still two major questions, including chemical standardization and efficacy of these herbs, remaining to be addressed. In this special issue, we received the latest studies on the chemical composition and health efficacy of medical and food dual-purpose herbs. These findings enrich our understanding of the chemical composition and health efficacy of medical and food dual-purpose herbs, which can be helpful to develop functional foods and drugs for the prevention and control of various diseases.

The cladodes and fruits of many Opuntia species that grow in the wild and are cultivated in México are consumed fresh or after processing in the form of jams and juices. Although the peels that result from this processing can be used as livestock feed, a large amount of this byproduct is discarded. In order to explore the possibility that this peel byproduct may represent a source of functional components, the polyphenol composition and antioxidant activity of the peels from the fruits of six Mexican Opuntia species (O. ficus-indica, O. megacantha, O. robusta, O. albicarpa, O. undulata, and O. joconostle) have been determined. Ferulic, protocatechuic, gallic, sinapic, and p-coumaric acids were the most abundant polyphenols. The main phenolic acid, ferulic acid, ranged from 30.5% to 41.5% in the extracts and from 23.2% to 40.9% in the encapsulated. The original polyphenol extracts exhibited higher antioxidant activity than the corresponding encapsulated extracts as determined using the ABTS, DPPH, and ORAC assays, but the antioxidant activity was higher in the encapsulate extracts when determined using the Caco-2/DCFH assay. O. ficus-indica polyphenol extracts showed the highest ABTS and DPPH scavenging activities with 59.4 and 41.2 μM Trolox equivalents/g_dw, while O. robusta-encapsulated polyphenols showed the highest ABTS and DPPH scavenging activities with 39.7% and 36.0% μM Trolox/g_dw, respectively. The encapsulated extracts from O. undulata and O. joconostle yielded the highest cell antioxidant activity at all the concentrations that were assayed. These results highlight the important effect that encapsulation has on the antioxidant activity and support the potential use of the Opuntia peel byproduct as a source of health-promoting components.

Myocardial ischemia-reperfusion injury (MIRI) stands as a critical determinant undermining the therapeutic efficacy of revascularization procedures in treating myocardial infarction cases. Among the various injury mechanisms discussed herein, oxidative stress plays a crucial role, with nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 4 (NOX4) identified as a key enzyme responsible for orchestrating the production of reactive oxygen species (ROS). Astragaloside IV (AS-IV), an extract derived from Astragalus membranaceus, a traditional Chinese medicinal herb, exhibits antioxidative stress properties. In this study, we aimed to investigate the efficacy of AS-IV in mitigating MIRI and to elucidate the underlying regulatory mechanisms. We established a model of MIRI in Sprague–Dawley (SD) rats and employed an oxygen-dependent glycan deprivation/reoxygenation (OGD/R) model using the rat myocardial H9C2 cell line. AS-IV treatment significantly mitigated cardiac functional injury, pathological damage, and the infarct area resulting from ischemia-reperfusion (I/R). Furthermore, AS-IV administration effectively reduced oxidative stress levels both in vitro and in vivo. It has been demonstrated that AS-IV modulates ROS production and alleviates oxidative stress associated with I/R injury by inhibiting NOX4 expression. Therefore, AS-IV exhibits considerable potential as a therapeutic intervention for the management of myocardial I/R.