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1.
Molecules ; 27(18)2022 Sep 08.
Article in English | MEDLINE | ID: mdl-36144552

ABSTRACT

This study aimed to produce bioactive protein hydrolysates from undervalued fish, namely Baltic herring, and its filleting by-products. Protein hydrolysates were produced with Alcalase and Flavourzyme to achieve effective hydrolysis. The hydrolysates were evaluated for chemical composition, molecular weight distribution, antioxidant capacity, dipeptidyl-peptidase 4 (DPP4) inhibitory activity, effects on cell proliferation and surface hydrophobicity. The protein content of the hydrolysates was high, from 86% to 91% (dm), while the fat content was low, from 0.3% to 0.4% (dm). The hydrolysates showed high DPP4 inhibition activities with IC50 values from 5.38 mg/mL to 7.92 mg/mL. The scavenging activity of the hydrolysates towards DPPH was low, but an intermediate Folin-Ciocalteu reducing capacity and Cu2+ chelating ability was observed. The solid phase extraction with Sep-Pak C18 cartridges increased the DPP4 inhibition activity and antioxidant capacity, indicating peptides' crucial role in the bioactivities. The cytotoxicity of the hydrolysates was evaluated on the HCT8, IMR90, and A549 cell lines. The hydrolysates inhibited cell growth in the cancer and normal cells, although they did not reduce cell viability and were not lethal. Overall, our results indicate that protein hydrolysates from Baltic herring have potential as health-promoting foods and nutraceuticals, especially for enhancing healthy blood glucose regulation.


Subject(s)
Dipeptidyl Peptidase 4 , Protein Hydrolysates , Animals , Antioxidants/chemistry , Antioxidants/pharmacology , Blood Glucose , Dipeptidyl Peptidase 4/chemistry , Fishes/metabolism , Hydrolysis , Peptides/chemistry , Peptides/pharmacology , Protein Hydrolysates/chemistry , Protein Hydrolysates/pharmacology , Subtilisins/metabolism
2.
Bioorg Chem ; 108: 104683, 2021 03.
Article in English | MEDLINE | ID: mdl-33545534

ABSTRACT

The EtOH extracts of the dried seeds of Alpinia katsumadai were revealed with hypoglycemic effects on db/db mice at the concentration of 200 mg/kg. In order to clarify the antidiabetic constituents, 16 new diarylheptanoid-chalcone hybrids, katsumadainols A1-A16 (1-16), together with 13 known analogues (17-29), were isolated from A. katsumadai under the guidance of bioassay. Most of the compounds showed α-glucosidase and PTP1B dual inhibition, among which compounds 1-3, 5-7, 11-14, 21-25, and 27 showed PTP1B/TCPTP selective inhibition with IC50 values ranging from 22.0 to 96.7 µM, which were 2-10 times more active than sodium orthovanadate (IC50, 215.7 µM). All compounds exhibited obvious inhibition against α-glucosidase with IC50 values of 2.9-29.5 µM, indicating 6-59 times more active than acarbose (IC50, 170.9 µM). Study of enzyme kinetics indicated compounds 1, 3, and 12 were PTP1B and α-glucosidase mixed-type inhibitors with Ki values of 13.1, 12.9, 21.6 µM, and 4.9, 7.4, 3.4 µM, respectively.


Subject(s)
Alpinia/enzymology , Chalcones/pharmacology , Diarylheptanoids/pharmacology , Enzyme Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/pharmacology , Hypoglycemic Agents/pharmacology , Animals , Chalcones/chemistry , Chalcones/isolation & purification , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/metabolism , Diarylheptanoids/chemistry , Diarylheptanoids/isolation & purification , Disease Models, Animal , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/isolation & purification , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Mice , Molecular Structure , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Protein Tyrosine Phosphatase, Non-Receptor Type 1/metabolism , Structure-Activity Relationship , alpha-Glucosidases/metabolism
3.
Crit Rev Food Sci Nutr ; 60(9): 1447-1474, 2020.
Article in English | MEDLINE | ID: mdl-30806077

ABSTRACT

The prevalence of type 2 diabetes mellitus (T2DM) has been increasing throughout the world. The cereals, as the high carbohydrate food and dominant portion of diet, have crucial impacts on glycemic control, especially for T2DM. Both components in whole cereals and processing are closely related to their glycemic response. The consumption of whole cereals is shown to reduce the risk of T2DM. The starch characteristic of cereal determines its hydrolysis rate and glycemic response. The soluble and insoluble dietary fiber, phenolic compounds, and other bioactive constituents may slow down the starch hydrolysis. Besides, they have other physiological mechanisms in regulation of T2DM, such as amelioration of lipid disorder, antioxidant, anti-inflammation, and regulation of gut microbiota, which contribute to further improvement of metabolic symptoms. Cereals are subjected to processing before consumption, which is involved in mechanical force, bioprocessing, thermal treatment, and cooling. The processing induces changes in nutritional composition and physical structure compared to the raw kernels. The key influences of processing on glycemic response are the starch gelatinization and starch retrogradation. However, physical structure of cereal and interactions among starch and other compounds greatly contribute to various glycemic responses of cereal products. This review highlights recent findings on the influences of both bioactive constituents and processing on the antidiabetic effects and physiological properties of cereals.


Subject(s)
Diabetes Mellitus, Type 2/metabolism , Edible Grain/metabolism , Blood Glucose/metabolism , Dietary Fiber/metabolism , Edible Grain/chemistry , Humans , Starch/metabolism
4.
Molecules ; 24(4)2019 Feb 21.
Article in English | MEDLINE | ID: mdl-30795583

ABSTRACT

Glucagon-like peptide-1 receptor (GLP-1R) agonists have emerged as treatment options for type 2 diabetes mellitus (T2DM). Here, we designed a high-throughput GLP-1R extracellular domain (ECD)-based system that enabled the screening of high-potency receptor-biased GLP-1R agonists demonstrating new pharmacological virtues. Firstly, six 12-mer peptides (termed PEP01⁻06), screened from a large phage displayed peptide library were fused to the N-terminus of Exendin-4 (29⁻39) to generate PEP07⁻12. By the use of four lysine-altered PEP07 (PEP13⁻16) as the starting point, a series of fatty chain conjugates (PEP17⁻20) were synthesized and evaluated by in vitro GLP-1R-based cell assays. In addition, the acute and long-term in vivo effects on diet-induced obesity (DIO) mice were further evaluated. All four conjugates showed good receptor activation efficacy, and PEP20 was selected to undergo further assessment. Preclinical experiments in DIO mice demonstrated that PEP20 had significant insulinotropic activities and glucose-lowering abilities. Moreover, a prolonged antidiabetic effect of PEP20 was also observed by the hypoglycemic test in DIO mice. Furthermore, long-term treatment with PEP20 achieved beneficial effects on the food intake, weight gain, hemoglobin A1C (HbA1C) lowering activity, and glucose tolerance compared with the control and was similar to the Liraglutide. In conclusion, PEP20, a GLP-1R ECD-biased agonist, may provide a novel therapeutic approach to T2DM.


Subject(s)
Glucagon-Like Peptide-1 Receptor/agonists , Glycoconjugates/pharmacology , Hyperglycemia/drug therapy , Hypoglycemic Agents/pharmacology , Insulin-Secreting Cells/drug effects , Obesity/drug therapy , Amino Acid Sequence , Animals , Binding Sites , Cell Line , Diet, High-Fat/adverse effects , Exenatide/genetics , Exenatide/metabolism , Fatty Acids/chemistry , Gene Expression Regulation , Glucagon-Like Peptide-1 Receptor/genetics , Glucagon-Like Peptide-1 Receptor/metabolism , Glucose Tolerance Test , Glycoconjugates/chemistry , Glycoconjugates/metabolism , Hyperglycemia/etiology , Hyperglycemia/genetics , Hyperglycemia/metabolism , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/metabolism , Insulin-Secreting Cells/metabolism , Insulin-Secreting Cells/pathology , Male , Mice , Obesity/etiology , Obesity/genetics , Obesity/metabolism , Peptide Library , Peptides/chemistry , Peptides/metabolism , Peptides/pharmacology , Protein Binding , Rats , Structure-Activity Relationship
5.
Vopr Pitan ; 88(1): 85-90, 2019.
Article in Russian | MEDLINE | ID: mdl-30811138

ABSTRACT

Antidiabetic properties of vanadium are known more than 100 years, however the researches of specific therapeutic usage of vanadium were conducted only in the last two decades. Along with, the organic vanadium compounds are more harmless in comparison with inorganic vanadium salts. Thus, the development of method of obtaining the organic source of vanadium with high bioavailability is prospective field. Aim of the work was to obtain and provide the physical-chemical characterization of vanadium complex with enzymatic hydrolysate of soy protein isolate (SPI), obtained by one-stage enzymatic hydrolysis. MATERIAL AND METHODS: The complex was obtained at room temperature: 10% water solution of SPI was mixed with 25% solution of vanadium salt (VOSO4×хH2O) in ratio 10:1 (in dry matter). The reaction was kept during 1 h at constant mixing with pH kept at 7.0- 7.1 with 1.0 M NaOH. The concentration of vanadium was determined in dry product by means of inductively coupled plasma mass-spectrometry. The chromatograms of SPI and V-SPI were obtained by means of size-exclusion high-pressure liquid chromatography, and then were integrated by weight method in the range of free till full column volume. RESULTS AND DISCUSSION: The obtained complex of vanadium with SPI enzymatic hydrolysate (V-SPI) was water-soluble and contained 15.8 mg of vanadium per gram of product dry weight. Analysis of the molecular weight distribution of the peptide fractions of the original SPI enzymatic hydrolysate and the V-SPI complex showed that more than 87% of the vanadium complex was in peptide fractions with molecular weights more than 4.1 kD, including more than 75% of vanadium contained in fractions with molecular weights from 14.6 to 4.1 kD. CONCLUSION: The experimental evaluation in vivo will be the next stage of this research. The complex bioavailability and its effects on carbohydrate and lipid metabolism of Wistar rats with obesity will be evaluated.


Subject(s)
Hypoglycemic Agents/analysis , Protein Hydrolysates/analysis , Soybean Proteins/analysis , Vanadium/analysis , Animals , Chromatography, High Pressure Liquid , Hypoglycemic Agents/chemistry , Mass Spectrometry , Obesity , Protein Hydrolysates/chemistry , Rats , Rats, Wistar , Soybean Proteins/chemistry , Vanadium/chemistry
6.
Pharm Biol ; 55(1): 2020-2025, 2017 Dec.
Article in English | MEDLINE | ID: mdl-28832229

ABSTRACT

CONTEXT: Diabetic liver injury is a serious diabetic complication. The alterations of intestinal microbiota play an important role in induction and promotion of liver injury progression. Physalis alkekengi L. var. francheti (Mast.) Makino (Solanaceae) has been used as a water decoction for treating diabetes. OBJECTIVE: To study the effects of a polysaccharide (PPSB) from Physalis alkekengi var. francheti on liver injury and intestinal microflora in type-2 diabetic mice. MATERIALS AND METHODS: Streptozotocin (160 mg/kg) was injected i.p. for 3 days to build model. The diabetic mice were randomly divided into four groups together with control group (10 mice in each group). The doses of PPSB were 50 and 100 mg/kg, respectively. After 5 weeks administration, level of blood glucose, ALT and AST were measured. Alterations of intestinal microflora, and protein expression of TGF-ß1, TNF-α and DCN were detected. RESULTS: Level of blood glucose decreased from (25.38 ± 2.21) mmol/L to (18.01 ± 2.53) mmol/L, ALT and AST decreased to (24.67 ± 4.86) U/L and (30.84 ± 7.50) U/L in PPSB-H group. Lactobacillus, Clostridium butyricum, and Bacteroides increased remarkably with increasing concentration of PPSB, but Enterobacter was inhibited. The relative expression of TGF-ß1 and TNF-α decreased to (0.70 ± 0.17) and (0.39 ± 0.06), and the expression of DCN increased to (0.65 ± 0.13). DISCUSSION AND CONCLUSIONS: Probiotics have been promoted by PPSB, and protein expressions have been modulated in the progression of liver injury. PPSB could be used as a natural agent for treating diabetic liver injury and intestinal microflora imbalance.


Subject(s)
Diabetes Complications/drug therapy , Diabetes Mellitus, Type 2/drug therapy , Gastrointestinal Microbiome/drug effects , Liver Diseases/drug therapy , Physalis , Polysaccharides/therapeutic use , Animals , Diabetes Complications/metabolism , Diabetes Complications/microbiology , Diabetes Mellitus, Type 2/metabolism , Diabetes Mellitus, Type 2/microbiology , Gastrointestinal Microbiome/physiology , Liver Diseases/metabolism , Liver Diseases/microbiology , Male , Mice , Polysaccharides/isolation & purification , Polysaccharides/pharmacology , Random Allocation
7.
Pharm Biol ; 54(12): 3086-3092, 2016 Dec.
Article in English | MEDLINE | ID: mdl-27558859

ABSTRACT

CONTEXT: Diabetes is a serious endocrine and metabolic disorder. Food supplements attract people's attention in mitigating health problems from the aspect of gastrointestinal microflora. Maydis stigma (Zea mays subsp. mays L. [Poaceae]), has been used as water decoction for treating diabetes in folk medicine. It has great potential, and feasibly a stable form of Maydis stigma commercial products could be developed to fulfil the health food market. OBJECTIVE: To study the effects of Maydis stigma polysaccharide (MSP) on the intestinal microflora in type-2 diabetes (T2D). MATERIALS AND METHODS: MSP was fractioned from Maydis stigma by distilled water, purified by DEAE-52 Cellulose chromatography and Sephadex G-200 gel column. Streptozotocin (160 mg/kg) was intraperitoneal injected for 3 days to build model. The diabetic mice were randomly divided into five groups together with control group (10 mice in each group). The doses of MSP were 400, 600 and 800 mg/kg, respectively. After 5 weeks of administration, antidiabetic effects and intestinal microflora balance restoring activities were evaluated by denaturing gradient gel electrophoresis. RESULTS: Blood glucose levels of MSP-treated groups showed extremely significant hypoglycemic effects (p < 0.01), body weight increased showed extremely significant (p < 0.01) differences. Bacteroides, Lactobacillus and Prevotella were dominant organisms in the intestinal tract. The quality and quantity of Lactobacillus and Bacteroides genus increased remarkably with increasing concentration of MSP. DISCUSSION AND CONCLUSION: Experimental results of this study suggest that MSP has the significant potential to be used as a natural agent for treating T2D and restoring the intestinal microflora balance.


Subject(s)
Diabetes Mellitus, Experimental/drug therapy , Gastrointestinal Microbiome/drug effects , Hypoglycemic Agents/pharmacology , Plant Extracts/pharmacology , Polysaccharides/pharmacology , Zea mays , Animals , Diabetes Mellitus, Experimental/metabolism , Gastrointestinal Microbiome/physiology , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/therapeutic use , Male , Mice , Plant Extracts/isolation & purification , Plant Extracts/therapeutic use , Polysaccharides/isolation & purification , Polysaccharides/therapeutic use
8.
Food Chem ; 447: 138916, 2024 Jul 30.
Article in English | MEDLINE | ID: mdl-38461723

ABSTRACT

As one of the most abundant plant polyphenols in the human diet, (-)-epicatechin (EC) can improve insulin sensitivity and regulate glucose homeostasis. However, the primary mechanisms involved in EC anti-T2DM benefits remain unclear. The present study explored the effects of EC on the gut microbiota and liver transcriptome in type 2 diabetes mellitus (T2DM) Goto-Kakizaki rats for the first time. The findings showed that EC protected glucose homeostasis, alleviated systemic oxidative stress, relieved liver damage, and increased serum insulin. Further investigation showed that EC reshaped gut microbiota structure, including inhibiting the proliferation of lipopolysaccharide (LPS)-producing bacteria and reducing serum LPS. In addition, transcriptome analysis revealed that the insulin signaling pathway may be the core pathway of the EC anti-T2DM effect. Therefore, EC may modulate the gut microbiota and liver insulin signaling pathways by the gut-liver axis to alleviate T2DM. As a diet supplement, EC has promising potential in T2DM prevention and treatment.


Subject(s)
Catechin , Diabetes Mellitus, Type 2 , Gastrointestinal Microbiome , Rats , Humans , Animals , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/genetics , Catechin/metabolism , Lipopolysaccharides/pharmacology , Blood Glucose/metabolism , Insulin , Liver/metabolism
9.
Heliyon ; 10(3): e25058, 2024 Feb 15.
Article in English | MEDLINE | ID: mdl-38317880

ABSTRACT

The purpose of this inquiry is to provide a conprehensive summary and analysis of the literature concerning the pharmacological properties of components that can be extracted from Desmodium styracifolium, a preparation in Chinese medicine. This study also aims to explore their potential application in elaborating medicinal products for the effective prevention and treatment of such conditions as urolithiasis, cholelithiasis, type 2 diabetes mellitus, metabolic syndrome, pro-oxidant and inflammatory processes, etc. Several experimental studies confirmed the potential of D. styracifolium to influence mineral metabolism, to decrease the concentration of constituents involved in the formation of urinary calculi, and to reduce mineral encrustation in the urinary tract, as well as to alleviate the damage caused by crystal structures. This beneficial impact is achieved through a combination of antioxidant and anti-inflammatory actions, along with urine alkalinization. The cholelitholytic, choleretic, and hepatoprotective effects of D. styracifolium plants have been confirmed, primarily ascribed to the activation of the hepatic Xα receptor and the bile acid receptor, farnesoid X receptor, by the flavonoid shaftoside. Special attention is focused on the potential therapeutic applications of flavonoids derived from D. styracifolium for diseases associated with the development of chronic inflammation and systemic response, emphasizing the ability of flavonoids to exert antioxidant and anti-inflammatory effects by acting directly and through the modulation of transcription factors. It is concluded that new strategies for the prevention and treatment of urolithiasis, cholelithiasis, type 2 diabetes mellitus, metabolic syndrome, acute and chronic inflammatory processes may rely on the promising development of dosage forms of D. styracifolium with their subsequent preclinical and clinical trials.

10.
Anaerobe ; 24: 4-11, 2013 Dec.
Article in English | MEDLINE | ID: mdl-23999246

ABSTRACT

This study aimed to assess the potential of the probiotic strain Lactobacillus plantarum TN627 for preventing alloxan-induced diabetes in rats. The oral administration of this probiotic was noted to significantly improve the immunological parameters, protect the pancreatic tissues, and reduce the pancreatic and plasmatic α-amylase activities and level of plasma glucose in the treated as compared to the control group of rats. Furthermore, this probiotic treatment was observed to markedly reduce pancreatic and plasmatic lipase activities and serum triglyceride and LDL-cholesterol rates and to increase the level of HDL-Cholesterol. It also exerted efficient protective effects on the liver and kidney functions evidenced by significant decreases in serum aspartate transaminase, alanine transaminase, lactate dehydrogenase, and gamma-glutamyl transpeptidase activities, as well as creatinine and urea contents. Taken together, the findings indicate that L. plantarum TN627 exhibits attractive in vivo antidiabetic effects that may be helpful in preventing diabetic complications in adult rats.


Subject(s)
Diabetes Mellitus, Experimental/prevention & control , Lactobacillus plantarum/physiology , Probiotics/pharmacology , Animals , Diabetes Mellitus, Experimental/pathology , Lactobacillus plantarum/growth & development , Male , Rats , Rats, Wistar
11.
Article in English | MEDLINE | ID: mdl-37194227

ABSTRACT

Diabetes mellitus is a metabolic disease recognized by abnormal glucose level due to defects in insulin action, insulin secretion, or both. Administration of soybean and isoflavones are accompanied by a lower risk of diabetes. The present review analyzed the previous published papers related to genistein. This isoflavone, which has been used for the prevention of some chronic diseases can inhibit hepatic glucose production, increase ß-cell proliferation, reduce ß-cell apoptosis, and show potential antioxidant and anti-diabetic effects. Therefore, genistein may be useful in the management of diabetes. The beneficial effects of this isoflavone on metabolic syndrome, diabetes, cardiovascular disease, osteoporosis, and cancer have been reported in animal and human studies. Moreover, genistein reduces hepatic glucose production, normalizes hyperglycemia, and gut microbiota and exhibits potential anti-oxidative, anti-apoptotic, and hypolipidemic effects. However, studies on the underlying mechanisms of the action of genistein are very limited. Therefore, the present study reviews multifaceted aspects of genistein to reveal a possible anti-diabetic mechanism of this agent. Genistein by regulating several signaling pathways can be used for the prevention and management of diabetes.

12.
J Nutr Biochem ; 111: 109173, 2023 01.
Article in English | MEDLINE | ID: mdl-36228975

ABSTRACT

The antidiabetic effects of green tea have been demonstrated in clinical trials and epidemiological studies. This study investigated the antidiabetic effects of green tea extract (GTE) and its underlying molecular mechanisms using a leptin receptor-deficient db/db mouse model (Leprdb/db). Treatment with GTE for 2 weeks improved glucose tolerance and insulin sensitivity in Leprdb/db mice. In addition, GTE treatment reduced the body weight and adiposity of Leprdb/db mice. Furthermore, GTE treatment reduced pro-inflammatory gene expression, including nuclear factor kappa B (NF-κB) in white adipose tissue (WAT), and also reduced dipeptidyl peptidase-4 (DPP4) expression levels in WAT as well as in the serum. The promoter region of Dpp4 contains the NF-κB binding site, and DPP4 was found to be a direct target of NF-κB. Consistently, in vitro treatment of cells with GTE or its main constituent epigallocatechin gallate reduced lipopolysaccharide-induced NF-κB/DPP4 expression in 3T3-L1 adipocytes and RAW264.7 cells. Overall, our data demonstrated that GTE exerts an anti-diabetic effect by regulating the expression levels of NF-κB and DPP4 in WAT.


Subject(s)
Dipeptidyl Peptidase 4 , Hypoglycemic Agents , Mice , Animals , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Hypoglycemic Agents/metabolism , Dipeptidyl Peptidase 4/genetics , Dipeptidyl Peptidase 4/metabolism , NF-kappa B/metabolism , Plant Extracts/therapeutic use , Adipose Tissue/metabolism , Tea/chemistry
13.
Biomed Pharmacother ; 165: 115126, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37494787

ABSTRACT

Several medicinal plants have drawn the attention of researchers by its phytochemical composition regarding their potential for treating chronic complications of diabetes mellitus. In this context, plants of the Myrtaceae family popularly used in Brazil for the treatment of diabetes mellitus, including Eugenia sonderiana, have shown beneficial effects due to the presence of phenolic compounds and saponins in their chemical constitution. Thus, the present work aimed to perform the phytochemical characterization of the hydroethanolic extract of E. sonderiana leaves using high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS), along with in vitro and in vivo studies of antidiabetic activity. The chemical characterization revealed the presence of phenolic compounds, flavonoids, neolignans, tannins, and saponins. In addition, the extract exhibited minimum inhibitory concentrations of alpha-amylase and alpha-glycosidase higher than the acarbose in the in vitro tests. Also, the in vivo tests revealed a slight increase in body mass in diabetic rats, as well as a significant decrease in water and feed consumption provided by the extract. Regarding serum biochemical parameters, the extract showed significant activity in decreasing the levels of glucose, hepatic enzymes, and triglycerides, in addition to maintaining HDL cholesterol levels within normal ranges, protecting the cell membranes against oxidative damage. Thus, the extract of E. sonderiana leaves was considered promising pharmaceutical ingredient in the production of a phytotherapy medication.


Subject(s)
Diabetes Mellitus, Experimental , Eugenia , Saponins , Rats , Animals , Hypoglycemic Agents/therapeutic use , Plant Extracts/therapeutic use , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Phytochemicals/therapeutic use , Phenols/pharmacology , Plant Leaves/chemistry , Saponins/therapeutic use
14.
Curr Res Food Sci ; 6: 100446, 2023.
Article in English | MEDLINE | ID: mdl-36816000

ABSTRACT

In the present study, the antidiabetic properties of Trachinotus ovatus protein hydrolysates (TOH) in streptozotocin-induced diabetic mice were investigated, and peptides with α-amylase (AAM) and dipeptidyl peptidase IV (DPP-IV) inhibitory activities were identified and screened. The results showed that TOH alleviated body weight loss, polyphagia, blood glucose elevation and insulin secretion decline in diabetic mice. After 4 weeks of TOH administration, random blood glucose (RBG) decreased significantly. The TOH groups showed a dose-dependent reduction in fasting blood glucose (FBG), especially in the high-dose TOH group, which reduced FBG by 58% versus the effect of metformin. Moreover, TOH exerted a remarkable protective effect on hepatorenal function, as evidenced by increased superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) and decreased serum urea levels. Histopathological studies confirmed that TOH can significantly protect the kidney and pancreas from histological changes, which was of great benefit for ensuring the normal secretion of insulin and preventing the occurrence of complications such as diabetic nephropathy. Two fractions with higher inhibitory activity against AAM and DPP-IV, F4 and F6, were obtained from the ultrafiltration of TOH-2 (≤3 kDa). A total of 19 potentially active peptides from F4 and 3 potentially active peptides from F6 were screened by LC‒MS/MS combined with bioinformatic analysis. These peptides are small molecular peptides composed of 2-6 amino acids, rich in characteristic amino acids such as proline, arginine, phenylalanine and asparagine, and contain high proportions of peptides (68% for F4, 67% for F6) with hydrophobicity ≥50%. They offer potent antidiabetic potential and could potentially bind to the active sites in the internal cavities of the target enzymes AAM and DPP-IV. In summary, this study revealed for the first time the antidiabetic effects of protein hydrolysates of Trachinotus ovatus and their derived peptides, which are promising natural ingredients with the potential to be used for the treatment or prevention of diabetes.

15.
Fitoterapia ; 167: 105502, 2023 Jun.
Article in English | MEDLINE | ID: mdl-37023930

ABSTRACT

Five new diarylheptanoids, kaemgalangins A-E (1-5), and seven known ones were isolated from the rhizomes of Kaempferia galanga. The structures of new compounds were identified by spectroscopic analyses involving 1D and 2D NMR, HRESIMS, IR, UV, [α]D, ECD calculations, and chemical methods. All compounds were tested for their hypoglycemic effects against α-glucosidase, Gpa and PTP1B enzymes, and stimulative effects on GLP-1 secretion. Kaemgalangins A (1) and E (5) showed significant inhibition on α-glucosidase with IC50 values of 45.3 and 116.0 µM; renealtin B (8) showed inhibition on GPa with an IC50 value of 68.1 µM; whereas all compounds were inactive to PTP1B. Docking study manifested that 1 well located in the catalytic pocket of α-glucosidase and OH-4″ played important roles in maintaining activity. Moreover, all compounds showed obviously stimulative effects on GLP-1 with promoting rates of 826.9%-1738.3% in NCI-H716 cells. This study suggests that the diarylheptanoids in K. galanga have antidiabetic potency by inhibiting α-glucosidase and Gpa enzymes, and promoting GLP-1 secretion.


Subject(s)
Alpinia , Zingiberaceae , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , alpha-Glucosidases , Rhizome/chemistry , Molecular Structure , Zingiberaceae/chemistry , Magnetic Resonance Spectroscopy , Diarylheptanoids/pharmacology , Diarylheptanoids/chemistry , Glycoside Hydrolase Inhibitors/pharmacology
16.
Antioxidants (Basel) ; 11(6)2022 Jun 06.
Article in English | MEDLINE | ID: mdl-35740019

ABSTRACT

The ameliorative and antioxidative stress effects of probiotic-enriched fermented oat (FOE) or fermented oat with honey (HFOE) extracts on streptozotocin-induced diabetes in rats were examined. The total phenolic content (TPC) and antioxidant activity (AOA) were increased in FOE and HFOE after 72 h of fermentation, and γ-aminobutyric acid (GABA) reached 7.35 mg 100 g-1 in FOE and 8.49 mg 100 g-1 in HFOE. The ß-glucan levels were slightly decreased to 2.45 g 100 g-1 DW in FOE and 2.63 g 100 g-1 DW in HFOE. The antidiabetic and hypolipidemic properties of FOE and HFOE were studied in a designed animal model with seven treated groups for 6 weeks. Groups were treated as follows: group 1 (negative group, NR) and group 2 (diabetic rats, DR) were administered 7 mL distilled water orally per day; group 3 (DR + MET) rats were orally administered 50 mg standard drug Metformin kg-1 daily; group 4 (DR + FOE1) diabetic rats were orally administered 3.5 mL FOE daily; group 5 (DR + FOE2) rats were orally administered 7 mL FOE daily; group 6 (DR + HFOE1) rats were orally administered 3.5 mL HFOE daily; and group 7 (DR + HFOE2) rats were orally administered 7 mL HFOE daily. The HFOE at the high dose had a synergistic effect, lowering random blood glucose (RBG) and fasting blood glucose (FBG). The hypolipidemic potential of HFOE at the high dose was indicated by significant reductions in triglycerides (TG), total cholesterol (CHO), high- and low-density lipoproteins (HDL and LDL), and very-low-density lipoproteins (VLDL). In addition, 7 mL of HFOE improved liver and kidney function more effectively than other fermented extracts or Metformin. As well as the antioxidant enzyme activity, reduced glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), and malonaldehyde (MDA) were significantly enhanced after the administration of HFOE at 7 mL by 68.6%, 71.5%, 55.69%, and 15.98%, respectively, compared to the DR group. In conclusion, administration of L. plantarum-fermented oats supplemented with honey demonstrated antidiabetic effects and a potential approach for controlling glucose levels and lipid profiles, and protecting against oxidative stress.

17.
J Agric Food Chem ; 70(17): 5369-5376, 2022 May 04.
Article in English | MEDLINE | ID: mdl-35445595

ABSTRACT

Branched fatty acid ester of hydroxy fatty acid (FAHFA) is a class of natural lipid with important biological functions. In this study, we first profiled natural-origin FAHFAs in different teas using the chemical labeling-assisted liquid chromatography-mass spectrometry method. Consequently, we observed rich molecular diversity of FAHFAs with multiple regioisomers in teas. Additionally, the FAHFA contents had a positive relationship with the tea fermentation degree and a negative relationship with homologous fatty acids. Moreover, the highly accumulated FAHFAs (e.g., 3-MAHMA) in some postfermented teas (e.g., Fu brick tea) were also basically interpreted with regiospecificity of FAHFAs in both teas and fungus. This study revealed that tea is a rich natural source of FAHFAs, and some abundant FAHFAs might be the functional molecules accounting for the antidiabetic function of teas.


Subject(s)
Esters , Fatty Acids , Chromatography, Liquid/methods , Esters/chemistry , Fatty Acids/chemistry , Mass Spectrometry , Tea
18.
J Prev Med Hyg ; 63(2 Suppl 3): E36-E43, 2022 Jun.
Article in English | MEDLINE | ID: mdl-36479477

ABSTRACT

The Mediterranean diet is the most well-known and researched dietary pattern worldwide. It is characterized by the consumption of a wide variety of foods, such as extra-virgin olive oil (EVOO), legumes, cereals, nuts, fruits, vegetables, dairy products, fish, and wine. Many of these foods provide several phytonutrients, among which polyphenols and vitamins play an important role. Data from several studies have strongly established that nutrition is a key factor in promoting a healthy lifestyle and preventing many chronic diseases. In particular, a large number of studies have established the protective effects of the Mediterranean diet against several chronic diseases, among which are diabetes, cardiovascular diseases, cancer, aging disorders, and against overall mortality. Animal and human translational studies have revealed the biological mechanisms regulating the beneficial effects of the traditional Mediterranean diet. Indeed, several studies demonstrated that this nutritional pattern has lipid-lowering, anticancer, antimicrobial, and anti-oxidative effects. Moreover, the Mediterranean diet is considered environmentally sustainable. In this review, we describe the composition of the Mediterranean diet, assess its beneficial effects, and analyze their epigenomic, genomic, metagenomic, and transcriptomic aspects. In the future it will be important to continue exploring the molecular mechanisms through which the Mediterranean diet exerts its protective effects and to standardize its components and serving sizes to understand more precisely its effects on human health.


Subject(s)
Diet, Mediterranean , Humans
19.
J Biomol Struct Dyn ; 40(23): 12491-12505, 2022.
Article in English | MEDLINE | ID: mdl-34488558

ABSTRACT

The amelioration of postprandial hyperglycemia in diabetic conditions could be accomplished by the inhibition of α-glucosidases, a set of intestinal carbohydrate digestive enzymes responsible for starch hydrolysis and its absorption. The ethnopharmacological profile of banana depicts the usage of different plant parts in conventional medicinal formulations. The antidiabetic studies of the plant have demonstrated their ability to inhibit α-glucosidase. Besides, our research group has reported the α-glucosidase inhibitory potential of the banana pseudostem and flower extracts in previous studies. In this study, we deliberate on the specific phytoconstituents of banana pseudostem and flower to evaluate their antidiabetic effects through an in silico perspective for the α-glucosidase inhibition. In this context, several phytoconstituents of banana pseudostem and flower identified through GC-MS analysis were retrieved from chemical databases. These phytochemicals were virtually screened through the molecular docking simulation process, from which only two flavonoids (catechin and quercetin) were selected based on their binding affinity and extent of interaction with the α-glucosidase target protein. The lower binding affinities of catechin and quercetin in comparison with that of acarbose as a control proved their binding efficiency with the target protein. In addition, acarbose showed subservient molecular interaction, forming an unfavourable acceptor-acceptor bond. The molecular dynamics simulations also depicted the effective binding and stability of the complexes formed with catechin and quercetin, in comparison with that of acarbose. Further, PASS analysis, druglikeliness, and pharmacokinetic assessments showed that both catechin and quercetin edge over acarbose in terms of drug-score and pharmacokinetic properties. With the positive results obtained from contemporary strategies, the two flavonoids from banana pseudostem and flower might be established as a considerable phototherapeutic approach to inhibit α-glucosidase. Communicated by Ramaswamy H. Sarma.


Subject(s)
Catechin , Musa , Flavonoids/pharmacology , Flavonoids/chemistry , alpha-Glucosidases/chemistry , Quercetin/pharmacology , Quercetin/chemistry , Acarbose/pharmacology , Musa/metabolism , Glycoside Hydrolase Inhibitors/chemistry , Molecular Docking Simulation , Plant Extracts/chemistry , Hypoglycemic Agents/chemistry , Flowers/chemistry , Flowers/metabolism , alpha-Amylases
20.
J Agric Food Chem ; 70(27): 8274-8287, 2022 Jul 13.
Article in English | MEDLINE | ID: mdl-35767631

ABSTRACT

The antidiabetic effects of Fu brick tea aqueous extract (FTE) and its underlying molecular mechanism in type 2 diabetes mellitus (T2DM) mice were investigated. FTE treatment significantly relieved dyslipidemia, insulin resistance (IR), and hepatic oxidative stress caused by T2DM. FTE also ameliorated the T2DM-induced gut dysbiosis by decreasing the Firmicutes/Bacteroidota (F/B) ratio at the phylum level and promoting the proliferation of Bifidobacterium, Parabacteroides, and Roseburia at the genus level. Besides, FTE significantly improved colonic short-chain fatty acid levels of T2DM mice. Furthermore, the antidiabetic effects of FTE were proved to be mediated by the IRS1/PI3K/Akt and AMPK-mediated gluconeogenesis signaling pathways. Metabolomics analysis illustrated that FTE recovered the levels of 28 metabolites associated with T2DM to the levels of normal mice. Taken together, these findings suggest that FTE can alleviate T2DM by reshaping the gut microbiota, activating the IRS1/PI3K/Akt pathway, and regulating intestinal metabolites.


Subject(s)
Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Gastrointestinal Microbiome , Animals , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Type 2/metabolism , Hypoglycemic Agents/pharmacology , Insulin Receptor Substrate Proteins/metabolism , Mice , Phosphatidylinositol 3-Kinases/genetics , Phosphatidylinositol 3-Kinases/metabolism , Proto-Oncogene Proteins c-akt/genetics , Proto-Oncogene Proteins c-akt/metabolism , Signal Transduction , Tea
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