FOOD CHEMISTRY
·
2022
·
IF 9.231
Yang Xu,Ahmed K. Rashwan,Zhiwei Ge,Yuting Li,Hengju Ge,Jiaxin Li,Jiahong Xie,Shiyu Liu,Jie Fang,Kejun Cheng,Wei Chen
Melastoma dodecandrum Lour. (MDL) extracts have shown potent α-glucosidase inhibitory activity, suggesting MDL might be a good source of α-glucosidase inhibitors. The aim of the study was to identify compounds in MDL extracts with α-glucosidase inhibitory activities and evaluate their effect on postprandial blood glucose as well as elucidating the underlying mechanisms of inhibition. A total of 34 polyphenols were identified in MDL fruits, among which 10 anthocyanins and three proanthocyanidin derivatives were discovered for the first time. Dosing mice with MDL extracts (100 mg/kg body weight, by gavage) was associated with a significantly decrease in postprandial blood glucose concentrations after oral administration of maltose. The most potent α-glucosidase inhibitor was identified as casuarictin (IC 50 of 0.21 μg/mL). Casuarictin bound competitively to α-glucosidase, occupying not only the catalytic site but also forming strong hydrogen bonds with α-glucosidase residues. Therefore, casuarictin derived from MDL fruits might be used as novel α-glucosidase inhibitor in functional foods or other dietary products.
研究领域:
药理学
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植物化学
·
代谢疾病
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
·
2024
·
IF 11
Yuxue Zheng,Siyu Chen,Yanyu Hu,Xingqian Ye,Shaoyun Wang,Jinhu Tian
The study aimed to investigate the cooperation of maize starch and ferulic acid under physical mixing (PM), heat treatment (HT) and extruded treatment (ET) and its impacts on postprandial blood glucose level. PM did not influence the surface structure, or long/short-range order of maize starch, yet it decreased rapidly digestive starch (RDS) content to 65.82 ± 1.67% and increased resistant starch (RS) content to 20.58 ± 1.71%. In the HT group, maize starch-ferulic acid (HMS-FRA) complexes was formed, maintaining A-type crystal structure, and binding amount increased as the addition of ferulic acid increased. And maize starch had the lowest RDS and highest RS, moreover, its postprandial blood glucose value was 7.93 ± 0.64 mmol/L·h when added 2.0% (w/w) ferulic acid. Besides, in the ET group, the crystal type of extruded maize starch-ferulic acid (EMS-FRA) complexes changed to A + V type. ET also led to increased RS content, with postprandial blood glucose level significantly reduced (6.16 ± 0.80 mmol/L·h) in EMS-2.0FRA. These results demonstrated that ferulic acid could form maize starch-ferulic acid complexes through ET, and effectively reducing its postprandial blood glucose level. Our results will provide an idea for the production of functional staple food .
研究领域:
食品科学
·
营养学
✓ 已验证
产品关联
DOI
高影响因子
DRUGS IN R&D
·
2024
·
IF 2.2
Jia Caiyun,Zhao Na,Song Haojing,Hu Yiting,Xu Yufang,Guo Caihui,Bai Wanjun,Dong Zhanjun
Background Ondansetron is a highly selective 5-HT3 receptor antagonist that alleviates nausea and vomiting. Bioequivalence evaluation ensures that the efficacy of generic drugs is consistent with that of the original drug. Objective The objective of this study was to evaluate the bioequivalence of ondansetron hydrochloride (HCl) tablets taken in single doses under fasting and postprandial conditions in healthy subjects. Methods In this randomized, open-label, two-cycle, crossover phase I study, liquid chromatography‒tandem mass spectrometry (LC‒MS/MS) was used to determine the ondansetron concentration in dipotassium-ethylenediaminetetraacetate (K 2 -EDTA) plasma after the subjects received a single 8 mg of ondansetron and reference formulation. Twenty-six healthy subjects received one tablet of ondansetron under fasting conditions and 28 subjects received one under postprandial conditions. Bioequivalence was established if the 90% confidence interval (CI) was 80.00–125.00%. The pharmacokinetic parameters were calculated via WinNonLin 8.1 software and the bioequivalence data were evaluated via Phoenix WinNonlin 8.1 statistics software. Results The geometric mean ratio (GMR) of the maximum observed concentration ( C max ), the area under the plasma concentration‒time curve (AUC) from time zero to the last sampling time (AUC 0– t ), and the AUC from time zero to infinity (AUC 0–∞ ) from the test/reference formulation under fasting conditions were 90.50, 90.43, and 90.25, respectively. The 90% CIs were 83.75–97.79, 82.64–98.95, and 82.25–99.03, respectively. The GMRs of C max , AUC 0– t , and AUC 0–∞ after a high-fat meal were 96.85, 93.57, and 93.77, respectively; the 90% CIs were 88.43–106.07, 87.35–100.24, and 87.35–100.68, respectively. Conclusion The test and reference formulations of ondansetron HCl have bioequivalence for healthy adult subjects under fasting and postprandial conditions.
研究领域:
药理学
·
临床药学
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产品关联
DOI
PubMed
高影响因子
Food Science and Human Wellness
·
2024
·
IF 5.6
Huafang Ding,Shouhe Huang,Chui Yiu Chook,Erika Kwek,Chi Yan,Kaying Ma,Jianhui Liu,Hanyue Zhu,Zhenyu Chen
α -Glucosidase inhibitors are effective in controlling postprandial hyperglycemia, which play crucial roles in the management of type 2 diabetes. Protocatechuic acid (PCA) is one of phenolic acids existing not only in various plant foods but also as a major microbial metabolite of dietary anthocyanins in the large colon. The present study investigated the inhibitory mechanism of PCA on α -glucosidase in vitro and examined its effect on postprandial blood glucose levels in vivo . Results from in vitro experiments demonstrated that PCA was a mix-type inhibitor of α -glucosidase. Driven by hydrogen bonds and van der Waals interactions, PCA reversibly bound with α -glucosidase to form a stable α -glucosidase-PCA complex in a spontaneous manner. The computational simulation found that PCA could insert into the active cavity of α -glucosidase and establish hydrogen bonds with catalytic amino acid residues. PCA binding aroused the steric hindrance for substrates to enter active sites and caused the structural changes of interacted catalytic amino acid residues. PCA also exhibited postprandial hypoglycemic capacity in diabetic mice. This study may provide the theoretical basis for the application of PCA as an active ingredient of functional foods in dietary management of diabetes.
研究领域:
营养学
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药理学
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分子生物学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yun Bian,Li Li,Wei Zhao,Lichun Guo
Polysaccharide-derived functional food ingredients are increasingly prevalent in the food industry for their health benefits and functional versatility. Among them, sodium alginate (SA), a natural polysaccharide, is widely valued for its sustainability, renewability, non-toxic nature, and broad applicability. However, its poor water solubility has limited its use as biomedical materials and food additives. Here, we enhanced SA through carboxymethylation to produce carboxymethylated SA (CMSA), aiming to develop functional food ingredients with improved physicochemical properties for health management. The synthesized CMSA was characterized for its physical properties and ability to form a hydrogel through cross-linking with Ca 2+ . We assessed its encapsulation efficiency for food particles in simulated gastric and intestinal fluids and evaluated its physiological effects in a rat model. Our findings demonstrated that CMSA-based hydrogels effectively encapsulate ingredients in the stomach, reducing nutrient diffusion in the intestine, and helping to manage postprandial hypoglycemia. Additionally, the hydrogel expands in the stomach and small intestine, contributing to modest weight loss. These findings suggest that CMSA-based hydrogels offer significant potential as functional food ingredients for managing postprandial hypoglycemia and supporting weight management. The development of such gelling systems presents promising applications in both medical and nutritional sciences, offering innovative strategies for addressing diet-related health concerns.
研究领域:
食品科学
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生物医学工程
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营养学
✓ 已验证
DOI
PubMed
高影响因子
Journal of Functional Foods
·
2024
·
IF 3.8
Yuyang Yao,Juer Liu,Qiming Miao,Xinyue Zhu,Lu Sun,Wei Hua,Na Zhang,Guangwei Huang,Roger Ruan,Yanling Cheng,Shengquan Mi
Controlling postprandial hyperglycemia is considered as a viable prophylactic treatment for type 2 diabetes mellitus. A major strategy in decreasing postprandial glucose involves inhibition of the carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase. The aim of this study was to evaluate the hypoglycemic potential of almond hull extract in vitro and in vivo. The in vitro results showed that, among the 0 %, 30 %, 50 % and 80 % ethanol extracts of almond hull, the 50 % ethanol extracts demonstrated the most significant inhibition of digestive enzymes. With in vivo tests, the blood glucose concentration in the control rats increased sharply near the peak glucose level in 15 min, while the peak glucose level of rats loading the almond hull extract occurred in 30 min. Therefore, almond hull extract can reduce postprandial blood glucose levels and delay the time to peak by about 15 min, providing a sustained and gradual release of energy.
研究领域:
药理学
·
代谢病研究
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2020
·
IF 5.162
Lichun Guo,Jie Xia,Shuhuai Yu,Jiai Yan,Fang He,Mengqing Zhang,Qilei Fan,Ruijin Yang,Wei Zhao
α-Amylase inhibitors (α-AIs) delay digestion of dietary starch by inhibiting α-amylase in the gut, thereby reducing the postprandial glycemia, which is beneficial to the patients with obesity and diabetes. The proteinaceous α-AIs from wheat can effectively control starch digestion and regulate postprandial hyperglycemia. However, their gastric intolerance remains a challenge, which limits its commercial production and industrial application. In this study, sodium alginate/chitosan aerogels loaded with wheat protein α-AIs were prepared and evaluated as potential transportation and protection matrices for important components in food or pharmaceutical applications. Specifically, the biodegradable aerogel cross-linked with sodium alginate-chitosan-calcium chloride, has a large surface area and open porous structure, which can adsorb staple wheat proteins as an integrated edible material to block around 88,660 U/g of α-amylase activity. The aerogel particles were able to protect the activity of wheat α-AIs in the stomach, leading to the slow passage of the wheat α-AIs through the small intestine to inhibit starch digestion more effectively. Animal experiments further showed that the postprandial blood glucose levels in rats were effectively controlled through delayed increase, after administration of wheat protein-functionalized aerogel particles loaded with wheat α-AIs, which are natural biological macromolecules. This is a novel, safe, and economical method for the prevention and pretreatment of diabetes.
研究领域:
食品科学
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生物医学
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材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
EUROPEAN FOOD RESEARCH AND TECHNOLOGY
·
2024
·
IF 3
Zhou Jian-Feng,Xu Hai-Xia,Yin Zhong-Ping,Chen Ji-Guang,Zhang Qing-Feng
Quercetin is the most abundant flavonoid found in human diet. In the present study, the effects of quercetin on postprandial hyperglycemia (PPHG) were investigated in two ways. First, the complexes of quercetin and starch were prepared and characterized. Quercetin can occupy the helix of starch and interact with it through secondary bonds. The digestibility of starch decreased with the increasing proportion of quercetin in the complexes. Second, the inhibitory activities of quercetin on α-glucosidase and α-amylase were investigated in both in vitro and in vivo. Quercetin showed very strong inhibitory activity on α-glucosidase, while its inhibitory activity on α-amylase was far weaker than acarbose. Quercetin is the non-competitive inhibitor of α-glucosidase. Fluorescence titration showed that quercetin and α-glucosidase had one binding site and the binding constant lgKa was 3.70. After oral administration of quercetin–starch complexes in rats, the maximum level of postprandial blood glucose was reduced and delayed. Besides, quercetin also improved the PPHG after administration of sucrose and maltose in rats. Hence, it is deduced that the regulation of quercetin on PPHG is the result of its combination effects on starch and digestive enzymes. The complexes of quercetin and starch may be useful for the development of low-glycemic food.
研究领域:
营养学
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药理学
·
食品科学
✓ 已验证
产品关联
DOI
高影响因子
Foods
·
2023
·Vol. 12
·期 24
·4425
·
IF 5.2
Xiaosan Zhang,Guangrong Huang,Hua Liu,Wenwei Chen,Jing Zhao,Zhenbao Jia,Fei Tao
Inhibiting α-amylase can lower postprandial blood glucose levels and delay glucose absorption, offering an effective approach for the development of antidiabetic diets. In this study, an active constituent with inhibitory activity against α-amylase was isolated and purified by bioassay-guided fractionation fromCarya cathayensisSarg. peel (CCSP). The active constituent was identified by NMR and Q-Exactive Orbitrap Mass Spectrometry as 5-O-p-coumaroylquinic acid (5-CQA). 5-CQA possessed strong inhibitory activity against α-amylase, with an IC50 value of 69.39 µM. In addition, the results of the kinetic study indicated that 5-CQA was a potent, reversible, noncompetitive inhibitor against α-amylase. The findings indicate that 5-CQA derived from CCSP has potential as a novel inhibitor against α-amylase, which can help mitigate postprandial blood sugar spikes, making it suitable for inclusion in antidiabetic diets.Keywords:Carya cathayensisSarg. Peel;postprandial hyperglycemia;5-O-p-coumaroylquinic acid;α-amylase inhibitor
研究领域:
植物化学
·
代谢病学
·
食品科学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Qianqian Feng,Wei Yang,Xue Ma,Zhiyun Peng,Guangcheng Wang
Diabetes mellitus characterized by abnormal glucose concentration is a metabolic disease. α-Glu inhibitors from natural sources are a good choice for searching for high-efficiency and low-toxicity hypoglycemic drugs. In this study, a naturally effective α-Glu inhibitor aspergillus triazolate A (ATA) with a peculiar structure was first found in Oxalis corniculate L., then its activity and mechanism were first elucidated through various methods. These mechanisms included enzyme kinetics, circular dichroism spectra, fluorescence spectra, synchronous fluorescence spectrum, 3D fluorescence spectrum, and molecular docking. Meanwhile, the ability to reduce postprandial blood glucose was further investigated in vivo . Research results revealed that ATA was a mixed type α-Glu inhibitor with an IC 50 value of 66.87 ± 1.50 μM, which bound to the enzyme from a single site through hydrogen bonding and hydrophobic forces causing the looser secondary structure of α-Glu. It was also found that the binding site of α-Glu was closer to the Trp residue, and the endogenous fluorescence of α-Glu was quenched in a static quenching form. Moreover, the sucrose loading test in vivo revealed that the ATA of 20 mg/kg could effectively reduce the postprandial blood glucose level. Hence, ATA could be used as lead compound to develop novel α-Glu inhibitors.
研究领域:
药理学
·
生物化学
·
糖尿病研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ANIMAL SCIENCE
·
2020
·Vol. 98
·期 10
·
IF 2.092
Sun Mingfa,Zhao Jingpeng,Wang Xiaojuan,Jiao Hongchao,Lin Hai
The supplementation of dietary limiting amino acids (AA) with crystalline AA makes the use of low-protein diets an option in poultry production. The differing absorption rates of crystalline and protein-bound AA may lead to temporally imbalanced AA in the postabsorptive period. In this study, two experiments were conducted to evaluate the effect of encapsulated L-lysine-HCl (L-Lys-HCl) and DL-methionine (DL-Met) on the laying performance of hens. In exp. 1, a total of 135 forty-seven-wk-old Hy-Line Brown hens were subjected to three dietary treatments for 8 wk: basal diet supplemented with 0.14% L-Lys-HCl and 0.17% DL-Met to satisfy the NRC (1994) total Lys and Met recommendation (control) and basal diet supplemented with encapsulated L-Lys-HCl and DL-Met at the levels of 60% (60CLM, 0.084% L-Lys-HCl and 0.102% DL-Met) or 80% of control (80CLM, 0.112% L-Lys-HCl and 0.136% DL-Met), respectively. In exp. 2, 24 fifty-five-wk-old Hy-Line Brown hens were individually reared in cages and subjected to the same treatments as in exp. 1. The plasma concentrations of free AA and nitrogen metabolites were measured 2, 4, and 6 h after fed. The results showed that dietary AA treatment had no significant influence on body weight (BW), feed intake, laying rate, egg weight, egg mass, or feed efficiency. The expression levels of AA transporters CAT-1, y+LAT1, b0,+AT, B0AT, rBAT, EAAT3, and PepT1 in the duodenum, jejunum, and ileum were not influenced (P > 0.05) by dietary treatment. There was an interaction of dietary AA treatment and time (P < 0.05) and the 80CLM hens exhibited higher concentrations of Lys (P < 0.05) than the controls at 2-h time point. In contrast, plasma Met concentration was not influenced (P > 0.05), while Cys was reduced in the 60CLM hens at every time point. The 80CLM hens had higher taurine concentrations than those receiving the control diet at every postprandial time point. In conclusion, these findings demonstrate that by using encapsulated form, the supplemental levels of synthetic L-Lys-HCl and DL-Met can be effectively reduced by approximately 20% with no negative effect on laying performance. The result suggests that encapsulated Lys and Met may ameliorate the postabsorptive AA balance and contribute to the reduced dietary AA supplemental levels.
研究领域:
动物营养学
·
家禽科学
·
氨基酸代谢
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
·
2018
·
IF 3.47
Xiaqing Wu,Huafang Ding,Xing Hu,Junhui Pan,Yijing Liao,Deming Gong,Guowen Zhang
The postprandial hyperglycemia of diabetic patients is associated with a -amylase and a -glucosidase, searching safer enzyme inhibitors and deciphering their inhibition mechanism are important. In this study, gallocatechin gallate (GCG) was found to exert strong inhibition on α- amylase and α- glucosidase in the mixed-type and non-competitive manners, respectively. GCG could bind with α- amylase and α- glucosidase to form the complexes, which induced conformational changes of the two carbohydrate digestive enzymes. Docking analysis verified that GCG interacted with pivotal amino acids within the active site of α- amylase, while it bound to a site close to the active site of α- glucosidase, which might affect active site, causing declines in a -amylase and α- glucosidase activities. Moreover, the combination of GCG with acarbose increased the inhibition of α- amylase and α- glucosidase and reduced the dosage of acarbose. This study may provide theoretical basis for designing novel functional foods of GCG for the prevention and treatment of diabetes.
研究领域:
药理学
·
生物化学
·
糖尿病研究
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）