Food Bioscience
·
2024
·
IF 4.8
Qianni Chen,Lianzhu Lin,Mouming Zhao
Fucoidan possesses a variety of biological activities beneficial for human wellness. It is a good candidate for ameliorating obesity and diabetes. However, high-purity fucoidan products are limited due to the co-extraction of impurities i.e. alginate, protein and small molecular substances. In this study, the optimal preparation strategy for high-purity fucoidan from a template brown alga ( Saccharina japonica ) was screened out by the exploration of key and auxiliary steps. The key step was confirmed as moderate-temperature acid extraction and the auxiliary steps were fixed on ethanol refluxing and ball milling pretreatment. The fucose content of S. japonica fucoidan increased by 7.15 times and the sulfate group content increased by 4.87 times compared with those of fucoidans prepared by classic high-temperature acid extraction. Ball milling-assisted moderate-temperature acid extraction performed great effectiveness and universality in the extraction of high-purity fucoidans derived from four brown algae including S. japonica , Undaria pinnatifida, Sargassum fusiforme, and Fucus vesiculosus . Glycolipid-lowering activities of four fucoidans were confirmed by their interactions with intestinal bile acid, cholesterol micellar, glucose and probiotics including butyrate-producing bacteria, Bacteroides , Bifidobacterium , and Lactobacillus . Our study provided an efficient and universal extraction process for high-purity fucoidan with glycolipid-lowering activity from typical brown algae.
研究领域:
海洋生物学
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食品科学
·
生物化学
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DOI
高影响因子
Journal of Functional Foods
·
2018
·
IF 3.47
Du-Xin Jin,Jun-Fang He,Xue-Gang Luo,Tong-Cun Zhang
Hypericum attenuatum Choisy, as an edible medicinal plant, possesses multiple therapeutic effects. Type 2 diabetes is a metabolic disorder that has become a major threat to public health. The objective of this study was to investigate the hypoglycemic effect of Hypericum attenuatum Choisy extracts (HaC) on T2DM mice and modulatory effect of HaC on composition of intestinal microflora. T2DM mice were treated with HaC for 5 weeks. HaC could modulate fasting blood glucose, improve hepatic insulin sensitivity and promote hepatic glycogen storage by activating IRS1/PI3K/AKT pathway. Moreover, HaC regulated dysfunctional lipid metabolism and reduced inflammation in T2DM mice. Additionally, HaC treatment could modulate the compositions of gut microbiota in small intestine and colon with the altered abundances of Firmicutes , Bacteroidetes and Proteobacteria . Meanwhile, HaC treatment could augment short chain fatty acids contents. These results demonstrate that H. attenuatum Choisy may be a potential therapy for the treatment of T2DM.
研究领域:
药理学
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糖尿病研究
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微生物学
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产品关联
DOI
高影响因子
BRITISH JOURNAL OF PHARMACOLOGY
·
2014
·Vol. 171
·期 23
·5252-5264
·
IF 4.99
Jing Han,Lidan Sun,Xun Huang,Zheng Li,Chenyu Zhang,Hai Qian,Wenlong Huang
Background and Purpose The short biological half-life limits the therapeutic use of glucagon-like peptide-1 (GLP-1) and chemical modification to improve the interaction of peptides with serum albumin represents an effective strategy to develop long-acting peptide analogues. Coumarin, a natural product, is known to bind tightly to plasma proteins and possesses many biological activities. Therefore, we designed and synthesized a series of coumarin-modified GLP-1 derivatives, hypothesizing that conjugation with coumarin would retain the therapeutic effects and prolong the biological half-life of the conjugates. Experimental Approach Four cysteine-modified GLP-1 analogues (1–4) were prepared using Gly 8 -GLP-1(7–36)-NH 2 peptide as a starting point. These analogues were conjugated with two coumarin maleimides to yield eight compounds (conjugates 6–13) for testing. Activation of human GLP-1 receptors, stability to enzymic inactivation in plasma and binding to human albumin were assessed in vitro . In vivo , effects on oral glucose tolerance tests (OGTT) in rats and on blood glucose levels in db/db mice were studied. Key Results Most conjugates showed well preserved receptor activation efficacy, enhanced albumin-binding properties and improved in vitro plasma stability and conjugate 7 was selected to undergo further assessment. In rats, conjugate 7 had a longer circulating t 1/2 than exendin-4 or liraglutide. A prolonged antidiabetic effect of conjugate 7 was observed after OGTT in rats and a prolonged hypoglycaemic effect in db/db mice. Conclusions and Implications Cysteine-specific coumarin conjugation with GLP-1 offers a useful approach to the development of long-acting incretin-based antidiabetic agents. Conjugate 7 is a promising long-lasting GLP-1 derivative deserving further investigation.
研究领域:
药理学
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糖尿病研究
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药物化学
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DOI
PubMed
高影响因子
CELLULOSE
·
2023
·Vol. 30
·期 16
·10285-10296
·
IF 5.7
Gao Yan,Zhang Yuangong,Wang Yu,Liu Bing,Liu Feng,Ba Xinwu
In this paper, a cellulose-based hydrogel with the ability to lower glucose levels, scavenge reactive oxygen species (ROS), and colorimetrically monitor early lesions was synthesized to address the issue of glucose and H 2 O 2 overexpression on the wound surface. Briefly, boronic acid pinacol ester containing phenolphthalein (BAPE-PPH) was employed as a crosslinker to react with hydroxypropyl methylcellulose (HPMC) to afford hydrogels (HPMC@PPH-Hs) with good biocompatibility. Because glucose has higher affinity for the phenylboronic ester group than cellulose derivatives, the HPMC@PPH-Hs showed excellent glucose-lowering performance. The presence of B-C bonds in the network endows the as-obtained hydrogel with H 2 O 2 sensitivity, and cleavage of the B-C bonds forces the transformation of BAPE-PPH moieties into PPH, giving rise to colorimetric behaviour. Thus, the obtained HPMC@PPH-Hs provide information to enrich the family of smart hydrogels, and its potential application in diabetic wound healing may be desirable. Graphical abstract
研究领域:
生物材料学
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医学工程
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伤口愈合研究
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DOI
高影响因子
CHEMISTRY OF MATERIALS
·
2024
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IF 7.2
Yufen Xiao,Jiamin Zhang,Tong Wu,Shuai Chen,Zhixiong Huang,Jianzhong Du
Natural modulators, such as insulin, play a significant role in modulating molecule levels. Inspired by the role of natural modulators, herein, we propose a glucose modulator that is composed of a glycopolymersome only to regulate glucose levels. This insulin- and drug-free strategy can smartly take in and snap out glucose according to the surrounding blood glucose levels (BGLs) by reversible sugar substituting. The glycopolymersome is self-assembled from a biodegradable glycopolymer that is composed of sugar and phenylboronic acid derivative, poly(ε-caprolactone)-block-poly[(3-acrylamidophenylboronic acid-stat-N-acryloyl glucosamine] [PCL-b-P(AAPBA-stat-AGA)]. It exhibits excellent long-term hypoglycemic effects toward type 1 diabetic mice for at least 3 days upon one shot without observed side effects, which is the longest effective sugar-regulation time for the insulin and drug-free strategy. Most notably, we explored the effect of the molecular structure of the glycopolymers on the BGL regulating efficacy, where the glucosyl moiety was polymerized with PBA either randomly or separately. Block-statistical glycopolymersomes exhibited lower binding energy to glucose, better glucose responsiveness, and prolonged hypoglycemic effect due to the abundant intramolecular and intermolecular dynamic covalent bonds between AAPBA and AGA. Our finding confirmed the importance of a block-statistical copolymer structure and the key role of sugar in regulating BGLs without involving medication, which may provide guidance and open new avenues for design blood glucose regulating materials.
研究领域:
生物材料学
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糖尿病研究
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高分子化学
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产品关联
DOI
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
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代谢病研究
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产品关联
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2021
·
IF 4.36
Hui Zhang,Ruoyu Chen,Cong Xu,Guimin Zhang,Yongxia Guan,Qun Feng,Jingchun Yao,Jizhong Yan
Background Due to the complexity of traditional Chinese medicine (TCM), the current quality evaluation of TCM are difficult to associate with clinical efficacy. Shenqi Jiangtang Granule (SJG), a classical TCM formula, is proven as a therapy for treatment of type II diabetes mellitus (DM) and complications while the substantial basis of the therapeutic effects is not clear. Purpose The present study proposed an integrated approach to discriminate the quality markers (Q-markers) based on multi-dimensional characteristic network for quality control of TCM. Methods The multi-dimensional characteristic network was established by “Spider-web” mode, which was comprehensively integrating “compatibility-content-activity- efficiency-stability” of the candidate ingredients. The activity dimension was evaluated by the inhibitory activity of SJG on α-glucosidase and aldose reductase . The efficacy dimension was assessed through the association between the compounds and the target pathway of diabetic nephropathy (DN) based on integrated pharmacology platform. Each dimension for the feature network was quantified by multivariate statistical analysis, and regression area of the candidate compounds was constructed in the network. Finally, the candidate compounds were sorted comprehensively by the regression area. Results A total of 30 chemical compounds with effective hypoglycemic activity were identified as the potential Q-markers. From the data analysis, three dimensions of activity, efficacy and content performed a greater impact on the regression area of the characteristic network. Among these compounds, ginsenoside Re , ginsenoside Rd , ginsenoside Rg 1, calycosin , ginsenoside Rb 1 , formononetin , astragaloside IV , ginsenoside Rf , ginsenoside Rc , notoginsenoside Fe, schisandrol A, gomisin D were screened out as the candidate Q-markers of SJG. Conclusion The multi-dimensional characteristic network integrating compatibility, content, activity, efficiency and stability is efficient to discriminate the potential Q-markers of TCM prescription. Our results demonstrated that 12 candidate compounds from Panax Ginseng , Radix Astragali and Schisandrae Chinensis might select as Q-markers for qualitative evaluation of SJG.
研究领域:
中药学
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生物信息学
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药理学
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产品关联
DOI
PubMed
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2025
·
IF 8
Shiqiang Peng,Lianzhu Lin,Mouming Zhao
Drinking tea is beneficial to reduce the incidence of obesity. Unlike Fuzhuan brick tea (DT, a typical dark tea) widely reported to have good glycolipid-lowering activity (GLA), there is little information on GLA of Dancong summer tea (OT, a typical oolong tea). A comparative study on GLA and chemical compositions of OT and DT was systematically conducted. The results showed that OT had advantages in high content of polyphenols, leading to its better GLA including glycolipid digestion enzyme inhibitory activity and cholesterol micellar solubility inhibition activity than DT’s. A total of 21 compounds mainly including catechins, flavonoids, phenolic acids and phenylpropanoids were screened as the key differentially active micromolecules (KDAM) by UPLC-QTOF-MS/MS-based untargeted metabolomic analysis combined with multivariate analysis, which resulted in the difference of GLA between OT and DT. Moreover, the high affinity capacity and interaction mode between KDAM with α -glucosidase/ α -amylase/pancreatic lipase/cholesterol esterase were validated by molecular docking. Although the accumulation of polyphenols makes OT has a poor flavor as a beverage, our research demonstrated that OT with high content of polyphenols could be used in functional foods to facilitate the prevention of obesity.
研究领域:
食品科学
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营养学
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植物化学
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产品关联
DOI
PubMed
高影响因子
Pharmaceutics
·
2019
·Vol. 11
·期 1
·18
·
IF 4.773
Lele Yang,Ling Li,Hao Hu,Jianbo Wan,Peng Li
Natural deep eutectic solvents (NADESs), composed of natural primary metabolites, are now widely used as green and sustainable extraction solvents of bioactive components. In the present study, various NADESs were prepared to extract multi-components from different preparations of an herbal formula (Chinese name: Jinqi Jiangtang, JQJT) using ultrasound-assisted extraction (UAE). Results showed that most prepared NADESs provided more effective extraction of phenolic acids and alkaloids from JQJT preparations than conventional solvents. Among the tested NADESs, the solvent formed by choline chloride and laevulinic acid was selected to optimize the operational parameters using response surface methodology. The optimized extraction method was successfully applied to extract six major components in four commercial JQJT products, and quantification analysis was performed by the validated high-performance liquid chromatography with ultraviolet detection (HPLC-UV) method. The quantitative results indicated that preparations from different manufacturers showed different chemical profiles. In conclusion, NADESs-based UAE shows considerable potential as an efficient and green method for extraction of multi-bioactive components from commercial herbal preparations.Keywords:deep eutectic solvents;Jinqi Jiangtang;ultrasound assisted extraction;response surface methodology;bioactive components
研究领域:
中药学
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分析化学
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 27
·14967-14974
·
IF 2.936
Lei Zhang,Shi-Tao Zhang,Yan-Chun Yin,Shu Xing,Wan-Nan Li,Xue-Qi Fu
Glucagon-like peptide (GLP)-1 is a potent glucose-dependent insulinotropic gut hormone released from intestinal L cells. The aim of this study was to investigate isoquercitrin as an inhibitor of dipeptidyl peptidase IV (DPP-IV) and determine whether it affects GLP-1 release in normal mice and NCI-H716 cells. In vitro, we used chromogenic substrate method detection methods to measure DPP-IV. We found that isoquercitrin was a competitive inhibitor, with IC50 and Ki values of 96.8 and 236 μM, respectively. Isoquercitrin and sitagliptin also stimulated GLP-1 release in NCI-H716 cells. In vivo, a type 2 diabetic mouse model was established, and oral treatment with different concentration of isoquercitrin and sitagliptin for 8 weeks significantly decreased the fasting blood glucose level. The weight and the levels of serum GLP-1 and insulin of the mice in the isoquercitrin group were higher than those in the model group (P < 0.001). An oral glucose tolerance test showed that the isoquercitrin significantly inhibited postprandial blood glucose changes in a dose-dependent manner. These findings demonstrated the hypoglycemic effects of isoquercitrin and indicated that isoquercitrin improved insulin sensitivity by targeting DPP-IV.
研究领域:
药理学
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内分泌学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
ANALYTICA CHIMICA ACTA
·
2024
·
IF 5.7
Hui Zhang,Jiangyu Yao,Guyu Xiao,Jianhui Xie,Shuying Mao,Chenghong Sun,Jingchun Yao,Jizhong Yan,Pengfei Tu
Target discovery of natural products is a key step in the development of new drugs, and it is also a difficult speed-limiting step. In this study, a traditional Chinese medicine microspheres (TCM-MPs) target fishing strategy was developed to discover the key drug targets from complex system. The microspheres are composed of Fe 3 O 4 magnetic nanolayer, oleic acid modified layer, the photoaffinity group (4- [3-(Trifluoromethyl)-3H-diazirin-3-yl] benzoic acid, TAD) layer and active small molecule layer from inside to outside. TAD produces highly reactive carbene under ultraviolet light, which can realize the self-assembly and fixation of drug active small molecules with non-selective properties. Here, taking Shenqi Jiangtang Granules (SJG) as an example, the constructed TCM-MPs was used to fish the related proteins of human glomerular mesangial cells (HMCs) lysate. 28 differential proteins were screened. According to the target analysis based on bioinformatics, GNAS was selected as the key target, which participated in insulin secretion and cAMP signaling pathway. To further verify the interaction effect of GNAS and small molecules, a reverse fishing technique was established based on bio-layer interferometry (BLI) coupled with UHPLC-Q/TOF-MS/MS. The results displayed that 26 small molecules may potentially interact with GNAS, and 7 of them were found to have strong binding activity. In vitro experiments for HMCs have shown that 7 active compounds can significantly activate the cAMP pathway by binding to GNAS. The developed TCM-MPs target fishing strategy combined with BLI reverse fishing technology to screen out key proteins that directly interact with active ingredients from complex target protein systems is significant for the discovery of drug targets for complex systems of TCM.
研究领域:
药学
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生物技术
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分子生物学
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中医药
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2024
·
IF 8.5
Hanliang Li,Lianzhu Lin,Mouming Zhao
This study aimed at recycling flavonoids with glycolipid lowering activity from Chenpi processing residue produced by essential oil extraction. The crude Chenpi flavonoids obtained by ethanol reflux mainly contained flavonone (hesperidin) and polymethoxyflavonoids (nobiletin, tangeretin, sinensetin, and isosinensetin), which complementally exerted strong glycolipid lowering activity as revealed by digestive enzyme inhibitory activity, molecular docking and network pharmacology. The reducing sugar and water-soluble impurities were efficiently removed by yeast fermentation and aqueous two-phase system (ATPS) extraction, respectively. The optimal combination use of yeast (2 % w / v , CN36) and ATPS formed by 22 % ( w /w) (NH 4 ) 2 SO 4 and 25 % (w/w) ethanol improved flavonoid purity to 60.25 %, enriched flavonone and polymethoxyflavonoids by 6.69-fold, and enhanced digestive enzyme inhibitory activity, which was superior to the use of individual yeast or ATPS, unoptimized combination, macroporous resin (XAD-16), and ethyl acetate. This study was the first to develop a recyclable biophysical method for simultaneous enrichment of flavonone and polymethoxyflavonoids.
研究领域:
药学
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生物技术
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食品科学
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药理学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）